naltrexone profile

Naltrexone: Derivative of noroxymorphone that is the N-cyclopropylmethyl congener of NALOXONE. It is a narcotic antagonist that is effective orally, longer lasting and more potent than naloxone, and has been proposed for the treatment of heroin addiction. The FDA has approved naltrexone for the treatment of alcohol dependence. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

naltrexone : An organic heteropentacyclic compound that is naloxone substituted in which the allyl group attached to the nitrogen is replaced by a cyclopropylmethyl group. A mu-opioid receptor antagonist, it is used to treat alcohol dependence. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

ID Source	ID
PubMed CID	5360515
CHEMBL ID	19019
CHEBI ID	7465
SCHEMBL ID	34681
MeSH ID	M0014445

Synonym
BIDD:GT0405
HY-76711
AB00174152-14
BRD-K88172511-310-03-8
3,14-dihydroxy-17-(cyclopropylmethyl)-4,5alpha-epoxymorphinan-6-one
CHEBI:7465 ,
(4r,4as,7ar,12bs)-3-(cyclopropylmethyl)-4a,9-dihydroxy-2,4,5,6,7a,13-hexahydro-1h-4,12-methanobenzofuro[3,2-e]isoquinolin-7-one
(-)naltrexone
gtpl1639
vivitrex
celupan
nemexin
vivitrol
revia
SMP1_000206
hsdb 6750
morphinan-6-one, 17-(cyclopropylmethyl)-4,5-alpha-epoxy-3,14-dihydroxy-
naltrexone [usan:inn:ban]
ccris 3506
naltrexonum [inn-latin]
um-792
einecs 240-649-9
naltrexona [inn-spanish]
morphinan-6-one, 17-(cyclopropylmethyl)-4,5-epoxy-3,14-dihydroxy-, (5alpha)-
brn 3596648
BPBIO1_000146
PDSP2_000847
vivitrol (tn)
naltrexone (usan/inn)
D05113
PRESTWICK3_000116
BSPBIO_000132
17-(cyclopropylmethyl)-4,5-epoxy-3,14-dihydroxmorphinan-6-one, (5.alpha.)-
cyclopropylmethyl(dihydroxy)[?]one
C07253
naltrexone
16590-41-3
DB00704
17-(cyclopropylmethyl)-4,5-epoxy-3,14-dihydroxymorphinan-6-one
n-cyclopropylmethylnoroxymorphone
17-(cyclopropylmethyl)-4,5alpha-epoxy-3,14-dihydroxymorphinan-6-one
n-cyclopropylmethyl-14-hydroxydihydromorphinone
PRESTWICK2_000116
PRESTWICK1_000116
SPBIO_002071
PRESTWICK0_000116
HMS2089O11
bdbm50000787
(1s,5r,13r,17s)-4-(cyclopropylmethyl)-10,17-dihydroxy-12-oxa-4-azapentacyclo[9.6.1.0^{1,13}.0^{5,17}.0^{7,18}]octadeca-7(18),8,10-trien-14-one
CHEMBL19019
nsc-758439
en-1639a free base
NCGC00024427-03
NCGC00024427-04
naltrexonum
nsc 758439
unii-5s6w795cqm
5s6w795cqm ,
naltrexona
dtxcid2026313
tox21_112007
dtxsid4046313 ,
cas-16590-41-3
AKOS015994596
pti-555
naltrexone [hsdb]
naltrexone [who-dd]
morphinan-6-one, 17-(cyclopropylmethyl)-4,5-epoxy-3,14-dihydroxy-, (5.alpha.)-
naltrexone [usp-rs]
naltrexone [mi]
naltrexone [vandf]
naltrexone [orange book]
naltrexone [inn]
naltrexone [usan]
naltrexone component of contrave
naltrexone [mart.]
CS-0880
(-)-naltrexone
DQCKKXVULJGBQN-XFWGSAIBSA-N
SCHEMBL34681
tox21_112007_1
NCGC00024427-05
HS-0002
us9107954, naltrexone
(4r,4as,7ar,12bs)-3-(cyclopropylmethyl)-4a,9-dihydroxy-2,4,5,6,7a,13-hexahydro-1h-4,12-methanobenzofuro[3,2-e]isoquinoline-7-one;hydrochloride
bdbm60212
cid_5485201
(4r,4as,7ar,12bs)-3-(cyclopropylmethyl)-4a,9-bis(oxidanyl)-2,4,5,6,7a,13-hexahydro-1h-4,12-methanobenzofuro[3,2-e]isoquinoline-7-one;hydrochloride
AB00174152_17
mfcd00242996
(4r,4as,7ar)-3-(cyclopropylmethyl)-4a,9-dihydroxy-2,4,5,6,7a,13-hexahydro-1h-4,12-methanobenzofuro[3,2-e]isoquinolin-7-one
BCP07022
Q409587
BRD-K88172511-003-21-1
AR-270/43507956
4-(cyclopropylmethyl)-10,17-dihydroxy-12-oxa-4-azapentacyclo[9.6.1.0~1,13~.0~5,17~.0~7,18~]octadeca-7(18),8,10-trien-14-one
EX-A4863
(4R,4AS,7AR,12BS)-3-(CYCLOPROPYLMETHYL)-4A,9-DIHYDROXY-2,3,4,4A,5,6-HEXAHYDRO-1H-4,12-METHANOBENZOFURO[3,2-E]ISOQUINOLIN-7(7AH)-ONE
EN300-19748946
AC-36726
(5alpha)-17-(cyclopropylmethyl)-4,5-epoxy-3,14-dihydroxymorphinan-6-one
naltrexone (usp-rs)
(5-alpha)-17-(cyclopropylmethyl-4,5-epoxy-3,14-dihydroxy morphinan-6-one
naltrexonum (inn-latin)
naltrexona (inn-spanish)
naltrexone (mart.)
addex-1000
n07bb04
naltrexon
naltrexonum (latin)

Research Excerpts

Toxicity

The combined use of scopolamine, naltrexone and naloxone is a rapid, safe and effective detoxification treatment protocol for heroin addicts. The aim of this review was to extensively evaluate the safety of oral n saltrexone by examining the risk of serious adverse events and adverse events in randomised controlled trials.

Excerpt	Reference	Relevance
" Naltrexone (10 mg/kg, ip) given 5 min before pentobarbital did not alter the LD50 of the latter."	( Studies of the possible role of brain endorphins in pentobarbital anesthesia and toxicity in mice. Bhargava, HN, 1979)	0.26
"61 mg/kg while the LD50 of cocaine in buprenorphine (0."	( Antagonism of acute cocaine toxicity by buprenorphine. Bansinath, M; Goldfrank, LR; Shukla, VK; Turndorf, H, 1991)	0.28
" The drug was well tolerated by all subjects, and no clinically significant adverse effects were observed during the seven-day administration period."	( Nalmefene: safety and kinetics after single and multiple oral doses of a new opioid antagonist. Dixon, R; Garg, D; Gentile, J; Howes, J; Hsiao, J; Hsu, HB; Weidler, D, 1987)	0.27
" We found no side-effect or toxicity due to naltrexone."	( Naltrexone treatment of heroin addiction: efficacy and safety in a double-blind dosage comparison. Carney, TM; Goldstein, A; Judson, BA, 1981)	0.26
" Nalmefene was well tolerated, with no serious adverse drug reactions."	( A double-blind, placebo-controlled pilot study to evaluate the efficacy and safety of oral nalmefene HCl for alcohol dependence. Goldberg, G; Mantero-Atienza, E; Mason, BJ; Morgan, RO; Ritvo, EC; Salvato, FR; Welch, B, 1994)	0.29
" No serious adverse events were judged to be related to nalmefene."	( Effectiveness and safety of intravenous nalmefene for emergency department patients with suspected narcotic overdose: a pilot study. Kaplan, JL; Marx, JA, 1993)	0.29
"Nalmefene is effective in the reversal of opiate overdose and appears to be safe in the management of patients with altered sensorium."	( Effectiveness and safety of intravenous nalmefene for emergency department patients with suspected narcotic overdose: a pilot study. Kaplan, JL; Marx, JA, 1993)	0.29
" We observed no adverse clinical effects in elk receiving < or = 500 mg naltrexone/mg carfentanil."	( Efficacy and safety of naltrexone hydrochloride for antagonizing carfentanil citrate immobilization in captive Rocky Mountain elk (Cervus elaphus nelsoni). Lance, WR; Miller, MW; Wild, MA, 1996)	0.29
" This study was designed to examine the safety and tolerance of methylnaltrexone in healthy human participants over a range of doses and to identify any adverse effects or toxicity associated with methylnaltrexone and the doses at which these adverse effects occur."	( Safety and tolerance of methylnaltrexone in healthy humans: a randomized, placebo-controlled, intravenous, ascending-dose, pharmacokinetic study. Foss, JF; Moss, J; Murphy, M; O'Connor, MF; Roizen, MF; Yuan, CS, 1997)	0.3
" An important clinical issue with naltrexone treatment is predicting patient compliance, which may be influenced by adverse side effects experienced during the medication."	( Naltrexone biotransformation and incidence of subjective side effects: a preliminary study. Gunduz, M; King, AC; Kreek, MJ; O'Brien, CP; Volpicelli, JR, 1997)	0.3
" The most common new-onset adverse clinical events in the naltrexone group were nausea (9."	( The safety profile of naltrexone in the treatment of alcoholism. Results from a multicenter usage study. The Naltrexone Usage Study Group. Croop, RS; Faulkner, EB; Labriola, DF, 1997)	0.3
" Adverse drug effects were restricted to the first 2 weeks of treatment and included nausea (11/50), fatigue (3/50), dizziness, heartburn, and diarrhea (1/50 each)."	( Efficacy and safety of naltrexone, an oral opiate receptor antagonist, in the treatment of pruritus in internal and dermatological diseases. Beissert, S; Luger, T; Metze, D; Reimann, S, 1999)	0.3
"Rapid opiate detoxification under general anaesthesia is a safe and efficient method to suppress withdrawal symptoms."	( Safety, efficacy, and long-term results of a modified version of rapid opiate detoxification under general anaesthesia: a prospective study in methadone, heroin, codeine and morphine addicts. Hensel, M; Kox, WJ, 2000)	0.31
"Anesthesia in the white rhinoceros (Ceratotherium simum) has routinely involved potent narcotic anesthetic agents such as etorphine or carfentanil with their associated adverse side effects."	( Butorphanol and azaperone as a safe alternative for repeated chemical restraint in captive white rhinoceros (Ceratotherium simum). Childs, SE; Ferrell, ST; Radcliffe, RW, 2000)	0.31
"Naltrexone treatment of alcohol dependence is associated with adverse events that may limit its effectiveness."	( Adverse effects of oral naltrexone: analysis of data from two clinical trials. Kranzler, HR; Oncken, C; Van Kirk, J, 2001)	0.31
"To examine the relations among adverse events, drinking behavior, medication compliance and study retention in alcoholics receiving naltrexone for relapse prevention."	( Adverse effects of oral naltrexone: analysis of data from two clinical trials. Kranzler, HR; Oncken, C; Van Kirk, J, 2001)	0.31
" Moderate or severe adverse effects were monitored weekly and categorized as either neuropsychiatric (NP) or gastrointestinal (GI)."	( Adverse effects of oral naltrexone: analysis of data from two clinical trials. Kranzler, HR; Oncken, C; Van Kirk, J, 2001)	0.31
" NP adverse events exerted little influence on medication compliance (beta = -0."	( Adverse effects of oral naltrexone: analysis of data from two clinical trials. Kranzler, HR; Oncken, C; Van Kirk, J, 2001)	0.31
"Future studies aimed at enhancing the effectiveness of naltrexone should examine ways of reducing both NP and GI adverse events, in order to enhance both medication compliance and treatment retention."	( Adverse effects of oral naltrexone: analysis of data from two clinical trials. Kranzler, HR; Oncken, C; Van Kirk, J, 2001)	0.31
"1%) had some adverse event (AA) during the study, including nausea/vomiting (13."	( [Naltrexone in the treatment of alcoholism. Clinical evolution, safety and efficacy in a sample of 198 patients]. Gual Solé, A, 2001)	0.31
"The combined use of scopolamine, naltrexone and naloxone is a rapid, safe and effective detoxification treatment protocol for heroin addicts."	( [The combined use of scopolamine, naltrexone and naloxone as a rapid, safe and effective detoxification treatment for heroin addicts]. Xu, K; Yang, G; Zhou, W, 1999)	0.3
" Most of the adverse events that occurred during the first 48 h of naltrexone therapy were consistent with opioid withdrawal-like phenomena and spontaneously disappeared 2 days after starting treatment."	( Efficacy and safety of oral naltrexone treatment for pruritus of cholestasis, a crossover, double blind, placebo-controlled study. Coronel, E; Findor, J; Muñoz, AE; Sordá, J; Terg, R, 2002)	0.31
"The study estimated serious adverse event (SAE) rates among entrants to pharmacotherapies for opioid dependence, during treatment and after leaving treatment."	( Serious adverse events in the Australian National Evaluation of Pharmacotherapies for Opioid Dependence (NEPOD). Digiusto, E; Mattick, RP; O'Brien, S; Ritter, A; Shakeshaft, A, 2004)	0.32
" Both drugs are safe and acceptably tolerated but issues of compliance need to be addressed adequately to assure their usefulness in clinical practice."	( Efficacy and safety of naltrexone and acamprosate in the treatment of alcohol dependence: a systematic review. Amate, JM; Angeles, M; Bouza, C; Magro, A; Muñoz, A, 2004)	0.32
" During the past decade, NTX has been shown to be safe and effective in the treatment of pruritus associated with severe jaundice caused by severe and sometimes life-threatening cirrhosis and other liver diseases."	( Naltrexone: report of lack of hepatotoxicity in acute viral hepatitis, with a review of the literature. Brewer, C; Wong, VS, 2004)	0.32
"Opioids are associated with a number of adverse effects, constipation being the most common long-term adverse effect in patients with advanced cancer."	( Clinical status of methylnaltrexone, a new agent to prevent and manage opioid-induced side effects. Yuan, CS, )	0.13
": Injectable naltrexone was generally safe and well tolerated."	( A pilot evaluation of the safety and tolerability of repeat dose administration of long-acting injectable naltrexone (Vivitrex) in patients with alcohol dependence. Ait-Daoud, N; Aubin, HJ; Ehrich, E; Guzzetta, R; Johnson, BA; Loewy, J; Silverman, B; Van Den Brink, W, 2004)	0.32
" The most common side effect experienced was injection site complications."	( Pharmacokinetics, safety, and tolerability of a depot formulation of naltrexone in alcoholics: an open-label trial. Cello, R; Galloway, GP; Koch, M; Smith, DE, 2005)	0.33
"Naltrexone Depot is safe and well tolerated in alcoholics and these findings support the further investigation of its utility in larger double-blind placebo controlled trials."	( Pharmacokinetics, safety, and tolerability of a depot formulation of naltrexone in alcoholics: an open-label trial. Cello, R; Galloway, GP; Koch, M; Smith, DE, 2005)	0.33
"In the many clinical studies conducted in the alcoholism field with psychotropic drugs--and throughout the drug development field in medicine, where evaluation of adverse events can be incomplete, arbitrary or misleading--few standardized methods have been developed for assessing adverse events, whereas defining standardized methods for evaluating clinical efficacy is typical."	( The COMBINE SAFTEE: a structured instrument for collecting adverse events adapted for clinical studies in the alcoholism field. Ait-Daoud, N; Johnson, BA; Roache, JD, 2005)	0.33
"We standardized use of the SAFTEE with training, supervision and clear guidelines for its implementation, including development of a nomenclature for the typical adverse events associated with these medications and a format for examining symptom severity."	( The COMBINE SAFTEE: a structured instrument for collecting adverse events adapted for clinical studies in the alcoholism field. Ait-Daoud, N; Johnson, BA; Roache, JD, 2005)	0.33
"The COMBINE SAFTEE was incorporated into the Medical Management therapy and showed high fidelity with its utility, consistency of deliverability and flexibility in measuring adverse events in both the human laboratory and clinical trial settings using intervals that varied from daily to weekly use."	( The COMBINE SAFTEE: a structured instrument for collecting adverse events adapted for clinical studies in the alcoholism field. Ait-Daoud, N; Johnson, BA; Roache, JD, 2005)	0.33
"The protocol of the prospective study may be recommended as a safe and effective detoxification method."	( [Safety and effectiveness of opiate antagonist detoxification under general anesthesia]. Badaras, R; Ivaskevicius, J; Jovaisa, T; Laurinenas, G; Sipylaite, J; Vosylius, S, 2005)	0.33
"5 million adverse drug reaction (ADR) reports for 8620 drugs/biologics that are listed for 1191 Coding Symbols for Thesaurus of Adverse Reaction (COSTAR) terms of adverse effects."	( Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling. Benz, RD; Contrera, JF; Kruhlak, NL; Matthews, EJ; Weaver, JL, 2004)	0.32
"Although limited in scope, these findings support the hypothesis that long-term use of high-dose oral naltrexone is safe in otherwise healthy patients with impulse-control disorders who restrict their intake of acetaminophen, aspirin, or nonaspirin nonsteroidal anti-inflammatory drugs (NSAID)."	( Safety of high-dose naltrexone treatment: hepatic transaminase profiles among outpatients. Grant, JE; Kim, SW; Remmel, RP; Williams, KA; Yoon, G, )	0.13
" Transient sedation was the most commonly reported adverse event."	( Efficacy and safety of naltrexone use in pediatric patients with autistic disorder. Augusto, LM; Elchaar, GM; Maisch, NM; Wehring, HJ, 2006)	0.33
" Serious adverse effects have not been reported in short-term studies."	( Efficacy and safety of naltrexone use in pediatric patients with autistic disorder. Augusto, LM; Elchaar, GM; Maisch, NM; Wehring, HJ, 2006)	0.33
"To review the mechanisms of action of methylnaltrexone and its effects on opioid bowel dysfunction, as well as its effects on other opioid-induced adverse effects (ADEs), and its potential roles in clinical practice."	( Methylnaltrexone mechanisms of action and effects on opioid bowel dysfunction and other opioid adverse effects. Yuan, CS, 2007)	0.34
" Both high (>3 times the upper limit of normal) liver chemistry tests (LCTs) and hepatic-related adverse events were infrequent in all study groups."	( Hepatic safety of once-monthly injectable extended-release naltrexone administered to actively drinking alcoholics. Illeperuma, A; Lucey, MR; O'Brien, CP; Silverman, BL, 2008)	0.35
" As part of the study of the safety profile of this therapy, we were interested to review both the treatment correlates of previously presented mortality data and of adverse events."	( Comparative treatment and mortality correlates and adverse event profile of implant naltrexone and sublingual buprenorphine. Reece, AS, 2009)	0.35
"31), WOMAC change-from-baseline (mean pain, physical function, composite scores), and adverse event frequency were similar."	( ALO-01 (morphine sulfate and naltrexone hydrochloride) extended-release capsules in the treatment of chronic pain of osteoarthritis of the hip or knee: pharmacokinetics, efficacy, and safety. Johnson, F; Katz, N; Stauffer, J; Sun, S, 2010)	0.36
" An understanding of structure-activity relationships (SARs) of chemicals can make a significant contribution to the identification of potential toxic effects early in the drug development process and aid in avoiding such problems."	( Developing structure-activity relationships for the prediction of hepatotoxicity. Fisk, L; Greene, N; Naven, RT; Note, RR; Patel, ML; Pelletier, DJ, 2010)	0.36
"Safety assessments included determining adverse events (AEs), laboratory assessments, and the Clinical Opiate Withdrawal Scale (COWS)."	( Long-term safety and efficacy of morphine sulfate and naltrexone hydrochloride extended release capsules, a novel formulation containing morphine and sequestered naltrexone, in patients with chronic, moderate to severe pain. Brewer, R; Johnson, FK; Morris, D; Sekora, D; Stauffer, J; Wang, C; Webster, LR, 2010)	0.36
"High-dose naltrexone was safe and well tolerated using the procedure described."	( Safety, tolerability, and feasibility of high-dose naltrexone in alcohol dependence: an open-label study. Kim, SW; Thuras, P; Westermeyer, J; Yoon, G, 2011)	0.37
" Safety was evaluated via standard assessments (ie, adverse events and related withdrawals, physical examinations, laboratory tests, vital signs, electrocardiograms) and assessment of surgical complications."	( Safety and efficacy of methylnaltrexone in shortening the duration of postoperative ileus following segmental colectomy: results of two randomized, placebo-controlled phase 3 trials. Carpenito, J; Chun, HK; Randazzo, B; Schulman, S; Stambler, N; Tzanis, E; Yu, CS, 2011)	0.37
" Rates of adverse events and serious adverse events were comparable across all treatment groups in both studies."	( Safety and efficacy of methylnaltrexone in shortening the duration of postoperative ileus following segmental colectomy: results of two randomized, placebo-controlled phase 3 trials. Carpenito, J; Chun, HK; Randazzo, B; Schulman, S; Stambler, N; Tzanis, E; Yu, CS, 2011)	0.37
"To review postmarketing adverse event (AE) reports received during first year following approval."	( Safety of EMBEda (morphine sulfate and naltrexone hydrochloride) extended-release capsules: review of postmarketing adverse events during the first year. Badalamenti, VC; Buckley, JW; Smith, ET, )	0.13
"There is an unmet need for safe and effective medicines to treat children with Crohn's disease."	( Safety and tolerability of low-dose naltrexone therapy in children with moderate to severe Crohn's disease: a pilot study. Bingaman, SI; Evans, R; Field, D; Mauger, DT; Smith, JP, 2013)	0.39
"Oral naltrexone was well tolerated without any serious adverse events in children with moderate to severe Crohn's disease."	( Safety and tolerability of low-dose naltrexone therapy in children with moderate to severe Crohn's disease: a pilot study. Bingaman, SI; Evans, R; Field, D; Mauger, DT; Smith, JP, 2013)	0.39
"Naltrexone therapy seems safe with limited toxicity when given to children with Crohn's disease and may reduce disease activity."	( Safety and tolerability of low-dose naltrexone therapy in children with moderate to severe Crohn's disease: a pilot study. Bingaman, SI; Evans, R; Field, D; Mauger, DT; Smith, JP, 2013)	0.39
"The completeness of self-reported serious adverse events (SAEs) in clinical trials can be reduced by inaccuracies in subject reporting and lost to follow-up."	( Assessing the usefulness of health data linkage in obtaining adverse event data in a randomised controlled trial of oral and implant naltrexone in the treatment of heroin dependence. Hulse, G; Kelty, E; Ngo, H, 2013)	0.39
"Monthly urine samples; reports of craving and functioning; adverse events."	( Injectable extended-release naltrexone (XR-NTX) for opioid dependence: long-term safety and effectiveness. Gastfriend, DR; Krupitsky, E; Ling, W; Memisoglu, A; Nunes, EV; Silverman, BL, 2013)	0.39
"4%); two patients discontinued as a result of lack of efficacy and one because of adverse events."	( Injectable extended-release naltrexone (XR-NTX) for opioid dependence: long-term safety and effectiveness. Gastfriend, DR; Krupitsky, E; Ling, W; Memisoglu, A; Nunes, EV; Silverman, BL, 2013)	0.39
" Taken together, these results demonstrate that MPClE is a novel, potent, orally active and safe analgesic drug that targets κ-opioid receptors."	( A novel, potent, oral active and safe antinociceptive pyrazole targeting kappa opioid receptors. Athayde, ML; Boligon, AA; Bonacorso, HG; Calixto, JB; Ferreira, J; Machado, P; Martins, MA; Oliveira, SM; Rosa, F; Rossato, MF; Rubin, MA; Silva, CR; Tonello, R; Trevisan, G; Walker, CI; Zanatta, N, 2013)	0.39
" Most adverse events were mild or moderate, and transient; adverse events, including those leading to dropout, were more common with nalmefene."	( Long-term efficacy, tolerability and safety of nalmefene as-needed in patients with alcohol dependence: A 1-year, randomised controlled study. Gual, A; Mann, K; Sørensen, P; Torup, L; van den Brink, W, 2014)	0.4
" Although the weight loss produced by phentermine/topiramate is superior to naltrexone/bupropion, the safety profile of naltrexone/bupropion has less severe adverse effects."	( Drug safety evaluation of naltrexone/bupropion for the treatment of obesity. Bello, NT; Verpeut, JL, 2014)	0.4
"It is now generally recognized that upon activation by an agonist, β-arrestin associates with G protein-coupled receptors and acts as a scaffold in creating a diverse signaling network that could lead to adverse effects."	( Putative kappa opioid heteromers as targets for developing analgesics free of adverse effects. Benneyworth, MA; Kalyuzhny, AE; Le Naour, M; Lunzer, MM; Portoghese, PS; Powers, MD; Thomas, MJ, 2014)	0.4
" However, in the existing studies PHEN/TPM ER had a superior weight loss profile to lorcaserin but the incidence of adverse effects was lower with lorcaserin."	( Tolerability and safety of the new anti-obesity medications. Aldhoon-Hainerová, I; Hainer, V, 2014)	0.4
" The main measurements were monthly urine samples (efficacy) and adverse events (safety)."	( [Injectable extended-release naltrexone for opioid dependence: an open label study of long-term safety and efficacy]. Blokhina, EA; Gastfriend, DR; Krupitsky, EM; Ling, W; Memisoglu, A; Nunes, EV; Silverman, BL, 2014)	0.4
" Adverse events were reported by 21."	( [Injectable extended-release naltrexone for opioid dependence: an open label study of long-term safety and efficacy]. Blokhina, EA; Gastfriend, DR; Krupitsky, EM; Ling, W; Memisoglu, A; Nunes, EV; Silverman, BL, 2014)	0.4
"7% on nalmefene in the total population had treatment-emergent adverse events (TEAEs)."	( Safety and tolerability of as-needed nalmefene in the treatment of alcohol dependence: results from the Phase III clinical programme. Gual, A; Jensen, TJ; Mann, K; Strang, J; Sørensen, P; van den Brink, W, 2015)	0.42
" There were no serious adverse events."	( Reduction of alcohol drinking in young adults by naltrexone: a double-blind, placebo-controlled, randomized clinical trial of efficacy and safety. Corbin, WR; DeMartini, KS; Fucito, LM; Gueorguieva, R; Ikomi, J; Kranzler, HR; Leeman, RF; O'Malley, SS; Romano, DM; Sher, KJ; Toll, BA; Wu, R, 2015)	0.42
" Thus, if following the appropriate guidelines according to package labels, the practitioner can feel safe in prescribing these medications."	( Safety and tolerability of medications approved for chronic weight management. Fujioka, K, 2015)	0.42
"0% of patients in the placebo group experienced a treatment-emergent adverse event (TEAE)."	( A randomized double-blind, placebo-controlled efficacy and safety study of ALO-02 (extended-release oxycodone surrounding sequestered naltrexone) for moderate-to-severe chronic low back pain treatment. Bass, A; Bramson, C; Hale, ME; Malhotra, BK; Meisner, P; Pixton, G; Rauck, RL; Setnik, B; Sommerville, KW; Wilson, JG; Wolfram, G, 2015)	0.42
" Serious adverse effects, which were very rare, included suicidal thoughts and seizures."	( The efficacy and safety of the naltrexone/bupropion combination for the treatment of obesity: an update. Christou, GA; Kiortsis, DN, )	0.13
" The most common adverse events during methylnaltrexone treatment were abdominal pain (9."	( Efficacy and Safety of Methylnaltrexone for Opioid-Induced Constipation in Patients With Chronic Noncancer Pain: A Placebo Crossover Analysis. Barrett, AC; Forbes, WP; Paterson, C; Viscusi, ER, )	0.13
"Subgroup analysis of patients aged ≥65 years and <65 years was performed on pooled data for adverse events (AEs), potentially clinically significant laboratory values (hematology/chemistry), and signs/symptoms of opioid withdrawal using the Clinical Opiate Withdrawal Scale (COWS) (phase 3 trials only) for patients who received at least one dose (short-term studies, maximum dose was 160 mg/d or 320 mg/d depending on study; long-term study, no maximum dose) of study medication during titration and maintenance phases."	( Safety profile of extended-release morphine sulfate with sequestered naltrexone hydrochloride in older patients: pooled analysis of three clinical trials. Pixton, GC; Setnik, B; Webster, LR, 2016)	0.43
" This case should pinpoint our attention on this adverse event for a careful choice of anticraving therapy in patients with severe alcohol use disorder."	( Clinical experience about an unexpected adverse event during nalmefene treatment in two patients with alcohol use disorder. Martelli, A; Mattioli, F; Milano, G; Natta, WM; Zavan, V, 2016)	0.43
"To compare weight loss and adverse events among drug treatments for obesity using a systematic review and network meta-analysis."	( Association of Pharmacological Treatments for Obesity With Weight Loss and Adverse Events: A Systematic Review and Meta-analysis. Camilleri, M; Chandar, AK; Dulai, PS; Khera, R; Loomba, R; Murad, MH; Prokop, LJ; Singh, S; Wang, Z, 2016)	0.43
"Proportions of patients with at least 5% weight loss and at least 10% weight loss, magnitude of decrease in weight, and discontinuation of therapy because of adverse events at 1 year."	( Association of Pharmacological Treatments for Obesity With Weight Loss and Adverse Events: A Systematic Review and Meta-analysis. Camilleri, M; Chandar, AK; Dulai, PS; Khera, R; Loomba, R; Murad, MH; Prokop, LJ; Singh, S; Wang, Z, 2016)	0.43
"35) were associated with the highest odds of adverse event-related treatment discontinuation."	( Association of Pharmacological Treatments for Obesity With Weight Loss and Adverse Events: A Systematic Review and Meta-analysis. Camilleri, M; Chandar, AK; Dulai, PS; Khera, R; Loomba, R; Murad, MH; Prokop, LJ; Singh, S; Wang, Z, 2016)	0.43
"Nephrotoxicity is a major side effect of cisplatin, a widely used chemotherapy agent."	( Enhancement of Cisplatin Nephrotoxicity by Morphine and Its Attenuation by the Opioid Antagonist Naltrexone. Aminian, A; Asadi Amoli, F; Dehpour, AR; Ejtemaei Mehr, S; Javadi, S; Moghaddas, P; Rahimian, R, 2016)	0.43
" Unfortunately, we have shown that morphine administered in the acute phase of SCI results in significant, adverse secondary consequences including compromised locomotor and sensory recovery."	( Nor-Binaltorphimine Blocks the Adverse Effects of Morphine after Spinal Cord Injury. Aceves, AR; Aceves, M; Bancroft, EA; Hook, MA, 2017)	0.46
"Extended-release naltrexone (XR-NTX) is feasible and safe for treatment of opioid use disorder and alcohol use disorder in HIV clinics."	( Feasibility and safety of extended-release naltrexone treatment of opioid and alcohol use disorder in HIV clinics: a pilot/feasibility randomized trial. Ahamad, K; Arenas, V; Ha, D; Korthuis, PT; Kunkel, LE; Lindblad, R; Lum, PJ; Mandler, RN; McCarty, D; Oden, NL; Sorensen, JL; Vergara-Rodriguez, P; Wood, E, 2017)	0.46
" Often the only therapeutic option is to use class 2 or 3 analgesic opioids in the WHO classification, as class 1 analgesics may be toxic or of limited efficacy."	( [Management of adverse effects of opioid therapy]. Wirz, S, 2017)	0.46
" Safety parameters assessed included adverse events, effects on analgesia, and opioid withdrawal symptoms."	( A Phase 2b, Randomized, Double-Blind Placebo-Controlled Study to Evaluate the Efficacy and Safety of Naldemedine for the Treatment of Opioid-Induced Constipation in Patients with Chronic Noncancer Pain. Arjona Ferreira, JC; Webster, LR; Yamada, T, 2017)	0.46
" Treatment-emergent adverse events were generally mild to moderate in severity; incidences increased with naldemedine dose."	( A Phase 2b, Randomized, Double-Blind Placebo-Controlled Study to Evaluate the Efficacy and Safety of Naldemedine for the Treatment of Opioid-Induced Constipation in Patients with Chronic Noncancer Pain. Arjona Ferreira, JC; Webster, LR; Yamada, T, 2017)	0.46
"This is the first study to compare frequency of sexual side effect reporting between paroxetine and desipramine."	( A Comparison of Sexual Side Effects of Antidepressants With and Without Naltrexone. Petrakis, I; Ralevski, E; Thapa, M, )	0.13
"The most common adverse events were gastrointestinal related (e."	( Long-Term Safety and Efficacy of Subcutaneous Methylnaltrexone in Patients with Opioid-Induced Constipation and Chronic Noncancer Pain: A Phase 3, Open-Label Trial. Harper, JR; Israel, RJ; Khan, A; Michna, E; Webster, LR, 2017)	0.46
"Naldemedine (S-297995) is a peripherally acting μ-opioid receptor antagonist for the treatment of opioid-induced constipation, a common side effect of opioid therapy."	( Phase 1, Randomized, Double-Blind, Placebo-Controlled Studies on the Safety, Tolerability, and Pharmacokinetics of Naldemedine in Healthy Volunteers. Arjona Ferreira, JC; Baba, Y; Fukumura, K; Yokota, T, 2018)	0.48
"Data on retention, use of heroin and other illicit substances, opioid craving, treatment satisfaction, addiction-related problems and adverse events were reported every fourth week."	( Effectiveness, safety and feasibility of extended-release naltrexone for opioid dependence: a 9-month follow-up to a 3-month randomized trial. Benth, JŠ; Krajci, P; Kunoe, N; Latif, ZE; Opheim, A; Sharma-Haase, K; Solli, KK; Tanum, L, 2018)	0.48
"Opioid-dependent individuals who elect to switch from buprenorphine-naltrexone treatment after 3 months to extended-release naltrexone treatment for 9 months appear to experience similar treatment completion and abstinence rates and similar adverse event profiles to individuals who had been on extended-release naltrexone from the start of treatment."	( Effectiveness, safety and feasibility of extended-release naltrexone for opioid dependence: a 9-month follow-up to a 3-month randomized trial. Benth, JŠ; Krajci, P; Kunoe, N; Latif, ZE; Opheim, A; Sharma-Haase, K; Solli, KK; Tanum, L, 2018)	0.48
"Constipation is the most common chronic adverse effect of opioid pain medications in patients who require long-term opioid administration, such as patients with advanced cancer, but conventional measures for ameliorating constipation often are insufficient."	( Identifying and Treating Opioid Side Effects: The Development of Methylnaltrexone. Moss, J, 2019)	0.51
" No opioid withdrawal was observed in any subject, and no significant adverse effects were reported by the subjects during the study."	( Identifying and Treating Opioid Side Effects: The Development of Methylnaltrexone. Moss, J, 2019)	0.51
") of amfetamine or methamfetamine after naltrexone treatment, adverse events and physiological changes (e."	( Efficacy and safety of naltrexone for amfetamine and methamfetamine use disorder: a systematic review of randomized controlled trials. Anand, S; Chan, EW; Lam, L; Li, X; Tse, ML; Zhao, JX, 2019)	0.51
" Both amfetamine and methamfetamine studies showed good tolerability of naltrexone, with few adverse events seen."	( Efficacy and safety of naltrexone for amfetamine and methamfetamine use disorder: a systematic review of randomized controlled trials. Anand, S; Chan, EW; Lam, L; Li, X; Tse, ML; Zhao, JX, 2019)	0.51
" The aim of this review was to extensively evaluate the safety of oral naltrexone by examining the risk of serious adverse events and adverse events in randomised controlled trials of naltrexone compared to placebo."	( Serious adverse events reported in placebo randomised controlled trials of oral naltrexone: a systematic review and meta-analysis. Boda, S; Bolton, M; Hodkinson, A; Mould, A; Panagioti, M; Rhodes, S; Riste, L; van Marwijk, H, 2019)	0.51
" Twenty-six studies (4,960 participants) recorded serious adverse events occurring by arm of study."	( Serious adverse events reported in placebo randomised controlled trials of oral naltrexone: a systematic review and meta-analysis. Boda, S; Bolton, M; Hodkinson, A; Mould, A; Panagioti, M; Rhodes, S; Riste, L; van Marwijk, H, 2019)	0.51
"Naltrexone does not appear to increase the risk of serious adverse events over placebo."	( Serious adverse events reported in placebo randomised controlled trials of oral naltrexone: a systematic review and meta-analysis. Boda, S; Bolton, M; Hodkinson, A; Mould, A; Panagioti, M; Rhodes, S; Riste, L; van Marwijk, H, 2019)	0.51
" Central nervous system-active medications have the potential to affect mood; therefore, post hoc analysis of clinical trial data was conducted to evaluate psychiatric adverse events (PAEs) and effects on mood of NB therapy versus placebo."	( Psychiatric adverse events and effects on mood with prolonged-release naltrexone/bupropion combination therapy: a pooled analysis. Acevedo, LM; Apovian, CM; Dunayevich, E; Greenway, FL; McElroy, SL; Pi-Sunyer, X, 2019)	0.51
"An investigational new eye drop containing 20 μg/ml NTX effectively reversed tear film deficits and restored corneal surface sensitivity in diabetic animals without causing toxic side effects."	( Efficacy and safety of a novel naltrexone treatment for dry eye in type 1 diabetes. McLaughlin, PJ; Sassani, JW; Titunick, MB; Zagon, IS, 2019)	0.51
" Three patients had adverse outcomes or complications, with only one (0."	( Methylnaltrexone is safe in cancer patients with peritoneal carcinomatosis. Mendelsohn, RB; Nelson, KK; Schattner, MA, 2019)	0.51
"Opioid-induced constipation (OIC), the most common side effect of opioid treatment, is under-recognized and undertreated in older patients."	( Safety and Efficacy of Naldemedine for the Treatment of Opioid-Induced Constipation in Patients with Chronic Non-Cancer Pain Receiving Opioid Therapy: A Subgroup Analysis of Patients ≥ 65 Years of Age. Hale, M; Webster, L; Wild, J; Yamada, T, 2020)	0.56
" Safety assessments included overall incidence of treatment-emergent adverse events (TEAEs), TEAEs in the gastrointestinal disorders System Organ Class, and TEAEs of opioid withdrawal or possible opioid withdrawal."	( Safety and Efficacy of Naldemedine for the Treatment of Opioid-Induced Constipation in Patients with Chronic Non-Cancer Pain Receiving Opioid Therapy: A Subgroup Analysis of Patients ≥ 65 Years of Age. Hale, M; Webster, L; Wild, J; Yamada, T, 2020)	0.56
" We analyzed adverse event data from ART-naïve participants (N = 155) who were randomized (2:1) to initiate ART plus NTX (N = 103) or ART plus placebo (N = 52)."	( Safety of oral naltrexone in HIV-positive men who have sex with men and transgender women with alcohol use disorder and initiating antiretroviral therapy. Altice, FL; Ding, R; Duerr, A; Gonzales, P; Grieco, A; Ignacio, RB; Lama, JR; Pinto-Santini, D; White, E, 2020)	0.56
" Adverse events (AEs) occurred in 54."	( Efficacy and Safety of a Combination of Olanzapine and Samidorphan in Adult Patients With an Acute Exacerbation of Schizophrenia: Outcomes From the Randomized, Phase 3 ENLIGHTEN-1 Study. DiPetrillo, L; Jiang, Y; Kunovac, J; McDonnell, D; Potkin, SG; Silverman, BL; Simmons, A, 2020)	0.56
"Over the past several decades, many antiobesity drugs have been withdrawn from the market due to unanticipated adverse events, often involving cardiotoxicity."	( The cardiovascular safety of antiobesity drugs-analysis of signals in the FDA Adverse Event Report System Database. Gorelik, B; Gorelik, E; Hirsh-Raccah, B; Masarwa, R; Matok, I; Perlman, A, 2020)	0.56
"We used the US Food and Drug Administration Adverse Event Reporting System (FAERS) database and retrieved data from January 2013 through December 2018."	( The cardiovascular safety of antiobesity drugs-analysis of signals in the FDA Adverse Event Report System Database. Gorelik, B; Gorelik, E; Hirsh-Raccah, B; Masarwa, R; Matok, I; Perlman, A, 2020)	0.56
"During the evaluated period, a total of 6,787,840 adverse event reports were submitted to FAERS."	( The cardiovascular safety of antiobesity drugs-analysis of signals in the FDA Adverse Event Report System Database. Gorelik, B; Gorelik, E; Hirsh-Raccah, B; Masarwa, R; Matok, I; Perlman, A, 2020)	0.56
" Treatment-emergent adverse events during the study period were recorded and change from baseline in the number of heavy drinking days and total alcohol consumption were calculated."	( Long-term safety and efficacy of nalmefene in Japanese patients with alcohol dependence. Higuchi, S; Meulien, D; Miyata, H; Murai, Y; Nakamura, I; Takahashi, M; Tsuneyoshi, K, 2020)	0.56
"Overall, long-term nalmefene 20 mg was well tolerated; the main treatment-emergent adverse events reported in ≥5% of patients included nasopharyngitis (37."	( Long-term safety and efficacy of nalmefene in Japanese patients with alcohol dependence. Higuchi, S; Meulien, D; Miyata, H; Murai, Y; Nakamura, I; Takahashi, M; Tsuneyoshi, K, 2020)	0.56
" Assessments included adverse events (AEs), weight, vital signs, Positive and Negative Syndrome Scale (PANSS), and Clinical Global Impression-Severity (CGI-S) scores."	( Long-term safety and durability of effect with a combination of olanzapine and samidorphan in patients with schizophrenia: results from a 1-year open-label extension study. Arevalo, C; Graham, C; Jiang, Y; McDonnell, D; Simmons, A; Yagoda, S, 2021)	0.62
" To offer more effective medical interventions to treat or prevent OUD, antiopioid vaccines are in development that reduce the distribution of the targeted opioids to brain and subsequently reduce the associated behavioral and toxic effects."	( Combining a Candidate Vaccine for Opioid Use Disorders with Extended-Release Naltrexone Increases Protection against Oxycodone-Induced Behavioral Effects and Toxicity. Accetturo, C; Pravetoni, M; Raleigh, MD, 2020)	0.56
" However, opioids are associated with adverse events, such as constipation and emesis/vomiting."	( Naldemedine: Peripherally Acting Opioid Receptor Antagonist for Treating Opioid-induced Adverse Effects. Inagaki, M; Kanemasa, T; Yokota, T, 2020)	0.56
" However, they are costly and may have adverse effects in some individuals."	( Long-Term Efficacy and Safety of Anti-Obesity Treatment: Where Do We Stand? Lee, SY; Tak, YJ, 2021)	0.62
" The purpose of the study is to determine the relationship between these treatments and the risk of major cardiovascular adverse events (MACE)."	( Cardiovascular safety of naltrexone and bupropion therapy: Systematic review and meta-analyses. Aguilar-Salinas, C; Benchimol, A; Bonilha, I; Carvalho, LSF; Cercato, C; Geloneze, B; Hohl, A; Luchiari, B; Moura, F; Nadruz, W; Sposito, AC, 2021)	0.62
" Eight and fifty-two adverse events were reported in the naltrexone and amitriptyline groups, respectively (P < ."	( Efficacy and safety of low-dose naltrexone in painful diabetic neuropathy: A randomized, double-blind, active-control, crossover clinical trial. Bansal, D; Bhansali, AK; Chakrabarti, A; Dutta, P; Hota, D; Srinivasan, A, 2021)	0.62
" Assessments included adverse events (AEs; each visit), weight/waist circumference (every other week for the first 8 weeks, then every 4 weeks thereafter), metabolic laboratory parameters (weeks 4, 12, 24, 36, and 52), Positive and Negative Syndrome Scale (PANSS) scores (weeks 2, 4, 8, 12, 24, 36, and 52), and Clinical Global Impression-Severity (CGI-S) scores (weeks 2 and 4, then every 4 weeks thereafter through week 48, and at week 52)."	( A phase 3, multicenter study to assess the 1-year safety and tolerability of a combination of olanzapine and samidorphan in patients with schizophrenia: Results from the ENLIGHTEN-2 long-term extension. Bhupathi, V; DiPetrillo, L; Graham, C; Hopkinson, C; Jiang, Y; Kahn, RS; McDonnell, D; Silverman, BL; Simmons, A; Yagoda, S; Yin, J; Yu, B, 2021)	0.62
" The most frequently reported adverse drug reactions (ADRs) were nausea (4."	( Safety and Persistence of Nalmefene Treatment for Alcohol Dependence. Results from Two Post-authorisation Safety Studies. Andersohn, F; Borchert, K; Braun, S; Chick, J; Guillo, S; Haas, JS; Kuppan, K; Lemming, OM; Reines, EH; Toussi, M; Tubach, F, 2021)	0.62
" The purpose of this study was to determine if MNTX is effective and safe for POI treatment."	( The Efficacy and Safety of Methylnaltrexone for the Treatment of Postoperative Ileus. Atchison, L; Beavers, J; Dennis, B; Guillamondegui, O; Medvecz, A; Orton, L; Smith, MC, 2022)	0.72
" In the safety analysis, adverse drug reactions (ADRs), including diarrhea as a special interest, were assessed."	( Post-marketing surveillance of the safety and effectiveness of naldemedine in the management of opioid-induced constipation in patients with cancer pain in Japan. Hashimoto, S; Honda, K; Nakazawa, M; Takata, K, 2022)	0.72
" Preclinical data regarding the abuse potential and other opioid-like adverse effects of tianeptine at supratherapeutic doses are sparse."	( Opioid-like adverse effects of tianeptine in male rats and mice. Akbarali, HI; Baird, TR; Dewey, WL; Elder, H; Kang, M; Marsh, SA; Negus, SS; Peace, MR; Poklis, JL; Santos, EJ, 2022)	0.72
"The present study evaluated tianeptine in a rat model of abuse potential assessment and in mouse models of motor, gastrointestinal, and respiratory adverse effects."	( Opioid-like adverse effects of tianeptine in male rats and mice. Akbarali, HI; Baird, TR; Dewey, WL; Elder, H; Kang, M; Marsh, SA; Negus, SS; Peace, MR; Poklis, JL; Santos, EJ, 2022)	0.72
" Nonetheless, tianeptine produces MOR agonist-like acute adverse effects that include motor impairment, constipation, and respiratory depression."	( Opioid-like adverse effects of tianeptine in male rats and mice. Akbarali, HI; Baird, TR; Dewey, WL; Elder, H; Kang, M; Marsh, SA; Negus, SS; Peace, MR; Poklis, JL; Santos, EJ, 2022)	0.72
" Diarrhea was the most common adverse event in all grades, occurring in 11 patients (27."	( A retrospective study of the efficacy and safety of naldemedine for opioid-induced constipation in thoracic cancer patients. Arai, K; Fujita, Y; Hiruta, E; Imai, H; Kaira, K; Kamiya, T; Masuno, T; Minato, K; Mogi, J; Nishiba, H; Sandoh, M; Takei, S; Tanaka, H; Yamazaki, S, 2022)	0.72
" While they can offer excellent analgesia, their use can be limited by adverse effects, including constipation, respiratory depression, tolerance, and abuse liability."	( OREX-1038: a potential new treatment for pain with low abuse liability and limited adverse effects. Acevedo, L; Belli, B; Cami-Kobeci, G; Flynn, P; France, CP; Gerak, LR; Husbands, SM; Maguire, DR; Olson, KM; Traynor, JR, 2022)	0.72
" Conclusion: Naltrexone is safe to use in patients with underlying LD, including those with compensated cirrhosis."	( Naltrexone for alcohol use disorder: Hepatic safety in patients with and without liver disease. Ayyala, D; Bottyan, T; Dodge, JL; Gonzalez, JL; Han, H; Pimienta, M; Stager, K; Stolz, A; Terrault, NA; Tien, C; Yoo, J, 2022)	0.72

Pharmacokinetics

The pharmacokinetic parameters of carfentanil and naltrexone were determined in the common eland (Taurotragus oryx) This is the first human pharmacokinetics and pharmacodynamic drug interaction study of acamprosate and nALTrexone. Pharmacokinetic analysis indicated that naltxone has a terminal elimination half-life of 4.

Excerpt	Reference	Relevance
" From our pharmacokinetic data an apparent chronic release rate (ACRR) for a sustained release preparation of naltrexone was calculated as 11."	( Estimation of the systemic availability and other pharmacokinetic parameters of naltrexone in man after acute and chronic oral administration. Kogan, MJ; Mule, SJ; Verebey, K, 1977)	0.26
" Although morphine coadministration did not significantly affect the terminal half-life of naltrexone, its clearances or apparent volumes of distribution by t-test of the differences between averages (with each dog equally weighted), drug coadministration did significantly (by t-test) affect the fraction of naltrexone dose secreted into bile as conjugate (fB), the fraction of the dose excreted as conjugate in urine, and the fraction excreted elsewhere (f'B)."	( Pharmacokinetics of morphine and its surrogates. XI: Effect of simultaneously administered naltrexone and morphine on the pharmacokinetics and pharmacodynamics of each in the dog. Garrett, ER; Khan, PJ; Langguth, P, 1990)	0.28
" The method requires calibration of the pharmacokinetic parameters of each monkey utilizing an intravenous bolus dose and assay of unchanged naltrexone levels in plasma as a function of time after dosing."	( Pharmacokinetic quantitation of naltrexone controlled release from a copolymer delivery system. Ashcraft, SB; Downs, DA; Harrigan, SE; Liao, SH; Reuning, RH; Staubus, AE; Wiley, JN; Wise, DL, 1983)	0.27
" The method consists of two phases: a single intravenous bolus dose quantitation of each monkey's pharmacokinetic parameters coupled with a delivery system study in which plasma naltrexone levels are measured throughout the time period of sustained-release."	( Pharmacokinetic quantitation of naltrexone release from several sustained-release delivery systems. Liao, SH; Reuning, RH; Staubus, AE, 1981)	0.26
"33 hours every hour, respectively), the area under the serum fentanyl concentration curve appeared to be independent of the time of infusion."	( Evaluation of diurnal variation in fentanyl clearance. Gupta, SK; Hwang, SS; Southam, MA, 1995)	0.29
"5 mg/kg) on the pharmacokinetic parameters area under the serum morphine concentration time curve (AUC0-->infinity), serum levels of morphine extrapolated to zero time (Cmax), half-life (t1/2), mean residence time (MRT), total body clearance (Clt), and volume of distribution at steady state (Vss) of morphine in serum was determined."	( Effects of naltrexone on pharmacodynamics and pharmacokinetics of intravenously administered morphine in the rat. Bhargava, HN; Larsen, AK; Rahmani, NH; Villar, VM, 1993)	0.29
" To determine the applicability of this method for human pharmacokinetic studies, nalmefene levels in plasma were measured at time points up to 24 h following oral and intravenous administration of 30 mg of nalmefene hydrochloride to two subjects."	( Determination of nalmefene in plasma by high-performance liquid chromatography with electrochemical detection and its application in pharmacokinetic studies. Albeck, H; Chou, JZ; Kreek, MJ, 1993)	0.29
" The concentration-time data were analyzed by noncompartmental methods and subsequently linked to the pharmacodynamic effect data by a competitive antagonism link model."	( Duration of opioid antagonism by nalmefene and naloxone in the dog: an integrated pharmacokinetic/pharmacodynamic comparison. Osifchin, E; Veng-Pedersen, P; Waters, SJ; Wilhelm, JA; Zakszewski, TB, 1995)	0.29
"The opioid antagonist nalmefene was compared in its pharmacodynamic properties to the structurally similar antagonist naloxone in a 2 x 2 cross-over study with 8 dogs."	( Duration of opioid antagonism by nalmefene and naloxone in the dog. A nonparametric pharmacodynamic comparison based on generalized cross-validated spline estimation. Osifchin, E; Veng-Pedersen, P; Waters, SJ; Wilhelm, JA; Zakszewski, TB, 1995)	0.29
" Terminal elimination half-life (t1/2) of both nalmefene and nalmefene glucuronide was prolonged in patients with ESRD compared with that in participants with normal renal function."	( The effect of renal insufficiency and hemodialysis on the pharmacokinetics of nalmefene. Alexander, AC; Dixon, R; Frye, RF; Johnston, J; Matzke, GR; Rault, RM; Reynolds, R, 1996)	0.29
" The elderly volunteers also had a significantly shorter distributional half-life (t1/2 lambda 1) than young volunteers (0."	( The effect of age on the pharmacokinetics of the opioid antagonist nalmefene. Bikhazi, GB; Frye, RF; Jallad, NS; Matzke, GR; Wilhelm, JA, 1996)	0.29
" Pharmacokinetic analysis revealed an elimination half-life of 117."	( Safety and tolerance of methylnaltrexone in healthy humans: a randomized, placebo-controlled, intravenous, ascending-dose, pharmacokinetic study. Foss, JF; Moss, J; Murphy, M; O'Connor, MF; Roizen, MF; Yuan, CS, 1997)	0.3
" Pharmacodynamic endpoints evaluated were respiratory depression, measured as the change in arterial blood pCO(2), pO(2), and pH levels; and antinociception, measured by the tail-flick technique."	( Pharmacokinetic-pharmacodynamic modeling of the antinociceptive effects of main active metabolites of tramadol, (+)-O-desmethyltramadol and (-)-O-desmethyltramadol, in rats. Calvo, R; Garrido, MJ; Pavón, JM; Trocóniz, IF; Valle, M, 2000)	0.31
" Concentration-time data were analyzed by a limited sampling strategy with adult pharmacokinetic parameters used as Bayesian priors."	( Nalmefene to prevent epidural narcotic side effects in pediatric patients: a pharmacokinetic and safety study. Chang, CT; Frye, RF; Gustafson, RA; Morris, JL; Nelson, ER; Rosen, DA; Rosen, KR; Steelman, RJ; Thackara, JW; Wilhelm, JA, 2000)	0.31
"5 Hz frequency band of the EEG as pharmacodynamic endpoint."	( Pharmacokinetic-pharmacodynamic analysis of the EEG effect of alfentanil in rats following beta-funaltrexamine-induced mu-opioid receptor "knockdown" in vivo. Cox, E; Danhof, M; Garrido, M; Gubbens-Stibbe, J; IJzerman, A; Künzel, D; Tukker, E; van der Graaf, PH; von Frijtag, J, 2000)	0.31
" The serum drug concentration-time profile fitted a two-compartment pharmacokinetic model."	( Pharmacokinetic profile of epidurally administered methylnaltrexone, a novel peripheral opioid antagonist in a rabbit model. Chan, VW; El Behiery, H; Foss, JF; Murph, DB, 2001)	0.31
" Thus, this is the first human pharmacokinetic and pharmacodynamic drug interaction study of acamprosate and naltrexone."	( A pharmacokinetic and pharmacodynamic drug interaction study of acamprosate and naltrexone. Boyeson, MG; Dixon, RM; Goodman, AM; Hameed, MH; Hulot, T; Hunter, JA; Mason, BJ; Wesnes, K, 2002)	0.31
" Pharmacokinetic studies in rats demonstrated that this formulation produced stable, pharmacologically relevant plasma levels of naltrexone for approximately 1 month following either subcutaneous or intramuscular injections."	( Vivitrex, an injectable, extended-release formulation of naltrexone, provides pharmacokinetic and pharmacodynamic evidence of efficacy for 1 month in rats. Bartus, RT; Basile, AS; Blaustein, M; Dean, RL; Emerich, DF; Hotz, J; Perdomo, B, 2003)	0.32
" The Cmax at the inlet and at the outlet the dialyzer were higher (255+/-117 ng/mL and 206+/-137 ng/ml respectively) in comparison with healthy subjects (9 - 44 ng/mL)."	( Pharmacokinetics and dialysability of naltrexone in patients undergoing hemodialysis. Azar, R; Bah, S; Brunet, C; Dine, T; Dupin-Spriet, T; Gressier, B; Kambia, NK; Luyckx, M; Odou, P, )	0.13
"Human pharmacokinetic parameters are often predicted prior to clinical study from in vivo preclinical pharmacokinetic data."	( Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure. Jolivette, LJ; Ward, KW, 2005)	0.33
" Based on pharmacokinetic considerations, the dose of long-acting naltrexone does not need to be adjusted in patients with mild or moderate hepatic impairment."	( Pharmacokinetics of long-acting naltrexone in subjects with mild to moderate hepatic impairment. Dilzer, SC; Dong, Q; Dunbar, JL; Ehrich, EW; Lasseter, KC; Silverman, BL; Turncliff, RZ, 2005)	0.33
" Steady state was reached within 5 days, consistent with the observed median half-life of approximately 22 hours following multiple doses."	( Single-dose and steady-state pharmacokinetics of fentanyl buccal tablet in healthy volunteers. Darwish, M; Hellriegel, E; Jiang, JG; Kirby, M; Robertson, P, 2007)	0.34
"The objective of this study was to compare the pharmacokinetic profile of a novel, once-daily, controlled-release formulation of hydromorphone (OROS hydromorphone) under fasting conditions with that immediately after a high-fat breakfast in healthy volunteers."	( Pharmacokinetic profile of a 24-hour controlled-release OROS formulation of hydromorphone in the presence and absence of food. Gupta, SK; Sathyan, G; Thipphawong, J; Xu, E, 2007)	0.34
" Confidence intervals were within 80% to 125% for AUC0-t and AUC0-infinity but were slightly higher for Cmax (105."	( Pharmacokinetic profile of a 24-hour controlled-release OROS formulation of hydromorphone in the presence and absence of food. Gupta, SK; Sathyan, G; Thipphawong, J; Xu, E, 2007)	0.34
"The pharmacokinetic parameters of carfentanil and naltrexone were determined in the common eland (Taurotragus oryx)."	( Pharmacokinetics and pharmacodynamics of carfentanil and naltrexone in female common eland (Taurotragus oryx). Carpenter, JW; Cole, A; Dresser, BL; Hunter, RP; Isaza, R; Koch, DE; Mutlow, A, 2006)	0.33
" A population pharmacokinetic (PPK) analysis examined the possibility of altered pharmacokinetics for naltrexone and its primary metabolite, 6beta-naltrexol, in subpopulations with a potential for alcohol-dependence treatment."	( Population pharmacokinetics of extended-release injectable naltrexone (XR-NTX) in patients with alcohol dependence. Dunbar, JL; Farrell, CB; Hayes, SC; Turncliff, RZ, 2007)	0.34
" pharmacokinetic data on 670 drugs representing, to our knowledge, the largest publicly available set of human clinical pharmacokinetic data."	( Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds. Lombardo, F; Obach, RS; Waters, NJ, 2008)	0.35
" After the single intravenous dose trial, 8 healthy volunteers received intravenous nalmefene at 2 mg once daily for 6 consecutive days, and the plasma drug concentrations were determined on the morning of days 4, 5 and 6 using liquid chromatography/tandem mass spectrometry and the pharmacokinetic parameters were calculated using PKS program."	( [Pharmacokinetics of nalmefene after a single or multiple intravenous doses in Chinese healthy volunteers]. Liao, RF; Wen, YG; Zeng, ZP, 2008)	0.35
" These results showed that plasma 6beta-naltrexol fits to a two compartment model with first-order absorption in dog after intramuscular administration and their pharmacokinetic parameters were reported."	( [Pharmacokinetics of 6beta-naltrexol after single and multiple intramuscular injections in Beagle dogs]. Cui, MX; Dong, HJ; Gong, ZH; Liu, J; Liu, YS; Yan, LD; Yao, XJ, 2009)	0.35
" Plasma samples were collected just before dosing through 72 hours postdose for pharmacokinetic analyses of morphine, and through 168 hours postdose for naltrexone and its major metabolite 6-β-naltrexol."	( Food effects on the pharmacokinetics of morphine sulfate and naltrexone hydrochloride extended release capsules. Boudriau, S; Ciric, S; Johnson, F; Stauffer, J; Swearingen, D, 2010)	0.36
"Studies conducted to date indicate that methylnaltrexone has high bioavailability after subcutaneous administration at therapeutic dose levels, a terminal half-life of ∼ 8 - 9 h, minimal metabolism, elimination involving renal and non-renal routes, and a limited potential for drug-drug interactions."	( Methylnaltrexone bromide: research update of pharmacokinetics following parenteral administration. Boyd, TA; Rotshteyn, Y; Yuan, CS, 2011)	0.37
" Furthermore, pharmacokinetic parameters of the drug in human plasma samples of healthy volunteers following the administration of an oral single dose of 50mg NAL."	( Voltammetry of naltrexone in commercial formulation and human body fluids: Quantification and pharmacokinetic studies. Abdel-Galeil, MM; El-Desoky, HS; Ghoneim, MM, 2011)	0.37
" This open-label, single-dose, 4-way crossover, pharmacokinetic drug interaction study compared the relative bioavailability of morphine and naltrexone when MS-sNT is administered (under fasting conditions) with increasing doses of alcohol."	( Effects of alcohol on the pharmacokinetics of morphine sulfate and naltrexone hydrochloride extended release capsules. Boudriau, S; Ciric, S; Johnson, FK; Kisicki, J; Stauffer, J, 2012)	0.38
" The oral pharmacodynamic study assessed drug liking and euphoria and pharmacokinetic properties of MS-sNTC and MS-sNTW compared with morphine sulfate solution (MSS) and placebo."	( Morphine sulfate and naltrexone hydrochloride extended-release capsules: naltrexone release, pharmacodynamics, and tolerability. Johnson, F; Setnik, B, )	0.13
" Tramadol is thought to have limited abuse potential compared to mu opioid agonists, but laboratory data indicate that it shares some of their pharmacodynamic effects."	( Pharmacodynamic profile of tramadol in humans: influence of naltrexone pretreatment. Craig, LB; Lofwall, MR; Nuzzo, PA; Siegel, AJ; Stoops, WW; Walsh, SL, 2012)	0.38
"This study evaluated the effect of mu opioid receptor blockade with naltrexone on the pharmacodynamic action of tramadol in humans."	( Pharmacodynamic profile of tramadol in humans: influence of naltrexone pretreatment. Craig, LB; Lofwall, MR; Nuzzo, PA; Siegel, AJ; Stoops, WW; Walsh, SL, 2012)	0.38
" Pharmacodynamic effects were measured before and for 7 h after initial drug administration."	( Pharmacodynamic profile of tramadol in humans: influence of naltrexone pretreatment. Craig, LB; Lofwall, MR; Nuzzo, PA; Siegel, AJ; Stoops, WW; Walsh, SL, 2012)	0.38
"The results of the current study of an ER formulation revealed no pharmacokinetic features that would preclude dosing in the elderly."	( An open-label pharmacokinetic study of oxymorphone extended release in the presence of naltrexone in the older adult. Gould, EM; Labhsetwar, S; Nagar, S; Pergolizzi, JV; Raffa, RB; Sinclair, N; Taylor, R, )	0.13
"The in vivo preclinical pharmacodynamic profile of TD-1211, a selective opioid receptor antagonist currently under development for the treatment of opioid-induced constipation, was compared to that of the clinically studied opioid antagonists, naltrexone, alvimopan, and ADL 08-0011 (the primary active metabolite of alvimopan)."	( The in vivo pharmacodynamics of the novel opioid receptor antagonist, TD-1211, in models of opioid-induced gastrointestinal and CNS activity. Armstrong, SR; Beattie, DT; Campbell, CB; Hegde, SS; Long, DD; Richardson, CL; Tsuruda, PR; Vickery, RG, 2013)	0.39
"To compare the pharmacodynamic effects, including self-reports of "drug liking" and "high," of crushed morphine sulfate and naltrexone hydrochloride extended-release capsules (MSN), crushed morphine sulfate controlled-release (CR) tablets, and placebo in an abuse potential study."	( Assessment of pharmacodynamic effects following oral administration of crushed morphine sulfate and naltrexone hydrochloride extended-release capsules compared with crushed morphine sulfate controlled-release tablets and placebo in nondependent recreation Goli, V; Han, L; Setnik, B; Sommerville, K; Webster, L, 2013)	0.39
"Subjective ratings (100-point visual analog scales) of positive drug effects (drug liking, high, good effects, take drug again, and overall drug liking), any effects, and negative effects (bad effects, feel sick, nausea, sleepy, and dizzy), along with pupillometry, pharmacokinetic (PK), and safety assessments."	( Assessment of pharmacodynamic effects following oral administration of crushed morphine sulfate and naltrexone hydrochloride extended-release capsules compared with crushed morphine sulfate controlled-release tablets and placebo in nondependent recreation Goli, V; Han, L; Setnik, B; Sommerville, K; Webster, L, 2013)	0.39
" PK analysis of morphine plasma concentrations indicated that Cmax was significantly lower and tmax significantly longer for crushed MSN compared with crushed morphine sulfate CR."	( Assessment of pharmacodynamic effects following oral administration of crushed morphine sulfate and naltrexone hydrochloride extended-release capsules compared with crushed morphine sulfate controlled-release tablets and placebo in nondependent recreation Goli, V; Han, L; Setnik, B; Sommerville, K; Webster, L, 2013)	0.39
" These results provide pharmacokinetic support for the long-lasting antagonistic effects of nor-BNI."	( Pharmacokinetic evidence for the long-lasting effect of nor-binaltorphimine, a potent kappa opioid receptor antagonist, in mice. Kiguchi, N; Kishioka, S; Ko, MC; Kobayashi, Y; Saika, F; Wakida, N; Woods, JH; Yamamoto, C, 2013)	0.39
" In both studies, samidorphan was rapidly absorbed, with a Tmax of 1 hour, and AUC increased with increasing dose."	( Single- and multiple-dose pharmacokinetics of samidorphan, a novel opioid antagonist, in healthy volunteers. DiPetrillo, L; Ehrich, E; Silverman, B; Turncliff, R, 2015)	0.42
"In these single- and multiple-dose studies in healthy volunteers, samidorphan exhibited a pharmacokinetic profile consistent with once-daily dosing."	( Single- and multiple-dose pharmacokinetics of samidorphan, a novel opioid antagonist, in healthy volunteers. DiPetrillo, L; Ehrich, E; Silverman, B; Turncliff, R, 2015)	0.42
" The 90 % confidence intervals (CIs) for AUC∞ and Cmax ratios of ALO-02 with 20 % ethanol versus water were within 80-125 %; upper 90 % CIs were >125 % for ALO-02 with 40 % ethanol versus water."	( Effects of ethanol on the pharmacokinetics of extended-release oxycodone with sequestered naltrexone (ALO-02). Bramson, C; Malhotra, BK; Matschke, K; Salageanu, J; Wang, Q, 2015)	0.42
"Oxycodone exposures (Cmax) were unaffected when ALO-02 was administered with 20 % ethanol but Cmax increased by 37 % with 40 % ethanol versus water."	( Effects of ethanol on the pharmacokinetics of extended-release oxycodone with sequestered naltrexone (ALO-02). Bramson, C; Malhotra, BK; Matschke, K; Salageanu, J; Wang, Q, 2015)	0.42
"The aims of this study were to develop a population pharmacokinetic (PK) model to describe the PK of nalmefene in healthy subjects and to relate the exposure of nalmefene to the μ-opioid receptor occupancy by simulations in the target population."	( Population pharmacokinetics of nalmefene in healthy subjects and its relation to μ-opioid receptor occupancy. Areberg, J; Faerch, KU; Kyhl, LE; Larsen, F; Li, S; Soegaard, B, 2016)	0.43
"The t1/2 and Tmax values for oxycodone were similar for all 3 treatments."	( Effect of food on the pharmacokinetics of oxycodone and naltrexone from ALO-02, an extended release formulation of oxycodone with sequestered naltrexone. Bramson, C; Gandelman, K; Lamson, M; Malhotra, B; Matschke, K; Salageanu, J, 2015)	0.42
" We determined the safety, tolerability, and pharmacokinetic profiles of oral naldemedine in healthy volunteers in 2 randomized, double-blind, placebo-controlled, phase 1 studies."	( Phase 1, Randomized, Double-Blind, Placebo-Controlled Studies on the Safety, Tolerability, and Pharmacokinetics of Naldemedine in Healthy Volunteers. Arjona Ferreira, JC; Baba, Y; Fukumura, K; Yokota, T, 2018)	0.48
"To characterize population pharmacokinetic (PK) of naldemedine, to identify factors which influence naldemedine PK, and to evaluate their clinical relevancy based on exposure-response relationships."	( Population Pharmacokinetics and Exposure-Response Relationships of Naldemedine. Fukumura, K; Kubota, R; Wajima, T, 2018)	0.48
" Pharmacokinetic parameters were calculated according to noncompartmental analysis."	( Pharmacokinetics and Short-term Safety of ALKS 3831, a Fixed-dose Combination of Olanzapine and Samidorphan, in Adult Subjects with Schizophrenia. McDonnell, D; Sun, L; von Moltke, L, 2018)	0.48
" At steady state, exposure to olanzapine increased dose proportionally from 10 mg (ALKS 3831 10/10) to 20 mg (ALKS 3831 20/10), and exposure to samidorphan was similar between the 2 ALKS 3831 dose groups, indicating that different dose levels of olanzapine in ALKS 3831 had no impact on the pharmacokinetic profile of samidorphan."	( Pharmacokinetics and Short-term Safety of ALKS 3831, a Fixed-dose Combination of Olanzapine and Samidorphan, in Adult Subjects with Schizophrenia. McDonnell, D; Sun, L; von Moltke, L, 2018)	0.48
" The present data indicate that combining olanzapine with samidorphan does not affect the pharmacokinetic profile of either drug and support continued clinical evaluation of ALKS 3831."	( Pharmacokinetics and Short-term Safety of ALKS 3831, a Fixed-dose Combination of Olanzapine and Samidorphan, in Adult Subjects with Schizophrenia. McDonnell, D; Sun, L; von Moltke, L, 2018)	0.48
" Olanzapine and samidorphan pharmacokinetic parameters were determined after OLZ/SAM dosing on days 1 and 22."	( A Phase I Open-Label Study to Evaluate the Effects of Rifampin on the Pharmacokinetics of Olanzapine and Samidorphan Administered in Combination in Healthy Human Subjects. Kumar, V; McDonnell, D; Sun, L; von Moltke, L; Yu, M, 2019)	0.51
" We report clinical pharmacokinetic (PK) properties of SAM following different routes of administration, and the effects of food and age on the PK of SAM following oral administration in healthy volunteers."	( Characterization of the Pharmacokinetics of Samidorphan in Healthy Volunteers: Absolute Bioavailability and the Effect of Food and Age. Hard, M; Kumar, V; Lu, H; von Moltke, L, 2019)	0.51
"7 L/h, volume of distribution of 341 L, and elimination half-life of 7-8 h."	( Characterization of the Pharmacokinetics of Samidorphan in Healthy Volunteers: Absolute Bioavailability and the Effect of Food and Age. Hard, M; Kumar, V; Lu, H; von Moltke, L, 2019)	0.51
" Pharmacokinetic parameters of lithium and valproate, including maximum plasma concentration and area under the plasma concentration-time curve over a 12-h dosing interval, were calculated."	( Combination of Olanzapine and Samidorphan Has No Clinically Significant Effect on the Pharmacokinetics of Lithium or Valproate. Graham, C; Sun, L; von Moltke, L; Yagoda, S; Yao, B, 2020)	0.56
" This study aimed to investigate the pharmacokinetic properties of the new OTR tablets and evaluate the bioequivalence of oxycodone from OTR and the original extended release (ER) formulation tablets administered with an opioid antagonist in patients with chronic pain."	( Pharmacokinetics and Bioequivalence Evaluation of a New Oxycodone Tamper-Resistant Tablet Administered with an Opioid Antagonist in Patients with Chronic Pain. Hu, C; Luo, Z; Miao, J; Shen, Y; Shu, S; Wang, Y; Zhu, X, 2020)	0.56
" After a single dose of 40 mg tablets, pharmacokinetic results of the new OTR tablet were found to be similar to those of original extended-release oxycodone tablet."	( Pharmacokinetics and Bioequivalence Evaluation of a New Oxycodone Tamper-Resistant Tablet Administered with an Opioid Antagonist in Patients with Chronic Pain. Hu, C; Luo, Z; Miao, J; Shen, Y; Shu, S; Wang, Y; Zhu, X, 2020)	0.56
" As cytochrome P450 (CYP) 1A2 and CYP3A4 are the major enzymes involved in metabolism of olanzapine and samidorphan, respectively, physiologically-based pharmacokinetic (PBPK) modeling was applied to predict any drug-drug interaction (DDI) potential between olanzapine and samidorphan or between OLZ/SAM and CYP3A4/CYP1A2 inhibitors/inducers."	( Physiologically-Based Pharmacokinetic Modeling for Predicting Drug Interactions of a Combination of Olanzapine and Samidorphan. Rowland Yeo, K; Sun, L; von Moltke, L, 2020)	0.56
" Blood samples were collected for pharmacokinetic analysis, and rectal temperature and sedation were assessed to evaluate opioid effects at predetermined times up to 24 hours after treatment."	( Pharmacokinetics and pharmacodynamics of a novel analgesic with a deterrent to human opioid abuse (methadone-fluconazole-naltrexone) after oral administration in dogs. Joo, H; KuKanich, B; KuKanich, K; Locuson, CW; Rankin, DC, 2020)	0.56
" Complementary to the clinical findings, physiologically based pharmacokinetic modeling was used to assess the effects of varying degrees of renal impairment on the pharmacokinetics of olanzapine and samidorphan."	( Application of Physiologically Based Pharmacokinetic Modeling to Predict the Effect of Renal Impairment on the Pharmacokinetics of Olanzapine and Samidorphan Given in Combination. Rowland Yeo, K; Sun, L; von Moltke, L, 2021)	0.62
"A physiologically based pharmacokinetic model for OLZ/SAM was developed and validated by comparing model-simulated data with observed clinical data."	( Application of Physiologically Based Pharmacokinetic Modeling to Predict the Effect of Renal Impairment on the Pharmacokinetics of Olanzapine and Samidorphan Given in Combination. Rowland Yeo, K; Sun, L; von Moltke, L, 2021)	0.62
"Physiologically based pharmacokinetic modeling extended the findings from a clinical study in severe renal impairment to other untested clinical scenarios; these data could be of interest to clinicians treating patients with renal impairment."	( Application of Physiologically Based Pharmacokinetic Modeling to Predict the Effect of Renal Impairment on the Pharmacokinetics of Olanzapine and Samidorphan Given in Combination. Rowland Yeo, K; Sun, L; von Moltke, L, 2021)	0.62
" Population pharmacokinetic models for olanzapine and samidorphan were developed using data from 11 clinical studies in healthy subjects or patients with schizophrenia."	( Population Pharmacokinetics of Olanzapine and Samidorphan When Administered in Combination in Healthy Subjects and Patients With Schizophrenia. Mills, R; Rege, B; Sadler, BM; Sun, L, 2021)	0.62
" Physiologically-based pharmacokinetic (PBPK) modeling was used to extend the clinical findings to predict the effects of varying degrees of hepatic impairment on the PKs of olanzapine and samidorphan."	( Using physiologically-based pharmacokinetic modeling for predicting the effects of hepatic impairment on the pharmacokinetics of olanzapine and samidorphan given as a combination tablet. Barter, Z; Rowland Yeo, K; Sun, L; von Moltke, L, 2021)	0.62
" The in vitro release of NTX and its pharmacokinetic results in rats indicted that the LLC-SMO system is more uniform than LLC-GDO and Vivitrol® during 35 days."	( Comparison of lipid liquid crystal formulation and Vivitrol® for sustained release of Naltrexone: In vitro evaluation and pharmacokinetics in rats. Abbaspour, M; Eisvand, F; Hadizadeh, F; Kamali, H; Karimi, M; Khodaverdi, E; Nadim, A, 2022)	0.72

Compound-Compound Interactions

This double-blind, placebo-controlled human laboratory study examined the effects of varenicline and naltrexone on alcohol-primed smoking behavior. Lofexidine (LFX), an α2A adrenergic receptor agonist, was assessed for effects on opioid use outcomes and NTX treatment compliance.

Excerpt	Reference	Relevance
"Effects of the kappa opioid agonists, spiradoline (U62,066), enadoline (CI-977) and U69,593, were examined alone and in combination with the opioid antagonists quadazocine and beta-funaltrexamine in squirrel monkeys that responded under a schedule of shock titration."	( Antinociceptive and response rate-altering effects of kappa opioid agonists, spiradoline, enadoline and U69,593, alone and in combination with opioid antagonists in squirrel monkeys. Dykstra, LA; Pitts, RC, 1994)	0.29
"Opiate receptor avidity (B(max)'/K(D)) was measured in four rhesus monkeys following unilateral lesioning of the optic tract combined with transection of the corpus callosum and the hippocampal and anterior commissures depriving one hemisphere of visual input (Tract and Split), two animals with transection of commissures only (Split), and nine healthy monkeys with positron emission tomography (PET) and 6-deoxy-6-beta-[(18)F]fluoronaltrexone (cyclofoxy, CF), a mu- and kappa-opiate receptor antagonist."	( Opiate receptor avidity is increased in rhesus monkeys following unilateral optic tract lesion combined with transections of corpus callosum and hippocampal and anterior commissures. Carson, RE; Cohen, RM; Doudet, DJ; Saunders, RC, 2000)	0.31
" The effects of this compound are probably more favorable when combined with a psychosocial intervention such as the Community Reinforcement Approach (CRA)."	( Experiences with an outpatient relapse program (community reinforcement approach) combined with naltrexone in the treatment of opioid-dependence: effect on addictive behaviors and the predictive value of psychiatric comorbidity. Kerkhof, AJ; Roozen, HG; van den Brink, W, 2003)	0.32
"5 mg/kg), a GABAB agonist, administered alone or in combination with a single dose of naltrexone (1."	( The effect of baclofen alone and in combination with naltrexone on ethanol consumption in the rat. Stromberg, MF, 2004)	0.32
"Although naltrexone has been shown to be effective in the treatment of alcohol dependence, less is known about its efficacy when combined with different behavioral therapies."	( Naltrexone combined with either cognitive behavioral or motivational enhancement therapy for alcohol dependence. Anton, RF; Latham, P; Moak, DH; Myrick, H; Thevos, A; Voronin, K; Waid, LR; Wang, W; Woolson, R, 2005)	0.33
" The present study evaluated the effect of chronic (once a day for 12 days) intragastric administration of a CO2 Hypericum perforatum extract (HPCO2), given alone or combined with naltrexone (NTX), on ethanol intake offered 2h/day in msP rats."	( Reduction of ethanol intake by chronic treatment with Hypericum perforatum, alone or combined with naltrexone in rats. Cucculelli, M; Massi, M; Mattioli, L; Perfumi, M, 2005)	0.33
" The opioid antagonist naltrexone (NTX) may work in combination with nicotine replacement therapy (NRT) to block the effects of smoking stimuli in abstinent smokers."	( Effects on smoking cessation: naltrexone combined with a cognitive behavioral treatment based on the community reinforcement approach. Breteler, MH; Kerkhof, AJ; Postmus, PE; Roozen, HG; Van Beers, SE; Weevers, HJ; Willemsen, MC, 2006)	0.33
" GHB is frequently combined with other recreational drugs although these interactions are not well characterised."	( Sedative and hypothermic effects of gamma-hydroxybutyrate (GHB) in rats alone and in combination with other drugs: assessment using biotelemetry. McGregor, IS; van Nieuwenhuijzen, PS, 2009)	0.35
"We describe the first case of stress cardiomyopathy secondary to a drug-drug interaction."	( First case of stress cardiomyopathy as a result of methadone withdrawal secondary to drug-drug interaction. Lemesle, F; Nicola, W; Pierre Jonville-Béra, A, 2010)	0.36
"Preclinical and clinical studies have shown that opioids combined with ultra-low-dose naltrexone (NTX) may have increased analgesic potency and have suggested reduced abuse or dependence liability."	( Human abuse liability assessment of oxycodone combined with ultra-low-dose naltrexone. Bigelow, GE; Harrison, JA; Lanier, RK; Strain, EC; Tompkins, DA, 2010)	0.36
" The present study examined whether modulation of opioid systems by the opioid antagonist naltrexone (NTX), alone or in combination with standard of care therapies (taxol/paclitaxel, cisplatin), alters human ovarian cancer cell proliferation in tissue culture and tumor progression in mice."	( Low-dose naltrexone suppresses ovarian cancer and exhibits enhanced inhibition in combination with cisplatin. Donahue, RN; McLaughlin, PJ; Zagon, IS, 2011)	0.37
"This study investigated whether ethanol combined with low doses of morphine produces rewarding effects in rats."	( Rewarding effects of ethanol combined with low doses of morphine through dopamine D1 receptors. Ise, Y; Katayama, S; Mori, T; Nagase, H; Suzuki, T, 2013)	0.39
"0 mg/kg, intraperitoneally (IP)), or prazosin in combination with propranolol (5 mg/kg (IP); Exp."	( Low-dose prazosin alone and in combination with propranolol or naltrexone: effects on ethanol and sucrose seeking and self-administration in the P rat. Czachowski, CL; Verplaetse, TL, 2015)	0.42
" Prazosin in combination with propranolol or naltrexone was more effective than either drug alone and also reduced sucrose-reinforced behaviors."	( Low-dose prazosin alone and in combination with propranolol or naltrexone: effects on ethanol and sucrose seeking and self-administration in the P rat. Czachowski, CL; Verplaetse, TL, 2015)	0.42
"Determine the abuse potential of intravenous oxycodone combined with naltrexone, which represents simulated crushed ALO-02 in solution, compared with intravenous oxycodone in nondependent, recreational opioid users."	( Intravenous abuse potential study of oxycodone alone or in combination with naltrexone in nondependent recreational opioid users. Backonja, M; Bass, A; Malhotra, BK; Matschke, K; Setnik, B; Sommerville, KW; Webster, LR; Wolfram, G, 2016)	0.43
"This double-blind, placebo-controlled human laboratory study examined the effects of varenicline (2 mg/d) and varenicline (2 mg/d), combined with a low dose of naltrexone (25 mg/d) on alcohol-primed smoking behavior in a laboratory model of smoking relapse in heavy-drinking tobacco users (n = 30)."	( Effects of Varenicline Alone and in Combination With Low-dose Naltrexone on Alcohol-primed Smoking in Heavy-drinking Tobacco Users: A Preliminary Laboratory Study. McKee, SA; Roberts, W; Shi, JM; Tetrault, JM, )	0.13
"3-3 mg/kg) or in combination with naltrexone (mu-opioid receptor antagonist at 1 mg/kg) altered alcohol "relapse" drinking using a mouse ADE paradigm."	( Effects of mesyl salvinorin B alone and in combination with naltrexone on alcohol deprivation effect in male and female mice. Crowley, R; Kreek, MJ; Prisinzano, T; Zhou, Y, 2018)	0.48
" This open-label trial compared the outcomes of patients with opioid use disorder treated with XR-naltrexone or oral naltrexone in combination with behavioral therapy."	( A Randomized Trial Comparing Extended-Release Injectable Suspension and Oral Naltrexone, Both Combined With Behavioral Therapy, for the Treatment of Opioid Use Disorder. Bisaga, A; Carpenter, KM; Choi, CJ; Levin, FR; Mariani, JJ; Mishlen, K; Nunes, EV; Pavlicova, M; Sullivan, MA, 2019)	0.51
" These results support the use of XR-naltrexone combined with behavioral therapy as an effective treatment for patients seeking opioid withdrawal and nonagonist treatment for preventing relapse to opioid use disorder."	( A Randomized Trial Comparing Extended-Release Injectable Suspension and Oral Naltrexone, Both Combined With Behavioral Therapy, for the Treatment of Opioid Use Disorder. Bisaga, A; Carpenter, KM; Choi, CJ; Levin, FR; Mariani, JJ; Mishlen, K; Nunes, EV; Pavlicova, M; Sullivan, MA, 2019)	0.51
" In SD rats, a low, but not a high, dose of SAM in combination with BUP counteracted swim-stress induced immobility."	( Locomotor and anti-immobility effects of buprenorphine in combination with the opioid receptor modulator samidorphan in rats. Burke, NN; Deaver, DR; Ferdousi, M; Finn, DP; Kelly, JP; Roche, M, 2019)	0.51
" Here, we assessed the effectiveness of the dopamine/norepinephrine re-uptake inhibitor, bupropion (BUP), alone and in combination with naltrexone (NAL), to reduce binge-like and chronic ethanol (EtOH) intake in mice."	( Bupropion, Alone and in Combination with Naltrexone, Blunts Binge-Like Ethanol Drinking and Intake Following Chronic Intermittent Access to Ethanol in Male C57BL/6J Mice. Garbutt, JC; Kampov-Polevoy, AB; Luhn, KL; Navarro, M; Thiele, TE, 2019)	0.51
"BUP, alone and in combination with NAL, may represent a novel approach to treating binge EtOH intake."	( Bupropion, Alone and in Combination with Naltrexone, Blunts Binge-Like Ethanol Drinking and Intake Following Chronic Intermittent Access to Ethanol in Male C57BL/6J Mice. Garbutt, JC; Kampov-Polevoy, AB; Luhn, KL; Navarro, M; Thiele, TE, 2019)	0.51
"Lofexidine (LFX), an α2A adrenergic receptor agonist, known to alleviate opioid withdrawal symptoms, was assessed in combination with oral naltrexone (NTX) for effects on opioid use outcomes and NTX treatment compliance."	( Lofexidine in Combination With Oral Naltrexone for Opioid Use Disorder Relapse Prevention: A Pilot Randomized, Double-Blind, Placebo-Controlled Study. Fogelman, N; Hermes, G; Hyman, SM; Kosten, TR; Sinha, R, 2019)	0.51
" Here, we further investigated whether NFF alone (1-10 μg/kg) or in combination with naltrexone (NTX, mu-opioid receptor [MOP-r] antagonist) altered alcohol relapse-like drinking using a mouse alcohol deprivation effect (ADE) paradigm to mimic the relapse episodes in human alcoholics."	( Clinically utilized kappa-opioid receptor agonist nalfurafine combined with low-dose naltrexone prevents alcohol relapse-like drinking in male and female mice. Kreek, MJ; Zhou, Y, 2019)	0.51
"1 mg/kg, subcutaneous) alone or in combination with samidorphan (0."	( Chronic administration of buprenorphine in combination with samidorphan produces sustained effects in olfactory bulbectomised rats and Wistar-Kyoto rats. Burke, NN; Deaver, DR; Eyerman, DJ; Finn, DP; Kelly, JP; Li, Y; Roche, M; Sanchez, C, 2019)	0.51
"Olfactory bulbectomised-induced hyperactivity was attenuated by chronic administration of buprenorphine alone and in combination with samidorphan, to that of sham control activity levels."	( Chronic administration of buprenorphine in combination with samidorphan produces sustained effects in olfactory bulbectomised rats and Wistar-Kyoto rats. Burke, NN; Deaver, DR; Eyerman, DJ; Finn, DP; Kelly, JP; Li, Y; Roche, M; Sanchez, C, 2019)	0.51
" This study aimed to investigate the pharmacokinetic properties of the new OTR tablets and evaluate the bioequivalence of oxycodone from OTR and the original extended release (ER) formulation tablets administered with an opioid antagonist in patients with chronic pain."	( Pharmacokinetics and Bioequivalence Evaluation of a New Oxycodone Tamper-Resistant Tablet Administered with an Opioid Antagonist in Patients with Chronic Pain. Hu, C; Luo, Z; Miao, J; Shen, Y; Shu, S; Wang, Y; Zhu, X, 2020)	0.56
" As cytochrome P450 (CYP) 1A2 and CYP3A4 are the major enzymes involved in metabolism of olanzapine and samidorphan, respectively, physiologically-based pharmacokinetic (PBPK) modeling was applied to predict any drug-drug interaction (DDI) potential between olanzapine and samidorphan or between OLZ/SAM and CYP3A4/CYP1A2 inhibitors/inducers."	( Physiologically-Based Pharmacokinetic Modeling for Predicting Drug Interactions of a Combination of Olanzapine and Samidorphan. Rowland Yeo, K; Sun, L; von Moltke, L, 2020)	0.56
"To assess the potential for drug-drug interactions between a single oral dose of naldemedine and the oral P-glycoprotein inhibitor cyclosporine, cytochrome P450 (CYP) 3A inhibitors itraconazole and fluconazole, and CYP3A inducer rifampin."	( Clinical Drug-Drug Interaction Studies to Evaluate the Effects of a P-Glycoprotein Inhibitor, CYP3A Inhibitors, and a CYP3A Inducer on the Pharmacokinetics of Naldemedine in Healthy Subjects. Fukumura, K; Ishibashi, T; Kawaguchi, N; Kubota, R; Ogura, E; Tada, Y, 2020)	0.56
" This is commonly known as drug-drug interactions."	( Clinical Drug-Drug Interaction Studies to Evaluate the Effects of a P-Glycoprotein Inhibitor, CYP3A Inhibitors, and a CYP3A Inducer on the Pharmacokinetics of Naldemedine in Healthy Subjects. Fukumura, K; Ishibashi, T; Kawaguchi, N; Kubota, R; Ogura, E; Tada, Y, 2020)	0.56
"In order to study the clinical effect of sufentanil combined with nalmefene in fiberoptic bronchoscopy tracheal intubation in airway patients, a method based on sufentanil combined with nalmefene-assisted topical anesthesia for fiberoptic bronchoscopy-guided nasotracheal intubation method is proposed."	( Effect of Sufentanil Combined with Nalmefene Assisted Surface Anesthesia on Transnasal Endotracheal Intubation Guided by Fiberoptic Bronchoscope. Wang, Z; Zhan, Y; Zhang, J; Zhao, Z, 2022)	0.72

Bioavailability

The primary aim of this study was to compare the oral bioavailability of naltrexone and its metabolite 6-beta-naltrexol. Secondary objectives were to assess food effects on the pharmacokinetics of IRO-A tablets. The results fail to support the view that naloxone has reduced bioavailability after oral administration.

Excerpt	Reference	Relevance
" Long bioavailability of the new metabolite is indicated by its slower excretion rate into the urine than naltrexone and beta-naltrexol."	( Isolation and identification of a new metabolite of naltrexone in human blood and urine. Chedekel, MA; Mule, SJ; Rosenthal, D; Verebely, K, 1975)	0.25
"), a slowly metabolized, orally bioavailable opiate antagonist, with 30 times the potency of naloxone."	( The effects of nalmefene, a potent oral opiate antagonist, on exercise-induced bronchospasm. Christopher, MA; Harman, E; Hendeles, L; Wyzan, D, 1988)	0.27
" Plasma concentration-time data for nalmefene indicate good oral bioavailability and a prolonged terminal elimination phase (mean t1/2 11."	( Prolonged blockade of opioid effect with oral nalmefene. DiFazio, CA; Dixon, R; Gal, TJ, 1986)	0.27
"In an effort to improve the oral bioavailability of naltrexone [17-(cyclopropylmethyl)-4,5 alpha-epoxy-3,14-dihydroxymorphinan-6-one;1], a number of prodrug esters on the 3-hydroxyl group were prepared: the anthranilate (2), acetylsalicylate (3), benzoate (4), and pivalate (5)."	( Improvement of the oral bioavailability of naltrexone in dogs: a prodrug approach. Hussain, MA; Koval, CA; Myers, MJ; Shami, EG; Shefter, E, 1987)	0.27
" This finding indicates the excellent bioavailability of naltrexone following oral or subcutaneous administration 3H-naltrexone and/or its metabolites were predominately excreted in the urine, and the renal excretion was similar for all three routes of administration."	( A comparative study of the oral, intravenous, and subcutaneous administration of 3H-naltrexone to normal male volunteers. Perez-Reyes, M; Wall, ME, 1981)	0.26
" Oral naltrexone and nalmefene have significantly more central nervous system (CNS) bioavailability than oral naloxone."	( Orally administered opioid antagonists reverse both mu and kappa opioid agonist delay of gastrointestinal transit in the guinea pig. Culpepper-Morgan, JA; Holt, PR; Kreek, MJ; LaRoche, D, 1995)	0.29
"Twenty-three normal volunteers who received morphine sulphate (MS Contin) with naltrexone completed this randomized, analytically blinded, two-way crossover comparison of the bioavailability of one 200-mg oral controlled-release morphine sulfate tablet with two 100-mg MSC tablets."	( A bioequivalence study of oral controlled-release morphine using naltrexone blockade. Goldenheim, PD; Grandy, RP; Kaiko, RF; Reder, RF; Sackler, RS, 1995)	0.29
"The effect of naltrexone hydrochloride on the bioavailability of 60 mg controlled-release oral morphine sulfate in normal volunteers was determined using a randomized, 2-way crossover, analytically blinded study design."	( Relative bioavailability of controlled-release oral morphine sulfate during naltrexone blockade. Bashaw, ED; Goldenheim, PD; Grandy, RP; Kaiko, RF; Reder, RF, 1995)	0.29
" The high mu receptor binding affinity and in vitro pharmacological selectivity of 5 coupled with its presumed low central nervous system bioavailability suggest that it may be a useful antagonist for the investigation of peripheral mu opioid receptors."	( Opioid antagonist activity of naltrexone-derived bivalent ligands: importance of a properly oriented molecular scaffold to guide "address" recognition at kappa opioid receptors. Bolognesi, ML; Farouz-Grant, F; Gleason, WB; Griffin, JF; Larson, DL; Ojala, WH; Portoghese, PS; Takemori, AE, 1996)	0.29
"5 to 2 g/kg of alcohol did not alter blood alcohol concentrations significantly, suggesting that the interactions between alcohol and naltrexone were unrelated to gross changes in alcohol metabolism or bioavailability factors."	( Interactions between alcohol- and opioid-induced suppression of rat testicular steroidogenesis in vivo. Adams, ML; Cicero, TJ; Meyer, ER, 1997)	0.3
" Although NTX could be absorbed rapidly in the dog after po administration, the plasma concentration of the parent drug was very low and its absolute bioavailability was 15."	( [Pharmacokinetics of naltrexone hydrochloride and naltrexone glucuronide in the dog]. Ge, ZH; Li, H; Wang, N; Zhao, SF, 1996)	0.29
" The increased bioavailability of the drug is not very important for opioid receptor antagonist activity but may play a role in naltrexone treatment safety."	( Serum time course of naltrexone and 6 beta-naltrexol levels during long-term treatment in drug addicts. Avico, U; Bertolotti, M; Dell'Utri, A; Ferrari, A; Sternieri, E, 1998)	0.3
"The bioavailability of a generic preparation of naltrexone (Narpan) was compared with the innovator product, Trexan."	( Comparative bioavailability study of a generic naltrexone tablet preparation. Billa, N; Peh, KK; Yuen, KH, 1999)	0.3
"These results fail to support the view that naloxone has reduced bioavailability after oral administration, as compared to naltrexone, or that its pharmacokinetic profile is particularly advantageous for some therapeutic settings (e."	( The discriminative stimulus effects of naloxone and naltrexone in morphine-treated rhesus monkeys: comparison of oral and subcutaneous administration. France, CP; Gauthier, CA, 1999)	0.3
"Intravenous naloxone frequently ameliorates the pruritus of cholestasis, but its low oral bioavailability precludes its use as a long-term therapy."	( Oral nalmefene therapy reduces scratching activity due to the pruritus of cholestasis: a controlled study. Alling, DW; Bergasa, NV; Jones, EA; Talbot, TL; Wells, MC, 1999)	0.3
"The quantitative structure-bioavailability relationship of 232 structurally diverse drugs was studied to evaluate the feasibility of constructing a predictive model for the human oral bioavailability of prospective new medicinal agents."	( QSAR model for drug human oral bioavailability. Topliss, JG; Yoshida, F, 2000)	0.31
" Bioavailability of MNTX is low after oral administration, and plasma levels do not correlate with its actions in the gut, suggesting a predominantly local luminal action of MNTX on the gut."	( A review of the potential role of methylnaltrexone in opioid bowel dysfunction. Foss, JF, 2001)	0.31
" NAL's excellent oral bioavailability and linear increases in the area under plasma concentration-time curve make it ideal for use in experimental studies."	( Efficacy of naltrexone on acetylcholine-induced alloknesis in atopic eczema. Groene, D; Heyer, G; Martus, P, 2002)	0.31
"Standard bioavailability measures show minimal effect of food on the bioavailability of hydromorphone from OROS hydromorphone."	( Pharmacokinetic profile of a 24-hour controlled-release OROS formulation of hydromorphone in the presence and absence of food. Gupta, SK; Sathyan, G; Thipphawong, J; Xu, E, 2007)	0.34
" ELN441958 is a novel small molecule bradykinin B(1) receptor antagonist exhibiting high oral bioavailability and potent systemic efficacy in rhesus monkey inflammatory pain."	( Pharmacological, pharmacokinetic, and primate analgesic efficacy profile of the novel bradykinin B1 Receptor antagonist ELN441958. Bova, MP; Butelman, ER; Chavez, RA; Chen, L; Dreyer, M; Fukuda, JY; Garofalo, AW; Hawkinson, JE; Holcomb, R; Hom, DS; Ko, MC; Liao, A; Malmberg, AB; Ruslim, L; Samant, B; Simmonds, S; Szoke, BG; Wadsworth, A; Zeitz, KP; Zhang, H; Zmolek, W, 2007)	0.34
" Human oral bioavailability is an important pharmacokinetic property, which is directly related to the amount of drug available in the systemic circulation to exert pharmacological and therapeutic effects."	( Hologram QSAR model for the prediction of human oral bioavailability. Andricopulo, AD; Moda, TL; Montanari, CA, 2007)	0.34
"The poor oral bioavailability of the opioid receptor antagonist naloxone (NA) when compared with naltrexone (NX) may be related to a greater interaction of naloxone with the efflux drug transporter P-glycoprotein (P-gp)."	( P-glycoprotein is not involved in the differential oral potency of naloxone and naltrexone. Daali, Y; Dayer, P; Desmeules, J; Kanaan, M, 2009)	0.35
" Our results demonstrate that cyclization might be a promising strategy to enhance bioavailability of peptides and may serve a role in the development of novel endomorphin analogs with increased therapeutic potential."	( Synthesis and biological evaluation of cyclic endomorphin-2 analogs. Cravezic, A; do-Rego, JC; Fichna, J; Janecka, A; Perlikowska, R; Toth, G; Wyrebska, A, 2010)	0.36
" Its current peroral administration induces various adverse side effects and has limited efficacy since bioavailability and patient compliance are poor."	( Bioavailability in vivo of naltrexone following transbuccal administration by an electronically-controlled intraoral device: a trial on pigs. Campisi, G; De Caro, V; Florena, AM; Giannola, LI; Göttsche, T; Paderni, C; Schumacher, A; Wolff, A, 2010)	0.36
"The primary aim of this study was to compare the oral bioavailability of naltrexone and its metabolite 6-beta-naltrexol, derived from crushed pellets from MS-sNT capsules, to naltrexone solution."	( Relative oral bioavailability of morphine and naltrexone derived from crushed morphine sulfate and naltrexone hydrochloride extended-release capsules versus intact product and versus naltrexone solution: a single-dose, randomized-sequence, open-label, thr Bieberdorf, FA; Johnson, FK; Stark, JG; Stauffer, J, 2010)	0.36
" The analysis of relative bioavailability was based on conventional FDA criteria for assuming bioequivalence; that is, 90% CIs for ratios of geometric means (natural logarithm [In]-transformed C(max) and AUC) fell within the range of 80% to 125%."	( Relative oral bioavailability of morphine and naltrexone derived from crushed morphine sulfate and naltrexone hydrochloride extended-release capsules versus intact product and versus naltrexone solution: a single-dose, randomized-sequence, open-label, thr Bieberdorf, FA; Johnson, FK; Stark, JG; Stauffer, J, 2010)	0.36
" The primary objective of this study was to assess single-dose relative bioavailability of morphine when morphine sulfate and naltrexone hydrochloride extended release capsules were taken under fed and fasting conditions and when pellets were sprinkled on apple sauce."	( Food effects on the pharmacokinetics of morphine sulfate and naltrexone hydrochloride extended release capsules. Boudriau, S; Ciric, S; Johnson, F; Stauffer, J; Swearingen, D, 2010)	0.36
"Morphine bioavailability was similar for all treatments."	( Food effects on the pharmacokinetics of morphine sulfate and naltrexone hydrochloride extended release capsules. Boudriau, S; Ciric, S; Johnson, F; Stauffer, J; Swearingen, D, 2010)	0.36
" This study shows that the bioavailability of extended-release hydromorphone is not affected by food and that the bioavailability of extended-release hydromorphone under fasting conditions is comparable with that of the immediate-release formulation when administered at the same total daily dose."	( A randomized study of the effects of food on the pharmacokinetics of once-daily extended-release hydromorphone in healthy volunteers. Ariyawansa, J; Marricco, NC; Moore, KT; Morelli, G; Natarajan, J; Pagé, V; Richarz, U; St-Fleur, D, 2011)	0.37
"Studies conducted to date indicate that methylnaltrexone has high bioavailability after subcutaneous administration at therapeutic dose levels, a terminal half-life of ∼ 8 - 9 h, minimal metabolism, elimination involving renal and non-renal routes, and a limited potential for drug-drug interactions."	( Methylnaltrexone bromide: research update of pharmacokinetics following parenteral administration. Boyd, TA; Rotshteyn, Y; Yuan, CS, 2011)	0.37
" This open-label, single-dose, 4-way crossover, pharmacokinetic drug interaction study compared the relative bioavailability of morphine and naltrexone when MS-sNT is administered (under fasting conditions) with increasing doses of alcohol."	( Effects of alcohol on the pharmacokinetics of morphine sulfate and naltrexone hydrochloride extended release capsules. Boudriau, S; Ciric, S; Johnson, FK; Kisicki, J; Stauffer, J, 2012)	0.38
"The naltrexone bioavailability study compared naltrexone release from MS-sNTC with that from whole intact MS-sNT capsules (MS-sNTW) and an equal naltrexone solution (NS) dose."	( Morphine sulfate and naltrexone hydrochloride extended-release capsules: naltrexone release, pharmacodynamics, and tolerability. Johnson, F; Setnik, B, )	0.13
"Naltrexone from MS-sNTC met criteria for equivalent bioavailability to NS."	( Morphine sulfate and naltrexone hydrochloride extended-release capsules: naltrexone release, pharmacodynamics, and tolerability. Johnson, F; Setnik, B, )	0.13
" Secondary objectives were to assess food effects on the pharmacokinetics of IRO-A tablets, to compare the relative bioavailability of oxycodone in IRO-A tablets versus marketed oxycodone hydrochloride (IRO) tablets under fed conditions and to evaluate the single-dose safety profile of the IRO-A tablets in healthy volunteers pretreated with naltrexone."	( Dose proportionality and the effects of food on bioavailability of an immediate-release oxycodone hydrochloride tablet designed to discourage tampering and its relative bioavailability compared with a marketed oxycodone tablet under fed conditions: a sing Bass, A; Leibowitz, M; Pixton, GC; Rolleri, R; Sommerville, KW; Stark, JG; Zamora, CA, 2012)	0.38
" Dose proportionality (IRO-A), food effects (IRO-A), and relative bioavailability in a fed state (IRO-A and IRO) were assessed by using bioequivalence criteria (90% CIs between 80% and 125% for C(max) and AUC)."	( Dose proportionality and the effects of food on bioavailability of an immediate-release oxycodone hydrochloride tablet designed to discourage tampering and its relative bioavailability compared with a marketed oxycodone tablet under fed conditions: a sing Bass, A; Leibowitz, M; Pixton, GC; Rolleri, R; Sommerville, KW; Stark, JG; Zamora, CA, 2012)	0.38
" The bioavailability of oxycodone from IRO-A tablets in the fed state was comparable with IRO tablets based on AUC parameters, although C(max) was ~16."	( Dose proportionality and the effects of food on bioavailability of an immediate-release oxycodone hydrochloride tablet designed to discourage tampering and its relative bioavailability compared with a marketed oxycodone tablet under fed conditions: a sing Bass, A; Leibowitz, M; Pixton, GC; Rolleri, R; Sommerville, KW; Stark, JG; Zamora, CA, 2012)	0.38
" Administration of IRO-A with food suggested increased overall bioavailability relative to fasting conditions and a reduction in peak systemic exposure of oxycodone that is not expected to be clinically significant."	( Dose proportionality and the effects of food on bioavailability of an immediate-release oxycodone hydrochloride tablet designed to discourage tampering and its relative bioavailability compared with a marketed oxycodone tablet under fed conditions: a sing Bass, A; Leibowitz, M; Pixton, GC; Rolleri, R; Sommerville, KW; Stark, JG; Zamora, CA, 2012)	0.38
" Since the bioavailability of oral MNTX is low, it is necessary to explore the oral formulations of MNTX that increase its bioavailability."	( Bioavailability of oral methylnaltrexone increases with a phosphatidylcholine-based formulation. Gu, M; Lin, DH; McEntee, E; Qin, LF; Wang, CZ; Wang, JT; Xie, XX; Yuan, CS, 2014)	0.4
" The physicochemical properties of MNTX-PC were analyzed, and its bioavailability was evaluated in rats."	( Bioavailability of oral methylnaltrexone increases with a phosphatidylcholine-based formulation. Gu, M; Lin, DH; McEntee, E; Qin, LF; Wang, CZ; Wang, JT; Xie, XX; Yuan, CS, 2014)	0.4
" Thus, the relative bioavailability after the oral administration of MNTX-PC was 410% compared to that of control."	( Bioavailability of oral methylnaltrexone increases with a phosphatidylcholine-based formulation. Gu, M; Lin, DH; McEntee, E; Qin, LF; Wang, CZ; Wang, JT; Xie, XX; Yuan, CS, 2014)	0.4
"MNTX-PC formulation significantly enhanced the oral bioavailability of MNTX."	( Bioavailability of oral methylnaltrexone increases with a phosphatidylcholine-based formulation. Gu, M; Lin, DH; McEntee, E; Qin, LF; Wang, CZ; Wang, JT; Xie, XX; Yuan, CS, 2014)	0.4
"The primary objective of this study was to determine the pharmacokinetics and dose proportionality of 5 different doses (100, 200, 400, 600, and 800 μg) of fentanyl sublingual spray in healthy subjects under fasted conditions (part A); the secondary objective was to assess the effects of temperature and pH in the oral cavity on relative bioavailability of fentanyl (part B)."	( Pharmacokinetics and dose proportionality of fentanyl sublingual spray: a single-dose 5-way crossover study. Chavan, A; Dillaha, L; Goskonda, V; Parikh, N, 2013)	0.39
" Altering the local environment of the oral cavity (temperature and pH) showed no effects on the bioavailability of fentanyl."	( Pharmacokinetics and dose proportionality of fentanyl sublingual spray: a single-dose 5-way crossover study. Chavan, A; Dillaha, L; Goskonda, V; Parikh, N, 2013)	0.39
"Naltrexone is widely used in the treatment of opiate addiction but its current peroral administration is characterized by low bioavailability with various side effects."	( Controlled delivery of naltrexone by an intraoral device: in vivo study on human subjects. Campisi, G; De Caro, V; Giannola, LI; Göttsche, T; Paderni, C; Schumacher, A; Wolff, A, 2013)	0.39
" Absolute oral bioavailability was estimated to 41% without food intake and with food about 53%."	( Population pharmacokinetics of nalmefene in healthy subjects and its relation to μ-opioid receptor occupancy. Areberg, J; Faerch, KU; Kyhl, LE; Larsen, F; Li, S; Soegaard, B, 2016)	0.43
"The objective of this study was to evaluate the relative bioavailability of olanzapine in 3 olanzapine-containing tablet formulations."	( Bioequivalence of Olanzapine Given in Combination With Samidorphan as a Bilayer Tablet (ALKS 3831) Compared With Olanzapine-Alone Tablets: Results From a Randomized, Crossover Relative Bioavailability Study. Liu, J; McDonnell, D; Sun, L; von Moltke, L, 2019)	0.51
"SAM has high bioavailability that is comparable following sublingual and oral administration and is not subject to extensive first-pass metabolism."	( Characterization of the Pharmacokinetics of Samidorphan in Healthy Volunteers: Absolute Bioavailability and the Effect of Food and Age. Hard, M; Kumar, V; Lu, H; von Moltke, L, 2019)	0.51
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."	( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019)	0.51
" Given the greater KOR potency and improved bioavailability compared to NTX, NMF may be a promising pharmacotherapeutic for cocaine use disorder (CUD)."	( Nalmefene, a mu opioid receptor antagonist/kappa opioid receptor partial agonist, potentiates cocaine motivation but not intake with extended access self-administration in adult male mice. Kreek, MJ; Morochnik, M; Reed, B; Windisch, KA, 2021)	0.62
" Modifications to model parameters, including absorption rate constant and fraction unbound to plasma protein, were made to recover the observed change in the PKs of olanzapine and samidorphan in individuals with moderate hepatic impairment."	( Using physiologically-based pharmacokinetic modeling for predicting the effects of hepatic impairment on the pharmacokinetics of olanzapine and samidorphan given as a combination tablet. Barter, Z; Rowland Yeo, K; Sun, L; von Moltke, L, 2021)	0.62
"25% (w/v) HP-β-CD, with absolute bioavailability of 76."	( Effect of Different Absorption Enhancers on the Nasal Absorption of Nalmefene Hydrochloride. Han, X; Li, M; Nie, G; Zhang, T; Zheng, A, 2022)	0.72

Dosage Studied

Dogs were randomly allocated (6 dogs/group) to receive 1 of 2 oral dosing regimens of methadone-fluconazole-naltrexone. A taste of alcohol and a series of alcohol-related pictures, neutral beverage pictures, and visual control images were provided to volunteers after 7 days of double-blind randomly assigned daily dosing. No change was observed in the rate of naltrex one disposition during chronic dosing vs. acute.

Excerpt	Relevance	Reference
"Neonatal mice were injected once daily with d,l-methadone in a dosage of 2 mg/kg."	( Inhibition by d,l-methadone of RNA and protein synthesis in neonatal mice: antagonism by naloxone or naltrexone. Hui, FW; Krikun, E; Smith, AA, 1978)	0.26
"In a controlled double-blind clinical study, 42 patients reported side effects and severity of side effects to naltrexone on three different first-day doses and maintenance dosage regimens."	( Controlled clinical study of naltrexone side effects comparing first-day doses and maintenance regimens. Brahen, LS; Capone, T; Heller, RC; Landy, HJ; Lewis, MJ; Linden, SL, 1978)	0.26
" Naltrexone appears to be a safe, nontoxic medication in the dosage range examined."	( Naltrexone: physiological and psychological effects of single doses. Charuvastra, VC; Gritz, ER; Jarvik, ME; Schlesinger, J; Shiffman, SM, 1976)	0.26
" Dosage forms of small implantable cylinders, 1/16'' diameter, (25 mg/rod, one rod/mouse) containing 33% by weight naltrexone pamoate in 90 L(+)/10 polylactic/glycolic acid have sustained the delivery of chemical for 20 days."	( Development of polylactic/glycolic acid delivery systems for use in treatment of narcotic addiction. Howes, JF; Schwope, AD; Wise, DL, 1976)	0.26
" These studies were carried out with a twice-a-day dosage regimen."	( Naltrexone and cyclazocine. A controlled treatment study. Brahen, LS; Capone, T; Desiderio, D; Wiechert, V, 1977)	0.26
" Thus far, the most useful of several dosage forms studied is a suspension in an aluminum monostearate gel."	( Long-acting narcotic antagonist complexes. Gray, AP; Guardina, WJ, 1976)	0.26
" We have demonstrated that the polypeptides can be fabricated into dosage forms that are amenable to administration by trochar."	( Use of synthetic polypeptides in the preparation of biodegradable delivery vehicles for narcotic antagonists. Arnold, DL; Granchelli, FE; Nelsen, L; Sheth, SG; Sidman, KR; Steber, WD; Strong, P, 1976)	0.26
" Thus far, the most useful of several dosage forms studied is s suspension in an aluminum monostearate gel."	( Long-acting narcotic antagonist complexes. Gray, AP; Guardina, WJ, 1975)	0.25
" We have demonstrated that the polypeptides can be fabricated into dosage forms that are amenable to administration by trochar."	( Use of synthetic polypeptides in the preparation of biodegradable delivery vehicles for narcotic antagonists. Arnold, DL; Granchelli, FE; Nelsen, L; Sheth, SG; Sidman, KR; Steber, WD; Strong, P, 1975)	0.25
" Dosage forms of small inplantable cylinders, 1/16 inch diameter, (25 mg/rod, one rod/mouse) containing 33 per cent by weight naltrexone pamoate in 90 L(+)/10 polylactic/glycolic acid have sustained the delivery of chemical for 200 days."	( Development of polylactic/glycolic acid delivery systems for use in treatment of narcotic addiction. Howes, JF; Schwope, AD; Wise, DL, 1975)	0.25
" At all pretreatment times, the antinociceptive dose-response lines for these kappa agonists were displaced to the right to various degrees in a parallel fashion; an increasing rightward displacement of the U69,593 and bremazocine antinociceptive dose-response lines was observed at 1 and 3 days after a single nor-BNI pretreatment, with a gradual return toward the control level at later times after pretreatment."	( Extremely long-lasting antagonistic actions of nor-binaltorphimine (nor-BNI) in the mouse tail-flick test. Horan, P; Porreca, F; Taylor, J; Yamamura, HI, 1992)	0.28
" Within regions intermediate between the dorsal posterior, mesencephalic tegmentum and posterior medulla, (-)-nicotine produced biphasic dose-response and time action curves."	( Opioid and nicotinic analgesic and hyperalgesic loci in the rat brain stem. Hamann, SR; Martin, WR, 1992)	0.28
" A dose-response curve was also made for the mu-opioid receptor agonist, morphine."	( Spinal antinociception by Tyr-D-Ser(otbu)-Gly-Phe-Leu-Thr, a selective delta-opioid receptor agonist. Dickenson, AH; Kalso, EA; McQuay, HJ; Sullivan, AF, 1992)	0.28
" 1) In the presence of a fixed dose of DPDPE (150 nmol), there was a left shift in the dose-response curve of the mu agonist, with the magnitude of the shifts being greater than those anticipated from a simple additive interaction: PL017 (31-fold) > or = DAMGO (20-fold) > morphine (6."	( Isobolographic and dose-response analyses of the interaction between intrathecal mu and delta agonists: effects of naltrindole and its benzofuran analog (NTB). Malmberg, AB; Yaksh, TL, 1992)	0.28
" The dextrorphan-trained birds generalized to l-cyclorphan at 10 mg/kg; naltrexone did not alter the l-cyclorphan dose-response curve for this effect."	( Discriminative stimulus effects of cyclorphan: selective antagonism with naltrexone. Bertalmio, AJ; Woods, JH, 1992)	0.28
" Further investigations need to be done to establish the most appropriate dosage rates for these preparations in ostriches."	( Ostrich (Struthio camelus) immobilisation using carfentanil and xylazine and reversal with yohimbine and naltrexone. Malan, JH; Quandt, SK; Raath, JP, 1992)	0.28
" catheters, dose-response curves were carried out using the hot plate (HP) test for a number of receptor-preferring opioids."	( Characteristics of dose-dependent antagonism by beta-funaltrexamine of the antinociceptive effects of intrathecal mu agonists. Mjanger, E; Yaksh, TL, 1991)	0.28
") of a 15 mg naltrexone pellet there was a significant shift to the right of the fentanyl dose-response curves for analgesia and lethality."	( Evaluation of receptor mechanism mediating fentanyl analgesia and toxicity. Jang, Y; Yoburn, BC, 1991)	0.28
"3 nmol/rat of DADELT II and shifted the dose-response curve to the right, without decreasing the maximum effect."	( Behavioural effects of deltorphins in rats. Angelucci, F; Negri, L; Noviello, V, 1991)	0.28
" The influence of chronic naltrexone treatment upon the antinociceptive effects of fentanyl was assessed in drug-naive (control) rats and in rats which had received fentanyl in the same dosage schedule as those in drug discrimination experiments."	( Paradoxical effect of chronic fentanyl treatment on naltrexone-induced supersensitivity and upregulation. Ableitner, A; Ayesta, FJ; Emmett-Oglesby, MW; Herz, A; Shippenberg, TS, 1992)	0.28
" In dose-response studies, beta-FNA antagonized all the actions with similar potencies (ID50 values of 12."	( Comparison of naloxonazine and beta-funaltrexamine antagonism of mu 1 and mu 2 opioid actions. Pasternak, GW; Paul, D; Pick, CG, 1991)	0.28
" The drug dosage was 50 mg/daily (100 mg/die)."	( [The role of opioid antagonists in the treatment of obesity. Results of a clinical trial with naltrexone]. Ardizzone, A; Francesetti, G; Lamberto, M; Mantovan, M; Maurino, M; Meluzzi, A; Molinatti, GM; Novi, RF; Visconti, P, )	0.13
" In Long-Evans rats, BW942C produced a biphasic dose-response curve for urine output with lower doses increasing and higher doses suppressing output."	( Kappa opioid partial agonist activity of the enkephalin-like pentapeptide BW942C based on urination and in vitro studies in humans and animals. Cone, EJ; Johnson, RE; Su, TP; Vaupel, DB, 1990)	0.28
" Butorphanol resulted in partial reversal of sedation at both dosage levels."	( Reversal of oxymorphone sedation by naloxone, nalmefene, and butorphanol. Anderson, GI; Doherty, T; Dyson, DH; McDonell, WN, )	0.13
" Using a cumulative dosing procedure, morphine and naltrexone were tested weekly for effects on rates of responding."	( Tolerance and dependence after continuous morphine infusion from osmotic pumps measured by operant responding in rats. Adams, JU; Holtzman, SG, 1990)	0.28
" The return to normal naltrexone sensitivity after elimination of the two highest doses suggests that a reliable association between the lower and higher doses in a cumulative dosing procedure can result in conditioned effects to the lower doses."	( Enhanced sensitivity to behavioral effects of naltrexone in rats. Goldberg, SR; Katz, JL; Schindler, CW; Su, TP; Wu, XZ, 1990)	0.28
" The naltrexone stimulus-generalization curve and dose-response curve for loss of body weight were shifted to the left by IBMX and Ro 20-1724, which produce quasi-withdrawal, but not by papaverine, which does not."	( Phosphodiesterase inhibitors potentiate opiate-antagonist discrimination by morphine-dependent rats. Holtzman, SG, 1989)	0.28
" However, in mice tested with the naltrexone pellets still implanted, the 15 mg naltrexone pellet was able to shift the dose-response function for morphine analgesia more than 300-fold."	( Chronic opioid antagonist treatment: assessment of receptor upregulation. Lutfy, K; Sierra, V; Yoburn, BC, 1989)	0.28
" Antinociceptive dose-response curves were constructed for mu ([D-Ala2,NMePhe4,Gly-ol]enkephalin, DAGO; morphine) and delta ([D-Pen2,D-Pen5]enkephalin, DPDPE)-agonists in the absence, and in the presence of the mu non-surmountable antagonist, beta-funaltrexamine (beta-FNA) or the delta-antagonist ICI 174,864 (N,N-diallyl-Tyr-Aib-Aib-Phe-Leu-OH, where Aib is alpha-amino-isobutyric acid)."	( Opioid delta-receptor involvement in supraspinal and spinal antinociception in mice. Heyman, JS; Mosberg, HI; Mulvaney, SA; Porreca, F, 1987)	0.27
" After drug combinations had been tested, the nicotine dose-response curve was unchanged from its previous values, and naltrexone alone produced no tendency to decrease response rate."	( Evidence for opioid mechanisms in the behavioral effects of nicotine. Coen, KM; Corrigall, WA; Herling, S, 1988)	0.27
" However, the dose-response curve for naltrexone was not parallel to the morphine or fentanyl dose-response curves."	( An analysis of naltrexone and naloxone's possible agonistic actions in the dog. Martin, WR; Wettstein, JG, 1985)	0.27
" Throughout the first 3 weeks of life, Sprague-Dawley rats were given daily subcutaneous injections of either 50 mg/kg naltrexone, a dosage that invoked a complete (24 hours/day) receptor blockade, or 1 mg/kg naltrexone, a dosage which intermittently blocked (4-6 hours/day) opioid receptors and exacerbated opioid action; animals injected with sterile water served as controls."	( Endogenous opioid systems and the regulation of dendritic growth and spine formation. Hauser, KF; McLaughlin, PJ; Zagon, IS, 1989)	0.28
" An inverted-U dose-response curve was obtained."	( Pharmacological evidence of a central effect of naltrexone, morphine, and beta-endorphin and a peripheral effect of met- and leu-enkephalin on retention of an inhibitory response in mice. Baratti, CM; Introini, IB; McGaugh, JL, 1985)	0.27
" Pretreatment with the opiate receptor antagonist naltrexone resulted in a parallel shift to the right of the dose-response curve for alpha-methyldopa, both for blood pressure and heart rate."	( Antagonism by naltrexone of the hypotension and bradycardia induced by alpha-methyldopa in conscious normotensive rats. de Jong, W; van Giersbergen, PL, 1988)	0.27
" However, these challenges have been conducted after relatively acute dosing with naltrexone, and tolerance to this antagonism after chronic treatment is possible."	( Nontolerance to the opioid antagonism of naltrexone. Gaspari, J; Kleber, HD; Kosten, TR; Topazian, M, 1985)	0.27
" In the mouse vas deferens, pre-treatment with beta-FNA (1 X 10(-6)M) produced a similar shift in the dose-response curves for normorphine as in the guinea-pig ileum."	( Determination of the receptor selectivity of opioid agonists in the guinea-pig ileum and mouse vas deferens by use of beta-funaltrexamine. Hayes, AG; Sheehan, MJ; Tyers, MB, 1985)	0.27
" In the dosage used, naltrexone appears not to be useful in Alzheimer-type dementia."	( Effect of naltrexone on senile dementia of the Alzheimer type. Damasio, AR; Eslinger, PJ; Hyman, BT, 1985)	0.27
" The dosage of beta-FNA utilized (5 mg/kg) blocked morphine-induced analgesia (2 mg/kg morphine sulfate, SC) for each injection period (i."	( beta-Funaltrexamine (beta-FNA) and the regulation of body and brain development in rats. McLaughlin, PJ; Zagon, IS, 1986)	0.27
"The effects of the delta-selective antagonist ICI 174864 and naltrexone on the dose-response curves to the mu-selective agonist RX 783006 and D-ala-D-leucine enkephalin (DADL) have been investigated in the rat isolated vas deferens preparation (RVD) set up in Krebs solution containing half the normal Ca++ concentration."	( Delta receptors in the rat vas deferens. Carter, A; Smith, CF, 1986)	0.27
"Systemic administration of beta-funaltrexamine (beta-FNA) 24 hr before analgesic testing produced approximately a 10-fold parallel shift in the dose-response curves of the prototypic mu agonists morphine, I-methadone, fentanyl and etorphine in the mouse abdominal constriction test."	( Use of beta-funaltrexamine to determine mu opioid receptor involvement in the analgesic activity of various opioid ligands. Hynes, MD; Leander, JD; Reel, JK; Zimmerman, DM, 1987)	0.27
" The daily dosage of naltrexone recommended for opioid addiction did not cause abnormalities of serum transaminase values in these studies."	( Naltrexone hydrochloride (Trexan): a review of serum transaminase elevations at high dosage. Allen, JI; Atkinson, RL; Knopman, DS; Malcolm, RJ; Mitchell, JE; Morley, JE; Pfohl, DN, 1986)	0.27
" To determine if these failures were due to inadequate dosage (pharmacokinetic failure) or lack of an inherent pharmacologic effect (pharmacodynamic failure), the present study was conducted with nalmefene (Key Pharmaceuticals, Inc."	( The effects of nalmefene, a potent oral opiate antagonist, on exercise-induced bronchospasm. Christopher, MA; Harman, E; Hendeles, L; Wyzan, D, 1988)	0.27
" Both antagonists produced large shifts in the dose-response curves to the mu-agonists, morphine and fentanyl, confirming their mu-antagonist activity."	( Reversal by beta-funaltrexamine and 16-methyl cyprenorphine of the antinociceptive effects of opioid agonists in the mouse and guinea-pig. Birch, PJ; Hayes, AG, 1988)	0.27
"32 days, despite lower clonidine dosage and significantly lower diazepam dosage on the second day."	( Opioid withdrawal and naltrexone induction in 48-72 hours with minimal drop-out, using a modification of the naltrexone-clonidine technique. Bailey, C; Brewer, C; Rezae, H, 1988)	0.27
" We communicate here findings demonstrating that (a) three different inbred strains of mice possess a clear-cut cycle of melatonin levels in serum, (b) that melatonin administered in the evening enhances primary antibody response (IgM and IgG immunoglobulins) in vivo according to a dose-response behaviour and that (c) the opioid receptors blocker naltrexone antagonizes the immunostimulatory effect of melatonin."	( Role of the pineal gland in immunity: II. Melatonin enhances the antibody response via an opiatergic mechanism. Conti, A; Maestroni, GJ; Pierpaoli, W, 1987)	0.27
" Any patient who showed cognitive/behavioral improvement on a given dose of naltrexone was then treated with this dosage in a double-blind crossover comparison to placebo."	( Naltrexone and Alzheimer's disease. Adler, J; Corwin, J; Jordan, B; Resnick, R; Rotrosen, JP; Serby, M, 1986)	0.27
" A dosing schedule of 20 mg q12h was then started and continued for seven days."	( Nalmefene: safety and kinetics after single and multiple oral doses of a new opioid antagonist. Dixon, R; Garg, D; Gentile, J; Howes, J; Hsiao, J; Hsu, HB; Weidler, D, 1987)	0.27
" Comparisons of dose-response curves and efficacies demonstrated that d-NANM was more similar to PCP in its effectiveness in depressing the flexor and skin twitch reflexes than was l-NANM."	( Pharmacologic and reinforcing properties of phencyclidine and the enantiomers of N-allylnormetazocine in the dog. Risner, ME; Shannon, HE; Vaupel, DB, 1986)	0.27
" However, the naltrexone was associated with hepatotoxicity when used at this dosage in this population."	( High-dose naltrexone therapy and dietary counseling for obesity. Gannon, M; Hatsukami, D; Levine, AS; Mitchell, JE; Morley, JE; Pfohl, D, 1987)	0.27
" In the present study naltrexone at a daily dosage of 200 mg did not appear to have efficacy in producing weight loss after eight weeks of treatment."	( A controlled trial of naltrexone in obese humans. Counts, C; Currey, HS; Malcolm, R; O'Neil, PM; Riddle, FE; Sexauer, JD, 1985)	0.27
" This dosing method produced high plasma naltrexone levels (350 ng/ml) by 1 hr which declined over an implant period of 192 hr (24 ng/ml)."	( Pharmacokinetics and pharmacodynamics of subcutaneous naltrexone pellets in the rat. Cohen, AH; Inturrisi, CE; Yoburn, BC, 1986)	0.27
" At 30 min, the dose-response curve was shifted to the right."	( Chronic stress, aging and morphine analgesia: chronic stress affects the reactivity to morphine in young mature but not old rats. Girardot, MN; Holloway, FA, 1985)	0.27
" Although the same organs in males and females within a dosage group were influenced by naltrexone, and usually to a similar degree, a dosage of 1 mg/kg naltrexone often affected different organ systems than the 50 mg/kg dosage."	( Opioid antagonist-induced regulation of organ development. McLaughlin, PJ; Zagon, IS, 1985)	0.27
" These results show that tumorigenic events are dictated by the duration of opiate receptor blockade rather than the dosage of opiate antagonist, and provide compelling evidence that endogenous opioid systems play a crucial role in neuro-oncogenic expression."	( Duration of opiate receptor blockade determines tumorigenic response in mice with neuroblastoma: a role for endogenous opioid systems in cancer. McLaughlin, PJ; Zagon, IS, 1984)	0.27
" Repetitive administration of low dosages (3 mg/kg naltrexone, 3 times daily), which blocked the receptor 24 hr/day, increased body and brain development by 31% and 10%, respectively, whereas a cumulative dosage of 9 mg/kg naltrexone given once daily retarded growth."	( Naltrexone modulates body and brain development in rats: a role for endogenous opioid systems in growth. McLaughlin, PJ; Zagon, IS, 1984)	0.27
" Thus, the interactions between these drugs and the narcotic antagonists allow the classification of the drugs into three groups, based on a marked shift, a moderate shift or no shift in the dose-response curve."	( Interactions between narcotic agonists, partial agonists and antagonists evaluated by schedule-controlled behavior. Harris, RA, 1980)	0.26
") produced a dose-response curve with a reduced maximum effect."	( Relative involvement of receptor subtypes in opioid-induced inhibition of intestinal motility in mice. Takemori, AE; Ward, SJ, )	0.13
"3 mg/kg) produced a 3-fold shift to the right of the cyclazocine dose-response curve but did not completely block the cyclazocine-like stimulus effects of either SKF 10,047 or ethylketocyclazocine."	( Discriminative stimulus effects of prototype opiate receptor agonists in monkeys. Holtzman, SG; Teal, JJ, 1980)	0.26
" A dose-response investigation of morphine's action (5, 10, 15 and 20 mg/kg) in additional animals receiving 10 daily administrations of ECS reveals that a greater tolerance to morphine's motor inhibitory effect than to its analgesic effect results from repeated ECS administration."	( Different opioid systems may participate in post-electro-convulsive shock (ECS) analgesia and catalepsy. Frenk, H; Urca, G; Yitzhaky, J, 1981)	0.26
" 2 Buprenorphine revealed a bell-shaped dose-response curve for antinociception peaking at approx."	( In vivo receptor binding of the opiate partial agonist, buprenorphine, correlated with its agonistic and antagonistic actions. Dum, JE; Herz, A, 1981)	0.26
" Naltrexone in a dosage of 1 mg/kg, which blocked morphine-induced analgesia for 4 hr/day, had the opposite effects."	( Naltrexone modulates growth in infant rats. McLaughlin, PJ; Zagon, IS, 1983)	0.27
"The basis for using narcotic antagonists for the treatment of opiate addiction is discussed briefly, and the chemistry, pharmacology, pharmacokinetics, clinical efficacy, adverse effects, and dosage of naltrexone hydrochloride, an opiate antagonist drug, are reviewed."	( Review of naltrexone, a long-acting opiate antagonist. Crabtree, BL, )	0.13
" Patients randomly assigned to the gradual group (group G) began 4-mg/wk reduction the Monday of week 9 and reached zero dosage (placebo) the Monday of week 23; patients in the abrupt group (group A) continued to receive 50, 50, and 65 mg until the Monday of week 23, when their dosage was dropped to zero (placebo)."	( Methadyl acetate (LAAM) in the treatment of heroin addicts. II. Double-blind comparison of gradual and abrupt detoxification. Goldstein, A; Inturrisi, CE; Judson, BA, 1983)	0.27
"0 mg/kg) produced dose-related shifts to the right in the dose-response curves for the discriminative stimulus and rate-decreasing effects of morphine and ethylketazocine without affecting the response produced by meperidine."	( Narcotic discrimination in pigeons: antagonism by naltrexone. Herling, S; Solomon, RE; Valentino, RJ; Woods, JH, 1984)	0.27
" Our observations indicate that, despite the continuous infusion of a dosage of 5 alpha-dihydrotestosterone that significantly suppresses LH pulse frequency, co-administration of an opiate-receptor antagonist effectively reinstates LH pulse frequency to control levels."	( Role of endogenous opiates in the expression of negative feedback actions of androgen and estrogen on pulsatile properties of luteinizing hormone secretion in man. Ertel, NH; Rogol, AD; Samojlik, E; Veldhuis, JD, 1984)	0.27
" The highest dosage administered produced transient weight depression and possibly increased resorption."	( Reproductive toxicity and teratology evaluations of naltrexone. Christian, MS, 1984)	0.27
"From birth to day 21, rat offspring received daily injections of naltrexone at a dosage that blocked morphine-induced analgesia 24 hours a day."	( Increased brain size and cellular content in infant rats treated with an opiate antagonist. McLaughlin, PJ; Zagon, IS, 1983)	0.27
" Furthermore, we observed that the antagonism between ethanol and naloxone appeared to be competitive in nature since a fixed dose of ethanol (1 g/kg, blood ethanol concentration 60 mg/dl) shifted the naloxone dose-response curve significantly to the right and high doses of the antagonist overcame ethanol's effects."	( Ethanol inhibits the naloxone-induced release of luteinizing hormone-releasing hormone from the hypothalamus of the male rat. Bell, RD; Cicero, TJ; Gerrity, M; Newman, KS; Schmoeker, PF, 1982)	0.26
" No change was observed in the rate of naltrexone disposition during chronic dosing vs."	( The clinical pharmacology of naltrexone: pharmacology and pharmacodynamics. Verebey, K, 1981)	0.26
" Maintaining particulate-free products and sterilization methods are two problems with all parenteral dosage forms."	( A review of parenteral sustained-release naltrexone systems. Kincl, FA; Olsen, JL, 1981)	0.26
" The factors affecting the release of drug from the delivery system were the ratio of cholesterol to naltrexone, drug loading level and surface area to unit volume of dosage form."	( An improved long-acting delivery system for narcotic antagonists. Misra, AL; Pontani, RB, 1981)	0.26
" At age 14, naloxone reduced the food consumed by all the pretreatment groups, and pretreatment with morphine altered the dose-response curves for feeding modulation induced by naloxone."	( Effects of chronic antenatal and postnatal administration of narcotics on naloxone-induced anorexia in preweanling rats. Aroyewun, OO; Barr, GA, 1983)	0.27
" Under controlled inpatient conditions established to assess dosage guidelines and to examine specific signs and symptoms of withdrawal, ten (91%) of 11 patients were able to withdraw completely from methadone therapy by the end of a six-day period."	( Clonidine and naltrexone. A safe, effective, and rapid treatment of abrupt withdrawal from methadone therapy. Braverman, P; Charney, DS; Heninger, GR; Kleber, HD; Murburg, M; Redmond, DE; Riordan, CE; Sternberg, DE, 1982)	0.26
" This insensitivity to morphine satisfied the two pharmacological criteria for tolerance: a parallel shift to the right in the morphine dose-response curve and a reduced effect of the drug at the same brain concentration."	( Development of tolerance to the effects of morphine on luteinizing hormone secretion as a function of castration in the male rat. Cicero, TJ; Meyer, ER; Schmoeker, PF, 1982)	0.26
"Naltrexone was given to ten opiate-free volunteer subjects following the same dosage schedule used for initiating treatment of opiate-dependent persons."	( Aversive effects of naltrexone in subjects not dependent on opiates. Boukhabza, D; Gillespie, HK; Hollister, LE; Johnson, K, 1981)	0.26
"01) compared to vehicle level resulted in a shallow dose-response curve across the dose range tested (0."	( Nitrous oxide induces feeding in the nondeprived rat that is antagonized by naltrexone. Czech, DA, 1995)	0.29
" Then all patients were administered naltrexone at the dosage 50 mg/d orally for 6 months."	( Naltrexone treatment restores menstrual cycles in patients with weight loss-related amenorrhea. Gamba, O; Gastaldi, M; Genazzani, AD; Genazzani, AR; Petraglia, F; Volpogni, C, 1995)	0.29
", the morphine dose-response curve shifted to the left and the ED50 value of morphine decreased."	( Effects of a highly selective nonpeptide delta opioid receptor agonist, TAN-67, on morphine-induced antinociception in mice. Endoh, T; Misawa, M; Mori, T; Nagase, H; Suzuki, T; Tsuji, M, 1995)	0.29
" The first dose of naltrexone was given 24 hours before MSC dosing, followed by a second dose at the time of MSC dosing and a third dose 24 hours after MSC administration."	( A bioequivalence study of oral controlled-release morphine using naltrexone blockade. Goldenheim, PD; Grandy, RP; Kaiko, RF; Reder, RF; Sackler, RS, 1995)	0.29
" Administration of U50,488H (3 mg/kg), in conjunction with several doses of cocaine, did not shift the cocaine dose-response curve."	( Assessment of the discriminative stimulus effects of cocaine in the rat: lack of interaction with opioids. Broadbent, J; Dworkin, SI; Gaspard, TM, )	0.13
" Dose-response curves were subsequently determined under conditions of no stress, restraint, corticosterone (3 mg/kg, IP), and saline."	( Effects of restraint stress and intra-ventral tegmental area injections of morphine and methyl naltrexone on the discriminative stimulus effects of heroin in the rat. Shaham, Y; Stewart, J, )	0.13
" The pellets were removed and 24 h later, mice were sacrificed and binding studies were conducted, or mice were tested in analgesia (tail-flick) dose-response studies."	( Supersensitivity to opioid analgesics following chronic opioid antagonist treatment: relationship to receptor selectivity. Chan, K; Davis, T; Duttaroy, A; Shah, S; Yoburn, BC, )	0.13
" These effects were gone 24 h after dosing in one child, but persisted in the other."	( Clinical case report: opiate antagonist and event-related desynchronization in 2 autistic boys. Klimesch, W; Klingler, D; Lensing, P; Panksepp, J; Pap, V; Schimke, H; Szemes, G, 1995)	0.29
"5 micrograms), parallel rightward shifts of both morphine and RB 101 (mixed enkephalin-degrading-enzyme inhibitor) dose-response curves, were observed, but the concentration of beta-FNA required to reduce the analgesic responses was about 10 times higher for RB 101 (0."	( Assessment of endogenous enkephalins efficacy in the hot plate test in mice: comparative study with morphine. Noble, F; Roques, BP, 1995)	0.29
" Although it was possible that the clinical findings in these horses may have resulted from use of an inadequate dosage of carfentanil or xylazine, or both, analysis of the results more likely indicated that domestic and exotic horses may respond differently to carfentanil, and domestic horses may not be a good model for use in studies of carfentanil."	( Complications with the use of carfentanil citrate and xylazine hydrochloride to immobilize domestic horses. Carpenter, JW; Leith, DE; Shaw, ML, 1995)	0.29
"4 mg/kg) reduced final ratios and an inverted U dose-response relationship was established for the unit heroin doses 12."	( Heroin self-administration in rats under a progressive ratio schedule of reinforcement. Bennett, SA; Roberts, DC, 1993)	0.29
" This EEG activation was greatly attenuated at DPDPE doses greater than 154 nmol/h, resulting in a U-shaped dose-response curve."	( Effects of the delta-opioid agonist, [D-Pen2,D-Pen5]-enkephalin, on fetal lamb EEG. Cheng, PY; Soong, Y; Szeto, HH; Wu, DL, 1994)	0.29
" Dose-response curves were generated for both delta 9-THC (i."	( Interactions between delta 9-tetrahydrocannabinol and kappa opioids in mice. Martin, BR; Smith, PB; Welch, SP, 1994)	0.29
" Case descriptions highlight some of the many changes veterans experienced on nalmefene dosage increases."	( A preliminary trial of nalmefene for the treatment of emotional numbing in combat veterans with post-traumatic stress disorder. Glover, H, 1993)	0.29
" dose-response studies with TCTAP (mu), naltrindole (delta) and norbinaltorphimine (kappa)."	( The role of multiple opioid receptors in the maintenance of stimulation-induced feeding. Carr, KD; Papadouka, V, 1994)	0.29
" dose-response studies with TCTAP (mu), norbinaltorphimine (kappa), and naltrindole (delta)."	( The role of multiple opioid receptors in the potentiation of reward by food restriction. Carr, KD; Papadouka, V, 1994)	0.29
"03 microgram of DAMGO resulting in a steeper dose-response relationship."	( Evidence for delta opioid receptor subtypes in rat spinal cord: studies with intrathecal naltriben, cyclic[D-Pen2, D-Pen5] enkephalin and [D-Ala2, Glu4]deltorphin. Hammond, DL; Stewart, PE, 1993)	0.29
" Multiple venous blood samples were taken throughout the dosing regimen, and the resulting fentanyl, nalmefene, or naloxone plasma concentrations were determined."	( Duration of opioid antagonism by nalmefene and naloxone in the dog: an integrated pharmacokinetic/pharmacodynamic comparison. Osifchin, E; Veng-Pedersen, P; Waters, SJ; Wilhelm, JA; Zakszewski, TB, 1995)	0.29
" Dose-response and antagonist testing commenced once stable rates of cocaine SA were achieved."	( Lack of involvement of delta-opioid receptors in mediating the rewarding effects of cocaine. Babovic-Vuksanovic, D; de Vries, TJ; Elmer, G; Shippenberg, TS, 1995)	0.29
" A naltrexone-insensitive component to beta-endorphin antinociception also was identified in studies which evaluated the ability of the antagonist to shift the beta-endorphin dose-response curve."	( Biochemical and pharmacological characterization of multiple beta-endorphinergic antinociceptive systems in the rat periaqueductal gray. Hawranko, AA; Monroe, PJ; Smith, DJ; Smith, DL, 1996)	0.29
" Preliminary experiments established the pharmacodynamics and dose-response for NorBNI."	( Cardiorespiratory and sleep-wake behavior in developing swine: kappa-opioid influence. Faltus, RE; Inman, JD; Laferrière, A; Moss, IR, 1995)	0.29
" When the regenerated cellulose acetate device filled with osmotic filler was implanted in rabbits which were subsequently dosed at day 7 and day 14 post-implant with 150 mg kg(-1) morphine sulphate, the concentration of morphine in the device was only about 10-fold less than that measured in rabbit blood."	( Biocompatibility and in vivo morphine diffusion into a placebo morphine-triggered naltrexone delivery device in rabbits. Fritzinger, BK; Heller, J; Nakayama, GR; Roskos, KV; Tefft, JA, 1995)	0.29
"8 micrograms carfentanil/kg, the lowest dosage used, was very excited during induction and required intravenous (IV) ketamine to permit safe examination."	( Immobilization of black bears (Ursus americanus) with orally administered carfentanil citrate. Clyde, VL; Ramsay, EC; Sleeman, JM, 1995)	0.29
" With all opioids, time course experiments showed that this analgesic effect lasted for at least 4 hr, with no untoward effects observed within each dosage range used."	( Relative analgesic potency of mu, delta and kappa opioids after spinal administration in amphibians. Stevens, CW, 1996)	0.29
" The decreases in labeling index evoked by OGF were blocked by concomitant administration of the opioid antagonist, naloxone (10 mg/kg); naloxone alone at the dosage utilized had no influence on cell replicative processes."	( The opioid growth factor, [Met5]-enkephalin, and the zeta opioid receptor are present in human and mouse skin and tonically act to inhibit DNA synthesis in the epidermis. McLaughlin, PJ; Wu, Y; Zagon, IS, 1996)	0.29
" Fifteen min after each elk became recumbent, we administered naltrexone HCl (25% of dose intravenously, 75% subcutaneously) dosed at 0 (control), 25, 50, or 100 mg/mg carfentanil; after an additional 15 min of immobilization, controls received 500 mg naltrexone HCl/mg carfentanil."	( Efficacy and safety of naltrexone hydrochloride for antagonizing carfentanil citrate immobilization in captive Rocky Mountain elk (Cervus elaphus nelsoni). Lance, WR; Miller, MW; Wild, MA, 1996)	0.29
" This regimen of dosing and daily opportunities to drink continued for 30 days."	( Naltrexone persistently reduces rats' intake of a palatable alcoholic beverage. Gardell, LR; Hubbell, CL; Reid, LD, 1996)	0.29
"In a double-blind placebo-controlled crossover trial 23 autistic children, aged 3-7 years, were treated with a mean daily dosage of 1 mg/kg naltrexone for 4 weeks."	( The effects of chronic naltrexone treatment in young autistic children: a double-blind placebo-controlled crossover study. Buitelaar, JK; van Engeland, H; Willemsen-Swinkels, SH, 1996)	0.29
"0 mg/kg) if the dosing interval was 10 min, whereas 30."	( Opioid antagonist profile of SC nor-binaltorphimine in the formalin paw assay. Grouhel, A; Wettstein, JG, 1996)	0.29
"A procedure was employed in the present study to obtain dose-response curves for heroin self-administration within each experimental session."	( Within-session determination of dose-response curves for heroin self-administration in rats: Comparison with between-session determination and effects of naltrexone. Dworkin, SI; Martin, TJ; Sizemore, GM; Smith, JE; Walker, LE, 1996)	0.29
" In rat, tissue distribution and metabolite plasma concentration-time data were obtained following intravenous bolus dosing of nalmefene."	( Disposition of the opioid antagonist, nalmefene, in rat and dog. Kvalo, LT; Lessor, RA; Mathur, C; Murthy, SS; Wilhelm, JA, 1996)	0.29
"1-fold leftward shift in the dose-response curve."	( Intrathecal Tyr-W-MIF-1 produces potent, naloxone-reversible analgesia modulated by alpha 2-adrenoceptors. Gergen, KA; Kastin, AJ; Paul, D; Zadina, JE, 1996)	0.29
" Once rats had acquired the discrimination an ethanol dose-response test was conducted."	( The influence of opioid antagonists on the discriminative stimulus effects of ethanol. Spanagel, R, 1996)	0.29
" We conclude that no dosage alteration is warranted in elderly patients."	( The effect of age on the pharmacokinetics of the opioid antagonist nalmefene. Bikhazi, GB; Frye, RF; Jallad, NS; Matzke, GR; Wilhelm, JA, 1996)	0.29
" The parallelism of the dose-response curves indicates activation of a common receptor subtype."	( alpha-Adrenoceptor and opioid receptor modulation of clonidine-induced antinociception. Miranda, HF; Naquira, D; Pinardi, G; Sierralta, F, 1996)	0.29
" Determining the best dosing strategy has been the goal of recent treatment studies with alcohol-dependent patients."	( Dosing issues in the pharmacotherapy of alcoholism. Mason, BJ, 1996)	0.29
" The most common adverse effects reported with the use of naltrexone at a dosage of 50 mg/day include nausea and vomiting."	( A risk-benefit assessment of naltrexone in the treatment of alcohol dependence. Berg, BJ; Pettinati, HM; Volpicelli, JR, 1996)	0.29
"Local perfusion with ibogaine (10(-6) M-10(-3) M) via microdialysis probes in the nucleus accumbens or striatum of rats produced a biphasic dose-response effect on extracellular dopamine levels."	( Neuropharmacological characterization of local ibogaine effects on dopamine release. Berger, SP; Broderick, PA; Hsu, K; Reid, MS; Souza, KH, 1996)	0.29
" However, because nalmefene will be primarily used in the acute care setting for reversal of opioid-induced effects, it is not likely that these alterations will necessitate a dosage modification."	( Effects of liver disease on the disposition of the opioid antagonist nalmefene. Dixon, R; Frye, RF; Matzke, GR; Rabinovitz, M; Schade, R, 1997)	0.3
" However, inhibition reached the maximal level only at 50 mM sodium, and typical sigmoidal dose-response curves were obtained only in the presence of 118 mM sodium."	( Regulation of mu-opioid receptor in neural cells by extracellular sodium. Medzihradsky, F; Yabaluri, N, 1997)	0.3
" At 7 weeks of age, dose-response curves were obtained with morphine (10, 31."	( Influence of chronic prenatal and postnatal administration of naltrexone in locomotor activity induced by morphine in mice. Luján Estrada, M; Medina Jiménez, M; Rodríguez, R, 1997)	0.3
" Antagonist dose-response curves were plotted."	( 5-HT spinal antinociception involves mu opioid receptors: cross tolerance and antagonist studies. Freeman, J; Gent, JP; Goodchild, CS; Guo, Z, 1997)	0.3
"5 g/kg) inhibited naltrexone-induced stimulation of testosterone secretion and shifted the naltrexone dose-response curve to the right."	( Interactions between alcohol- and opioid-induced suppression of rat testicular steroidogenesis in vivo. Adams, ML; Cicero, TJ; Meyer, ER, 1997)	0.3
" Little information seems to have been collected regarding the most effective dosing regimen for reducing alcohol craving and consumption, and the usefulness of opiate antagonists in the prevention of alcohol dependence in nonaddicts, rather than just as a treatment agent in addicted individuals, also deserves further study."	( Naltrexone effects on ethanol drinking acquisition and on established ethanol consumption in C57BL/6J mice. Dorow, JD; Phillips, TJ; Wenger, CD, 1997)	0.3
" The present study provides systematic dose-response analyses indicating that NTX elicited optimal enhancement of morphine's antinociceptive potency in mice when co-administered (i."	( Ultra-low doses of naltrexone or etorphine increase morphine's antinociceptive potency and attenuate tolerance/dependence in mice. Crain, SM; Shen, KF, 1997)	0.3
" In dose-response studies, 3-methoxynaltrexone (2."	( 3-Methoxynaltrexone, a selective heroin/morphine-6beta-glucuronide antagonist. Brown, GP; Chang, A; King, MA; Leventhal, L; Pasternak, GW; Rossi, GC; Yang, K, 1997)	0.3
" Females received daily injections of 50 mg/kg naltrexone (NTX), a dosage found to block opioids from interacting with opioid receptors for 24 h, throughout pregnancy."	( Chronic exposure to the opioid antagonist naltrexone during pregnancy: maternal and offspring effects. Lang, CM; McLaughlin, PJ; Tobias, SW; Zagon, IS, 1997)	0.3
" The usual dosage is 50 mg per day."	( Naltrexone for the treatment of alcoholism. Alpert, N; Ciraulo, AM; Franko, KJ, 1997)	0.3
" The formulation prepared from tablets provides flexible dosing in patients undergoing rapid withdrawal from methadone."	( Formulation and stability of naltrexone oral liquid for rapid withdrawal from methadone. Fawcett, JP; Morgan, NC; Woods, DJ, 1997)	0.3
" In dose-response tests, subjects rarely responded on the U-50,488H-appropriate key when morphine was administered or on the morphine-appropriate key when they received U-50,488H."	( Establishing morphine and U-50,488H as discriminative stimuli in a three-choice assay with pigeons. Makhay, MM; Poling, A; Young, AM, 1998)	0.3
" Dose-response curves for 1DMe in the presence of naltrindole or naltrexone, delta- and mu-opioid selective antagonists respectively, indicate that 1DMe preferentially reversed mu-receptor-mediated but increased delta-receptor-mediated analgesia."	( Differential modulation of mu- and delta-opioid antinociception by neuropeptide FF receptors in young mice. Desprat, C; Zajac, JM, 1997)	0.3
" The dissolution parameters were calculated "in vitro", then a correlation model was applied to determine the relationship between these parameters and the "in vivo" pharmacokinetic parameters of Naltrexone at each dosage level and also their degree of association."	( [The solubility and in vivo-in vitro correlation of naltrexone]. Lorduy Oses, L; Navarro Guerrero, J; Ruiz Ramirez, JC, 1998)	0.3
" Nalmefene has been shown to reverse opioid intoxication for as long as 8 h, reducing the need for continuous monitoring of intoxicated patients and repeated dosing of naloxone."	( Nalmefene: a long-acting opioid antagonist. Clinical applications in emergency medicine. Sternbach, G; Varon, J; Wang, DS, )	0.13
" Twenty-one patients meeting DSM-III criteria for schizophrenia were enrolled; all patients had been stabilized for at least 2 weeks on their dosage of neuroleptic medicine before entering the study."	( Naltrexone augmentation of neuroleptics in schizophrenia. Charney, DS; Glazer, WM; Heninger, GR; Krystal, JH; Petrakis, IL; Price, LH; Sernyak, MJ; Woods, SW, 1998)	0.3
"), shifted the dose-response relationships to the right for each of the antidepressant agents (dothiepin, amitriptyline, sibutramine, (+)-oxaprotiline and paroxetine)."	( The involvement of the opioidergic system in the antinociceptive mechanism of action of antidepressant compounds. Gray, AM; Sewell, RD; Spencer, PS, 1998)	0.3
" In particular, issues addressed include alternative dosage regimens, necessary duration of treatment, employment of medications in combination, integration of pharmacologic agents with behavioral interventions, enhancement of patient compliance, and concurrent treatment of psychiatric comorbidity."	( Advances in development of medications for alcoholism treatment. Allen, JP; Litten, RZ, 1998)	0.3
" We conclude that, due to behavioral, neurochemical, or other factors, individuals with both alcohol and cocaine use disorders are distinct from those dependent on alcohol alone, and that NTX at a dosage of 50 mg/day is not efficacious in this patient population."	( Naltrexone treatment of comorbid alcohol and cocaine use disorders. Hersh, D; Kranzler, HR; Van Kirk, JR, 1998)	0.3
" For patients in maintenance, methadone dosage and clinic policy were the most important factors for retention."	( Retention in treatment of heroin users in Italy: the role of treatment type and of methadone maintenance dosage. Bargagli, AM; D'Ippoliti, D; Davoli, M; Pasqualini, F; Perucci, CA, 1998)	0.3
" Significant increases in ACTH and cortisol were observed after both antagonists, without an apparent dose-response relationship; however, both doses of nalmefene resulted in greater HPA axis activation than either dose of naloxone (ACTH: p <0."	( Nalmefene causes greater hypothalamic-pituitary-adrenal axis activation than naloxone in normal volunteers: implications for the treatment of alcoholism. Borg, L; Gunduz, M; Ho, A; King, A; Kreek, MJ; Maniar, S; Perret, G; Porter, M; Schluger, JH, 1998)	0.3
" It is concluded that blockade of the kappa-opioid receptor by nor-binaltorphimine may produce a rightward shift of the unit dose-response relationship of cocaine reward, thus decreasing the sensitivity to cocaine reward."	( Kappa-opioid receptor blockade with nor-binaltorphimine modulates cocaine self-administration in drug-naive rats. Gerrits, MA; Kuzmin, AV; Van Ree, JM, 1998)	0.3
" In the presence of the opioid receptor antagonists, naloxone or naltrindole, the resulting nefopam dose-response relationships were shifted to the right."	( The involvement of opioidergic and noradrenergic mechanisms in nefopam antinociception. Gray, AM; Nevinson, MJ; Sewell, RD, 1999)	0.3
" Thus, under similar motivational and dosing conditions, the opiate antagonist attenuated the reinforcing, but not the discriminative properties of ethanol, suggesting that the latter is mediated by either different or additional neural mechanisms in C57BL/6 mice."	( Naltrexone effects on ethanol reward and discrimination in C57BL/6 mice. Cuison, ER; Groseclose, CH; Kelley, BM; Middaugh, LD, 1999)	0.3
" This study was designed to determine the dose-response relation for nalmefene for the prevention of morphine-related side effects in patients receiving intravenous patient-controlled analgesia."	( Effects of prophylactic nalmefene on the incidence of morphine-related side effects in patients receiving intravenous patient-controlled analgesia. Chehade, J; Duffy, L; Gajraj, N; Johnson, ER; Joshi, GP; Wesevich, J, 1999)	0.3
" Naltrexone, an opioid receptor antagonist, was administered to three female patients with Borderline Personality Disorder in a dosage of 50 mg (q."	( [Treatment of dissociative symptoms in borderline patients with naltrexone]. Böhme, R; Bohus, M; Schmahl, C; Stiglmayr, C, 1999)	0.3
" The 2 d agonist exposure (1 microM) caused a shift in the U69,593 dose-response curve that was greater in the potassium-stimulated paradigm (140-fold) than in the spontaneous release assay (sixfold)."	( kappa-Opioid tolerance and dependence in cultures of dopaminergic midbrain neurons. Dalman, FC; O'Malley, KL, 1999)	0.3
" with a placebo or 15 mg naltrexone pellet for 8 days, the pellets removed and 24 hr later opioid receptor density (mu, delta) and receptor mRNA level (mu) determined in whole brain; or morphine dose-response studies conducted."	( Opioid receptor upregulation in mu-opioid receptor deficient CXBK and outbred Swiss Webster mice. Carroll, J; Chen, B; Duttaroy, A; Sehba, F; Shah, S; Shen, J; Yoburn, BC, 1999)	0.3
" Tachyphylaxis was infrequent (6/50), occurred late, and could be counterbalanced by raising the dosage in 2 patients."	( Efficacy and safety of naltrexone, an oral opiate receptor antagonist, in the treatment of pruritus in internal and dermatological diseases. Beissert, S; Luger, T; Metze, D; Reimann, S, 1999)	0.3
"5 mg kg-1) and the time point at which nociceptive responses were recorded (30 min after the administration of the drug) were chosen on the basis of dose-response (0."	( Preweanling naltrindole administration differentially affects clonidine induced antinociception and plasma adrenaline levels in male and female neonatal rats. Aguilar, A; Alberti, I; Alguacil, LF; Caamaño, M; Fernández, B; Romero, EM; Viveros, MP, 1999)	0.3
" Inclusion of a fixed dose of 3-O-methylnaltrexone significantly shifted the analgesic dose-response curves for 6-acetylmorphine and heroin without altering the morphine dose-response curves."	( Antagonism of heroin and morphine self-administration in rats by the morphine-6beta-glucuronide antagonist 3-O-methylnaltrexone. Izzo, E; King, M; Koob, GF; Pasternak, GW; Walker, JR, 1999)	0.3
" Diazoxide (2 microg/mouse) shifted morphine's dose-response curve 47-fold, while levcromakalim (0."	( ATP-gated K(+) channel openers enhance opioid antinociception: indirect evidence for the release of endogenous opioid peptides. Lohmann, AB; Welch, SP, 1999)	0.3
" The dose-response of intrathecal morphine (1-320 microg) for both scratching and antinociception in all subjects was established."	( An experimental itch model in monkeys: characterization of intrathecal morphine-induced scratching and antinociception. Ko, MC; Naughton, NN, 2000)	0.31
" Pretreatment with nalmefene (32 microg/kg subcutaneously) produced approximately 10-fold rightward shifts of intrathecal morphine dose-response curves for both behavioral effects."	( An experimental itch model in monkeys: characterization of intrathecal morphine-induced scratching and antinociception. Ko, MC; Naughton, NN, 2000)	0.31
" TAPA dose-response curve for antinociception."	( Selective antagonism by naloxonazine of antinociception by Tyr-D-Arg-Phe-beta-Ala, a novel dermorphin analogue with high affinity at mu-opioid receptors. Hayashi, T; Kisara, K; Kutsuwa, M; Sakurada, C; Sakurada, S; Sakurada, T; Sato, T; Takeda, S; Tan-No, K; Yuki, M, 2000)	0.31
" Electroacupuncture enhanced the antinociceptive effect of intrathecal endomorphin-1 in the formalin test, resulting in a significant leftward shift in the dose-response curves for intrathecal endomorphin-1 antinociception."	( Electroacupuncture potentiates the antinociceptive effect of intrathecal endomorphin-1 in the rat formalin test. Hao, S; Iwasaki, H; Takahata, O, 2000)	0.31
" Concomitant administration of naloxone (10 mg/kg) with OGF blocked the inhibition of DNA synthesis; naloxone alone at the dosage utilized had no effect on cell labelling."	( The opioid growth factor, [Met5]-enkephalin, inhibits DNA synthesis during recornification of mouse tail skin. Lang, CM; McLaughlin, PJ; Wilson, RP; Zagon, IS, 2000)	0.31
" The relative paucity of dose-response studies on naltrexone's effects in treating alcoholics is an important gap in the literature."	( Neuropharmacological treatments for alcoholism: scientific basis and clinical findings. Ait-Daoud, N; Johnson, BA, 2000)	0.31
" An optimal dosage regimen is critical for the treatment patient compliance in ambulatory opiate detoxification programs."	( Preclinical study of an oral controlled release naltrexone complex in mice. Alvarez-Fuentes, J; Caraballo, I; Fernández-Arévalo, M; Holgado, MA; Micó, JA; Rojas-Corrales, MO, 2000)	0.31
" Twenty-four hours later, a morphine dose-response study was conducted (tail flick); or mice were sacrificed and saturation binding studies ([3H]DAMGO) were performed in whole brain."	( The effect of nimodipine on opioid antagonist-induced upregulation and supersensitivity. Lee, SC; Yoburn, BC, 2000)	0.31
" In contrast, agonist-stimulated coupling was diminished (desensitization), resulting in a substantially flattened morphine dose-response curve."	( Calmodulin regulation of basal and agonist-stimulated G protein coupling by the mu-opioid receptor (OP(3)) in morphine-pretreated cell. Sadée, W; Surratt, CK; Wang, D, 2000)	0.31
"8 mg/kg) produced a 74-fold increase in the ED(50) of morphine while showing no effect on bremazocine or BW373U86 dose-response curves."	( Methocinnamox is a potent, long-lasting, and selective antagonist of morphine-mediated antinociception in the mouse: comparison with clocinnamox, beta-funaltrexamine, and beta-chlornaltrexamine. Broadbear, JH; Burke, TF; Husbands, SM; Lewis, JW; Sumpter, TL; Traynor, JR; Woods, JH, 2000)	0.31
" Once rats had acquired the ethanol-saline discrimination, ethanol dose-response tests were conducted with 15-min pretest injections."	( Opiate delta-2-receptor antagonist naltriben does not alter discriminative stimulus effects of ethanol. Carl, K; Garrett, KM; Holloway, FA; Mhatre, MC, 2000)	0.31
" Naltrexone attenuated the expression of ethanol place conditioning in a U-shaped dose-response function."	( Naltrexone effects on ethanol consumption and response to ethanol conditioned cues in C57BL/6 mice. Bandy, AL; Middaugh, LD, 2000)	0.31
") that was inactive against DAMGO, did not affect endomorphin-1-induced antinociception but shifted the dose-response curve of endomorphin-2 3-fold to the right."	( Differential antagonism of endomorphin-1 and endomorphin-2 spinal antinociception by naloxonazine and 3-methoxynaltrexone. Fujimura, T; Hayashi, T; Kastin, AJ; Murayama, K; Sakurada, C; Sakurada, S; Sakurada, T; Takeshita, M; Yonezawa, A; Yuhki, M; Zadina, JE, 2000)	0.31
" However, since inadequate dosing and other modifiable factors may limit its deterrent effects, the identification of a more potent metabolite of disulfiram appears to warrant further evaluation."	( Pharmacotherapy of alcoholism: gaps in knowledge and opportunities for research. Kranzler, HR, )	0.13
" In adults, results found with the use of naltrexone in eating disorders are different, when considering the duration and the dosage of the treatment and the kind of eating disorder (bulimia, binge eating or anorexia nervosa)."	( Opiate antagonists in children and adolescents. Chabane, N; Leboyer, M; Mouren-Simeoni, MC, 2000)	0.31
"1 times more potent during acute and chronic CO, and the E(max) values of the dose-response curves increased 35% during inflammation."	( Intestinal inflammation enhances the inhibitory effects of opioids on intestinal permeability in mice. Pol, O; Puig, MM; Valle, L, 2001)	0.31
" NTB (30 nM) shifted the dose-response curve of DAMGO to the right and attenuated the maximal effect."	( Pharmacological effects of naltriben as a ligand for opioid mu and kappa receptors in rat cerebral cortex. Cho, KP; Kim, KW; Shin, BS; Son, Y, 2001)	0.31
" Daily dosing clearly is effective in reducing intakes, and suspension of dosing leads to higher intakes."	( Research with rats germane to medication for alcoholism: consequences of noncompliance. Boedeker, KL; Douglass, AV; Hubbell, CL; Reid, LD; Reid, ML, 2001)	0.31
" Various dosage forms of nicotine replacement therapy increase smoking quit rates relative to placebo, but they generally do not result in 1-year quit rates of over 20%."	( Effect of nonnicotine pharmacotherapy on smoking behavior. Golding, M; Hatsukami, DK; Jamerson, BD; Kotlyar, M, 2001)	0.31
"Stimulus control by buprenorphine was maintained throughout the study and was not changed by repeated daily dosing or by an acute injection of large doses of buprenorphine."	( Characterization of the discriminative stimulus effects of buprenorphine in pigeons. Brandt, MR; France, CP; Galici, R, 2002)	0.31
" Because its pharmacological characterization has not been fully identified, the present study examined whether a dose-response range of general and selective opioid antagonists as well as antisense oligodeoxynucleotide (AS ODN) opioid probes altered daytime feeding over a 4-h time course elicited by dynorphin."	( Dynorphin A(1-17)-induced feeding: pharmacological characterization using selective opioid antagonists and antisense probes in rats. Bodnar, RJ; Grossman, HC; Hadjimarkou, MM; Pasternak, GW; Rossi, GC; Silva, RM, 2002)	0.31
" Anesthesia was rapidly and completely reversed by intravenous injections of naltrexone at 30 times the THAI dosage (0."	( Anesthesia of boma-captured Lichtenstein's hartebeest (Sigmoceros lichtensteinii) with a combination of thiafentanil, medetomidine, and ketamine. Bush, M; Citino, SB; Grobler, D; Lance, W, 2002)	0.31
" and co-administration of 3-methylnaltrexone shifted the dose-response curves for endomorphin-2 induced antinociception to the right by 4-fold."	( Differential antagonism of endomorphin-1 and endomorphin-2 supraspinal antinociception by naloxonazine and 3-methylnaltrexone. Fujimura, T; Hayashi, T; Kastin, AJ; Murayama, K; Sakurada, C; Sakurada, S; Sakurada, T; Sato, T; Takeshita, M; Yonezawa, A; Yuhki, M; Zadina, JE, 2002)	0.31
"01) extension indicates an appropriate dosage of our treatment for this experiment."	( Efficacy of naltrexone on acetylcholine-induced alloknesis in atopic eczema. Groene, D; Heyer, G; Martus, P, 2002)	0.31
" Antinociceptive dose-response curves were constructed for spinal Delta(9)-THC and WIN 55,212-2 in prodynorphin knock-out mice and in wild-type littermates."	( Dynorphin-independent spinal cannabinoid antinociception. Gardell, LR; Lai, J; Ossipov, MH; Porreca, F; Vanderah, TW, 2002)	0.31
" Additional preclinical and clinical work is warranted to identify dosing strategies that ensure adequate drug levels while reducing the possibility of developing tolerance to naltrexone."	( Advances in the use of naltrexone: an integration of preclinical and clinical findings. Froehlich, JC; O'Malley, SS, 2003)	0.32
" However, injection of nifedipine into the vPAG potentiated the antinociceptive effect of endomorphin-1, producing a significant leftward shift in the dose-response curve of endomorphin-1 in both the tail-flick and tail-pressure tests."	( Nifedipine potentiates the antinociceptive effect of endomorphin-1 microinjected into the periaqueductal gray in rats. Cousins, MJ; Fink, DJ; Hao, S; Iwasaki, H; Mamiya, K; Mata, M; Takahata, O, 2003)	0.32
" Using three human cancer cell lines: MIA PaCa-2 pancreatic adenocarcinoma, HT-29 colon adenocarcinoma, and CAL-27 squamous cell carcinoma of the head and neck, and OGF and the opioid antagonist naltrexone (NTX) at a dosage (10(-6)M) selected because it is known to repress or increase, respectively, cell replication, the effects on apoptosis (TUNEL, Annexin V) and necrosis (trypan blue) were investigated on days 2, 5, and 7 of exposure."	( Opioids and the apoptotic pathway in human cancer cells. McLaughlin, PJ; Zagon, IS, 2003)	0.32
" COMBINE incorporates a number of innovative design aspects, including a no-pill psychotherapy-alone condition, behavioral interventions that are both manual-guided and individualized, and pharmacotherapy dosing that is greater than in some previous trials."	( Testing combined pharmacotherapies and behavioral interventions in alcohol dependence: rationale and methods. , 2003)	0.32
" Patients were trained to develop personal cues as dosing reminders."	( Medication compliance feedback and monitoring in a clinical trial: predictors and outcomes. Cramer, J; Kirk, G; Krol, W; Krystal, J; Rosenheck, R, )	0.13
" 5-HT-evoked scratching was significantly reduced by systemic administration of the opiate antagonist naltrexone but was not affected by systemic morphine at a dosage (3 mg/kg) that induces analgesia."	( Opioid modulation of scratching and spinal c-fos expression evoked by intradermal serotonin. Carstens, E; Carstens, MI; Cuellar, JM; Moore, JA; Nojima, H; Simons, CT, 2003)	0.32
" However, combined oral dosing of nalmefene and subthreshold doses of AM251, a cannabinoid CB1 receptor inverse agonist, led to a significant reduction in food intake in both lean and diet-induced obese (DIO) mice."	( Synergistic effects of cannabinoid inverse agonist AM251 and opioid antagonist nalmefene on food intake in mice. Chen, RZ; Fong, TM; Huang, RR; MacNeil, DJ; Shen, CP, 2004)	0.32
" Experiment 3 confirmed the differential involvement of micro and delta receptors in ethanol intake through a more comprehensive dose-response analysis of beta-FNA and naltrindole."	( Social learning about ethanol in preweanling rats: role of endogenous opioids. Hallmark, RA; Hunt, PS, 2004)	0.32
" Naltrexone produced significant and surmountable dose-dependent rightward shifts in the morphine dose-response curves for both groups, but did not differ in potency across diets."	( Naltrexone antagonism of morphine antinociception in sucrose- and chow-fed rats. D'Anci, KE; Kanarek, RB, 2004)	0.32
" Thirty patients were randomized to treatment with injectable naltrexone (400 mg; n = 25) or a matching placebo injection (n = 5) and were dosed once every 28 days over 4 months."	( A pilot evaluation of the safety and tolerability of repeat dose administration of long-acting injectable naltrexone (Vivitrex) in patients with alcohol dependence. Ait-Daoud, N; Aubin, HJ; Ehrich, E; Guzzetta, R; Johnson, BA; Loewy, J; Silverman, B; Van Den Brink, W, 2004)	0.32
" The rapid disappearance from human plasma of dolasetron given intravenously and its virtual absence after oral dosage are explained by its liability to reduction by several enzymes, including CR which shows widespread expression in human tissues."	( Carbonyl reduction of naltrexone and dolasetron by oxidoreductases isolated from human liver cytosol. Breyer-Pfaff, U; Nill, K, 2004)	0.32
" These two compounds also exhibited nanomolar potencies in dose-response experiments performed on wild-type, M262T, Y308H, and C328R CAM receptors."	( Inverse agonism and neutral antagonism at wild-type and constitutively active mutant delta opioid receptors. Befort, K; Décaillot, FM; Filliol, D; Kieffer, BL; Lazarus, LH; Schiller, PW; Schmidhammer, H; Tryoen-Tóth, P, 2005)	0.33
" However, heroin, but not SNC-80 or U50488, significantly shifted the dose-response curve for THC discrimination to the left."	( Involvement of mu-, delta- and kappa-opioid receptor subtypes in the discriminative-stimulus effects of delta-9-tetrahydrocannabinol (THC) in rats. Goldberg, SR; Solinas, M, 2005)	0.33
" ICR mice were used to generate full antagonist dose-response curves for naloxone, naltrexone, nalbuphine, and 6beta-naltrexol in blocking acute antinociceptive effects of morphine and precipitating opioid withdrawal in models of physical dependence."	( In vivo characterization of 6beta-naltrexol, an opioid ligand with less inverse agonist activity compared with naltrexone and naloxone in opioid-dependent mice. Bhamidipati, CM; Bilsky, EJ; Blair, JR; Lowery, JJ; Paolino, RM; Raehal, KM; Sadée, W; Wang, D, 2005)	0.33
" Thus, dosage adjustement is not required in the presence of advanced dialysis-dependant renal failure."	( Pharmacokinetics and dialysability of naltrexone in patients undergoing hemodialysis. Azar, R; Bah, S; Brunet, C; Dine, T; Dupin-Spriet, T; Gressier, B; Kambia, NK; Luyckx, M; Odou, P, )	0.13
"Naltrexone is an effective medication for treatment of alcohol dependence, but its efficacy is limited by lack of adherence to the oral dosage form."	( Pharmacokinetics, safety, and tolerability of a depot formulation of naltrexone in alcoholics: an open-label trial. Cello, R; Galloway, GP; Koch, M; Smith, DE, 2005)	0.33
" Steady state was achieved rapidly, and after repeated dosing for 3 days, methylnaltrexone decreased oral-cecal transit time from a pretreatment baseline value of 101."	( Tolerability, gut effects, and pharmacokinetics of methylnaltrexone following repeated intravenous administration in humans. Charney, MR; Doshan, H; Israel, RJ; Karrison, T; Maleckar, SA; Moss, J; O'connor, M; Yuan, CS, 2005)	0.33
" In this Phase II dose-ranging study, Oxytrex bid demonstrated greater pain relief with a more convenient dosing schedule compared to oxycodone qid."	( Adding ultralow-dose naltrexone to oxycodone enhances and prolongs analgesia: a randomized, controlled trial of Oxytrex. Burns, LH; Butera, PG; Chindalore, VL; Craven, RA; Friedmann, N; Yu, KP, 2005)	0.33
" Pharmacokinetics and mu-opioid receptor occupancy of nalmefene after single and repeated dosing over 7 days was studied in 12 healthy subjects."	( Prolonged central mu-opioid receptor occupancy after single and repeated nalmefene dosing. Aalto, S; Hagelberg, N; Hietala, J; Ingman, K; Juhakoski, A; Kallio, A; Karhuvaara, S; Någren, K; Oikonen, V; Scheinin, H, 2005)	0.33
" Three human cancer cell lines (SK-N-SH neuroblastoma and SCC-1 and CAL-27 squamous cell carcinoma of the head and neck), along with OGF and the opioid antagonist naltrexone (NTX) at a dosage (10(-6) M) known to repress or increase, respectively, cell replication, were utilized."	( Opioids and differentiation in human cancer cells. McLaughlin, PJ; Zagon, IS, 2005)	0.33
" Data from dose-response studies for acamprosate alone suggest that the augmentation of acamprosate plasma levels by co-administration of naltrexone may have clinical benefits."	( Rationale for combining acamprosate and naltrexone for treating alcohol dependence. Mason, BJ, 2005)	0.33
" A dose-response study with the selective kappa antagonist nor-binaltorphimine (nor-BNI) showed that a low dose (1."	( The dynamic relationship between mu and kappa opioid receptors in body temperature regulation. Adler, MW; Chen, X; Geller, EB; McClatchy, DB; Tallarida, RJ, 2005)	0.33
"2 mg/kg) dose-dependently produced parallel rightward shifts of the dose-response curve of alfentanil-induced antinociception."	( Differential in vivo potencies of naltrexone and 6beta-naltrexol in the monkey. Divin, MF; Ko, MC; Lee, H; Traynor, JR; Woods, JH, 2006)	0.33
"5-5 mg/kg) produced a rightward shift of a heroin dose-response curve, while vigabatrin (75-300 mg/kg), baclofen (0."	( Role of opioidergic mechanisms and GABA uptake inhibition in the heroin-induced discriminative stimulus effects in rats. Filip, M; Krówka, T; Przewłocki, R; Solecki, W, )	0.13
"0 mg/kg) dose-response and time-course (10, 20, and 30 min) effects in a thermal nociceptive assay, and 2) the ability for the KOP antagonist norBNI (10."	( Antinociceptive profile of salvinorin A, a structurally unique kappa opioid receptor agonist. McCurdy, CR; Nieto, MJ; Smith, GH; Sufka, KJ; Warnick, JE, 2006)	0.33
"Oral naltrexone is effective in the treatment of alcohol dependence; however, a major limitation of its clinical utility is poor patient adherence to the daily dosing schedule."	( Single- and multiple-dose pharmacokinetics of long-acting injectable naltrexone. Dong, Q; Dunbar, JL; Ehrich, EW; Lasseter, KC; Silverman, BL; Turncliff, RZ, 2006)	0.33
" In chronic studies, the morphine dosing regimen was adjusted in each strain/sex to produce comparable levels of tolerance."	( Influence of low doses of naltrexone on morphine antinociception and morphine tolerance in male and female rats of four strains. Barrett, AC; Lomas, LM; Negus, SS; Picker, MJ; Terner, JM, 2006)	0.33
" A dose-response was constructed by administering the delta-receptor opioid methionine-enkephalin-arginine-phenylalanine (MEAP) by microdialysis into the interstitium of the canine sinoatrial node during vagal and sympathetic stimulation."	( Vagotonic effects of enkephalin are not mediated by sympatholytic mechanisms. Barlow, MA; Caffrey, JL; Deo, S; Johnson, S, 2006)	0.33
" During the treatment period, differential effects on alcohol intake were seen between periadolescent and adult animals: (a) lower doses of NTX were more effective in the periadolescent than the adult P rats, and (b) greater tolerance to repeated dosing was displayed by adult, compared with periadolescent, rats."	( Effects of naltrexone on the acquisition of alcohol intake in male and female periadolescent and adult alcohol-preferring (P) rats. Bell, RL; McBride, WJ; Rodd, ZA; Sable, HJ, )	0.13
"A variety of factors have been recognized that influence media optimization for drug release studies of implant dosage forms."	( Characterization of a potential medium for 'biorelevant' in vitro release testing of a naltrexone implant, employing a validated stability-indicating HPLC method. Barr, WH; Iyer, SS; Karnes, HT, 2007)	0.34
" Progenics is conducting clinical trials with three methylnaltrexone dosage forms: subcutaneous, IV and oral."	( Methylnaltrexone: MNTX. , 2006)	0.33
" In the presence of fixed doses of 1 or 10 microg CTAP, increasing doses of naltrexone produced dose-dependent shifts to the right in the morphine dose-response curve."	( In vivo pharmacological resultant analysis reveals noncompetitive interactions between opioid antagonists in the rat tail-withdrawal assay. Walker, EA, 2006)	0.33
"Topical application of NTX over a 10,000-fold range of dosage had no overt toxicity for the parameters studied, indicating that efficacy studies for the use of NTX in corneal wound healing are warranted."	( Corneal safety of topically applied naltrexone. Klocek, MS; Mauger, DT; McLaughlin, PJ; Sassani, JW; Zagon, IS, 2006)	0.33
" Intracerebroventricular 14-methoxymetopon administration rapidly altered ethanol intake per an inverted U-shaped dose-response function, increasing it at a 10 pg dose, while suppressing it at a 10,000-fold higher dose."	( 14-Methoxymetopon, a highly potent mu opioid agonist, biphasically affects ethanol intake in Sardinian alcohol-preferring rats. Cottone, P; Sabino, V; Schmidhammer, H; Steardo, L; Zorrilla, EP, 2007)	0.34
"OXC at a dosage of 1500-1800 mg/day might be beneficial in terms of alcohol relapse prevention."	( High and low dosage oxcarbazepine versus naltrexone for the prevention of relapse in alcohol-dependent patients. Andreoli, S; Di Nicola, M; Janiri, L; Martinotti, G; Moroni, N; Pozzi, G; Romanelli, R, 2007)	0.34
" The feeding adaptations were dissociable in onset, across individuals, and in their dose-response to the opioid-receptor antagonist nalmefene, suggesting that they represent distinct palatability-motivated processes."	( Opioid-dependent anticipatory negative contrast and binge-like eating in rats with limited access to highly preferred food. Cottone, P; Sabino, V; Steardo, L; Zorrilla, EP, 2008)	0.35
"Topically applied NTX is not only feasible, but also effective over a one hundredfold dosage for accelerating corneal wound healing in diabetic subjects."	( Topically applied naltrexone restores corneal reepithelialization in diabetic rats. Klocek, MS; McLaughlin, PJ; Sassani, JW; Zagon, IS, 2007)	0.34
" Buccal tablets containing NLX may represent a potential alternative dosage form in addiction management."	( Release of naltrexone on buccal mucosa: permeation studies, histological aspects and matrix system design. Campisi, G; De Caro, V; Florena, AM; Giandalia, G; Giannola, LI; Siragusa, MG; Tripodo, C, 2007)	0.34
"2-20 mg/kg/day), and spinal micro-opioid receptor density was examined, or morphine analgesia dose-response studies were conducted."	( Mu-opioid receptor up-regulation and functional supersensitivity are independent of antagonist efficacy. Kumar, P; Sirohi, S; Yoburn, BC, 2007)	0.34
" Outcomes for XR-NTX 190 mg (n = 26) were generally intermediate, demonstrating a dose-response effect."	( Efficacy of extended-release naltrexone in alcohol-dependent patients who are abstinent before treatment. Dong, Q; Garbutt, JC; Gastfriend, DR; Kranzler, HR; O'Malley, SS, 2007)	0.34
"Although statistically significant covariate-parameter relationships were identified, they were not considered clinically meaningful, suggesting that dosing adjustments of XR-NTX based on weight, age, gender, health status, smoking status, creatinine CL, and hepatic function differences should not be necessary."	( Population pharmacokinetics of extended-release injectable naltrexone (XR-NTX) in patients with alcohol dependence. Dunbar, JL; Farrell, CB; Hayes, SC; Turncliff, RZ, 2007)	0.34
" This study was carried out in order to determine percutaneous absorption of a transdermal codrug of naltrexol, 6-beta-naltrexol-hydroxybupropion codrug (CB-NTXOL-BUPOH), in hairless guinea pigs as well as to evaluate the safety of 6-beta-naltrexol for development as a transdermal dosage form."	( In vivo evaluation of a transdermal codrug of 6-beta-naltrexol linked to hydroxybupropion in hairless guinea pigs. Crooks, PA; Hamad, MO; Hammell, DC; Kiptoo, PK; Paudel, KS; Stinchcomb, AL, 2008)	0.35
" A dose-response effect was observed, with intermediate results for XR-NTX 190 mg."	( Early treatment response in alcohol dependence with extended-release naltrexone. Ciraulo, DA; Dong, Q; Gastfriend, DR; Pettinati, HM; Silverman, BL, 2008)	0.35
" Methadone maintenance dosage was generally dispensed daily by registered community pharmacies."	( Comparing drug-related hospital morbidity following heroin dependence treatment with methadone maintenance or naltrexone implantation. Hulse, GK; Ngo, HT; Tait, RJ, 2008)	0.35
" There was no apparent dose-response above 5mg."	( Subcutaneous methylnaltrexone for the treatment of opioid-induced constipation in patients with advanced illness: a double-blind, randomized, parallel group, dose-ranging study. Galasso, FL; Israel, RJ; Moehl Boatwright, ML; Portenoy, RK; Stambler, N; Thomas, J; Tran, D; Von Gunten, CF, 2008)	0.35
" In cumulative dosing studies (0."	( The effects of herkinorin, the first mu-selective ligand from a salvinorin A-derived scaffold, in a neuroendocrine biomarker assay in nonhuman primates. Butelman, ER; Kreek, MJ; Prisinzano, TE; Rus, S; Simpson, DS; Wolf, A, 2008)	0.35
" Further analyses of these data, clinical trial designs and the various dosage forms are necessary to determine the potential role of methylnaltrexone in the treatment of POI."	( Methylnaltrexone, a new peripherally acting mu-opioid receptor antagonist being evaluated for the treatment of postoperative ileus. Kraft, MD, 2008)	0.35
" Conclusions This case suggests that, in some circumstances, the opioid blockade may be overcome when naltrexone levels drop towards the end of the dosing interval, producing vulnerability to subsequent naltrexone-induced withdrawal."	( Precipitated withdrawal during maintenance opioid blockade with extended release naltrexone. Fishman, M, 2008)	0.35
"), dose-dependently produced rightward shifts of the dose-response curve of Ro 64-6198-induced antinociception."	( Behavioral effects of a synthetic agonist selective for nociceptin/orphanin FQ peptide receptors in monkeys. Fantegrossi, WE; Galuska, CM; Ko, MC; Prinssen, EP; Wichmann, J; Woods, JH, 2009)	0.35
"To review the chemistry, pharmacodynamics, pharmacokinetics, clinical efficacy, tolerability, indications, and dosing and administration of methylnaltrexone methobromide, the first approved peripherally selective opioid receptor-antagonist."	( Methylnaltrexone methobromide: the first peripherally active, centrally inactive opioid receptor-antagonist. Guay, DR, 2009)	0.35
"Methylnaltrexone methobromide is administered into the upper arm, abdomen, or thigh once every other day, with the frequency of dosing being increased, if needed, to a maximum of once daily."	( Methylnaltrexone methobromide: the first peripherally active, centrally inactive opioid receptor-antagonist. Guay, DR, 2009)	0.35
" Following 14 ethanol consumption sessions during adulthood, a naltrexone dose-response challenge (0-0."	( Appetitive motivational experience during adolescence results in enhanced alcohol consumption during adulthood. Ehlers, CL; Walker, BM, 2009)	0.35
" The main parameters of single dosing were as follows: t1/2alpha was (0."	( [Pharmacokinetics of 6beta-naltrexol after single and multiple intramuscular injections in Beagle dogs]. Cui, MX; Dong, HJ; Gong, ZH; Liu, J; Liu, YS; Yan, LD; Yao, XJ, 2009)	0.35
"0 mg/kg) attenuated the priming effects of cocaine, shifting the cocaine dose-response function rightward and downward."	( Attenuation of cocaine-induced reinstatement of drug seeking in squirrel monkeys: kappa opioid and serotonergic mechanisms. Platt, DM; Rowlett, JK; Rüedi-Bettschen, D; Spealman, RD, 2010)	0.36
" The same sequence of experiments was repeated in the isolated heart model using the maximal protective dose of remifentanil from the dose-response studies."	( Remifentanil post-conditioning attenuates cardiac ischemia-reperfusion injury via kappa or delta opioid receptor activation. Irwin, MG; Jiang, LL; Li, R; Wong, GT, 2010)	0.36
" Also, an analysis of medians was calculated for each of the dosage groupings using Bonett-Price confidence intervals for both raw and adjusted LC-MS-MS values."	( Use of an algorithm applied to urine drug screening to assess adherence to an oxycontin regimen. Couto, JE; Leider, HL; Linden, A; Romney, MC; Webster, L, )	0.13
"ICR mice were used to generate antagonist dose-response curves with intraperitoneal (i."	( In vivo characterization of the opioid antagonist nalmefene in mice. Bilsky, EJ; Giuvelis, D; Lowery, JJ; Osborn, MD; Skorput, AG, 2010)	0.36
" Microinjection of dynamin-DN and ConA also decreased the antinociceptive potency of the unlabeled opioid agonist dermorphin when microinjected into the vlPAG as demonstrated by rightward shifts in the dose-response curves."	( Opioid receptor internalization contributes to dermorphin-mediated antinociception. Aicher, SA; Arttamangkul, S; Bobeck, EN; Hegarty, DM; Ingram, SL; Macey, TA; Morgan, MM, 2010)	0.36
" Sustained release naltrexone seems promising in reducing opioid use, but the extent to which patients remain in treatment beyond the first dosage of naltrexone is not clear."	( Retention in naltrexone implant treatment for opioid dependence. Gossop, M; Hegstad, S; Hjerkinn, B; Kristensen, O; Kunøe, N; Lobmaier, P; Vederhus, JK; Waal, H, 2010)	0.36
" When subjects who vomited during the 12-hour dosing interval were excluded, the confidence interval for AUC0-t and AUCinf fell within the 80%-125% range, but the lower limit for Cmax was 76."	( The relative bioavailability of morphine sulfate and naltrexone hydrochloride extended release capsules (EMBEDA®) and an extended release morphine sulfate capsule formulation (KADIAN®) in healthy adults under fasting conditions. Boudriau, S; Ciric, S; Johnson, FK; Kisicki, JC; Stauffer, J, 2011)	0.37
" These findings suggest that medication dosing may be an important consideration in achieving symptom control."	( Nalmefene in the treatment of pathological gambling: multicentre, double-blind, placebo-controlled study. Grant, JE; Hollander, E; Kim, SW; Odlaug, BL; Potenza, MN, 2010)	0.36
" Plasma samples were collected just before dosing through 72 hours postdose for pharmacokinetic analyses of morphine, and through 168 hours postdose for naltrexone and its major metabolite 6-β-naltrexol."	( Food effects on the pharmacokinetics of morphine sulfate and naltrexone hydrochloride extended release capsules. Boudriau, S; Ciric, S; Johnson, F; Stauffer, J; Swearingen, D, 2010)	0.36
"The main objective of this study was to investigate thermosensitive Pluronic F-127 (PF-127) hydrogel for the modified release of a potent alcohol and opioid antagonist, naltrexone (NTX) hydrochloride, in a subcutaneous injectable dosage form."	( Thermosensitive Pluronic hydrogel: prolonged injectable formulation for drug abuse. Derakhshandeh, K; Fashi, M; Seifoleslami, S, 2010)	0.36
"Twenty healthy volunteers received 20, 60 and 120 mg daily doses of hydrocodone dosed to steady-state at each level while under a naltrexone blockade."	( Use of an algorithm applied to urine drug screening to assess adherence to a hydrocodone regimen. Couto, JE; Leider, HL; Linden, A; Romney, MC; Webster, L, 2011)	0.37
" Plasma fentanyl reached steady state within the 72-hour dosing period and accumulation was approximately 2-fold."	( Pharmacokinetics, safety, and tolerability of ascending doses of sublingual fentanyl, with and without naltrexone, in Japanese subjects. Boyce, M; Eriksson, C; Kilborn, J; Lister, N; Tamaoka, M; Warrington, S, 2011)	0.37
"A total of 469 subjects on opioids for chronic non-malignant pain with opioid-induced constipation were randomized to methylnaltrexone SC with once daily (QD) or every other day (QOD) dosing or placebo for 4 weeks."	( Effect of subcutaneous methylnaltrexone on patient-reported constipation symptoms. Iyer, SS; Manley, AL; Randazzo, BP; Schulman, SL; Tzanis, EL; Wang, W; Zhang, H, 2011)	0.37
" Differences in change from baseline in abdominal symptoms and pain scores between the methylnaltrexone SC QD or QOD dosing arms and placebo were not significant."	( Effect of subcutaneous methylnaltrexone on patient-reported constipation symptoms. Iyer, SS; Manley, AL; Randazzo, BP; Schulman, SL; Tzanis, EL; Wang, W; Zhang, H, 2011)	0.37
"The results of our study indicate significant improvement in constipation symptoms with methylnaltrexone QD or QOD dosing compared to placebo without a significant effect on pain scores."	( Effect of subcutaneous methylnaltrexone on patient-reported constipation symptoms. Iyer, SS; Manley, AL; Randazzo, BP; Schulman, SL; Tzanis, EL; Wang, W; Zhang, H, 2011)	0.37
" Patients of the group 1 received naltrexone (N) in dosage 50 mg/day and fluoxetine (F) in dosage 20 mg/day during 6 months."	( [Naltrexone and fluoxetine for maintenance of remission in patients with heroin addiction: a double-blind randomized placebo-controlled trial]. Bespalov, AIu; Burakov, AM; Didenko, TIu; Egorova, VIu; Grineneko, AIa; Ivanova, EB; Krupitskiĭ, EM; Masalov, DV; Neznanov, NG; O'Brien, C; Romanova, TN; Tsoĭ-Podosenin, MV; Verbitskaia, EV; Woody, D; Zvartau, EE, 2010)	0.36
" Administration of a low dosage of NTX (LDN) blocks endogenous opioids from opioid receptors for a short period of time (4-6 h) each day, providing a window of 18-20 h for the upregulated opioids and receptors to interact."	( The opioid growth factor (OGF) and low dose naltrexone (LDN) suppress human ovarian cancer progression in mice. Donahue, RN; McLaughlin, PJ; Zagon, IS, 2011)	0.37
" We proposed a systematic classification scheme using FDA-approved drug labeling to assess the DILI potential of drugs, which yielded a benchmark dataset with 287 drugs representing a wide range of therapeutic categories and daily dosage amounts."	( FDA-approved drug labeling for the study of drug-induced liver injury. Chen, M; Fang, H; Liu, Z; Shi, Q; Tong, W; Vijay, V, 2011)	0.37
" Mice with established ovarian tumors and treated with a low dosage of NTX (LDN), which invokes a short period of opioid receptor blockade, repressed tumor progression in a non-toxic fashion by reducing DNA synthesis and angiogenesis but not altering cell survival."	( Low-dose naltrexone suppresses ovarian cancer and exhibits enhanced inhibition in combination with cisplatin. Donahue, RN; McLaughlin, PJ; Zagon, IS, 2011)	0.37
" Dose-response curves were generally quantal under the FR and graded under the FI schedules, but highly variable among subjects under the FI."	( Drug discrimination in pigeons trained to discriminate among morphine, U50488, a combination of these drugs, and saline. Li, M; McMillan, DE; Wessinger, WD, 2011)	0.37
" Based on conservative extrapolation of data from adult dosing, a methylnaltrexone dosing regimen was selected and the naloxone was weaned over two days in an effort to avoid a relative opioid overdose."	( Methylnaltrexone in treatment of opioid-induced constipation in a pediatric patient. Lee, JM; Mooney, J, 2012)	0.38
" If an increase in thermal threshold was found, naltrexone administration was repeated at decreasing intervals in the next experiment (all cats were not used for all dosing intervals)."	( Use of naltrexone to antagonize high doses of remifentanil in cats: a dose-finding study. Brosnan, RJ; Ilkiw, JE; Pypendop, BH, 2011)	0.37
" Of the three high-assurance studies, one used direct supervision of thrice-weekly oral dosing of naltrexone, and two used extended-release injectable formulations of naltrexone administered once per month."	( Adherence monitoring in naltrexone pharmacotherapy trials: a systematic review. Alexander, M; Forman, R; Oslin, DW; Swift, R, 2011)	0.37
"To evaluate error processing in contrasting opioid treatment samples by finding the relative risk of fatal dosing errors leading to opioid overdose in a controlled cohort of detoxified patients with opioid dependence."	( Opioid-dependent error processing. Fellows-Smith, J, )	0.13
"Naltrexone increases vulnerability to overdose as enhanced opioid effects following neuroanatomical blockade can reverse behavioral tolerance and lead to greater fatal dosing errors on reinstatement of opioid dependence."	( Opioid-dependent error processing. Fellows-Smith, J, )	0.13
" In one patient, higher dose of naltrexone resulted in hepatic abnormalities, which resolved after dosage reduction."	( Opioid antagonist naltrexone for the treatment of pathological gambling in Parkinson disease. Arianna, S; Bosco, D; Bosco, F; Colica, C; Consoli, A; Consoli, D; Cristiano, D; Galati, F; Plastino, M; Vecchio, A, )	0.13
" When rats were co-infused with MOR and NAL, MOR-induced effects were not reversed by either dosage of NAL, and some measures of MOR-induced movement suppression were enhanced by NAL at the 1x dosage."	( The role of mu-opioid receptor signaling in the dorsolateral periaqueductal gray on conditional and unconditional responding to threatening and aversive stimuli. Blair, HT; Halladay, LR, 2012)	0.38
"Of the 35 adults enrolled in the study, 33 completed at least 1 dosing period."	( Dose proportionality and the effects of food on bioavailability of an immediate-release oxycodone hydrochloride tablet designed to discourage tampering and its relative bioavailability compared with a marketed oxycodone tablet under fed conditions: a sing Bass, A; Leibowitz, M; Pixton, GC; Rolleri, R; Sommerville, KW; Stark, JG; Zamora, CA, 2012)	0.38
" While the addition of naloxone to oxycodone seems to act by preventing OIC, the intermittent dosing of methylnaltrexone every other day seems to stimulate defaecation by provoking an intestinal withdrawal response."	( Non-analgesic effects of opioids: management of opioid-induced constipation by peripheral opioid receptor antagonists: prevention or withdrawal? Holzer, P, 2012)	0.38
" MOPr agonist efficacy was evaluated by microinjecting the irreversible opioid receptor antagonist β-funaltrexamine hydrochloride (β-FNA) into the vlPAG prior to a dose-response analysis of morphine and fentanyl antinociception."	( Differential development of antinociceptive tolerance to morphine and fentanyl is not linked to efficacy in the ventrolateral periaqueductal gray of the rat. Bobeck, EN; Haseman, RA; Hong, D; Ingram, SL; Morgan, MM, 2012)	0.38
" The results suggest that the combination of buprenorphine and naltrexone at an appropriate dosage decreases compulsive cocaine self-administration with minimal liability to produce opioid dependence and may be useful as a treatment for cocaine addiction."	( A combination of buprenorphine and naltrexone blocks compulsive cocaine intake in rodents without producing dependence. Koob, GF; Misra, KK; Schlosburg, JE; Vendruscolo, LF; Wee, S, 2012)	0.38
" In March 2011, all dosage forms of Embeda® were recalled because the product failed to meet routine stability standards, and its return date to the market is currently unknown."	( Will abuse-deterrent formulations of opioid analgesics be successful in achieving their purpose? Bannwarth, B, 2012)	0.38
"Nalmefene provides clinical benefit, constitutes a potential new pharmacological treatment paradigm in terms of the treatment goal and dosing regimen, and provides a method to address the unmet medical need in patients with alcohol dependence that need to reduce their alcohol consumption."	( Extending the treatment options in alcohol dependence: a randomized controlled study of as-needed nalmefene. Bladström, A; Gual, A; Mann, K; Torup, L; van den Brink, W, 2013)	0.39
"The results of the current study of an ER formulation revealed no pharmacokinetic features that would preclude dosing in the elderly."	( An open-label pharmacokinetic study of oxymorphone extended release in the presence of naltrexone in the older adult. Gould, EM; Labhsetwar, S; Nagar, S; Pergolizzi, JV; Raffa, RB; Sinclair, N; Taylor, R, )	0.13
" Here, we used clinically relevant dosing to examine the effects of maternally administered sustained-release naltrexone on the rat brain by examining offspring at birth and in adulthood."	( Maternally administered sustained-release naltrexone in rats affects offspring neurochemistry and behaviour in adulthood. Dunlop, SA; Farid, WO; Hulse, GK; Krstew, EV; Lawrence, AJ; Tait, RJ, 2012)	0.38
" This study provides evidence for the efficacy of nalmefene, which constitutes a new pharmacological treatment paradigm in terms of treatment goal (reduced drinking) and dosing regimen (as-needed), in alcohol dependent patients unable to reduce alcohol consumption on their own."	( A randomised, double-blind, placebo-controlled, efficacy study of nalmefene, as-needed use, in patients with alcohol dependence. Gual, A; He, Y; Mann, K; Torup, L; van den Brink, W, 2013)	0.39
" To test this hypothesis, separate cohorts of male Wistar rats were trained in one of the two animal models of impulsivity: delay-discounting (DD) or stop-signal reaction time (SSRT) tasks, and once stable responding was observed, received intracerebroventricular (ICV) infusions of the KOR agonist U50,488 (0-50 μg) according to a within-subject dosing regimen."	( Dissociable effects of kappa-opioid receptor activation on impulsive phenotypes in wistar rats. Kissler, JL; Walker, BM, 2013)	0.39
" One way to interpret this pattern of effects is that pretreatment with naloxone appeared to produce a shift in the dose-response curve for METH."	( The selective μ opioid receptor antagonist β-funaltrexamine attenuates methamphetamine-induced stereotypical biting in mice. Fukushima, Y; Hall, FS; Kitanaka, J; Kitanaka, N; Kubo, H; Morita, Y; Nishiyama, N; Sawai, T; Takahashi, H; Takemura, M; Tanaka, K; Tatsuta, T; Uhl, GR; Watabe, K, 2013)	0.39
" Demographic, clinical, efficacy, and safety data were collected, including; opioid, laxative, and methylnatrexone dosing and frequency."	( Methylnaltrexone for opioid-induced constipation in pediatric oncology patients. Alexander, S; Dupuis, LL; Lau, E; Mattiussi, A; Rodrigues, A; Wong, C, 2013)	0.39
" At once, daily dosing NTX is systemically absorbed; however, the degree of systemic absorption is not likely to be clinically significant."	( Effect of topical naltrexone 0.3% on corneal sensitivity and tear parameters in normal brachycephalic dogs. Arnold, TS; Powell, CC; Wittenburg, LA, 2014)	0.4
" Adequate dosage appears important, as low-dose naltrexone resembled the placebo group; opiate positive urines were likely to be followed by dropout from treatment."	( Naltrexone treatment for opioid dependence: does its effectiveness depend on testing the blockade? Bisaga, A; Comer, SD; Glass, A; Levin, FR; Mariani, JJ; Nunes, EV; Sullivan, MA, 2013)	0.39
" OGF treatment inhibited TNBC cells in a dosage related, receptor mediated, and reversible manner."	( Opioid growth factor - opioid growth factor receptor axis inhibits proliferation of triple negative breast cancer. McLaughlin, PJ; Porterfield, NK; Zagon, IS, 2013)	0.39
"7, respectively) following dosing compared with MS (Emax 87."	( Assessing the subjective and physiological effects of intranasally administered crushed extended-release morphine formulations with and without a sequestered naltrexone core in recreational opioid users. Goli, V; Levy-Cooperman, N; Mills, C; Setnik, B; Shram, M; Smith, I, )	0.13
" A distinct dose-response effects of these peptides on cocaine locomotion probably arise from differential functional activation (targeting) of the DOR and MOR by both deltorphins analogs."	( Involvement of delta and mu opioid receptors in the acute and sensitized locomotor action of cocaine in mice. Gibula-Bruzda, E; Izdebski, J; Kotlinska, JH; Witkowska, E, 2013)	0.39
" Experiment 1 characterised the dose-response profile of mCPP (0."	( On the behavioural specificity of hypophagia induced in male rats by mCPP, naltrexone, and their combination. Rodgers, RJ; Wright, FL, 2014)	0.4
" This approach is intended to reduce the opioid subjective rewarding effects such as euphoria which are prominent following swallowing the dosage form without tampering."	( Sequestered naltrexone in sustained release morphine or oxycodone - a way to inhibit illicit use? Pergolizzi, JV; Raffa, RB; Taylor, R, 2014)	0.4
"Although conventional pharmaceuticals have many drug dosage forms on the market, the development of new therapeutic molecules and the low efficacy of instant release formulations for the treatment of some chronic diseases and specific conditions encourage scientists to invent different delivery systems."	( Hydrogels composed of cyclodextrin inclusion complexes with PLGA-PEG-PLGA triblock copolymers as drug delivery systems. Esmaeel, H; Hadizadeh, F; Khodaverdi, E; Mirzazadeh Tekie, FS; Mohajeri, SA; Sajadi Tabassi, SA; Zohuri, G, 2014)	0.4
" The markedly delayed efficacy of all 3 glial modulatory drugs may prove instructive for interpretation of apparent drug failures after shorter dosing regimens."	( Systemic administration of propentofylline, ibudilast, and (+)-naltrexone each reverses mechanical allodynia in a novel rat model of central neuropathic pain. Ellis, A; Falci, S; Favret, J; Johnson, KW; Maier, SF; Rice, KC; Watkins, LR; Wieseler, J, 2014)	0.4
"The present results support the continued evaluation of an opioid receptor antagonist combined with a GABAA-positive modulator using more clinically relevant experimental conditions like examining the effect of chronic dosing with these drugs on methamphetamine self-administration."	( Separate and combined impact of acute naltrexone and alprazolam on subjective and physiological effects of oral d-amphetamine in stimulant users. Lile, JA; Marks, KR; Rush, CR; Stoops, WW, 2014)	0.4
"Experiment 1 examined the dose-response effects of exendin-4 (0."	( Behavioural profile of exendin-4/naltrexone dose combinations in male rats during tests of palatable food consumption. Rodgers, RJ; Wright, FL, 2014)	0.4
" Factors such as dosing frequency, potential adverse events, and availability of treatments may guide medication choice."	( Pharmacotherapy for adults with alcohol use disorders in outpatient settings: a systematic review and meta-analysis. Amick, HR; Bobashev, G; Feltner, C; Garbutt, JC; Gass, CE; Jonas, DE; Kim, MM; Rowe, CJ; Shanahan, E; Thomas, K; Wines, R, 2014)	0.4
" As-needed dosage is a novel concept in the addictions field, which may overcome limitations of traditional regimens."	( Nalmefene and its use in alcohol dependence. Bruguera, P; Gual, A; López-Pelayo, H, 2014)	0.4
"We found no studies that assessed the clinical utility of genotype-guided dosing strategies or genotype-guided medication selection, and none randomized by genotype."	( Genetic polymorphisms and response to medications for alcohol use disorders: a systematic review and meta-analysis. Amick, HR; Feltner, C; Garbutt, JC; Jonas, DE; Rowe, CJ; Shanahan, E; Wines, R, 2014)	0.4
"3-10 µg/kg/infusion) generated a biphasic dose-response curve, characteristic of drugs with reinforcing properties."	( Effects of the NOP agonist SCH221510 on producing and attenuating reinforcing effects as measured by drug self-administration in rats. Ko, MC; Lagorio, CH; Sukhtankar, DD, 2014)	0.4
" We compared the efficacy and safety of naltrexone administered daily plus targeted dosing with placebo to reduce drinking in young adults who engage in heavy drinking."	( Reduction of alcohol drinking in young adults by naltrexone: a double-blind, placebo-controlled, randomized clinical trial of efficacy and safety. Corbin, WR; DeMartini, KS; Fucito, LM; Gueorguieva, R; Ikomi, J; Kranzler, HR; Leeman, RF; O'Malley, SS; Romano, DM; Sher, KJ; Toll, BA; Wu, R, 2015)	0.42
"Six-week old female mice were immunized with MOG35-55 and were injected intraperitoneally with OGF or a low dosage of naltrexone (LDN) beginning at the time of immunization; saline-injected immunized mice served as controls."	( Endogenous opioid inhibition of proliferation of T and B cell subpopulations in response to immunization for experimental autoimmune encephalomyelitis. Magister, MJ; McHugh, DP; McLaughlin, PJ; Zagon, IS, 2015)	0.42
"Subcutaneous methylnaltrexone (MNTX), dosed based on body weight, is efficacious and well tolerated in inducing bowel movements in patients with advanced illness and opioid-induced constipation (OIC); however, fixed-dose administration of MNTX may improve ease of administration."	( Fixed-Dose Subcutaneous Methylnaltrexone in Patients with Advanced Illness and Opioid-Induced Constipation: Results of a Randomized, Placebo-Controlled Study and Open-Label Extension. Barrett, AC; Bull, J; Forbes, WP; Israel, RJ; Paterson, C; Wellman, CV, 2015)	0.42
"A secondary descriptive data analysis of demographics, substance use history, current substance use behaviors, health-related variables, and dosing records was conducted on 609 patients who received XR-NTX from Los Angeles County substance use disorder (SUD) treatment facilities from April 2010 through July 2013."	( A demonstration project implementing extended-release naltrexone in Los Angeles County. Barger, J; Cousins, SJ; Crèvecoeur-MacPhail, D; Denering, L; Kim, T; Rawson, RA; Sugita, W; Viernes, J; Weimann, S, 2016)	0.43
" The OGF-OGFr axis can be activated through exogenous administration of OGF or a low dosage of naltrexone (LDN), an opioid antagonist."	( Opioid growth factor and low-dose naltrexone impair central nervous system infiltration by CD4 + T lymphocytes in established experimental autoimmune encephalomyelitis, a model of multiple sclerosis. Hammer, LA; McLaughlin, PJ; Waldner, H; Zagon, IS, 2016)	0.43
" Hits were evaluated in direct and orthogonal dose-response counterscreens using a standard recRSV reporter strain expressing Renilla luciferase."	( Replication-Competent Influenza Virus and Respiratory Syncytial Virus Luciferase Reporter Strains Engineered for Co-Infections Identify Antiviral Compounds in Combination Screens. Chung, HK; Lamb, K; Lin, MZ; Plemper, RK; Weisshaar, M; Yan, D, 2015)	0.42
" MNTX in oral immediate-release (MNTX-IR) and extended-release (MNTX-ER) dosage forms may antagonize the opioid induced delay in oro-cecal transit time (OCT) as measured by using radiolabeled lactulose."	( Extended-release but not immediate-release and subcutaneous methylnaltrexone antagonizes the loperamide-induced delay of whole-gut transit time in healthy subjects. Kolbow, J; Maritz, MA; Modess, C; Oswald, S; Rey, H; Siegmund, W; Wegner, D; Weitschies, W, 2016)	0.43
"Among the currently available agonist therapies, new dosage forms of buprenorphine can increase patient acceptability and compliance."	( Therapies in early development for the treatment of opiate addiction. Aguilar, MA; Miñarro, J; Rodríguez-Arias, M, 2015)	0.42
" Its efficacy has been demonstrated in the treatment of alcohol and opioid dependence, but adherence to daily dosing has been recognized as a factor limiting long-term effectiveness."	( Naltrexone: Not Just for Opioids Anymore. Sudakin, D, 2016)	0.43
" Possible genetic and epigenetic factors, and practical considerations including once-daily dosing also make naltrexone an appealing agent in this population."	( Should naltrexone be the first-line medicine to treat alcohol dependence in Aboriginal and Torres Strait Islander populations? An Australian perspective. Brett, J; Conigrave, K; Doyle, M; Ivers, R; Lawrence, L, 2015)	0.42
" ECG data were extracted from a continuous recording predose and serially after dosing on the treatment day."	( Differentiating the Effect of an Opioid Agonist on Cardiac Repolarization From µ-Receptor-mediated, Indirect Effects on the QT Interval: A Randomized, 3-way Crossover Study in Healthy Subjects. Bai, SA; Darpo, B; Ferber, G; Finn, A; Xiang, Q; Zhou, M, 2016)	0.43
"This study developed a stability-indicating reversed-phase HPLC method for the simultaneous determination of morphine sulfate and naltrexone hydrochloride content in bulk, Solid dosage forms and in-vitro dissolution samples to support product development and quality control efforts."	( A stability-indicating HPLC method for simultaneous determination of morphine and naltrexone. Barzin, J; Jafari-Nodoushan, M; Mobedi, H, 2016)	0.43
" Participants were randomly assigned to receive adjunctive treatment with 2 mg/2 mg of buprenorphine/samidorphan (the 2/2 dosage group), 8 mg/8 mg of buprenorphine/samidorphan (the 8/8 dosage group), or placebo."	( Opioid Modulation With Buprenorphine/Samidorphan as Adjunctive Treatment for Inadequate Response to Antidepressants: A Randomized Double-Blind Placebo-Controlled Trial. Bodkin, JA; de Somer, M; DiPetrillo, L; Du, Y; Ehrich, E; Fava, M; Leigh-Pemberton, R; Memisoglu, A; Silverman, B; Thase, ME; Trivedi, MH, 2016)	0.43
"Compared with the placebo group, there were significantly greater improvements in the 2/2 dosage group across the three depression outcome measures (HAM-D: -2."	( Opioid Modulation With Buprenorphine/Samidorphan as Adjunctive Treatment for Inadequate Response to Antidepressants: A Randomized Double-Blind Placebo-Controlled Trial. Bodkin, JA; de Somer, M; DiPetrillo, L; Du, Y; Ehrich, E; Fava, M; Leigh-Pemberton, R; Memisoglu, A; Silverman, B; Thase, ME; Trivedi, MH, 2016)	0.43
"0ng/mL for a one-month period when dosed intramuscular to dogs or minipigs."	( Lipophilic nalmefene prodrugs to achieve a one-month sustained release. Annaert, PP; Atack, JR; Borghys, H; de Vries, R; De Zwart, LL; Embrechts, RC; Gaekens, T; Guillaume, M; Herdewijn, P; Leysen, JE; Megens, AA; Vermeulen, A, 2016)	0.43
" Plasma samples were analyzed just before dosing through 48 hours postdose for oxycodone, and through 120 hours postdose for naltrexone and its major metabolite, 6-ß-naltrexol."	( Effect of food on the pharmacokinetics of oxycodone and naltrexone from ALO-02, an extended release formulation of oxycodone with sequestered naltrexone. Bramson, C; Gandelman, K; Lamson, M; Malhotra, B; Matschke, K; Salageanu, J, 2015)	0.42
" From a clinical perspective, these results may provide additional evidence regarding naltrexone's efficacy in the context of acute or subacute dosing regimens."	( Effects of naltrexone on alcohol self-administration and craving: meta-analysis of human laboratory studies. Hendershot, CS; Rehm, J; Samokhvalov, AV; Wardell, JD, 2017)	0.46
" Furthermore, when dosing was discontinued after ten once-daily doses, all nicotine groups (nicotine-only and nicotine+naloxone combination) demonstrated significant decreases in sucrose reinforcement compared to the saline group."	( Nicotine enhancement and reinforcer devaluation: Interaction with opioid receptors. Kirshenbaum, AP; Phillips, JL; Suhaka, JA; Voltolini de Souza Pinto, M, )	0.13
"In this phase 3, double-blind trial, adults with chronic noncancer pain receiving opioid doses of ≥ 50 mg/day oral morphine equivalents with OIC were randomly assigned to oral methylnaltrexone (150, 300, or 450 mg) or placebo once daily (QD) for 4 weeks followed by as-needed dosing for 8 weeks."	( Randomized, Double-Blind Trial of Oral Methylnaltrexone for the Treatment of Opioid-Induced Constipation in Patients with Chronic Noncancer Pain. Harper, JR; Israel, RJ; Rauck, R; Slatkin, NE; Stambler, N, 2017)	0.46
" A significantly greater percentage of patients had an increase in mean percentage of dosing days resulting in an RFBM within 4 hours of dosing during weeks 1 through 4 (QD period; primary endpoint) with methylnaltrexone (300 mg/day [24."	( Randomized, Double-Blind Trial of Oral Methylnaltrexone for the Treatment of Opioid-Induced Constipation in Patients with Chronic Noncancer Pain. Harper, JR; Israel, RJ; Rauck, R; Slatkin, NE; Stambler, N, 2017)	0.46
"Post-hoc combined analysis of three earlier randomized controlled trials that showed individually that incentives for adherence to oral and to extended-release injection naltrexone dosing schedules increased naltrexone adherence, but not opiate abstinence."	( Effects of incentives for naltrexone adherence on opiate abstinence in heroin-dependent adults. Bigelow, GE; DeFulio, A; Dunn, KE; Everly, JJ; Fingerhood, M; Holtyn, AF; Jarvis, BP; Leoutsakos, JS; Silverman, K; Umbricht, A, 2017)	0.46
"These results demonstrate the safety, efficacy, and tolerability of low-dose naltrexone, in conjunction with single-day buprenorphine dosing and adjunctive nonopioid medications, for initiating adults with opioid dependence to XR-naltrexone."	( Long-Acting Injectable Naltrexone Induction: A Randomized Trial of Outpatient Opioid Detoxification With Naltrexone Versus Buprenorphine. Bisaga, A; Carpenter, KM; Choi, CJ; Dakwar, E; Levin, FR; Mariani, JJ; Mishlen, K; Nunes, EV; Pavlicova, M; Sullivan, M, 2017)	0.46
" In the rat, but not the mouse, 2-year carcinogenicity study a change in tumour pattern with an increase in testicular Leydig cell tumours (LCT) was observed after dosing at high (supra-pharmacological) concentrations."	( Naloxegol, an opioid antagonist with reduced CNS penetration: Mode-of-action and human relevance for rat testicular tumours. Andersson, H; Floettmann, E; Johnson, N; Mitchard, T, 2017)	0.46
" Notably, chronic dosing of oral naltrexone decreases self-administration of cannabis in human laboratory studies."	( Open-label pilot study of injectable naltrexone for cannabis dependence. Brooks, DJ; Choi, CJ; Kelly, MA; Levin, FR; Mahony, AL; Mariani, JJ; Notzon, DP; Pavlicova, M, 2018)	0.48
" ADFs have been created with chemical properties that make it difficult for people who non-medically use prescription drugs to crush and dissolve opioid tablets, as well as by combining opioids with antagonists such as naloxone or naltrexone, which are released only when the dosage form has been manipulated or the drug is taken by a non-intended route."	( Abuse-Deterrent Opioid Formulations: A Key Ingredient in the Recipe to Prevent Opioid Disasters? Hagemeier, NE; Harirforoosh, S; Salwan, AJ, 2018)	0.48
" Within a specific dosage window, LDN can act as an immunomodulator in multiple autoimmune diseases and malignant tumors as well as alleviate the symptoms of some mental disorders."	( Low-dose naltrexone (LDN): A promising treatment in immune-related diseases and cancer therapy. Feng, J; Griffin, N; Li, Z; Shan, F; You, Y, 2018)	0.48
" Expert opinion: Methylnaltrexone has both subcutaneous injection and oral dosage forms available in the market."	( Methylnaltrexone bromide for the treatment of opioid-induced constipation. Abdollahi, M; Mozaffari, S; Nikfar, S, 2018)	0.48
" Low-dose naltrexone has the potential for the treatment of chronic inflammatory skin conditions; however, additional evidence is needed for dosing and long-term treatment guidelines."	( Utility of Naltrexone Treatment for Chronic Inflammatory Dermatologic Conditions: A Systematic Review. Ekelem, C; Juhasz, M; Khera, P; Mesinkovska, NA, 2019)	0.51
"Extended-release naltrexone hydrochloride, 380 mg, administered as an injection every 4 weeks or flexible doses (4-24 mg; target dosage 16 mg/d) of daily oral combined BP-NLX."	( Anxiety, Depression, and Insomnia Among Adults With Opioid Dependence Treated With Extended-Release Naltrexone vs Buprenorphine-Naloxone: A Randomized Clinical Trial and Follow-up Study. Krajci, P; Kunoe, N; Latif, ZE; Opheim, A; Šaltyte Benth, J; Sharma-Haase, K; Solli, KK; Tanum, L, 2019)	0.51
" A novel polytherapeutic proof-of-principle approach using PXT3003, a low-dose combination of baclofen, naltrexone and sorbitol, slowed disease progression after long-term dosing in adult Pmp22 transgenic rats, a known animal model of CMT1A."	( Early short-term PXT3003 combinational therapy delays disease onset in a transgenic rat model of Charcot-Marie-Tooth disease 1A (CMT1A). Adam, J; Cohen, D; Ewers, D; Hajj, R; Kungl, T; Mroczek, M; Nabirotchkin, S; Nave, KA; Prukop, T; Sereda, MW; Stenzel, J; Wernick, S, 2019)	0.51
" Three weekly directly observed active or placebo oral naltrexone tablets (2 × 50 mg, Monday and Wednesday; 3 × 50 mg, Friday) at day 0 of study week 1 (for 4 weeks) and then an 8-week regimen of patient-administered dosing at the same dosing level."	( Extended-release naltrexone versus standard oral naltrexone versus placebo for opioid use disorder: the NEAT three-arm RCT. Byford, S; Day, E; Hellier, J; Kelleher, M; Marsden, J; Mayet, S; McLennan, B; Murphy, C; Ryan, E; Shearer, J; Strang, J, 2019)	0.51
" We examine the feasibility, utility, and acceptability of using smartphones to capture dosing videos from the perspectives of participants and staff."	( Medication Adherence Monitoring Using Smartphone Video Dosing in an Open-label Pilot Study of Monthly Naltrexone Plus Once-daily Bupropion for Methamphetamine Use Disorder: Feasibility and Acceptability. Hillhouse, M; Ling, W; Mooney, L; Perrochet, B; Sparenborg, S; Walker, R, )	0.13
" BRP was dispensed once weekly for dosing on nonclinic days."	( Medication Adherence Monitoring Using Smartphone Video Dosing in an Open-label Pilot Study of Monthly Naltrexone Plus Once-daily Bupropion for Methamphetamine Use Disorder: Feasibility and Acceptability. Hillhouse, M; Ling, W; Mooney, L; Perrochet, B; Sparenborg, S; Walker, R, )	0.13
"6% of dispensed doses were confirmed via dosing video and in-person observations."	( Medication Adherence Monitoring Using Smartphone Video Dosing in an Open-label Pilot Study of Monthly Naltrexone Plus Once-daily Bupropion for Methamphetamine Use Disorder: Feasibility and Acceptability. Hillhouse, M; Ling, W; Mooney, L; Perrochet, B; Sparenborg, S; Walker, R, )	0.13
"The use of smartphones for video-based oral medication dosing in this study provided a feasible and acceptable mechanism to encourage, monitor, and confirm medication adherence."	( Medication Adherence Monitoring Using Smartphone Video Dosing in an Open-label Pilot Study of Monthly Naltrexone Plus Once-daily Bupropion for Methamphetamine Use Disorder: Feasibility and Acceptability. Hillhouse, M; Ling, W; Mooney, L; Perrochet, B; Sparenborg, S; Walker, R, )	0.13
" Olanzapine and samidorphan pharmacokinetic parameters were determined after OLZ/SAM dosing on days 1 and 22."	( A Phase I Open-Label Study to Evaluate the Effects of Rifampin on the Pharmacokinetics of Olanzapine and Samidorphan Administered in Combination in Healthy Human Subjects. Kumar, V; McDonnell, D; Sun, L; von Moltke, L; Yu, M, 2019)	0.51
" The dosing schedule of naltrexone hydrochloride in detoxification protocols needs to be flexible to permit precise, customized dose titration for individual patients."	( Physicochemical Stability of Compounded Naltrexone Hydrochloride Solutions in PCCA Base SuspendIt. Bostanian, LA; Graves, RA; Mandal, TK; Morris, TC; Nguyen, AT; Pramar, YV, )	0.13
" However, respective intragastrical administration of NTX (20 or 40 mg/kg) failed to alter the dose-response curve of METH under fixed ratio 2 program and intraperitoneal injection of METH (1."	( Inhibition of naltrexone on relapse in methamphetamine self-administration and conditioned place preference in rats. Dong, GM; Guo, LK; Li, J; Lu, GY; Ma, CM; Song, R; Wang, ZY; Wu, N; Zhang, RL, 2019)	0.51
" Emergent themes were: (1) general satisfaction with XR-NTX's long-acting antagonist effects and control of cravings; (2) "testing" XR-NTX's blockade with heroin upon reentry was common; (3) early discontinuation of XR-NTX treatment was most common among persons with high self-efficacy and/or heavy exposure to drug use environments and peers; (4) similar satisfaction regarding effects of methadone and buprenorphine maintenance among retained-in-treatment individuals, alongside general dissatisfaction with daily observed dosing requirements and misinformation and stigmas regarding methadone adverse effects; (5) unstable housing, economic insecurity, and exposure to actively using peers were attributed to early termination of treatment and relapse; (6) individual motivation and willpower as central to long-term opioid abstinence and reentry success."	( Perceptions of extended-release naltrexone, methadone, and buprenorphine treatments following release from jail. Badolato, R; Flannery, M; Garment, AR; Giftos, J; Lee, JD; McDonald, RD; Tofighi, B; Velasquez, M; Vittitow, A, 2019)	0.51
" Multiple daily doses of olanzapine do not affect the pharmacokinetics of lithium or valproate; therefore, concomitant olanzapine administration does not require dosage adjustment of lithium or valproate."	( Combination of Olanzapine and Samidorphan Has No Clinically Significant Effect on the Pharmacokinetics of Lithium or Valproate. Graham, C; Sun, L; von Moltke, L; Yagoda, S; Yao, B, 2020)	0.56
" Pharmacokinetic parameters of lithium and valproate, including maximum plasma concentration and area under the plasma concentration-time curve over a 12-h dosing interval, were calculated."	( Combination of Olanzapine and Samidorphan Has No Clinically Significant Effect on the Pharmacokinetics of Lithium or Valproate. Graham, C; Sun, L; von Moltke, L; Yagoda, S; Yao, B, 2020)	0.56
" absence of OLZ/SAM, were within the equivalence interval of 80-125% for both maximum plasma concentration and area under the plasma concentration-time curve over a 12-h dosing interval of lithium and of valproate."	( Combination of Olanzapine and Samidorphan Has No Clinically Significant Effect on the Pharmacokinetics of Lithium or Valproate. Graham, C; Sun, L; von Moltke, L; Yagoda, S; Yao, B, 2020)	0.56
"5 mg naltrexone oral dose (SI group) or escalating dosage regimen starting from 50 μg up to a cumulative dose of 12."	( Dose Escalation of Naltrexone to Reduce Stress Responses Associated With Opioid Antagonist Induction: A Double-blind Randomized Trial. Badaras, R; Ivaskevicius, J; Jovaisa, T; Lapinskiene, I, )	0.13
"5-mg dose, the escalating naltrexone dosing regimen produced no significant increase in stress response and withdrawal scores during antagonist induction."	( Dose Escalation of Naltrexone to Reduce Stress Responses Associated With Opioid Antagonist Induction: A Double-blind Randomized Trial. Badaras, R; Ivaskevicius, J; Jovaisa, T; Lapinskiene, I, )	0.13
" There was a dose-response association between increasing LDN exposure and reductions in the number of users of antiepileptics, antipsychotics and antidepressants."	( Changes in the consumption of antiepileptics and psychotropic medicines after starting low dose naltrexone: A nation-wide register-based controlled before-after study. Raknes, G; Småbrekke, L, 2019)	0.51
" Study durations ranged from 3 to 13 weeks, and memantine dosing ranged from 5 to 60 mg/day."	( Adjunctive memantine for opioid use disorder treatment: A systematic review. Brown, JN; Elias, AM; Pepin, MJ, 2019)	0.51
"This study explores dose-response relationships when treating fibromyalgia with low-dose naltrexone."	( Low-Dose Naltrexone for the Treatment of Fibromyalgia: Investigation of Dose-Response Relationships. Amris, K; Blichfeldt-Eckhardt, MR; Bruun-Plesner, K; Lauridsen, JT; Toft, P; Vaegter, HB, 2020)	0.56
"This study is the first to explore dose-response relationships in the treatment of fibromyalgia with low-dose naltrexone."	( Low-Dose Naltrexone for the Treatment of Fibromyalgia: Investigation of Dose-Response Relationships. Amris, K; Blichfeldt-Eckhardt, MR; Bruun-Plesner, K; Lauridsen, JT; Toft, P; Vaegter, HB, 2020)	0.56
" Understanding these pharmacologically driven patterns then guides the judicious choice of drug and dosing schedule and the proactive risk management that is crucial to minimising the risk of death in treatment."	( Impact of Pharmacological Treatments for Opioid Use Disorder on Mortality. Hulse, G; Joyce, D; Kelty, E; Preen, DB, 2020)	0.56
" Several factors at the individual, interpersonal, and institutional levels, such as concurrent substance use, MOUD adherence, family conflict, and MOUD dosage and flexibility, appeared to have roles in MOUD retention among adolescents and young adults."	( Adherence to and Retention in Medications for Opioid Use Disorder Among Adolescents and Young Adults. Altice, FL; Bromberg, DJ; Nyhan, K; Refsland, BM; Stanojlović, M; Viera, A; Whittaker, S, 2020)	0.56
"8-fold compared to saline; this effect was similar to that obtained with daily naltrexone injections, demonstrating the formulation efficacy and its ability to reduce dosing frequency."	( Bioresponsive nanostructured systems for sustained naltrexone release and treatment of alcohol use disorder: Development and biological evaluation. Camarini, R; Dartora, VFMC; Lopes, LB; Matos, JKR; Rae, M; Santos, RA, 2020)	0.56
" These effects appear to unique at low dosage compared to dosage for food and drug administration approved use for alcohol and opioid dependence."	( Low-Dose Naltrexone for Chronic Pain: Update and Systemic Review. Fishman, MA; Kim, PS, 2020)	0.56
" Buprenorphine's bell-shaped dose-response curve may also result from opposing effects on MOR-μ and MOR-μ*."	( Biased Opioid Antagonists as Modulators of Opioid Dependence: Opportunities to Improve Pain Therapy and Opioid Use Management. Oberdick, J; Sadee, W; Wang, Z, 2020)	0.56
" XR-NTX appealed to participants due to the autonomy it affords with once-monthly dosing and no physical dependence."	( Patients' perspectives on initiating treatment with extended-release naltrexone (XR-NTX). Desai, A; Gauthier, P; Greco, P; Meyers-Ohki, S; Rotrosen, J, 2021)	0.62
" Patients may be vulnerable to opioid overdose if they attempt to override the blockade during treatment, at the end of a dosing interval, after missing a dose, or after discontinuing treatment."	( Evaluation of Opioid Overdose Reports in Patients Treated with Extended-Release Naltrexone: Postmarketing Data from 2006 to 2018. Akerman, SC; Bloomgren, G; Desai, A; Fratantonio, J; Jain, P; Liles-Burden, MA; Marino, R; McKinnell, K; Sullivan, MA; Vunnava, P; Wenten, M, 2021)	0.62
" Nalmefene provides a clinical benefit, constitutes a potential pharmacological treatment paradigm in terms of the treatment goal and dosing regimen, and addresses an unmet medical need in patients with alcohol dependence who need to reduce their alcohol consumption."	( [Four cases of alcoholic liver cirrhosis in alcohol-dependent patients treated with nalmefene]. Tamaki, K, 2021)	0.62
"To assess the pharmacokinetics and opioid effects of methadone after administration of multiple doses by means of 2 dosing regimens of methadone-fluconazole-naltrexone."	( Multiple-dose pharmacokinetics and opioid effects of a novel analgesic with a deterrent to human opioid abuse (methadone-fluconazole-naltrexone) after oral administration in dogs. Cho, P; Fitzgerald, AH; Komp, MS; KuKanich, B; KuKanich, K; Locuson, CW; Rankin, DC, 2021)	0.62
"Dogs were randomly allocated (6 dogs/group) to receive 1 of 2 oral dosing regimens of methadone-fluconazole-naltrexone."	( Multiple-dose pharmacokinetics and opioid effects of a novel analgesic with a deterrent to human opioid abuse (methadone-fluconazole-naltrexone) after oral administration in dogs. Cho, P; Fitzgerald, AH; Komp, MS; KuKanich, B; KuKanich, K; Locuson, CW; Rankin, DC, 2021)	0.62
" Additional studies will be needed to identify effective opioid receptor antagonist dosing regimens for patients undergoing either short- or long-segment spinal arthrodesis procedures."	( Perioperative subcutaneous methylnaltrexone does not enhance gastrointestinal recovery after posterior short-segment spinal arthrodesis surgery: a randomized controlled trial. Farhadi, HF; Gifford, CS; McGahan, BG; Minnema, AJ; Miracle, SD; Murphy, CV; Vazquez, DE; Weaver, TE, 2022)	0.72
" Recent reports, however, suggest that higher doses or repeated dosing of naloxone (due to recurrence of respiratory depression) may be required to reverse fully fentanyl-induced respiratory depression, rendering this treatment inadequate."	( Design, synthesis, and preliminary evaluation of a potential synthetic opioid rescue agent. Baynard, C; Butelman, ER; Hedrick, SL; Horn, J; Jackson, K; Kaska, S; Kreek, MJ; Leggas, M; Luo, D; Niloy, KK; Prisinzano, TE; Sarma, R, 2021)	0.62
"This review details the pharmacologic, pharmacokinetic, associated dosing and indications, and adverse effects for the drug combination olanzapine/samidorphan."	( Olanzapine/Samidorphan: New Drug Approved for Treating Bipolar I Disorder and Schizophrenia. Gums, JG; McCoy, L; Monahan, C; Powell, J, 2022)	0.72
" placebo) and medication dosage (i."	( Within- and between-person effects of naltrexone on the subjective response to alcohol and craving: A daily diary investigation. Corbin, WR; DeMartini, KS; Fucito, LM; Kranzler, HR; Leeman, RF; MacKinnon, DP; O'Malley, SS; Waddell, JT, 2022)	0.72
" Treatment condition did not moderate the within-person effects of dosing on outcomes."	( Within- and between-person effects of naltrexone on the subjective response to alcohol and craving: A daily diary investigation. Corbin, WR; DeMartini, KS; Fucito, LM; Kranzler, HR; Leeman, RF; MacKinnon, DP; O'Malley, SS; Waddell, JT, 2022)	0.72
"Adequate dosing of MOUD leads to improved retention on MOUD."	( Factors associated with retention on medications for opioid use disorder among a cohort of adults seeking treatment in the community. Biondi, BE; Schlossberg, EF; Shaw, A; Springer, SA; Vander Wyk, B, 2022)	0.72
" The effects of buprenorphine on sleep-like measures resulted in a biphasic dose-response function, with the highest doses not disrupting actigraphy-based sleep."	( Effects of methadone, buprenorphine, and naltrexone on actigraphy-based sleep-like parameters in male rhesus monkeys. Berro, LF; Freeman, KB; Rowlett, JK; Talley, JT; Zamarripa, CA, 2022)	0.72
" Moreover, there were insufficient studies to conduct meta-analyses on many outcome measures; to compare efficacy across and within major categories of interventions; to explore dosage effects; or to examine effects beyond post-treatment."	( Pharmacological interventions for the treatment of disordered and problem gambling. Bowden-Jones, H; Cowlishaw, S; Dowling, N; Lubman, D; Merkouris, S; Thomas, S, 2022)	0.72
"3 mg/kg) produced the same degree of rightward shift in the dose-response curves for heroin- and THC-induced antinociception, respectively."	( Functional consequences of short-term exposure to opioids versus cannabinoids in nonhuman primates. Ding, H; Kiguchi, N; Kishioka, S; Ko, MC; Mabry, KM, 2023)	0.91
" Oral and injectable naltrexone administration is the most widely used, presenting some inconveniences: poor patient adherence to the oral daily dosing schedule, cases of hepatitis and clinically significant liver dysfunction."	( Promising biomedical subcutaneous delivery system in opioid disaccustom process: In vitro/in vivo evaluation of naloxone microparticles on antagonist effect of morphine. Benéitez García, MC; Colmena Crespo, I; Díez-Orejas, RM; Gil-Alegre, ME; Girón Moreno, R; Goicoechea García, C; Martín Fontelles, MI; Sánchez-Robles, EM, 2023)	0.91
"0-10 mg/kg) were studied in combination with the peak oxycodone dose and a dose on the descending limb of the dose-effect curve; NTX and (±)VK4-40 were also studied at the peak of the PR dose-response curve (N = 4)."	( Effects of selective dopamine D3 receptor partial agonist/antagonists on oxycodone self-administration and antinociception in monkeys. Allen, MI; Banks, ML; Cornelissen, JC; Nader, MA; Newman, AH; Woodlief, K, 2023)	0.91
" Variability in dosing paradigms and the time to patient response was present in the reviewed studies."	( Low-dose naltrexone's utility for non-cancer centralized pain conditions: a scoping review. Chadwick, AL; Rupp, A; Young, E, 2023)	0.91
"4 mg were found to reduce pain in 95% of patients with fibromyalgia (SOR, B; single prospective dose-response study)."	( Is low-dose naltrexone effective in chronic pain management? DeSanto, K; Huang, H; Lyon, C; Radi, R; Rivera, J, 2023)	0.91

[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Role	Description
mu-opioid receptor antagonist	Any compound that exhibits antagonist activity at the mu-opioid receptor
central nervous system depressant	A loosely defined group of drugs that tend to reduce the activity of the central nervous system.
environmental contaminant	Any minor or unwanted substance introduced into the environment that can have undesired effects.
xenobiotic	A xenobiotic (Greek, xenos "foreign"; bios "life") is a compound that is foreign to a living organism. Principal xenobiotics include: drugs, carcinogens and various compounds that have been introduced into the environment by artificial means.
antidote to opioid poisoning	A role borne by a molecule that acts to counteract or neutralise the deleterious effects of opioids.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Class	Description
organic heteropentacyclic compound
morphinane-like compound	Any organonitrogen heterocyclic compound based on a morphinan skeleton. These are synthetic or semi-synthetic compounds that resemble the morphinane (opioid) alkaloids in their pharmacological effects.
cyclopropanes	Cyclopropane and its derivatives formed by substitution.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Pathway	Proteins	Compounds
Naltrexone Action Pathway	31	11
Differentiation pathway	0	12
Pluripotent stem cell differentiation pathway	0	11

Protein	Taxonomy	Measurement	Average (µ)	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
RAR-related orphan receptor gamma	Mus musculus (house mouse)	Potency	25.6358	0.0060	38.0041	19,952.5996	AID1159521; AID1159523
glucocorticoid receptor [Homo sapiens]	Homo sapiens (human)	Potency	10.6822	0.0002	14.3764	60.0339	AID720691
retinoic acid nuclear receptor alpha variant 1	Homo sapiens (human)	Potency	21.5491	0.0030	41.6115	22,387.1992	AID1159552; AID1159555
cytochrome P450 2D6	Homo sapiens (human)	Potency	9.7717	0.0010	8.3798	61.1304	AID1645840
nuclear factor erythroid 2-related factor 2 isoform 1	Homo sapiens (human)	Potency	25.1547	0.0006	27.2152	1,122.0200	AID743202; AID743219
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
5-hydroxytryptamine receptor 3E	Homo sapiens (human)	Ki	0.0600	0.0010	0.8835	9.9000	AID239162
Solute carrier family 22 member 1	Homo sapiens (human)	IC50 (µMol)	157.5100	0.2100	5.5537	10.0000	AID1526751
5-hydroxytryptamine receptor 3B	Homo sapiens (human)	Ki	0.0600	0.0010	0.8711	9.9000	AID239162
Bile salt export pump	Homo sapiens (human)	IC50 (µMol)	1,000.0000	0.1100	7.1903	10.0000	AID1449628
Cytochrome P450 2D6	Homo sapiens (human)	IC50 (µMol)	1.0000	0.0000	2.0151	10.0000	AID625249
Delta-type opioid receptor	Mus musculus (house mouse)	IC50 (µMol)	0.0051	0.0001	0.7298	10.0000	AID148621; AID148624; AID148748
Delta-type opioid receptor	Mus musculus (house mouse)	Ki	0.0466	0.0000	0.5393	9.4000	AID1194121; AID148739; AID149086; AID149087; AID395294; AID622100; AID692551; AID767592
Delta-type opioid receptor	Rattus norvegicus (Norway rat)	IC50 (µMol)	0.0063	0.0003	0.3887	7.0000	AID149041; AID149626; AID150392
Delta-type opioid receptor	Rattus norvegicus (Norway rat)	Ki	0.0377	0.0000	0.6068	9.2330	AID149795; AID149918; AID149927; AID149934; AID149944; AID150044; AID150398
Kappa-type opioid receptor	Mus musculus (house mouse)	IC50 (µMol)	0.0060	0.0013	1.5380	10.0000	AID148748
Kappa-type opioid receptor	Mus musculus (house mouse)	Ki	0.0027	0.0003	0.3594	2.7500	AID1194120; AID148739; AID767593
Mu-type opioid receptor	Rattus norvegicus (Norway rat)	IC50 (µMol)	0.0005	0.0001	0.8874	10.0000	AID149041; AID150392
Mu-type opioid receptor	Rattus norvegicus (Norway rat)	Ki	0.0026	0.0000	0.3845	8.6000	AID141762; AID150044; AID150398; AID151889; AID151894; AID151909; AID152204; AID152386; AID152388; AID152389; AID224588
Kappa-type opioid receptor	Rattus norvegicus (Norway rat)	IC50 (µMol)	0.0005	0.0005	0.3698	7.0000	AID149041; AID150392
Kappa-type opioid receptor	Rattus norvegicus (Norway rat)	Ki	0.0040	0.0000	0.1868	3.9500	AID148584; AID148585; AID148586; AID150398
Mu-type opioid receptor	Homo sapiens (human)	IC50 (µMol)	0.0060	0.0001	0.8133	10.0000	AID1121819; AID1194142; AID148621; AID148624; AID148748; AID150239; AID1713965; AID1726158; AID273141; AID274396; AID274417; AID286314; AID417162; AID625163; AID779520
Mu-type opioid receptor	Homo sapiens (human)	Ki	0.0009	0.0000	0.4197	10.0000	AID1054699; AID1121821; AID1181414; AID1191373; AID1268024; AID1268040; AID148739; AID150841; AID150852; AID152204; AID152386; AID1611793; AID238974; AID239328; AID269569; AID273130; AID274390; AID274411; AID286302; AID298631; AID301031; AID301034; AID303905; AID317853; AID347309; AID395293; AID410718; AID415721; AID416813; AID450016; AID450029; AID551424; AID603169; AID603170; AID603171; AID625163; AID756080; AID779520
Delta-type opioid receptor	Homo sapiens (human)	IC50 (µMol)	0.0319	0.0002	0.7521	8.0140	AID148621; AID148624; AID148748; AID149626; AID149748; AID149750; AID150239; AID273143; AID417164; AID625161
Delta-type opioid receptor	Homo sapiens (human)	Ki	0.0290	0.0000	0.5978	9.9300	AID1054697; AID1181416; AID148220; AID148229; AID148739; AID149901; AID149906; AID149913; AID149918; AID150032; AID150033; AID150034; AID150044; AID152386; AID1611794; AID239162; AID239407; AID269569; AID269571; AID273131; AID273132; AID274392; AID274413; AID286304; AID298633; AID301033; AID301036; AID303907; AID317854; AID347310; AID395294; AID410719; AID415722; AID416814; AID450017; AID450030; AID551425; AID625161; AID756078
Kappa-type opioid receptor	Cavia porcellus (domestic guinea pig)	IC50 (µMol)	0.0093	0.0003	0.7123	7.0700	AID147958; AID147963; AID148688; AID148692; AID148748; AID148849
Kappa-type opioid receptor	Cavia porcellus (domestic guinea pig)	Ki	0.0042	0.0000	0.2018	6.4240	AID148739; AID149113; AID149262; AID149266; AID149274; AID149276; AID149277; AID149409; AID149415; AID149420; AID149427; AID149428; AID149431; AID149435; AID149546; AID149552; AID149968; AID1611795; AID223587; AID223596; AID269571
Kappa-type opioid receptor	Homo sapiens (human)	IC50 (µMol)	0.0377	0.0000	1.2011	10.0000	AID148621; AID148624; AID148748; AID150239; AID273145; AID286310; AID417165; AID625162
Kappa-type opioid receptor	Homo sapiens (human)	Ki	0.0024	0.0000	0.3624	10.0000	AID1054698; AID1181415; AID147987; AID147999; AID148739; AID152386; AID239076; AID239386; AID269573; AID273131; AID274391; AID274412; AID286303; AID298632; AID301032; AID301035; AID303906; AID317855; AID347311; AID395295; AID410720; AID415723; AID416815; AID450018; AID450031; AID551426; AID625162; AID756079
Nociceptin receptor	Homo sapiens (human)	Ki	10.0000	0.0000	0.0337	0.5000	AID450032
Mu-type opioid receptor	Mus musculus (house mouse)	IC50 (µMol)	0.0076	0.0008	1.6992	10.0000	AID148748; AID1820200; AID779522
Mu-type opioid receptor	Mus musculus (house mouse)	Ki	0.0013	0.0000	0.1228	1.3000	AID1194119; AID148739; AID1694865; AID1713966; AID1726155; AID1820198; AID395293; AID622099; AID692550; AID692551; AID767594; AID779522
5-hydroxytryptamine receptor 3A	Homo sapiens (human)	Ki	0.0600	0.0000	0.7411	9.9000	AID239162
Mu-type opioid receptor	Cavia porcellus (domestic guinea pig)	IC50 (µMol)	0.0004	0.0002	0.6603	10.0000	AID141490; AID148992; AID149863
Mu-type opioid receptor	Cavia porcellus (domestic guinea pig)	Ki	0.0011	0.0000	0.2786	9.0000	AID141506; AID141511; AID148030; AID148038; AID148045; AID148055; AID148056; AID148057; AID148182; AID152226; AID273132; AID348692; AID354251; AID452924; AID456914; AID484374
5-hydroxytryptamine receptor 3D	Homo sapiens (human)	Ki	0.0600	0.0010	0.8835	9.9000	AID239162
5-hydroxytryptamine receptor 3C	Homo sapiens (human)	Ki	0.0600	0.0010	0.8835	9.9000	AID239162
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Histidine decarboxylase	Rattus norvegicus (Norway rat)	EC50 (µMol)	0.0005	0.0005	0.0015	0.0030	AID1133438
Delta-type opioid receptor	Mus musculus (house mouse)	EC50 (µMol)	0.0044	0.0011	0.4014	4.8000	AID1194135
Delta-type opioid receptor	Rattus norvegicus (Norway rat)	EC50 (µMol)	0.0005	0.0005	0.3649	6.9000	AID1133438
Kappa-type opioid receptor	Mus musculus (house mouse)	EC50 (µMol)	0.0008	0.0008	0.8056	4.8860	AID1194131
Mu-type opioid receptor	Rattus norvegicus (Norway rat)	EC50 (µMol)	0.0005	0.0000	0.0647	0.9320	AID1133438
Kappa-type opioid receptor	Rattus norvegicus (Norway rat)	EC50 (µMol)	0.0005	0.0004	0.0039	0.0180	AID1133438
Mu-type opioid receptor	Homo sapiens (human)	EC50 (µMol)	0.0057	0.0000	0.3263	9.4000	AID148339; AID417156; AID756075
Mu-type opioid receptor	Homo sapiens (human)	Kd	0.0001	0.0001	0.1825	0.8300	AID317858
Delta-type opioid receptor	Homo sapiens (human)	EC50 (µMol)	0.0091	0.0000	0.4332	8.3000	AID1054691; AID1181424; AID148065; AID417158
Delta-type opioid receptor	Homo sapiens (human)	Kd	0.0016	0.0004	0.5147	1.9800	AID317859
Kappa-type opioid receptor	Homo sapiens (human)	EC50 (µMol)	0.0020	0.0000	0.2244	8.9900	AID1054701; AID149987; AID417160
Mu-type opioid receptor	Mus musculus (house mouse)	EC50 (µMol)	0.0002	0.0002	0.0393	0.2030	AID1194124; AID767589
Mu-type opioid receptor	Cavia porcellus (domestic guinea pig)	EC50 (µMol)	0.0019	0.0000	0.0493	0.9320	AID149987
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Cytochrome P450 2D6	Homo sapiens (human)	Kb	0.0006	0.0000	0.0003	0.0006	AID303908
UDP-glucuronosyltransferase 1A1	Homo sapiens (human)	Km	1,310.0000	4.4900	6.5133	9.0000	AID624630
Delta-type opioid receptor	Mus musculus (house mouse)	Ke	0.0318	0.0001	0.1472	6.1080	AID148389; AID148810; AID148930; AID148933; AID148937; AID238168
Mu-type opioid receptor	Homo sapiens (human)	Kb	0.0006	0.0000	0.0331	0.1792	AID303908
Mu-type opioid receptor	Homo sapiens (human)	Ke	0.0018	0.0000	0.2488	3.0700	AID1181420; AID238166; AID256843; AID269581; AID298652; AID298654; AID311281; AID317858; AID395299; AID577293; AID595125
Delta-type opioid receptor	Homo sapiens (human)	Kb	0.0111	0.0012	0.1000	0.5502	AID303910
Delta-type opioid receptor	Homo sapiens (human)	Ke	0.0275	0.0001	0.6979	9.0700	AID149760; AID238168; AID256844; AID269582; AID311282; AID317859; AID395300; AID595126
Kappa-type opioid receptor	Cavia porcellus (domestic guinea pig)	Ke	0.0041	0.0000	0.0389	1.1570	AID148835; AID148841; AID148966
Kappa-type opioid receptor	Homo sapiens (human)	Kb	0.0030	0.0003	0.0500	0.2640	AID303909
Kappa-type opioid receptor	Homo sapiens (human)	Ke	0.0026	0.0000	0.3540	5.8100	AID1181423; AID238169; AID256845; AID269583; AID298653; AID311280; AID317860; AID395301; AID595127
Kappa-type opioid receptor	Homo sapiens (human)	pA2	0.0097	0.0097	0.0097	0.0097	AID317860
Mu-type opioid receptor	Mus musculus (house mouse)	Ke	0.0002	0.0002	0.0233	0.0554	AID151148
Mu-type opioid receptor	Cavia porcellus (domestic guinea pig)	Ke	0.0010	0.0000	0.0159	0.0430	AID147884; AID150010; AID150018
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Process	via Protein(s)	Taxonomy
serotonin receptor signaling pathway	5-hydroxytryptamine receptor 3E	Homo sapiens (human)
monoatomic ion transmembrane transport	5-hydroxytryptamine receptor 3E	Homo sapiens (human)
excitatory postsynaptic potential	5-hydroxytryptamine receptor 3E	Homo sapiens (human)
inorganic cation transmembrane transport	5-hydroxytryptamine receptor 3E	Homo sapiens (human)
regulation of membrane potential	5-hydroxytryptamine receptor 3E	Homo sapiens (human)
chemical synaptic transmission	5-hydroxytryptamine receptor 3E	Homo sapiens (human)
xenobiotic metabolic process	Solute carrier family 22 member 1	Homo sapiens (human)
neurotransmitter transport	Solute carrier family 22 member 1	Homo sapiens (human)
serotonin transport	Solute carrier family 22 member 1	Homo sapiens (human)
establishment or maintenance of transmembrane electrochemical gradient	Solute carrier family 22 member 1	Homo sapiens (human)
organic cation transport	Solute carrier family 22 member 1	Homo sapiens (human)
quaternary ammonium group transport	Solute carrier family 22 member 1	Homo sapiens (human)
prostaglandin transport	Solute carrier family 22 member 1	Homo sapiens (human)
monoamine transport	Solute carrier family 22 member 1	Homo sapiens (human)
putrescine transport	Solute carrier family 22 member 1	Homo sapiens (human)
spermidine transport	Solute carrier family 22 member 1	Homo sapiens (human)
acetylcholine transport	Solute carrier family 22 member 1	Homo sapiens (human)
dopamine transport	Solute carrier family 22 member 1	Homo sapiens (human)
norepinephrine transport	Solute carrier family 22 member 1	Homo sapiens (human)
thiamine transport	Solute carrier family 22 member 1	Homo sapiens (human)
xenobiotic transport	Solute carrier family 22 member 1	Homo sapiens (human)
epinephrine transport	Solute carrier family 22 member 1	Homo sapiens (human)
serotonin uptake	Solute carrier family 22 member 1	Homo sapiens (human)
norepinephrine uptake	Solute carrier family 22 member 1	Homo sapiens (human)
thiamine transmembrane transport	Solute carrier family 22 member 1	Homo sapiens (human)
metanephric proximal tubule development	Solute carrier family 22 member 1	Homo sapiens (human)
purine-containing compound transmembrane transport	Solute carrier family 22 member 1	Homo sapiens (human)
dopamine uptake	Solute carrier family 22 member 1	Homo sapiens (human)
monoatomic cation transmembrane transport	Solute carrier family 22 member 1	Homo sapiens (human)
transport across blood-brain barrier	Solute carrier family 22 member 1	Homo sapiens (human)
(R)-carnitine transmembrane transport	Solute carrier family 22 member 1	Homo sapiens (human)
acyl carnitine transmembrane transport	Solute carrier family 22 member 1	Homo sapiens (human)
spermidine transmembrane transport	Solute carrier family 22 member 1	Homo sapiens (human)
cellular detoxification	Solute carrier family 22 member 1	Homo sapiens (human)
xenobiotic transport across blood-brain barrier	Solute carrier family 22 member 1	Homo sapiens (human)
serotonin receptor signaling pathway	5-hydroxytryptamine receptor 3B	Homo sapiens (human)
monoatomic ion transmembrane transport	5-hydroxytryptamine receptor 3B	Homo sapiens (human)
excitatory postsynaptic potential	5-hydroxytryptamine receptor 3B	Homo sapiens (human)
inorganic cation transmembrane transport	5-hydroxytryptamine receptor 3B	Homo sapiens (human)
chemical synaptic transmission	5-hydroxytryptamine receptor 3B	Homo sapiens (human)
regulation of membrane potential	5-hydroxytryptamine receptor 3B	Homo sapiens (human)
fatty acid metabolic process	Bile salt export pump	Homo sapiens (human)
bile acid biosynthetic process	Bile salt export pump	Homo sapiens (human)
xenobiotic metabolic process	Bile salt export pump	Homo sapiens (human)
xenobiotic transmembrane transport	Bile salt export pump	Homo sapiens (human)
response to oxidative stress	Bile salt export pump	Homo sapiens (human)
bile acid metabolic process	Bile salt export pump	Homo sapiens (human)
response to organic cyclic compound	Bile salt export pump	Homo sapiens (human)
bile acid and bile salt transport	Bile salt export pump	Homo sapiens (human)
canalicular bile acid transport	Bile salt export pump	Homo sapiens (human)
protein ubiquitination	Bile salt export pump	Homo sapiens (human)
regulation of fatty acid beta-oxidation	Bile salt export pump	Homo sapiens (human)
carbohydrate transmembrane transport	Bile salt export pump	Homo sapiens (human)
bile acid signaling pathway	Bile salt export pump	Homo sapiens (human)
cholesterol homeostasis	Bile salt export pump	Homo sapiens (human)
response to estrogen	Bile salt export pump	Homo sapiens (human)
response to ethanol	Bile salt export pump	Homo sapiens (human)
xenobiotic export from cell	Bile salt export pump	Homo sapiens (human)
lipid homeostasis	Bile salt export pump	Homo sapiens (human)
phospholipid homeostasis	Bile salt export pump	Homo sapiens (human)
positive regulation of bile acid secretion	Bile salt export pump	Homo sapiens (human)
regulation of bile acid metabolic process	Bile salt export pump	Homo sapiens (human)
transmembrane transport	Bile salt export pump	Homo sapiens (human)
xenobiotic metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
steroid metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
cholesterol metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
estrogen metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
coumarin metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
alkaloid metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
alkaloid catabolic process	Cytochrome P450 2D6	Homo sapiens (human)
monoterpenoid metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
isoquinoline alkaloid metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
xenobiotic catabolic process	Cytochrome P450 2D6	Homo sapiens (human)
retinol metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
long-chain fatty acid biosynthetic process	Cytochrome P450 2D6	Homo sapiens (human)
negative regulation of binding	Cytochrome P450 2D6	Homo sapiens (human)
oxidative demethylation	Cytochrome P450 2D6	Homo sapiens (human)
negative regulation of cellular organofluorine metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
arachidonic acid metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
liver development	UDP-glucuronosyltransferase 1A1	Homo sapiens (human)
bilirubin conjugation	UDP-glucuronosyltransferase 1A1	Homo sapiens (human)
xenobiotic metabolic process	UDP-glucuronosyltransferase 1A1	Homo sapiens (human)
acute-phase response	UDP-glucuronosyltransferase 1A1	Homo sapiens (human)
response to nutrient	UDP-glucuronosyltransferase 1A1	Homo sapiens (human)
steroid metabolic process	UDP-glucuronosyltransferase 1A1	Homo sapiens (human)
estrogen metabolic process	UDP-glucuronosyltransferase 1A1	Homo sapiens (human)
animal organ regeneration	UDP-glucuronosyltransferase 1A1	Homo sapiens (human)
response to lipopolysaccharide	UDP-glucuronosyltransferase 1A1	Homo sapiens (human)
retinoic acid metabolic process	UDP-glucuronosyltransferase 1A1	Homo sapiens (human)
response to starvation	UDP-glucuronosyltransferase 1A1	Homo sapiens (human)
negative regulation of steroid metabolic process	UDP-glucuronosyltransferase 1A1	Homo sapiens (human)
flavone metabolic process	UDP-glucuronosyltransferase 1A1	Homo sapiens (human)
cellular glucuronidation	UDP-glucuronosyltransferase 1A1	Homo sapiens (human)
flavonoid glucuronidation	UDP-glucuronosyltransferase 1A1	Homo sapiens (human)
xenobiotic glucuronidation	UDP-glucuronosyltransferase 1A1	Homo sapiens (human)
biphenyl catabolic process	UDP-glucuronosyltransferase 1A1	Homo sapiens (human)
cellular response to ethanol	UDP-glucuronosyltransferase 1A1	Homo sapiens (human)
cellular response to glucocorticoid stimulus	UDP-glucuronosyltransferase 1A1	Homo sapiens (human)
cellular response to estradiol stimulus	UDP-glucuronosyltransferase 1A1	Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger	Mu-type opioid receptor	Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathway	Mu-type opioid receptor	Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathway	Mu-type opioid receptor	Homo sapiens (human)
sensory perception	Mu-type opioid receptor	Homo sapiens (human)
negative regulation of cell population proliferation	Mu-type opioid receptor	Homo sapiens (human)
sensory perception of pain	Mu-type opioid receptor	Homo sapiens (human)
G protein-coupled opioid receptor signaling pathway	Mu-type opioid receptor	Homo sapiens (human)
behavioral response to ethanol	Mu-type opioid receptor	Homo sapiens (human)
positive regulation of neurogenesis	Mu-type opioid receptor	Homo sapiens (human)
negative regulation of Wnt protein secretion	Mu-type opioid receptor	Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascade	Mu-type opioid receptor	Homo sapiens (human)
calcium ion transmembrane transport	Mu-type opioid receptor	Homo sapiens (human)
cellular response to morphine	Mu-type opioid receptor	Homo sapiens (human)
regulation of cellular response to stress	Mu-type opioid receptor	Homo sapiens (human)
regulation of NMDA receptor activity	Mu-type opioid receptor	Homo sapiens (human)
neuropeptide signaling pathway	Mu-type opioid receptor	Homo sapiens (human)
immune response	Delta-type opioid receptor	Homo sapiens (human)
G protein-coupled receptor signaling pathway	Delta-type opioid receptor	Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger	Delta-type opioid receptor	Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway	Delta-type opioid receptor	Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathway	Delta-type opioid receptor	Homo sapiens (human)
adult locomotory behavior	Delta-type opioid receptor	Homo sapiens (human)
negative regulation of gene expression	Delta-type opioid receptor	Homo sapiens (human)
negative regulation of protein-containing complex assembly	Delta-type opioid receptor	Homo sapiens (human)
positive regulation of CREB transcription factor activity	Delta-type opioid receptor	Homo sapiens (human)
positive regulation of peptidyl-serine phosphorylation	Delta-type opioid receptor	Homo sapiens (human)
response to nicotine	Delta-type opioid receptor	Homo sapiens (human)
G protein-coupled opioid receptor signaling pathway	Delta-type opioid receptor	Homo sapiens (human)
eating behavior	Delta-type opioid receptor	Homo sapiens (human)
regulation of mitochondrial membrane potential	Delta-type opioid receptor	Homo sapiens (human)
regulation of calcium ion transport	Delta-type opioid receptor	Homo sapiens (human)
cellular response to growth factor stimulus	Delta-type opioid receptor	Homo sapiens (human)
cellular response to hypoxia	Delta-type opioid receptor	Homo sapiens (human)
cellular response to toxic substance	Delta-type opioid receptor	Homo sapiens (human)
neuropeptide signaling pathway	Delta-type opioid receptor	Homo sapiens (human)
immune response	Kappa-type opioid receptor	Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway	Kappa-type opioid receptor	Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathway	Kappa-type opioid receptor	Homo sapiens (human)
chemical synaptic transmission	Kappa-type opioid receptor	Homo sapiens (human)
sensory perception	Kappa-type opioid receptor	Homo sapiens (human)
locomotory behavior	Kappa-type opioid receptor	Homo sapiens (human)
sensory perception of pain	Kappa-type opioid receptor	Homo sapiens (human)
adenylate cyclase-inhibiting opioid receptor signaling pathway	Kappa-type opioid receptor	Homo sapiens (human)
response to insulin	Kappa-type opioid receptor	Homo sapiens (human)
positive regulation of dopamine secretion	Kappa-type opioid receptor	Homo sapiens (human)
negative regulation of luteinizing hormone secretion	Kappa-type opioid receptor	Homo sapiens (human)
response to nicotine	Kappa-type opioid receptor	Homo sapiens (human)
G protein-coupled opioid receptor signaling pathway	Kappa-type opioid receptor	Homo sapiens (human)
maternal behavior	Kappa-type opioid receptor	Homo sapiens (human)
eating behavior	Kappa-type opioid receptor	Homo sapiens (human)
response to estrogen	Kappa-type opioid receptor	Homo sapiens (human)
estrous cycle	Kappa-type opioid receptor	Homo sapiens (human)
response to ethanol	Kappa-type opioid receptor	Homo sapiens (human)
regulation of saliva secretion	Kappa-type opioid receptor	Homo sapiens (human)
behavioral response to cocaine	Kappa-type opioid receptor	Homo sapiens (human)
sensory perception of temperature stimulus	Kappa-type opioid receptor	Homo sapiens (human)
defense response to virus	Kappa-type opioid receptor	Homo sapiens (human)
cellular response to lipopolysaccharide	Kappa-type opioid receptor	Homo sapiens (human)
cellular response to glucose stimulus	Kappa-type opioid receptor	Homo sapiens (human)
positive regulation of p38MAPK cascade	Kappa-type opioid receptor	Homo sapiens (human)
positive regulation of potassium ion transmembrane transport	Kappa-type opioid receptor	Homo sapiens (human)
response to acrylamide	Kappa-type opioid receptor	Homo sapiens (human)
positive regulation of eating behavior	Kappa-type opioid receptor	Homo sapiens (human)
conditioned place preference	Kappa-type opioid receptor	Homo sapiens (human)
neuropeptide signaling pathway	Kappa-type opioid receptor	Homo sapiens (human)
calcium-mediated signaling	Nociceptin receptor	Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway	Nociceptin receptor	Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathway	Nociceptin receptor	Homo sapiens (human)
sensory perception	Nociceptin receptor	Homo sapiens (human)
sensory perception of pain	Nociceptin receptor	Homo sapiens (human)
response to estradiol	Nociceptin receptor	Homo sapiens (human)
positive regulation of urine volume	Nociceptin receptor	Homo sapiens (human)
G protein-coupled opioid receptor signaling pathway	Nociceptin receptor	Homo sapiens (human)
eating behavior	Nociceptin receptor	Homo sapiens (human)
negative regulation of cAMP-mediated signaling	Nociceptin receptor	Homo sapiens (human)
estrous cycle	Nociceptin receptor	Homo sapiens (human)
negative regulation of blood pressure	Nociceptin receptor	Homo sapiens (human)
negative regulation of adenylate cyclase-activating G protein-coupled receptor signaling pathway	Nociceptin receptor	Homo sapiens (human)
regulation of locomotor rhythm	Nociceptin receptor	Homo sapiens (human)
conditioned place preference	Nociceptin receptor	Homo sapiens (human)
neuropeptide signaling pathway	Nociceptin receptor	Homo sapiens (human)
serotonin receptor signaling pathway	5-hydroxytryptamine receptor 3A	Homo sapiens (human)
monoatomic ion transmembrane transport	5-hydroxytryptamine receptor 3A	Homo sapiens (human)
excitatory postsynaptic potential	5-hydroxytryptamine receptor 3A	Homo sapiens (human)
inorganic cation transmembrane transport	5-hydroxytryptamine receptor 3A	Homo sapiens (human)
regulation of presynaptic membrane potential	5-hydroxytryptamine receptor 3A	Homo sapiens (human)
chemical synaptic transmission	5-hydroxytryptamine receptor 3A	Homo sapiens (human)
regulation of membrane potential	5-hydroxytryptamine receptor 3A	Homo sapiens (human)
serotonin receptor signaling pathway	5-hydroxytryptamine receptor 3D	Homo sapiens (human)
monoatomic ion transmembrane transport	5-hydroxytryptamine receptor 3D	Homo sapiens (human)
excitatory postsynaptic potential	5-hydroxytryptamine receptor 3D	Homo sapiens (human)
inorganic cation transmembrane transport	5-hydroxytryptamine receptor 3D	Homo sapiens (human)
chemical synaptic transmission	5-hydroxytryptamine receptor 3D	Homo sapiens (human)
regulation of membrane potential	5-hydroxytryptamine receptor 3D	Homo sapiens (human)
serotonin receptor signaling pathway	5-hydroxytryptamine receptor 3C	Homo sapiens (human)
monoatomic ion transmembrane transport	5-hydroxytryptamine receptor 3C	Homo sapiens (human)
excitatory postsynaptic potential	5-hydroxytryptamine receptor 3C	Homo sapiens (human)
inorganic cation transmembrane transport	5-hydroxytryptamine receptor 3C	Homo sapiens (human)
regulation of membrane potential	5-hydroxytryptamine receptor 3C	Homo sapiens (human)
chemical synaptic transmission	5-hydroxytryptamine receptor 3C	Homo sapiens (human)
fatty acid metabolic process	UDP-glucuronosyltransferase 1A8	Homo sapiens (human)
steroid metabolic process	UDP-glucuronosyltransferase 1A8	Homo sapiens (human)
coumarin metabolic process	UDP-glucuronosyltransferase 1A8	Homo sapiens (human)
retinoic acid metabolic process	UDP-glucuronosyltransferase 1A8	Homo sapiens (human)
negative regulation of fatty acid metabolic process	UDP-glucuronosyltransferase 1A8	Homo sapiens (human)
negative regulation of steroid metabolic process	UDP-glucuronosyltransferase 1A8	Homo sapiens (human)
flavone metabolic process	UDP-glucuronosyltransferase 1A8	Homo sapiens (human)
flavonoid glucuronidation	UDP-glucuronosyltransferase 1A8	Homo sapiens (human)
xenobiotic glucuronidation	UDP-glucuronosyltransferase 1A8	Homo sapiens (human)
liver development	UDP-glucuronosyltransferase 1A8	Homo sapiens (human)
cellular glucuronidation	UDP-glucuronosyltransferase 1A8	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
serotonin-gated monoatomic cation channel activity	5-hydroxytryptamine receptor 3E	Homo sapiens (human)
excitatory extracellular ligand-gated monoatomic ion channel activity	5-hydroxytryptamine receptor 3E	Homo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potential	5-hydroxytryptamine receptor 3E	Homo sapiens (human)
acetylcholine transmembrane transporter activity	Solute carrier family 22 member 1	Homo sapiens (human)
neurotransmitter transmembrane transporter activity	Solute carrier family 22 member 1	Homo sapiens (human)
dopamine:sodium symporter activity	Solute carrier family 22 member 1	Homo sapiens (human)
norepinephrine:sodium symporter activity	Solute carrier family 22 member 1	Homo sapiens (human)
protein binding	Solute carrier family 22 member 1	Homo sapiens (human)
monoamine transmembrane transporter activity	Solute carrier family 22 member 1	Homo sapiens (human)
secondary active organic cation transmembrane transporter activity	Solute carrier family 22 member 1	Homo sapiens (human)
organic anion transmembrane transporter activity	Solute carrier family 22 member 1	Homo sapiens (human)
organic cation transmembrane transporter activity	Solute carrier family 22 member 1	Homo sapiens (human)
prostaglandin transmembrane transporter activity	Solute carrier family 22 member 1	Homo sapiens (human)
pyrimidine nucleoside transmembrane transporter activity	Solute carrier family 22 member 1	Homo sapiens (human)
thiamine transmembrane transporter activity	Solute carrier family 22 member 1	Homo sapiens (human)
putrescine transmembrane transporter activity	Solute carrier family 22 member 1	Homo sapiens (human)
spermidine transmembrane transporter activity	Solute carrier family 22 member 1	Homo sapiens (human)
quaternary ammonium group transmembrane transporter activity	Solute carrier family 22 member 1	Homo sapiens (human)
toxin transmembrane transporter activity	Solute carrier family 22 member 1	Homo sapiens (human)
identical protein binding	Solute carrier family 22 member 1	Homo sapiens (human)
xenobiotic transmembrane transporter activity	Solute carrier family 22 member 1	Homo sapiens (human)
(R)-carnitine transmembrane transporter activity	Solute carrier family 22 member 1	Homo sapiens (human)
serotonin-gated monoatomic cation channel activity	5-hydroxytryptamine receptor 3B	Homo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potential	5-hydroxytryptamine receptor 3B	Homo sapiens (human)
excitatory extracellular ligand-gated monoatomic ion channel activity	5-hydroxytryptamine receptor 3B	Homo sapiens (human)
protein binding	Bile salt export pump	Homo sapiens (human)
ATP binding	Bile salt export pump	Homo sapiens (human)
ABC-type xenobiotic transporter activity	Bile salt export pump	Homo sapiens (human)
bile acid transmembrane transporter activity	Bile salt export pump	Homo sapiens (human)
canalicular bile acid transmembrane transporter activity	Bile salt export pump	Homo sapiens (human)
carbohydrate transmembrane transporter activity	Bile salt export pump	Homo sapiens (human)
ABC-type bile acid transporter activity	Bile salt export pump	Homo sapiens (human)
ATP hydrolysis activity	Bile salt export pump	Homo sapiens (human)
monooxygenase activity	Cytochrome P450 2D6	Homo sapiens (human)
iron ion binding	Cytochrome P450 2D6	Homo sapiens (human)
oxidoreductase activity	Cytochrome P450 2D6	Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen	Cytochrome P450 2D6	Homo sapiens (human)
heme binding	Cytochrome P450 2D6	Homo sapiens (human)
anandamide 8,9 epoxidase activity	Cytochrome P450 2D6	Homo sapiens (human)
anandamide 11,12 epoxidase activity	Cytochrome P450 2D6	Homo sapiens (human)
anandamide 14,15 epoxidase activity	Cytochrome P450 2D6	Homo sapiens (human)
retinoic acid binding	UDP-glucuronosyltransferase 1A1	Homo sapiens (human)
enzyme inhibitor activity	UDP-glucuronosyltransferase 1A1	Homo sapiens (human)
steroid binding	UDP-glucuronosyltransferase 1A1	Homo sapiens (human)
glucuronosyltransferase activity	UDP-glucuronosyltransferase 1A1	Homo sapiens (human)
enzyme binding	UDP-glucuronosyltransferase 1A1	Homo sapiens (human)
protein homodimerization activity	UDP-glucuronosyltransferase 1A1	Homo sapiens (human)
protein heterodimerization activity	UDP-glucuronosyltransferase 1A1	Homo sapiens (human)
G-protein alpha-subunit binding	Mu-type opioid receptor	Homo sapiens (human)
G protein-coupled receptor activity	Mu-type opioid receptor	Homo sapiens (human)
beta-endorphin receptor activity	Mu-type opioid receptor	Homo sapiens (human)
voltage-gated calcium channel activity	Mu-type opioid receptor	Homo sapiens (human)
protein binding	Mu-type opioid receptor	Homo sapiens (human)
morphine receptor activity	Mu-type opioid receptor	Homo sapiens (human)
G-protein beta-subunit binding	Mu-type opioid receptor	Homo sapiens (human)
neuropeptide binding	Mu-type opioid receptor	Homo sapiens (human)
G protein-coupled opioid receptor activity	Delta-type opioid receptor	Homo sapiens (human)
protein binding	Delta-type opioid receptor	Homo sapiens (human)
receptor serine/threonine kinase binding	Delta-type opioid receptor	Homo sapiens (human)
G protein-coupled enkephalin receptor activity	Delta-type opioid receptor	Homo sapiens (human)
neuropeptide binding	Delta-type opioid receptor	Homo sapiens (human)
G protein-coupled opioid receptor activity	Kappa-type opioid receptor	Homo sapiens (human)
protein binding	Kappa-type opioid receptor	Homo sapiens (human)
receptor serine/threonine kinase binding	Kappa-type opioid receptor	Homo sapiens (human)
dynorphin receptor activity	Kappa-type opioid receptor	Homo sapiens (human)
neuropeptide binding	Kappa-type opioid receptor	Homo sapiens (human)
nociceptin receptor activity	Nociceptin receptor	Homo sapiens (human)
G protein-coupled receptor activity	Nociceptin receptor	Homo sapiens (human)
protein binding	Nociceptin receptor	Homo sapiens (human)
neuropeptide binding	Nociceptin receptor	Homo sapiens (human)
protein binding	5-hydroxytryptamine receptor 3A	Homo sapiens (human)
serotonin-gated monoatomic cation channel activity	5-hydroxytryptamine receptor 3A	Homo sapiens (human)
identical protein binding	5-hydroxytryptamine receptor 3A	Homo sapiens (human)
serotonin binding	5-hydroxytryptamine receptor 3A	Homo sapiens (human)
ligand-gated monoatomic ion channel activity involved in regulation of presynaptic membrane potential	5-hydroxytryptamine receptor 3A	Homo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potential	5-hydroxytryptamine receptor 3A	Homo sapiens (human)
excitatory extracellular ligand-gated monoatomic ion channel activity	5-hydroxytryptamine receptor 3A	Homo sapiens (human)
protein binding	5-hydroxytryptamine receptor 3D	Homo sapiens (human)
serotonin-gated monoatomic cation channel activity	5-hydroxytryptamine receptor 3D	Homo sapiens (human)
excitatory extracellular ligand-gated monoatomic ion channel activity	5-hydroxytryptamine receptor 3D	Homo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potential	5-hydroxytryptamine receptor 3D	Homo sapiens (human)
protein binding	5-hydroxytryptamine receptor 3C	Homo sapiens (human)
serotonin-gated monoatomic cation channel activity	5-hydroxytryptamine receptor 3C	Homo sapiens (human)
excitatory extracellular ligand-gated monoatomic ion channel activity	5-hydroxytryptamine receptor 3C	Homo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potential	5-hydroxytryptamine receptor 3C	Homo sapiens (human)
retinoic acid binding	UDP-glucuronosyltransferase 1A8	Homo sapiens (human)
enzyme inhibitor activity	UDP-glucuronosyltransferase 1A8	Homo sapiens (human)
steroid binding	UDP-glucuronosyltransferase 1A8	Homo sapiens (human)
fatty acid binding	UDP-glucuronosyltransferase 1A8	Homo sapiens (human)
glucuronosyltransferase activity	UDP-glucuronosyltransferase 1A8	Homo sapiens (human)
enzyme binding	UDP-glucuronosyltransferase 1A8	Homo sapiens (human)
protein homodimerization activity	UDP-glucuronosyltransferase 1A8	Homo sapiens (human)
protein heterodimerization activity	UDP-glucuronosyltransferase 1A8	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
plasma membrane	5-hydroxytryptamine receptor 3E	Homo sapiens (human)
postsynaptic membrane	5-hydroxytryptamine receptor 3E	Homo sapiens (human)
serotonin-activated cation-selective channel complex	5-hydroxytryptamine receptor 3E	Homo sapiens (human)
neuron projection	5-hydroxytryptamine receptor 3E	Homo sapiens (human)
transmembrane transporter complex	5-hydroxytryptamine receptor 3E	Homo sapiens (human)
synapse	5-hydroxytryptamine receptor 3E	Homo sapiens (human)
plasma membrane	5-hydroxytryptamine receptor 3E	Homo sapiens (human)
plasma membrane	Solute carrier family 22 member 1	Homo sapiens (human)
basal plasma membrane	Solute carrier family 22 member 1	Homo sapiens (human)
membrane	Solute carrier family 22 member 1	Homo sapiens (human)
basolateral plasma membrane	Solute carrier family 22 member 1	Homo sapiens (human)
apical plasma membrane	Solute carrier family 22 member 1	Homo sapiens (human)
lateral plasma membrane	Solute carrier family 22 member 1	Homo sapiens (human)
presynapse	Solute carrier family 22 member 1	Homo sapiens (human)
plasma membrane	5-hydroxytryptamine receptor 3B	Homo sapiens (human)
postsynaptic membrane	5-hydroxytryptamine receptor 3B	Homo sapiens (human)
serotonin-activated cation-selective channel complex	5-hydroxytryptamine receptor 3B	Homo sapiens (human)
cell surface	5-hydroxytryptamine receptor 3B	Homo sapiens (human)
transmembrane transporter complex	5-hydroxytryptamine receptor 3B	Homo sapiens (human)
synapse	5-hydroxytryptamine receptor 3B	Homo sapiens (human)
plasma membrane	5-hydroxytryptamine receptor 3B	Homo sapiens (human)
neuron projection	5-hydroxytryptamine receptor 3B	Homo sapiens (human)
basolateral plasma membrane	Bile salt export pump	Homo sapiens (human)
Golgi membrane	Bile salt export pump	Homo sapiens (human)
endosome	Bile salt export pump	Homo sapiens (human)
plasma membrane	Bile salt export pump	Homo sapiens (human)
cell surface	Bile salt export pump	Homo sapiens (human)
apical plasma membrane	Bile salt export pump	Homo sapiens (human)
intercellular canaliculus	Bile salt export pump	Homo sapiens (human)
intracellular canaliculus	Bile salt export pump	Homo sapiens (human)
recycling endosome	Bile salt export pump	Homo sapiens (human)
recycling endosome membrane	Bile salt export pump	Homo sapiens (human)
extracellular exosome	Bile salt export pump	Homo sapiens (human)
membrane	Bile salt export pump	Homo sapiens (human)
mitochondrion	Cytochrome P450 2D6	Homo sapiens (human)
endoplasmic reticulum	Cytochrome P450 2D6	Homo sapiens (human)
endoplasmic reticulum membrane	Cytochrome P450 2D6	Homo sapiens (human)
cytoplasm	Cytochrome P450 2D6	Homo sapiens (human)
intracellular membrane-bounded organelle	Cytochrome P450 2D6	Homo sapiens (human)
endoplasmic reticulum	UDP-glucuronosyltransferase 1A1	Homo sapiens (human)
endoplasmic reticulum membrane	UDP-glucuronosyltransferase 1A1	Homo sapiens (human)
plasma membrane	UDP-glucuronosyltransferase 1A1	Homo sapiens (human)
perinuclear region of cytoplasm	UDP-glucuronosyltransferase 1A1	Homo sapiens (human)
endoplasmic reticulum chaperone complex	UDP-glucuronosyltransferase 1A1	Homo sapiens (human)
cytochrome complex	UDP-glucuronosyltransferase 1A1	Homo sapiens (human)
endoplasmic reticulum	UDP-glucuronosyltransferase 1A1	Homo sapiens (human)
plasma membrane	Kappa-type opioid receptor	Mus musculus (house mouse)
endosome	Mu-type opioid receptor	Homo sapiens (human)
endoplasmic reticulum	Mu-type opioid receptor	Homo sapiens (human)
Golgi apparatus	Mu-type opioid receptor	Homo sapiens (human)
plasma membrane	Mu-type opioid receptor	Homo sapiens (human)
axon	Mu-type opioid receptor	Homo sapiens (human)
dendrite	Mu-type opioid receptor	Homo sapiens (human)
perikaryon	Mu-type opioid receptor	Homo sapiens (human)
synapse	Mu-type opioid receptor	Homo sapiens (human)
plasma membrane	Mu-type opioid receptor	Homo sapiens (human)
neuron projection	Mu-type opioid receptor	Homo sapiens (human)
plasma membrane	Delta-type opioid receptor	Homo sapiens (human)
synaptic vesicle membrane	Delta-type opioid receptor	Homo sapiens (human)
dendrite membrane	Delta-type opioid receptor	Homo sapiens (human)
presynaptic membrane	Delta-type opioid receptor	Homo sapiens (human)
axon terminus	Delta-type opioid receptor	Homo sapiens (human)
spine apparatus	Delta-type opioid receptor	Homo sapiens (human)
postsynaptic density membrane	Delta-type opioid receptor	Homo sapiens (human)
neuronal dense core vesicle	Delta-type opioid receptor	Homo sapiens (human)
plasma membrane	Delta-type opioid receptor	Homo sapiens (human)
neuron projection	Delta-type opioid receptor	Homo sapiens (human)
nucleoplasm	Kappa-type opioid receptor	Homo sapiens (human)
mitochondrion	Kappa-type opioid receptor	Homo sapiens (human)
cytosol	Kappa-type opioid receptor	Homo sapiens (human)
plasma membrane	Kappa-type opioid receptor	Homo sapiens (human)
membrane	Kappa-type opioid receptor	Homo sapiens (human)
sarcoplasmic reticulum	Kappa-type opioid receptor	Homo sapiens (human)
T-tubule	Kappa-type opioid receptor	Homo sapiens (human)
dendrite	Kappa-type opioid receptor	Homo sapiens (human)
synaptic vesicle membrane	Kappa-type opioid receptor	Homo sapiens (human)
presynaptic membrane	Kappa-type opioid receptor	Homo sapiens (human)
perikaryon	Kappa-type opioid receptor	Homo sapiens (human)
axon terminus	Kappa-type opioid receptor	Homo sapiens (human)
postsynaptic membrane	Kappa-type opioid receptor	Homo sapiens (human)
plasma membrane	Kappa-type opioid receptor	Homo sapiens (human)
neuron projection	Kappa-type opioid receptor	Homo sapiens (human)
plasma membrane	Nociceptin receptor	Homo sapiens (human)
cytoplasmic vesicle	Nociceptin receptor	Homo sapiens (human)
plasma membrane	Nociceptin receptor	Homo sapiens (human)
neuron projection	Nociceptin receptor	Homo sapiens (human)
plasma membrane	Mu-type opioid receptor	Mus musculus (house mouse)
plasma membrane	5-hydroxytryptamine receptor 3A	Homo sapiens (human)
cleavage furrow	5-hydroxytryptamine receptor 3A	Homo sapiens (human)
postsynaptic membrane	5-hydroxytryptamine receptor 3A	Homo sapiens (human)
serotonin-activated cation-selective channel complex	5-hydroxytryptamine receptor 3A	Homo sapiens (human)
synapse	5-hydroxytryptamine receptor 3A	Homo sapiens (human)
plasma membrane	5-hydroxytryptamine receptor 3A	Homo sapiens (human)
transmembrane transporter complex	5-hydroxytryptamine receptor 3A	Homo sapiens (human)
neuron projection	5-hydroxytryptamine receptor 3A	Homo sapiens (human)
plasma membrane	5-hydroxytryptamine receptor 3D	Homo sapiens (human)
postsynaptic membrane	5-hydroxytryptamine receptor 3D	Homo sapiens (human)
serotonin-activated cation-selective channel complex	5-hydroxytryptamine receptor 3D	Homo sapiens (human)
synapse	5-hydroxytryptamine receptor 3D	Homo sapiens (human)
transmembrane transporter complex	5-hydroxytryptamine receptor 3D	Homo sapiens (human)
plasma membrane	5-hydroxytryptamine receptor 3D	Homo sapiens (human)
neuron projection	5-hydroxytryptamine receptor 3D	Homo sapiens (human)
plasma membrane	5-hydroxytryptamine receptor 3C	Homo sapiens (human)
postsynaptic membrane	5-hydroxytryptamine receptor 3C	Homo sapiens (human)
serotonin-activated cation-selective channel complex	5-hydroxytryptamine receptor 3C	Homo sapiens (human)
synapse	5-hydroxytryptamine receptor 3C	Homo sapiens (human)
transmembrane transporter complex	5-hydroxytryptamine receptor 3C	Homo sapiens (human)
neuron projection	5-hydroxytryptamine receptor 3C	Homo sapiens (human)
plasma membrane	5-hydroxytryptamine receptor 3C	Homo sapiens (human)
endoplasmic reticulum	UDP-glucuronosyltransferase 1A8	Homo sapiens (human)
endoplasmic reticulum membrane	UDP-glucuronosyltransferase 1A8	Homo sapiens (human)
endoplasmic reticulum	UDP-glucuronosyltransferase 1A8	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (713)

Assay ID	Title	Year	Journal	Article
AID1346987	P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen	2019	Molecular pharmacology, 11, Volume: 96, Issue:5	A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1296008	Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening	2020	SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1	Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346986	P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen	2019	Molecular pharmacology, 11, Volume: 96, Issue:5	A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346364	Human mu receptor (Opioid receptors)	2015	Psychopharmacology, Jan, Volume: 232, Issue:1	The opioid receptor pharmacology of GSK1521498 compared to other ligands with differential effects on compulsive reward-related behaviours.
AID1346341	Mouse kappa receptor (Opioid receptors)	1993	Proceedings of the National Academy of Sciences of the United States of America, Jul-15, Volume: 90, Issue:14	Cloning and functional comparison of kappa and delta opioid receptors from mouse brain.
AID1346329	Human kappa receptor (Opioid receptors)	1995	Proceedings of the National Academy of Sciences of the United States of America, Jul-18, Volume: 92, Issue:15	kappa-Opioid receptor in humans: cDNA and genomic cloning, chromosomal assignment, functional expression, pharmacology, and expression pattern in the central nervous system.
AID1346373	Mouse delta receptor (Opioid receptors)	1994	Molecular pharmacology, Feb, Volume: 45, Issue:2	Pharmacological characterization of the cloned kappa-, delta-, and mu-opioid receptors.
AID1346364	Human mu receptor (Opioid receptors)	1998	NIDA research monograph, Mar, Volume: 178	Standard binding and functional assays related to medications development division testing for potential cocaine and opiate narcotic treatment medications.
AID1346329	Human kappa receptor (Opioid receptors)	1998	NIDA research monograph, Mar, Volume: 178	Standard binding and functional assays related to medications development division testing for potential cocaine and opiate narcotic treatment medications.
AID1346361	Human delta receptor (Opioid receptors)	1998	NIDA research monograph, Mar, Volume: 178	Standard binding and functional assays related to medications development division testing for potential cocaine and opiate narcotic treatment medications.
AID148030	Binding affinity towards Opioid receptor mu 1 of guinea pig brain membranes using radioligand 0.25 nM [3H]DAMGO	2001	Bioorganic & medicinal chemistry letters, Jul-09, Volume: 11, Issue:13	3-Carboxamido analogues of morphine and naltrexone. synthesis and opioid receptor binding properties.
AID301034	Displacement of [3H]diprenorphine from human mu opioid receptor expressed in CHO cells in presence of high sodium by SPA	2007	Bioorganic & medicinal chemistry letters, Oct-01, Volume: 17, Issue:19	Structure-activity relationship studies of carboxamido-biaryl ethers as opioid receptor antagonists (OpRAs). Part 1.
AID756078	Displacement of [3H]NTI from delta opioid receptor (unknown origin) after 1.5 hrs	2013	Bioorganic & medicinal chemistry letters, Jul-01, Volume: 23, Issue:13	Opioid receptor selectivity profile change via isosterism for 14-O-substituted naltrexone derivatives.
AID141490	Tested for the binding affinity against the Mu opioid receptor in guinea pig brain using [3H]-DAMGO	1994	Journal of medicinal chemistry, Dec-09, Volume: 37, Issue:25	Synthesis and opioid receptor affinity of a series of aralkyl ethers of 6 alpha- and 6 beta-naltrexol.
AID269581	Reversal of stimulation of [35S]GTP-gamma-S binding to human recombinant MOR transfected in CHO cells relative to DAMGO	2006	Journal of medicinal chemistry, Aug-24, Volume: 49, Issue:17	Structural determinants of opioid activity in derivatives of 14-aminomorphinones: effect of substitution in the aromatic ring of cinnamoylaminomorphinones and codeinones.
AID150010	Antagonist potency was determined as the ratio of [antagonist] to (IC50 ratio-1) for Opioid receptor mu 1	1990	Journal of medicinal chemistry, Jun, Volume: 33, Issue:6	Design of peptidomimetic delta opioid receptor antagonists using the message-address concept.
AID149996	Stimulation of U-69,593 binding at human recombinant Opioid receptor kappa 1 transfected into CHO cells.	2003	Journal of medicinal chemistry, Apr-10, Volume: 46, Issue:8	14-amino, 14-alkylamino, and 14-acylamino analogs of oxymorphindole. Differential effects on opioid receptor binding and functional profiles.
AID551425	Antagonist activity at human delta opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding by SPA	2011	Bioorganic & medicinal chemistry letters, Jan-15, Volume: 21, Issue:2	Tetrahydroquinoline derivatives as opioid receptor antagonists.
AID1194128	Reversal of morphine-induced antinociceptive activity in sc dosed Swiss-Webster mouse administered 5 mins prior to morphine challenge measured after 20 mins by warm water tail-flick test relative to control	2015	Bioorganic & medicinal chemistry, Apr-15, Volume: 23, Issue:8	Design, syntheses, and pharmacological characterization of 17-cyclopropylmethyl-3,14β-dihydroxy-4,5α-epoxy-6α-(isoquinoline-3'-carboxamido)morphinan analogues as opioid receptor ligands.
AID150392	Inhibition of [3H]naloxone binding to opioid receptor in presence of NaCl	1989	Journal of medicinal chemistry, Feb, Volume: 32, Issue:2	Synthesis and biological evaluation of 14-alkoxymorphinans. 2. (-)-N-(cyclopropylmethyl)-4,14-dimethoxymorphinan-6-one, a selective mu opioid receptor antagonist.
AID229500	Ratio of IC50 morphine and antagonist binding to opioid receptor	1988	Journal of medicinal chemistry, Apr, Volume: 31, Issue:4	Binaltorphimine-related bivalent ligands and their kappa opioid receptor antagonist selectivity.
AID456916	Displacement of [3H]U69,593 from kappa opioid receptor in guinea pig cerebellum	2010	Bioorganic & medicinal chemistry letters, Feb-01, Volume: 20, Issue:3	Investigation of Beckett-Casy model 1: synthesis of novel 16,17-seco-naltrexone derivatives and their pharmacology.
AID226742	In vitro narcotic agonist potency of compound as ratio to normorphine (=1) was assessed in mouse vas deferens	1982	Journal of medicinal chemistry, Feb, Volume: 25, Issue:2	Common anionic receptor site hypothesis: its relevance to the antagonist action of naloxone.
AID320419	Displacement of 3.0 nM [3H]etorphine from opioid receptor in rat cerebrum	2008	Bioorganic & medicinal chemistry, Jan-15, Volume: 16, Issue:2	The influence of esters and carboxylic acids as the N-substituent of opioids. Part 1: Benzomorphans.
AID1135653	Residual inhibition of morphine-induced analgesia in mouse at 2.4 nmol, icv measured after 2 hrs by tail-flick assay	1978	Journal of medicinal chemistry, Jul, Volume: 21, Issue:7	6beta-[N,N-Bis(2-chloroethyl)amino]-17-(cyclopropylmethyl)-4,5alpha-epoxy-3,14-dihydroxymorphinan(chlornaltrexamine) a potent opioid receptor alkylating agent with ultralong narcotic antagonist actitivty.
AID301031	Antagonist activity at human mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay	2007	Bioorganic & medicinal chemistry letters, Oct-01, Volume: 17, Issue:19	Structure-activity relationship studies of carboxamido-biaryl ethers as opioid receptor antagonists (OpRAs). Part 1.
AID148688	Inhibitory concentration against Opioid receptor kappa 1 using [3H]- U-69,593 radioligand	1995	Journal of medicinal chemistry, Feb-03, Volume: 38, Issue:3	Isothiocyanate-substituted benzyl ether opioid receptor ligands derived from 6 beta-naltrexol.
AID228131	Ratio of kappa/delta-opioid receptors Binding affinity	2003	Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14	Opioid binding and in vitro profiles of a series of 4-hdroxy-3-methoxyindolomorphinans. Transformation of a delta-selective ligand into a high affinity kappa-selective ligand by introduction of a 5,14-substituted bridge.
AID147882	In vitro inhibitory activity against Opioid receptor mu 1 of guinea pig ileum was determined	2004	Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3	Structure-activity study on the Phe side chain arrangement of endomorphins using conformationally constrained analogues.
AID347309	Displacement of [3H]naloxone from monocloned mu opioid receptor expressed in CHO cells	2009	Journal of medicinal chemistry, Mar-12, Volume: 52, Issue:5	Design, synthesis, and biological evaluation of 6alpha- and 6beta-N-heterocyclic substituted naltrexamine derivatives as mu opioid receptor selective antagonists.
AID1713966	Displacement of [3H]NLX from mouse MOR expressed in CHO cell membrane incubated for 90 mins by liquid scintillation spectrophotometry	2016	Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22	Exploration of bivalent ligands targeting putative mu opioid receptor and chemokine receptor CCR5 dimerization.
AID149337	In vito concentration required to displace [3H]DADLE (Kd = 1.6 nM and concentration is 1.9 nM) from high affinity delta-site in rat brain membranes.	1992	Journal of medicinal chemistry, Jul-24, Volume: 35, Issue:15	Probes for narcotic receptor mediated phenomena. 18. Epimeric 6 alpha- and 6 beta-iodo-3,14-dihydroxy-17-(cyclopropylmethyl)-4,5 alpha-epoxymorphinans as potential ligands for opioid receptor single photon emission computed tomography: synthesis, evaluati
AID1079938	Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source]
AID588216	FDA HLAED, serum glutamic oxaloacetic transaminase (SGOT) increase	2004	Current drug discovery technologies, Dec, Volume: 1, Issue:4	Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID410718	Displacement of [3H]DAMGO form human mu opioid receptor expressed in CHO cells	2009	Bioorganic & medicinal chemistry letters, Jan-01, Volume: 19, Issue:1	Syntheses and opioid receptor binding properties of carboxamido-substituted opioids.
AID148041	Compound was evaluated for binding affinity at Opioid receptor mu 1 in guinea pig brain membranes	1991	Journal of medicinal chemistry, Jun, Volume: 34, Issue:6	An approach to the design of receptor-type-selective non-peptide antagonists of peptidergic receptors: delta opioid antagonists.
AID273136	Displacement of [3H]U-69593 from kappa opioid receptor in guinea pig brain homogenate	2006	Journal of medicinal chemistry, Oct-05, Volume: 49, Issue:20	Structural determinants of opioid activity in derivatives of 14-aminomorphinones: effects of changes to the chain linking of the C14-amino group to the aryl ring.
AID1079942	Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID1449628	Inhibition of human BSEP expressed in baculovirus transfected fall armyworm Sf21 cell membranes vesicles assessed as reduction in ATP-dependent [3H]-taurocholate transport into vesicles incubated for 5 mins by Topcount based rapid filtration method	2012	Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12	Mitigating the inhibition of human bile salt export pump by drugs: opportunities provided by physicochemical property modulation, in silico modeling, and structural modification.
AID224576	Antagonistic activity towards morphine induced mu-opioid receptor by mouse writhing assay at 1.25 mg/kg subcutaneously	1993	Journal of medicinal chemistry, Oct-01, Volume: 36, Issue:20	3,4-Dimethyl-4-(3-hydroxyphenyl)piperidines: opioid antagonists with potent anorectant activity.
AID148056	Inhibition of [35S]GTP-gamma-S, binding from Opioid receptor mu 1 in Guinea pig Caudate stimulated by DAMGO	1998	Journal of medicinal chemistry, Dec-17, Volume: 41, Issue:26	Identification of an opioid kappa receptor subtype-selective N-substituent for (+)-(3R,4R)-dimethyl-4-(3-hydroxyphenyl)piperidine.
AID149026	Selectivity ratio is Ki value of mu-opioid receptor to that of delta-opioid receptor	1991	Journal of medicinal chemistry, May, Volume: 34, Issue:5	Role of spacer and address components in peptidomimetic delta opioid receptor antagonists related to naltrindole.
AID149872	Opioid receptor mu 1 antagonistic activity was measured by the displacement of morphine in the guinea pig ileum at a concentration of 100 nM	1990	Journal of medicinal chemistry, Jun, Volume: 33, Issue:6	Design of peptidomimetic delta opioid receptor antagonists using the message-address concept.
AID298654	Agonist activity at human delta opioid receptor expressed in CHO cells assessed as effect on [35S]GTP-gamma-S binding	2007	Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21	Cinnamoyl derivatives of 7alpha-aminomethyl-6,14-endo-ethanotetrahydrothebaine and 7alpha-aminomethyl-6,14-endo-ethanotetrahydrooripavine and related opioid ligands.
AID1123204	Inhibition of morphine-induced analgesia in Swiss Webster mouse assessed as change in morphine ED50 at 2.4 nmol, icv after 2 hrs by tail flick test	1979	Journal of medicinal chemistry, Feb, Volume: 22, Issue:2	Synthesis and pharmacologic characterization of an alkylating analogue (chlornaltrexamine) of naltrexone with ultralong-lasting narcotic antagonist properties.
AID274392	Displacement of [3H]diprenorphine from human cloned delta opioid receptor expressed in CHO cells	2006	Journal of medicinal chemistry, Dec-14, Volume: 49, Issue:25	Synthesis and pharmacological evaluation of novel octahydro-1H-pyrido[1,2-a]pyrazine as mu-opioid receptor antagonists.
AID298633	Displacement of [3H]DPDPE from human cloned delta opioid receptor	2007	Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21	Cinnamoyl derivatives of 7alpha-aminomethyl-6,14-endo-ethanotetrahydrothebaine and 7alpha-aminomethyl-6,14-endo-ethanotetrahydrooripavine and related opioid ligands.
AID229497	Ratio of IC50 DADLE and antagonist binding to delta opioid receptor	1988	Journal of medicinal chemistry, Apr, Volume: 31, Issue:4	Binaltorphimine-related bivalent ligands and their kappa opioid receptor antagonist selectivity.
AID1474167	Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status	2016	Drug discovery today, Apr, Volume: 21, Issue:4	DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID1121814	Binding affinity to CCR5/MOR in human astrocytes assessed as inhibition of R5 HIV-1 SF162 infection by measuring Tat protein expression at 1.5 uM preincubated for 30 to 60 mins followed by viral infection measured after 18 hrs by luciferase reporter gene	2013	MedChemComm, May-01, Volume: 4, Issue:5	A Bivalent Ligand Targeting the Putative Mu Opioid Receptor and Chemokine Receptor CCR5 Heterodimers: Binding Affinity versus Functional Activities.
AID484375	Displacement of [3H]U69493 from kappa opioid receptor in Hartley guinea pig cerebellum by liquid scintillation counter	2010	Bioorganic & medicinal chemistry letters, Jun-15, Volume: 20, Issue:12	Investigation of Beckett-Casy model 2: synthesis of novel 15-16 nornaltrexone derivatives and their pharmacology.
AID450016	Displacement of [3H]DAMGO from mu opioid receptor expressed in HEK293 cells by visible spectrophotometry	2009	Bioorganic & medicinal chemistry, Sep-15, Volume: 17, Issue:18	Synthesis and pharmacological evaluation of 6-naltrexamine analogs for alcohol cessation.
AID149552	The compound was tested for antagonist activity by selective inhibition of [35S]GTP-gamma-S, binding in Guinea pig caudate stimulated by U69,593 to Opioid receptor kappa 1	1998	Journal of medicinal chemistry, May-21, Volume: 41, Issue:11	Investigation of the N-substituent conformation governing potency and mu receptor subtype-selectivity in (+)-(3R, 4R)-dimethyl-4-(3-hydroxyphenyl)piperidine opioid antagonists.
AID317856	Selectivity ratio of Ki for human mu opioid receptor over Ki for human delta opioid receptor	2008	Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6	Synthesis and biological evaluation of alpha- and beta-6-amido derivatives of 17-cyclopropylmethyl-3, 14beta-dihydroxy-4, 5alpha-epoxymorphinan: potential alcohol-cessation agents.
AID1054680	Induction of withdrawal symptoms in chronic morphine-exposed Swiss-Webster mouse assessed as decrease in escape jumps at 1 mg/kg, sc measured over 20 mins	2013	Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22	Design, synthesis, and biological evaluation of 14-heteroaromatic-substituted naltrexone derivatives: pharmacological profile switch from mu opioid receptor selectivity to mu/kappa opioid receptor dual selectivity.
AID273131	Displacement of [3H]U-69593 from human recombinant kappa opioid receptor expressed in CHO cells	2006	Journal of medicinal chemistry, Oct-05, Volume: 49, Issue:20	Structural determinants of opioid activity in derivatives of 14-aminomorphinones: effects of changes to the chain linking of the C14-amino group to the aryl ring.
AID1133440	Narcotic agonist activity in mouse by writhing test	1978	Journal of medicinal chemistry, Jan, Volume: 21, Issue:1	Quantum chemical studies of N-substituent variation in the oxymorphone series of opiate narcotics.
AID233094	Ratio of antagonistic activity for delta and kappa receptors	1988	Journal of medicinal chemistry, Apr, Volume: 31, Issue:4	Binaltorphimine-related bivalent ligands and their kappa opioid receptor antagonist selectivity.
AID1054697	Displacement of [3H]NTI from delta opioid receptor (unknown origin) expressed in CHO cell membranes after 1.5 hrs	2013	Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22	Design, synthesis, and biological evaluation of 14-heteroaromatic-substituted naltrexone derivatives: pharmacological profile switch from mu opioid receptor selectivity to mu/kappa opioid receptor dual selectivity.
AID595126	Antagonist activity at human delta opioid receptor expressed in CHO cells assessed as inhibition of DPDPE stimulated [35S]GTPgammaS binding	2010	ACS medicinal chemistry letters, Oct-14, Volume: 1, Issue:7	1-Substituted 4-(3-Hydroxyphenyl)piperazines Are Pure Opioid Receptor Antagonists.
AID282143	Reversal of 1'-benzyl-6,7-didehydro-3,14-dihydroxy-4,5alpha-epoxy-17-methyl-4',5',6',7'-tetrahydroindolo[2',3':6,7]morphinan-induced antinociceptive activity in mouse	2004	Journal of medicinal chemistry, Dec-16, Volume: 47, Issue:26	Effects of substitution on the pyrrole N atom in derivatives of tetrahydronaltrindole, tetrahydrooxymorphindole, and a related 4,5-epoxyphenylpyrrolomorphinan.
AID148220	Displacement of [3H]C1-DPDPE from human recombinant Opioid receptor delta 1 on CHO cell membranes.	2003	Journal of medicinal chemistry, Apr-10, Volume: 46, Issue:8	14-amino, 14-alkylamino, and 14-acylamino analogs of oxymorphindole. Differential effects on opioid receptor binding and functional profiles.
AID303909	Antagonist activity at cloned human kappa opioid receptor expressed in CHO cells assessed as inhibition of agonist-stimulated GTPgammaS binding	2007	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24	Structure activity relationship studies of carboxamido-biaryl ethers as opioid receptor antagonists (OpRAs). Part 2.
AID625287	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID317853	Displacement of [3H]DAMGO from human mu opioid receptor expressed in CHO cells	2008	Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6	Synthesis and biological evaluation of alpha- and beta-6-amido derivatives of 17-cyclopropylmethyl-3, 14beta-dihydroxy-4, 5alpha-epoxymorphinan: potential alcohol-cessation agents.
AID150393	Inhibition of stereospecific [3H]diprenorphine binding to opioid receptors of rat brain homogenates by 50% in the absence of Na	1982	Journal of medicinal chemistry, Feb, Volume: 25, Issue:2	Common anionic receptor site hypothesis: its relevance to the antagonist action of naloxone.
AID625283	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID149779	Binding affinity determined on Opioid receptor delta 1 in Guinea pig brain membranes using radioligand [3H]DADLE	1998	Journal of medicinal chemistry, Dec-17, Volume: 41, Issue:26	Identification of an opioid kappa receptor subtype-selective N-substituent for (+)-(3R,4R)-dimethyl-4-(3-hydroxyphenyl)piperidine.
AID1079934	Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID1194135	Agonist activity at mouse DOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assay	2015	Bioorganic & medicinal chemistry, Apr-15, Volume: 23, Issue:8	Design, syntheses, and pharmacological characterization of 17-cyclopropylmethyl-3,14β-dihydroxy-4,5α-epoxy-6α-(isoquinoline-3'-carboxamido)morphinan analogues as opioid receptor ligands.
AID149918	Compound was tested for the inhibition of [35S]GTP-gamma-S, binding in Guinea pig Caudate stimulated by the Opioid receptor delta 1 agonist Delta-SNC80	1998	Bioorganic & medicinal chemistry letters, Nov-17, Volume: 8, Issue:22	N-substituted octahydro-4a-(3-hydroxyphenyl)-10a-methyl-benzo[g]isoquinolines are opioid receptor pure antagonists.
AID151436	Evaluated for the inhibition of [3H]naltrexone binding to Opioid receptor mu 1 in rat brain homogenates.	1985	Journal of medicinal chemistry, Dec, Volume: 28, Issue:12	Hybromet: a ligand for purifying opioid receptors.
AID1611793	Displacement of [3H]-DPN from recombinant human mu opioid receptor expressed in CHO-K1 cell membranes by radioligand binding assay	2019	ACS medicinal chemistry letters, Dec-12, Volume: 10, Issue:12	Discovery of Axelopran (TD-1211): A Peripherally Restricted μ-Opioid Receptor Antagonist.
AID149427	Inhibition of [35S]GTP-gamma-S, binding in guinea pig caudate stimulated by U69,593 in Opioid receptor kappa 1	1998	Journal of medicinal chemistry, Oct-08, Volume: 41, Issue:21	N-Substituted 9beta-methyl-5-(3-hydroxyphenyl)morphans are opioid receptor pure antagonists.
AID624636	Drug glucuronidation reaction catalyzed by human recombinant UGT1A8	2005	Pharmacology & therapeutics, Apr, Volume: 106, Issue:1	UDP-glucuronosyltransferases and clinical drug-drug interactions.
AID779522	Binding affinity to MOR W318A mutant (unknown origin) expressed in CHO cells after 15 mins by Ca2+ mobilization assay	2013	Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21	Binding mode characterization of 6α- and 6β-N-heterocyclic substituted naltrexamine derivatives via docking in opioid receptor crystal structures and site-directed mutagenesis studies: application of the 'message-address' concept in development of mu opio
AID233878	Selectivity ratio was determined from Ke value of Opioid receptor mu 1 and Opioid receptor delta 1	1990	Journal of medicinal chemistry, Jun, Volume: 33, Issue:6	Design of peptidomimetic delta opioid receptor antagonists using the message-address concept.
AID551424	Antagonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding by SPA	2011	Bioorganic & medicinal chemistry letters, Jan-15, Volume: 21, Issue:2	Tetrahydroquinoline derivatives as opioid receptor antagonists.
AID779521	Binding affinity to MOR Y210A mutant (unknown origin) expressed in CHO cells after 15 mins by Ca2+ mobilization assay	2013	Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21	Binding mode characterization of 6α- and 6β-N-heterocyclic substituted naltrexamine derivatives via docking in opioid receptor crystal structures and site-directed mutagenesis studies: application of the 'message-address' concept in development of mu opio
AID149913	Binding affinity against Opioid receptor delta 1 of guinea pig brain membranes using 1 nM of [3H]DADLE as radioligand	1986	Journal of medicinal chemistry, Jul, Volume: 29, Issue:7	Peptides as receptor selectivity modulators of opiate pharmacophores.
AID417165	Antagonist activity against human kappa opioid receptor expressed in CHO cells assessed as inhibition of U50488-stimulated [35S]GTPgammaS binding	2009	Bioorganic & medicinal chemistry letters, Apr-15, Volume: 19, Issue:8	Syntheses of novel high affinity ligands for opioid receptors.
AID540215	Volume of distribution at steady state in rat after iv administration	2005	Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7	Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure.
AID147884	Inhibition of [35S]GTP-gamma-S, binding in guines pig caudate stimulated by DAMGO for Opioid receptor mu 1	2003	Journal of medicinal chemistry, May-08, Volume: 46, Issue:10	2002 Medicinal Chemistry Division Award address: monoamine transporters and opioid receptors. Targets for addiction therapy.
AID624630	Drug glucuronidation reaction catalyzed by human recombinant UGT1A1	2005	Pharmacology & therapeutics, Apr, Volume: 106, Issue:1	UDP-glucuronosyltransferases and clinical drug-drug interactions.
AID229499	Ratio of IC50 ethylketazocine and antagonist binding to opioid receptor	1988	Journal of medicinal chemistry, Apr, Volume: 31, Issue:4	Binaltorphimine-related bivalent ligands and their kappa opioid receptor antagonist selectivity.
AID147963	Displacement of [3H]bremazocine from opioid receptor kappa of guinea pig membrane.	1991	Journal of medicinal chemistry, Aug, Volume: 34, Issue:8	Electrophilic gamma-lactone kappa-opioid receptor probes. Analogues of 2'-hydroxy-2-tetrahydrofurfuryl-5,9-dimethyl-6,7-benzomorphan diastereomers.
AID320417	Displacement of [3H]etorphine from opioid receptor in rat cerebrum	2008	Bioorganic & medicinal chemistry, Jan-15, Volume: 16, Issue:2	The influence of esters and carboxylic acids as the N-substituent of opioids. Part 1: Benzomorphans.
AID416813	Displacement of [3H]DAMGO from human mu opioid receptor expressed in CHO cells after 60 mins by scintillation counting	2009	Bioorganic & medicinal chemistry letters, Apr-15, Volume: 19, Issue:8	Syntheses of novel high affinity ligands for opioid receptors.
AID588217	FDA HLAED, serum glutamic pyruvic transaminase (SGPT) increase	2004	Current drug discovery technologies, Dec, Volume: 1, Issue:4	Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID76403	Beta-Funaltrexamine antagonism of morphine agonism in the presence of compound was determined in Guinea pig ileum at concentration of 20 nM	1986	Journal of medicinal chemistry, Aug, Volume: 29, Issue:8	Activity of N-methyl-alpha- and -beta-funaltrexamine at opioid receptors.
AID1194120	Displacement of [3H]diprenorphine from mouse KOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assay	2015	Bioorganic & medicinal chemistry, Apr-15, Volume: 23, Issue:8	Design, syntheses, and pharmacological characterization of 17-cyclopropylmethyl-3,14β-dihydroxy-4,5α-epoxy-6α-(isoquinoline-3'-carboxamido)morphinan analogues as opioid receptor ligands.
AID1079940	Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID410720	Displacement of [3H]U69593 form human kappa opioid receptor expressed in CHO cells	2009	Bioorganic & medicinal chemistry letters, Jan-01, Volume: 19, Issue:1	Syntheses and opioid receptor binding properties of carboxamido-substituted opioids.
AID540210	Clearance in human after iv administration	2008	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7	Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID625282	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID238168	Antagonist potency towards human delta opioid receptor in [35S]GTP-gamma-S, assay	2004	Journal of medicinal chemistry, Oct-07, Volume: 47, Issue:21	Identification of a new scaffold for opioid receptor antagonism based on the 2-amino-1,1-dimethyl-7-hydroxytetralin pharmacophore.
AID148045	Binding affinity against Opioid receptor mu 1 of guinea pig brain membranes using 0.5 nM of [3H]naloxone as radioligand	1986	Journal of medicinal chemistry, Jul, Volume: 29, Issue:7	Peptides as receptor selectivity modulators of opiate pharmacophores.
AID239407	Inhibition of [3H]C1-DPDPE binding to human delta opioid receptor expressed in CHO cells	2004	Journal of medicinal chemistry, Oct-07, Volume: 47, Issue:21	Identification of a new scaffold for opioid receptor antagonism based on the 2-amino-1,1-dimethyl-7-hydroxytetralin pharmacophore.
AID317859	Activity at human delta opioid receptor by [35S]GTPgammaS binding assay	2008	Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6	Synthesis and biological evaluation of alpha- and beta-6-amido derivatives of 17-cyclopropylmethyl-3, 14beta-dihydroxy-4, 5alpha-epoxymorphinan: potential alcohol-cessation agents.
AID149086	Displacement of [3H]- diprenorphine from delta-W284E-receptor expressed in HEK 293 cells	2001	Journal of medicinal chemistry, Mar-15, Volume: 44, Issue:6	Investigation of the selectivity of oxymorphone- and naltrexone-derived ligands via site-directed mutagenesis of opioid receptors: exploring the "address" recognition locus.
AID150036	Inhibitory binding constant in guinea pig brain homogenate was reported at Opioid receptor delta 1 at a a temperature 25 degree Celsius labeled with [3H](D-Ala2-D-Leu5)-enkephalin (0.7 nM)	1985	Journal of medicinal chemistry, Jul, Volume: 28, Issue:7	10-Ketonaltrexone and 10-ketooxymorphone.
AID625285	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID269569	Displacement of [3H]DAMGO from human recombinant MOR expressed in CHO cells	2006	Journal of medicinal chemistry, Aug-24, Volume: 49, Issue:17	Structural determinants of opioid activity in derivatives of 14-aminomorphinones: effect of substitution in the aromatic ring of cinnamoylaminomorphinones and codeinones.
AID152406	Inhibition of [3H]DADLE binding to opioid receptor	1989	Journal of medicinal chemistry, Feb, Volume: 32, Issue:2	Synthesis and biological evaluation of 14-alkoxymorphinans. 2. (-)-N-(cyclopropylmethyl)-4,14-dimethoxymorphinan-6-one, a selective mu opioid receptor antagonist.
AID151889	Inhibition of [3H]DAMGO binding to Opioid receptor mu 1 of rat brain membranes	1998	Journal of medicinal chemistry, May-21, Volume: 41, Issue:11	Investigation of the N-substituent conformation governing potency and mu receptor subtype-selectivity in (+)-(3R, 4R)-dimethyl-4-(3-hydroxyphenyl)piperidine opioid antagonists.
AID148123	Compound was evaluated for the binding affinity to opioid receptor kappa using [3H]EK as radioligand in guinea pig brain membrane	1991	Journal of medicinal chemistry, May, Volume: 34, Issue:5	Role of spacer and address components in peptidomimetic delta opioid receptor antagonists related to naltrindole.
AID286310	Antagonist activity at human opioid kappa receptor expressed in CHO cells assessed as inhibition of U-50488-stimulated [35S]GTP-gamma-S binding	2007	Journal of medicinal chemistry, May-03, Volume: 50, Issue:9	Pharmacological properties of bivalent ligands containing butorphan linked to nalbuphine, naltrexone, and naloxone at mu, delta, and kappa opioid receptors.
AID625291	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1121820	Agonist activity at human mu opioid receptor expressed in Gqi5 transfected CHO cells after 15 mins	2013	MedChemComm, May-01, Volume: 4, Issue:5	A Bivalent Ligand Targeting the Putative Mu Opioid Receptor and Chemokine Receptor CCR5 Heterodimers: Binding Affinity versus Functional Activities.
AID286307	Agonist activity at human opioid kappa receptor expressed in CHO cells assessed as maximal stimulation of [35S]GTP-gamma-S binding	2007	Journal of medicinal chemistry, May-03, Volume: 50, Issue:9	Pharmacological properties of bivalent ligands containing butorphan linked to nalbuphine, naltrexone, and naloxone at mu, delta, and kappa opioid receptors.
AID410721	Ratio of Ki for human mu opioid receptor to Ki for human kappa opioid receptor expressed in CHO cells	2009	Bioorganic & medicinal chemistry letters, Jan-01, Volume: 19, Issue:1	Syntheses and opioid receptor binding properties of carboxamido-substituted opioids.
AID149428	Inhibition of [35S]GTP-gamma-S, binding from Opioid receptor kappa 1 in Guinea pig Caudate stimulated by U69,593	1998	Journal of medicinal chemistry, Dec-17, Volume: 41, Issue:26	Identification of an opioid kappa receptor subtype-selective N-substituent for (+)-(3R,4R)-dimethyl-4-(3-hydroxyphenyl)piperidine.
AID195694	The ability of compound was measured to replace [3H]-labeled [D-Ala2, Met5]-enkephalinamide in rat brain homogenates by using [3H]-opiate binding assay	1980	Journal of medicinal chemistry, Jun, Volume: 23, Issue:6	Long-acting opiate agonists and antagonists: 14-hydroxydihydromorphinone hydrazones.
AID148344	Stimulation of DAMGO binding in recombinant human Opioid receptor mu 1 transfected into CHO cells	2003	Journal of medicinal chemistry, Apr-10, Volume: 46, Issue:8	14-amino, 14-alkylamino, and 14-acylamino analogs of oxymorphindole. Differential effects on opioid receptor binding and functional profiles.
AID1123190	Displacement of [3H]-naloxone from opioid receptor in rat brain homogenate at 1x10'-8 M preincubated for 5 mins measured after third washout by liquid scintillation counting analysis relative to control	1979	Journal of medicinal chemistry, Feb, Volume: 22, Issue:2	Synthesis and pharmacologic characterization of an alkylating analogue (chlornaltrexamine) of naltrexone with ultralong-lasting narcotic antagonist properties.
AID348692	Binding affinity to mu opioid receptor in guinea pig forebrain	2008	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 18, Issue:18	Synthesis of N-isobutylnoroxymorphone from naltrexone by a selective cyclopropane ring opening reaction.
AID149654	Binding activity against Opioid receptor delta 1 using [3H]DADLE as radioligand in rat brain membranes.	1998	Journal of medicinal chemistry, Oct-08, Volume: 41, Issue:21	N-Substituted 9beta-methyl-5-(3-hydroxyphenyl)morphans are opioid receptor pure antagonists.
AID178685	Inhibition of morphine analgesia in modified rat tail flick test.	1981	Journal of medicinal chemistry, Dec, Volume: 24, Issue:12	Analgesic narcotic antagonists. 9. 6-Methylene-8 beta-alkyl-N-(cycloalkylmethyl)-3-hydroxy- or -methoxymorphinans.
AID303908	Antagonist activity at cloned human mu opioid receptor expressed in CHO cells assessed as inhibition of agonist-stimulated GTPgammaS binding	2007	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24	Structure activity relationship studies of carboxamido-biaryl ethers as opioid receptor antagonists (OpRAs). Part 2.
AID149113	Binding activity against Opioid receptor kappa 1 using [3H]U-69593 as radioligand in guinea pig membranes.	1998	Journal of medicinal chemistry, Oct-08, Volume: 41, Issue:21	N-Substituted 9beta-methyl-5-(3-hydroxyphenyl)morphans are opioid receptor pure antagonists.
AID229506	Ratio of IC50 in the presence of morphine to that of control IC50 in guinea pig ileum at 100 nM	1988	Journal of medicinal chemistry, Jul, Volume: 31, Issue:7	Only one pharmacophore is required for the kappa opioid antagonist selectivity of norbinaltorphimine.
AID622103	Selectivity ratio of Ki for mouse delta opioid receptor to mouse mu receptor	2011	Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20	Synthesis of novel triplet drugs with 1,3,5-trioxazatriquinane skeletons and their pharmacologies. Part 2: Synthesis of novel triplet drugs with the epoxymethano structure (capped homotriplet).
AID151894	Inhibition of [3H]DAGO binding to rat brain membrane Opioid receptor mu 1	1990	Journal of medicinal chemistry, Sep, Volume: 33, Issue:9	Photoactivatable opiate derivatives as irreversible probes of the mu-opioid receptor.
AID756079	Displacement of [3H]DPN from kappa opioid receptor (unknown origin) after 1.5 hrs	2013	Bioorganic & medicinal chemistry letters, Jul-01, Volume: 23, Issue:13	Opioid receptor selectivity profile change via isosterism for 14-O-substituted naltrexone derivatives.
AID147947	Percent stimulation of [35S]GTP-gamma-S, binding in recombinant human Opioid receptor delta 1 transfected into CHO cells	2003	Journal of medicinal chemistry, Apr-10, Volume: 46, Issue:8	14-amino, 14-alkylamino, and 14-acylamino analogs of oxymorphindole. Differential effects on opioid receptor binding and functional profiles.
AID415721	Displacement of [3H]DAMGO from mu opioid receptor expressed in CHO cells	2009	Bioorganic & medicinal chemistry letters, Mar-15, Volume: 19, Issue:6	14-O-Heterocyclic-substituted naltrexone derivatives as non-peptide mu opioid receptor selective antagonists: design, synthesis, and biological studies.
AID229502	Ratio of IC50 in the presence of DADLE to that of control IC50 in guinea pig ileum at 100 nM	1988	Journal of medicinal chemistry, Jul, Volume: 31, Issue:7	Only one pharmacophore is required for the kappa opioid antagonist selectivity of norbinaltorphimine.
AID1079946	Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID395293	Displacement of [3H]DAMGO from human mu opioid receptor expressed in CHO cells	2009	Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6	14 beta-O-cinnamoylnaltrexone and related dihydrocodeinones are mu opioid receptor partial agonists with predominant antagonist activity.
AID148500	Dose ratio due to Antagonist Effect at a concentration of 100 nM by (D-Ala2,D-Leu5)enkephalin Opioid receptor delta 1 in mouse vas deferens.	1985	Journal of medicinal chemistry, Jul, Volume: 28, Issue:7	10-Ketonaltrexone and 10-ketooxymorphone.
AID670417	Displacement of [3H]U69593 from kappa opioid receptor in rat brain homogenate after 1 hr by liquid scintillation counting	2012	Bioorganic & medicinal chemistry, Jul-15, Volume: 20, Issue:14	Deconstructing 14-phenylpropyloxymetopon: minimal requirements for binding to mu opioid receptors.
AID223589	Antagonism of opioid analgesia using a mouse writhing model to block U-50,488 (2.5 mg/kg) induced kappa-opioid receptor subcutaneously	1993	Journal of medicinal chemistry, Oct-01, Volume: 36, Issue:20	Structure-activity relationships of trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidine antagonists for mu- and kappa-opioid receptors.
AID148038	Binding affinity was determined in a crude membrane preparation from guinea pig brain by displacement of [3H]DAMGO from Opioid receptor mu 1	1997	Journal of medicinal chemistry, Feb-28, Volume: 40, Issue:5	(E)- and (Z)-7-arylidenenaltrexones: synthesis and opioid receptor radioligand displacement assays.
AID286311	Agonist activity at human opioid gamma receptor expressed in CHO cells assessed as maximal stimulation of [35S]GTP-gamma-S binding	2007	Journal of medicinal chemistry, May-03, Volume: 50, Issue:9	Pharmacological properties of bivalent ligands containing butorphan linked to nalbuphine, naltrexone, and naloxone at mu, delta, and kappa opioid receptors.
AID450031	Antagonist activity at kappa opioid receptor expressed in HEK293 cells assessed as inhibition of compound 16-induced [35S]GTPgammaS binding	2009	Bioorganic & medicinal chemistry, Sep-15, Volume: 17, Issue:18	Synthesis and pharmacological evaluation of 6-naltrexamine analogs for alcohol cessation.
AID149659	Binding affinity at opioid receptor delta 1 by displacement of [3H]DADLE in rat brain membrane	2004	Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6	Identification of opioid ligands possessing mixed micro agonist/delta antagonist activity among pyridomorphinans derived from naloxone, oxymorphone, and hydromorphone [correction of hydropmorphone].
AID146644	Blockage of Nicotinic acetylcholine receptor alpha4-beta2 noncompetitively in cultured hippocampal neurons	2004	Bioorganic & medicinal chemistry letters, Apr-19, Volume: 14, Issue:8	Sensitivity of neuronal nicotinic acetylcholine receptors to the opiate antagonists naltrexone and naloxone: receptor blockade and up-regulation.
AID148055	Inhibition of [35S]GTP-gamma-S, binding in guinea pig caudate stimulated by DAMGO (Opioid receptor mu 1)	1998	Journal of medicinal chemistry, Oct-08, Volume: 41, Issue:21	N-Substituted 9beta-methyl-5-(3-hydroxyphenyl)morphans are opioid receptor pure antagonists.
AID320416	Antinociceptive activity in sc dosed mouse assessed as inhibition of morphin response by tail flick assay	2008	Bioorganic & medicinal chemistry, Jan-15, Volume: 16, Issue:2	The influence of esters and carboxylic acids as the N-substituent of opioids. Part 1: Benzomorphans.
AID149907	Binding affinity was measured by the displacement of [3H]- DADLE in guinea pig brain membrane of Opioid receptor delta 1	1990	Journal of medicinal chemistry, Jun, Volume: 33, Issue:6	Design of peptidomimetic delta opioid receptor antagonists using the message-address concept.
AID456914	Displacement of [3H]DAMGO from mu opioid receptor in guinea pig forebrain	2010	Bioorganic & medicinal chemistry letters, Feb-01, Volume: 20, Issue:3	Investigation of Beckett-Casy model 1: synthesis of novel 16,17-seco-naltrexone derivatives and their pharmacology.
AID149347	In vito concentration required to displace [3H]DADLE (Kd = 12.2 nM and concentration is 2.1 nM) from low affinity delta-site in rat brain membranes.	1992	Journal of medicinal chemistry, Jul-24, Volume: 35, Issue:15	Probes for narcotic receptor mediated phenomena. 18. Epimeric 6 alpha- and 6 beta-iodo-3,14-dihydroxy-17-(cyclopropylmethyl)-4,5 alpha-epoxymorphinans as potential ligands for opioid receptor single photon emission computed tomography: synthesis, evaluati
AID220525	Tested for binding affinity against delta-opioid receptor by displacement of [3H]-DADL	1993	Journal of medicinal chemistry, Oct-01, Volume: 36, Issue:20	3,4-Dimethyl-4-(3-hydroxyphenyl)piperidines: opioid antagonists with potent anorectant activity.
AID595125	Antagonist activity at human mu opioid receptor expressed in CHO cells assessed as inhibition of DAMGO stimulated [35S]GTPgammaS binding	2010	ACS medicinal chemistry letters, Oct-14, Volume: 1, Issue:7	1-Substituted 4-(3-Hydroxyphenyl)piperazines Are Pure Opioid Receptor Antagonists.
AID551426	Antagonist activity at human kappa opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding by SPA	2011	Bioorganic & medicinal chemistry letters, Jan-15, Volume: 21, Issue:2	Tetrahydroquinoline derivatives as opioid receptor antagonists.
AID230902	Ratio of antagonistic activity at mu to kappa receptor	1988	Journal of medicinal chemistry, Jul, Volume: 31, Issue:7	Only one pharmacophore is required for the kappa opioid antagonist selectivity of norbinaltorphimine.
AID1194124	Stimulation of mouse MOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assay	2015	Bioorganic & medicinal chemistry, Apr-15, Volume: 23, Issue:8	Design, syntheses, and pharmacological characterization of 17-cyclopropylmethyl-3,14β-dihydroxy-4,5α-epoxy-6α-(isoquinoline-3'-carboxamido)morphinan analogues as opioid receptor ligands.
AID1611795	Displacement of [3H]-DPN from guinea pig kappa opioid receptor expressed in CHO-K1 cell membranes by radioligand binding assay	2019	ACS medicinal chemistry letters, Dec-12, Volume: 10, Issue:12	Discovery of Axelopran (TD-1211): A Peripherally Restricted μ-Opioid Receptor Antagonist.
AID149439	Inhibitory binding constant in guinea pig brain homogenate was reported at Opioid receptor kappa 1 at temperature 25 degree Celsius labeled with (-)-[3H]immazocine (0.1 nM).	1985	Journal of medicinal chemistry, Jul, Volume: 28, Issue:7	10-Ketonaltrexone and 10-ketooxymorphone.
AID617022	Agonist activity against mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding	2011	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18	Structure selectivity relationship studies of 17-cyclopropylmethyl-3,14β-dihydroxy-4,5α-epoxy-6β-[(4'-pyridyl)carboxamido]morphinan derivatives toward the development of the mu opioid receptor antagonists.
AID148841	Antagonistic activity for Opioid receptor kappa 1 of guinea pig ileal longitudinal muscle at 100 nM	1988	Journal of medicinal chemistry, Apr, Volume: 31, Issue:4	Binaltorphimine-related bivalent ligands and their kappa opioid receptor antagonist selectivity.
AID233096	Ratio of antagonistic activity for mu and kappa receptors	1988	Journal of medicinal chemistry, Apr, Volume: 31, Issue:4	Binaltorphimine-related bivalent ligands and their kappa opioid receptor antagonist selectivity.
AID148621	Tested for the binding affinity against the opioid receptor in guinea pig brain using [3H]bremazocine	1994	Journal of medicinal chemistry, Dec-09, Volume: 37, Issue:25	Synthesis and opioid receptor affinity of a series of aralkyl ethers of 6 alpha- and 6 beta-naltrexol.
AID303907	Displacement of [3H]bremazocine from cloned human delta opioid receptor expressed in CHO cells	2007	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24	Structure activity relationship studies of carboxamido-biaryl ethers as opioid receptor antagonists (OpRAs). Part 2.
AID603171	Displacement of [125I]-IBOxyA from MOR-1 expressed in CHO cells	2011	Bioorganic & medicinal chemistry letters, Jul-01, Volume: 21, Issue:13	Generation of novel radiolabeled opiates through site-selective iodination.
AID1079949	Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID112396	Withdrawl jumping activity was measured in mice at the specified dose	1989	Journal of medicinal chemistry, Feb, Volume: 32, Issue:2	Synthesis and biological evaluation of 14-alkoxymorphinans. 2. (-)-N-(cyclopropylmethyl)-4,14-dimethoxymorphinan-6-one, a selective mu opioid receptor antagonist.
AID148835	Antagonist potency was determined as the ratio of [antagonist] to (IC50 ratio-1) for Opioid receptor kappa 1	1990	Journal of medicinal chemistry, Jun, Volume: 33, Issue:6	Design of peptidomimetic delta opioid receptor antagonists using the message-address concept.
AID415723	Displacement of [3H]norBNI from kappa opioid receptor expressed in CHO cells	2009	Bioorganic & medicinal chemistry letters, Mar-15, Volume: 19, Issue:6	14-O-Heterocyclic-substituted naltrexone derivatives as non-peptide mu opioid receptor selective antagonists: design, synthesis, and biological studies.
AID149175	In vito concentration required to displace [3H]DAGO (Kd = 0.7 nM and concentration is 1.7 nM) from opioid receptor mu in rat brain membranes.	1992	Journal of medicinal chemistry, Jul-24, Volume: 35, Issue:15	Probes for narcotic receptor mediated phenomena. 18. Epimeric 6 alpha- and 6 beta-iodo-3,14-dihydroxy-17-(cyclopropylmethyl)-4,5 alpha-epoxymorphinans as potential ligands for opioid receptor single photon emission computed tomography: synthesis, evaluati
AID1079939	Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID148937	Ke value was obtained from IC50 ratio values when compared with delta opioid agonist in MVD preparations using DPDPE as radioligand	1996	Journal of medicinal chemistry, Apr-26, Volume: 39, Issue:9	Opioid antagonist activity of naltrexone-derived bivalent ligands: importance of a properly oriented molecular scaffold to guide "address" recognition at kappa opioid receptors.
AID273142	Activity at human recombinant mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding relative to DAMGO	2006	Journal of medicinal chemistry, Oct-05, Volume: 49, Issue:20	Structural determinants of opioid activity in derivatives of 14-aminomorphinones: effects of changes to the chain linking of the C14-amino group to the aryl ring.
AID273143	Activity at human recombinant delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding	2006	Journal of medicinal chemistry, Oct-05, Volume: 49, Issue:20	Structural determinants of opioid activity in derivatives of 14-aminomorphinones: effects of changes to the chain linking of the C14-amino group to the aryl ring.
AID148849	In vito concentration required to displace [3H]BRM (Kd = 1.0 nM and concentration is 1.8 nM) from opioid receptor kappa 2 in guinea brain membranes.	1992	Journal of medicinal chemistry, Jul-24, Volume: 35, Issue:15	Probes for narcotic receptor mediated phenomena. 18. Epimeric 6 alpha- and 6 beta-iodo-3,14-dihydroxy-17-(cyclopropylmethyl)-4,5 alpha-epoxymorphinans as potential ligands for opioid receptor single photon emission computed tomography: synthesis, evaluati
AID779520	Binding affinity to wild type MOR (unknown origin) expressed in CHO cells after 15 mins by Ca2+ mobilization assay	2013	Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21	Binding mode characterization of 6α- and 6β-N-heterocyclic substituted naltrexamine derivatives via docking in opioid receptor crystal structures and site-directed mutagenesis studies: application of the 'message-address' concept in development of mu opio
AID1526752	Passive membrane permeability by LC-MS/MS analysis based PAMPA	2019	Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21	Opioids as Substrates and Inhibitors of the Genetically Highly Variable Organic Cation Transporter OCT1.
AID232963	Ke selectivity ratio (mu/delta) of the compound	1991	Journal of medicinal chemistry, Jun, Volume: 34, Issue:6	An approach to the design of receptor-type-selective non-peptide antagonists of peptidergic receptors: delta opioid antagonists.
AID603513	Displacement of [3H]-U69593 from kappa opioid receptor in guinea pig cerebellum homogenates	2011	Bioorganic & medicinal chemistry letters, Jul-01, Volume: 21, Issue:13	Synthesis of novel triplet drugs with 1,3,5-trioxazatriquinane skeletons and their pharmacologies. 1: Synthesis of triplet drugs with morphinan skeletons.
AID417158	Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	2009	Bioorganic & medicinal chemistry letters, Apr-15, Volume: 19, Issue:8	Syntheses of novel high affinity ligands for opioid receptors.
AID1194131	Agonist activity at mouse KOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assay	2015	Bioorganic & medicinal chemistry, Apr-15, Volume: 23, Issue:8	Design, syntheses, and pharmacological characterization of 17-cyclopropylmethyl-3,14β-dihydroxy-4,5α-epoxy-6α-(isoquinoline-3'-carboxamido)morphinan analogues as opioid receptor ligands.
AID1133441	Narcotic antagonist activity in sc dosed rat assessed as inhibition of oxymorphone-induced straub tail effect	1978	Journal of medicinal chemistry, Jan, Volume: 21, Issue:1	Quantum chemical studies of N-substituent variation in the oxymorphone series of opiate narcotics.
AID1194136	Agonist activity at mouse DOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assay relative to SNC80	2015	Bioorganic & medicinal chemistry, Apr-15, Volume: 23, Issue:8	Design, syntheses, and pharmacological characterization of 17-cyclopropylmethyl-3,14β-dihydroxy-4,5α-epoxy-6α-(isoquinoline-3'-carboxamido)morphinan analogues as opioid receptor ligands.
AID622100	Displacement of [3H]DPDPE from mouse delta opioid receptor in whole brain without cerebellum	2011	Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20	Synthesis of novel triplet drugs with 1,3,5-trioxazatriquinane skeletons and their pharmacologies. Part 2: Synthesis of novel triplet drugs with the epoxymethano structure (capped homotriplet).
AID1820199	Agonist activity at mouse MOR expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 1 hr by scintillation counting analysis relative to DAMGO	2021	Journal of medicinal chemistry, 06-10, Volume: 64, Issue:11	Structure-Based Design and Development of Chemical Probes Targeting Putative MOR-CCR5 Heterodimers to Inhibit Opioid Exacerbated HIV-1 Infectivity.
AID395301	Antagonist activity against human kappa opioid receptor expressed in CHO cells assessed as inhibition of U69593-induced [35S]GTPgammaS binding	2009	Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6	14 beta-O-cinnamoylnaltrexone and related dihydrocodeinones are mu opioid receptor partial agonists with predominant antagonist activity.
AID224715	Antagonism of opioid analgesia using a mouse writhing model to block morphine (2.5 mg/kg) induced mu-opioid receptor (subcutaneously dosed)	1993	Journal of medicinal chemistry, Oct-01, Volume: 36, Issue:20	Structure-activity relationships of trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidine antagonists for mu- and kappa-opioid receptors.
AID624611	Specific activity of expressed human recombinant UGT1A8	2000	Annual review of pharmacology and toxicology, , Volume: 40	Human UDP-glucuronosyltransferases: metabolism, expression, and disease.
AID148993	Inhibition of opioid receptor mu by displacing 1 nM [3H]DAGO in guinea pig brain membrane	1992	Journal of medicinal chemistry, Nov-27, Volume: 35, Issue:24	O3-(2-carbomethoxyallyl) ethers of opioid ligands derived from oxymorphone, naltrexone, etorphine, diprenorphine, norbinaltorphimine, and naltrindole. Unexpected O3-dealkylation in the opioid radioligand displacement assay.
AID1526733	Substrate activity at human OCT1 expressed in HEK293 cells assessed as increase in compound uptake at 0.5 uM incubated for 2 mins by LC-MS/MS analysis relative to control empty vector transfected cells	2019	Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21	Opioids as Substrates and Inhibitors of the Genetically Highly Variable Organic Cation Transporter OCT1.
AID711133	Agonist activity at mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTP-gammaS binding at 100 nM relative to DAMGO	2012	Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22	Design, synthesis, and biological evaluation of 17-cyclopropylmethyl-3,14β-dihydroxy-4,5α-epoxy-6β-[(4'-pyridyl)carboxamido]morphinan derivatives as peripheral selective μ opioid receptor Agents.
AID767593	Displacement of [3H]-diprenorphine from mouse kappa opioid receptor expressed in CHO cells after 1.5 hrs	2013	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 23, Issue:18	Structure activity relationship studies of 17-cyclopropylmethyl-3,14β-dihydroxy-4,5α-epoxy-6α-(isoquinoline-3'-carboxamido)morphinan (NAQ) analogues as potent opioid receptor ligands: preliminary results on the role of electronic characteristics for affin
AID622099	Displacement of [3H]DAMGO from mouse mu opioid receptor in whole brain without cerebellum	2011	Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20	Synthesis of novel triplet drugs with 1,3,5-trioxazatriquinane skeletons and their pharmacologies. Part 2: Synthesis of novel triplet drugs with the epoxymethano structure (capped homotriplet).
AID1611796	Antagonist activity at human recombinant mu opioid receptor expressed in CHO-K1 cell membranes assessed as intrinsic activity at 10 pM to 20 uM incubated for 30 mins in presence of Eu-GTP by DELFIA GTP binding assay relative to DAMGO	2019	ACS medicinal chemistry letters, Dec-12, Volume: 10, Issue:12	Discovery of Axelopran (TD-1211): A Peripherally Restricted μ-Opioid Receptor Antagonist.
AID1726155	Displacement of [3H]-NLX from mouse mu opioid receptor expressed in CHO cells measured after 1.5 hrs by competitive-binding assay	2020	ACS medicinal chemistry letters, Nov-12, Volume: 11, Issue:11	Bivalent Ligand Aiming Putative Mu Opioid Receptor and Chemokine Receptor CXCR4 Dimers in Opioid Enhanced HIV-1 Entry.
AID670415	Displacement of [3H]DAMGO from mu opioid receptor in rat brain homogenate after 1 hr by liquid scintillation counting	2012	Bioorganic & medicinal chemistry, Jul-15, Volume: 20, Issue:14	Deconstructing 14-phenylpropyloxymetopon: minimal requirements for binding to mu opioid receptors.
AID88603	Increase in the charge carried by ACh- induced currents in 68-day-old organotypic hippocampal cultures by naltrexone (0.3 uM)	2004	Bioorganic & medicinal chemistry letters, Apr-19, Volume: 14, Issue:8	Sensitivity of neuronal nicotinic acetylcholine receptors to the opiate antagonists naltrexone and naloxone: receptor blockade and up-regulation.
AID1181414	Displacement of [3H]DAMGO from human recombinant mu opioid receptor expressed in CHO cell membranes after 60 mins by scintillation counting method	2014	Bioorganic & medicinal chemistry, Aug-01, Volume: 22, Issue:15	Pyrrolo- and pyridomorphinans: non-selective opioid antagonists and delta opioid agonists/mu opioid partial agonists.
AID149338	In vito concentration required to displace [3H]-DADLE (Kd = 12.2 nM and concentration is 2.1 nM) from low affinity delta-site in rat brain membranes.	1992	Journal of medicinal chemistry, Jul-24, Volume: 35, Issue:15	Probes for narcotic receptor mediated phenomena. 18. Epimeric 6 alpha- and 6 beta-iodo-3,14-dihydroxy-17-(cyclopropylmethyl)-4,5 alpha-epoxymorphinans as potential ligands for opioid receptor single photon emission computed tomography: synthesis, evaluati
AID395299	Antagonist activity against human mu opioid receptor expressed in CHO cells assessed as inhibition of DAMGO-induced [35S]GTPgammaS binding	2009	Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6	14 beta-O-cinnamoylnaltrexone and related dihydrocodeinones are mu opioid receptor partial agonists with predominant antagonist activity.
AID1179653	Activity at human P-glycoprotein assessed as ATPase activity using firefly luciferase at 200 uM by Pgp-Glo assay in presence of MgATP	2014	Bioorganic & medicinal chemistry letters, Aug-01, Volume: 24, Issue:15	Opioids and efflux transporters. Part 4: influence of N-substitution on P-glycoprotein substrate activity of noroxymorphone analogues.
AID1611801	Permeability coefficient, Kp in human Caco2 cells	2019	ACS medicinal chemistry letters, Dec-12, Volume: 10, Issue:12	Discovery of Axelopran (TD-1211): A Peripherally Restricted μ-Opioid Receptor Antagonist.
AID223591	Tested for the antagonism of kappa opioid receptor diuresis at a dose of 0.08 mg/kg subcutaneously	1993	Journal of medicinal chemistry, Oct-01, Volume: 36, Issue:20	Structure-activity relationships of trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidine antagonists for mu- and kappa-opioid receptors.
AID320426	Antagonist activity at delta opioid receptor in Swiss mouse vas deferens assessed as reversal of DSLET effect on electrically-induced driven twitch	2008	Bioorganic & medicinal chemistry, Jan-15, Volume: 16, Issue:2	The influence of esters and carboxylic acids as the N-substituent of opioids. Part 1: Benzomorphans.
AID1079935	Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source]
AID588213	Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in non-rodents	2010	Chemical research in toxicology, Jan, Volume: 23, Issue:1	Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID231054	Oral/parenteral ratio of the compound	1982	Journal of medicinal chemistry, Feb, Volume: 25, Issue:2	Common anionic receptor site hypothesis: its relevance to the antagonist action of naloxone.
AID228132	Ratio of mu/delta-opioid receptors Binding affinity	2003	Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14	Opioid binding and in vitro profiles of a series of 4-hdroxy-3-methoxyindolomorphinans. Transformation of a delta-selective ligand into a high affinity kappa-selective ligand by introduction of a 5,14-substituted bridge.
AID149906	Binding affinity was determined in a crude membrane preparation from guinea pig brain by displacement of [3H]DPDPE from Opioid receptor delta 1	1997	Journal of medicinal chemistry, Feb-28, Volume: 40, Issue:5	(E)- and (Z)-7-arylidenenaltrexones: synthesis and opioid receptor radioligand displacement assays.
AID1611814	Inhibition of morphine-induced delays in gastric emptying in po dosed ICR mouse administered via gavage pretreated with compound and 30 mins later injected with morphine followed 5 mins later by ingestion of test meal and measured after 60 mins	2019	ACS medicinal chemistry letters, Dec-12, Volume: 10, Issue:12	Discovery of Axelopran (TD-1211): A Peripherally Restricted μ-Opioid Receptor Antagonist.
AID148584	Displacement of [3H]diprenorphine from k-E297A-receptor expressed in HEK 293 cells	2001	Journal of medicinal chemistry, Mar-15, Volume: 44, Issue:6	Investigation of the selectivity of oxymorphone- and naltrexone-derived ligands via site-directed mutagenesis of opioid receptors: exploring the "address" recognition locus.
AID228108	Selectivity ratio between delta to that of mu opioid receptor	1996	Journal of medicinal chemistry, Apr-26, Volume: 39, Issue:9	Opioid antagonist activity of naltrexone-derived bivalent ligands: importance of a properly oriented molecular scaffold to guide "address" recognition at kappa opioid receptors.
AID238169	Antagonist potency towards human kappa opioid receptor in [35S]GTP-gamma-S, assay	2004	Journal of medicinal chemistry, Oct-07, Volume: 47, Issue:21	Identification of a new scaffold for opioid receptor antagonism based on the 2-amino-1,1-dimethyl-7-hydroxytetralin pharmacophore.
AID603170	Displacement of [125I]-IBNalA from MOR-1 expressed in CHO cells	2011	Bioorganic & medicinal chemistry letters, Jul-01, Volume: 21, Issue:13	Generation of novel radiolabeled opiates through site-selective iodination.
AID625279	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID273144	Activity at human recombinant delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding relative to DPDPE	2006	Journal of medicinal chemistry, Oct-05, Volume: 49, Issue:20	Structural determinants of opioid activity in derivatives of 14-aminomorphinones: effects of changes to the chain linking of the C14-amino group to the aryl ring.
AID624621	Specific activity of expressed human recombinant UGT2B7Y	2000	Annual review of pharmacology and toxicology, , Volume: 40	Human UDP-glucuronosyltransferases: metabolism, expression, and disease.
AID150841	Displacement of [3H]DAMGO from human recombinant Opioid receptor mu 1 on CHO cell membranes.	2003	Journal of medicinal chemistry, Apr-10, Volume: 46, Issue:8	14-amino, 14-alkylamino, and 14-acylamino analogs of oxymorphindole. Differential effects on opioid receptor binding and functional profiles.
AID233862	Selectivity between mu opioid receptor and delta opioid receptor.	2003	Journal of medicinal chemistry, Apr-10, Volume: 46, Issue:8	14-amino, 14-alkylamino, and 14-acylamino analogs of oxymorphindole. Differential effects on opioid receptor binding and functional profiles.
AID1181423	Antagonist activity at human recombinant kappa opioid receptor expressed in CHO cell membranes assessed as inhibition of U69593-induced response after 60 mins by [35S]GTPgammaS binding assay	2014	Bioorganic & medicinal chemistry, Aug-01, Volume: 22, Issue:15	Pyrrolo- and pyridomorphinans: non-selective opioid antagonists and delta opioid agonists/mu opioid partial agonists.
AID169599	Antagonistic potency of compound after subcutaneous administration in rats	1982	Journal of medicinal chemistry, Feb, Volume: 25, Issue:2	Common anionic receptor site hypothesis: its relevance to the antagonist action of naloxone.
AID224718	Binding affinity towards mu opioid receptor by displacement of [3H]NAL from rat brain homogenates	1993	Journal of medicinal chemistry, Oct-01, Volume: 36, Issue:20	Structure-activity relationships of trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidine antagonists for mu- and kappa-opioid receptors.
AID1054696	Selectivity ratio of Ki for mu opioid receptor (unknown origin) to Ki for kappa opioid receptor (unknown origin)	2013	Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22	Design, synthesis, and biological evaluation of 14-heteroaromatic-substituted naltrexone derivatives: pharmacological profile switch from mu opioid receptor selectivity to mu/kappa opioid receptor dual selectivity.
AID1123210	Effect on development of dependence to morphine in Swiss Webster mouse assessed as increase in naloxone ED50 for eliciting withdrawal jumping at 0.24 nmol, icv after 24 hrs relative to control	1979	Journal of medicinal chemistry, Feb, Volume: 22, Issue:2	Synthesis and pharmacologic characterization of an alkylating analogue (chlornaltrexamine) of naltrexone with ultralong-lasting narcotic antagonist properties.
AID417160	Agonist activity at human kappa opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	2009	Bioorganic & medicinal chemistry letters, Apr-15, Volume: 19, Issue:8	Syntheses of novel high affinity ligands for opioid receptors.
AID135326	BBB penetration classification	2000	Journal of medicinal chemistry, Jun-01, Volume: 43, Issue:11	Predicting blood-brain barrier permeation from three-dimensional molecular structure.
AID229504	Ratio of IC50 in the presence of ethylketazocine to that of control IC50 in guinea pig ileum at 100 nM	1988	Journal of medicinal chemistry, Jul, Volume: 31, Issue:7	Only one pharmacophore is required for the kappa opioid antagonist selectivity of norbinaltorphimine.
AID149163	Antagonistic potency at opioid receptor mu (100 nM) (Ke =IC50 in the presence of antagonist divided by the control IC50 value)	1991	Journal of medicinal chemistry, May, Volume: 34, Issue:5	Role of spacer and address components in peptidomimetic delta opioid receptor antagonists related to naltrindole.
AID395300	Antagonist activity against human delta opioid receptor expressed in CHO cells assessed as inhibition of DPDPE-induced [35S]GTPgammaS binding	2009	Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6	14 beta-O-cinnamoylnaltrexone and related dihydrocodeinones are mu opioid receptor partial agonists with predominant antagonist activity.
AID29359	Ionization constant (pKa)	2000	Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13	QSAR model for drug human oral bioavailability.
AID269573	Displacement of [3H]U-69593 from human recombinant KOR expressed in CHO cells	2006	Journal of medicinal chemistry, Aug-24, Volume: 49, Issue:17	Structural determinants of opioid activity in derivatives of 14-aminomorphinones: effect of substitution in the aromatic ring of cinnamoylaminomorphinones and codeinones.
AID347312	Selectivity ratio of Ki for monocloned delta opioid receptor to Ki for monocloned mu opioid receptor	2009	Journal of medicinal chemistry, Mar-12, Volume: 52, Issue:5	Design, synthesis, and biological evaluation of 6alpha- and 6beta-N-heterocyclic substituted naltrexamine derivatives as mu opioid receptor selective antagonists.
AID178684	Narcotic antagonist activity in heat stimulus rat tail flick assay after subcutaneous administration	1981	Journal of medicinal chemistry, Dec, Volume: 24, Issue:12	Analgesic narcotic antagonists. 8. 7 alpha-Alkyl-4,5 alpha-epoxymorphinan-6-ones.
AID148692	Tested for the binding affinity against the Kappa opioid receptor in guinea pig brain using [3H]U-69593	1994	Journal of medicinal chemistry, Dec-09, Volume: 37, Issue:25	Synthesis and opioid receptor affinity of a series of aralkyl ethers of 6 alpha- and 6 beta-naltrexol.
AID165733	Percent change of volume in the respiratory activity was measured in rabbit at 0.1 mg/kg dose given intravenously	1989	Journal of medicinal chemistry, Feb, Volume: 32, Issue:2	Synthesis and biological evaluation of 14-alkoxymorphinans. 2. (-)-N-(cyclopropylmethyl)-4,14-dimethoxymorphinan-6-one, a selective mu opioid receptor antagonist.
AID1194121	Displacement of [3H]naltrindole from mouse DOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assay	2015	Bioorganic & medicinal chemistry, Apr-15, Volume: 23, Issue:8	Design, syntheses, and pharmacological characterization of 17-cyclopropylmethyl-3,14β-dihydroxy-4,5α-epoxy-6α-(isoquinoline-3'-carboxamido)morphinan analogues as opioid receptor ligands.
AID227973	Selectivity ratio between Ke value to that of DAMGO (using DPDPE as agonist; delta agonist/DAMGO)	1996	Journal of medicinal chemistry, Apr-26, Volume: 39, Issue:9	Opioid antagonist activity of naltrexone-derived bivalent ligands: importance of a properly oriented molecular scaffold to guide "address" recognition at kappa opioid receptors.
AID1054695	Selectivity ratio of Ki for delta opioid receptor (unknown origin) to Ki for kappa opioid receptor (unknown origin)	2013	Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22	Design, synthesis, and biological evaluation of 14-heteroaromatic-substituted naltrexone derivatives: pharmacological profile switch from mu opioid receptor selectivity to mu/kappa opioid receptor dual selectivity.
AID148229	Binding affinity for human Opioid receptor delta 1 transfected into chinese hamster ovary cells by displacing [3H]CI-DPDPE radioligand	2003	Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14	Opioid binding and in vitro profiles of a series of 4-hdroxy-3-methoxyindolomorphinans. Transformation of a delta-selective ligand into a high affinity kappa-selective ligand by introduction of a 5,14-substituted bridge.
AID670416	Displacement of [3H]DPDPE from delta opioid receptor in rat brain homogenate after 1 hr by liquid scintillation counting	2012	Bioorganic & medicinal chemistry, Jul-15, Volume: 20, Issue:14	Deconstructing 14-phenylpropyloxymetopon: minimal requirements for binding to mu opioid receptors.
AID1526751	Inhibition of human OCT1 expressed in HEK293 cells assessed as reduction in ASP+ substrate uptake by microplate reader based analysis	2019	Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21	Opioids as Substrates and Inhibitors of the Genetically Highly Variable Organic Cation Transporter OCT1.
AID273132	Displacement of [3H]Cl-DPDPE from human recombinant delta opioid receptor expressed in CHO cells	2006	Journal of medicinal chemistry, Oct-05, Volume: 49, Issue:20	Structural determinants of opioid activity in derivatives of 14-aminomorphinones: effects of changes to the chain linking of the C14-amino group to the aryl ring.
AID269571	Displacement of [3H]Cl-DPDPE from human recombinant DOR expressed in CHO cells	2006	Journal of medicinal chemistry, Aug-24, Volume: 49, Issue:17	Structural determinants of opioid activity in derivatives of 14-aminomorphinones: effect of substitution in the aromatic ring of cinnamoylaminomorphinones and codeinones.
AID1054701	Agonist activity at kappa opioid receptor (unknown origin) expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrs	2013	Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22	Design, synthesis, and biological evaluation of 14-heteroaromatic-substituted naltrexone derivatives: pharmacological profile switch from mu opioid receptor selectivity to mu/kappa opioid receptor dual selectivity.
AID147886	Ke value was obtained from IC50 ratio value when compared with Opioid receptor mu 1 agonist in Guinea pig Ileum using DAMGO as radioligand	1996	Journal of medicinal chemistry, Apr-26, Volume: 39, Issue:9	Opioid antagonist activity of naltrexone-derived bivalent ligands: importance of a properly oriented molecular scaffold to guide "address" recognition at kappa opioid receptors.
AID417164	Antagonist activity against human delta opioid receptor expressed in CHO cells assessed as inhibition of SNC80-stimulated [35S]GTPgammaS binding	2009	Bioorganic & medicinal chemistry letters, Apr-15, Volume: 19, Issue:8	Syntheses of novel high affinity ligands for opioid receptors.
AID149324	Selectivity ratio is IC50 value of mu-opioid receptor to that of delta-opioid receptor	1991	Journal of medicinal chemistry, May, Volume: 34, Issue:5	Role of spacer and address components in peptidomimetic delta opioid receptor antagonists related to naltrindole.
AID148065	Agonistic activity towards Opioid receptor delta 1	2003	Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14	Opioid binding and in vitro profiles of a series of 4-hdroxy-3-methoxyindolomorphinans. Transformation of a delta-selective ligand into a high affinity kappa-selective ligand by introduction of a 5,14-substituted bridge.
AID1123191	Displacement of [3H]-naloxone from opioid receptor in rat brain homogenate at 1x10'-8 M preincubated for 5 mins measured after fourth washout by liquid scintillation counting analysis relative to control	1979	Journal of medicinal chemistry, Feb, Volume: 22, Issue:2	Synthesis and pharmacologic characterization of an alkylating analogue (chlornaltrexamine) of naltrexone with ultralong-lasting narcotic antagonist properties.
AID147088	Blockage of Nicotinic acetylcholine receptor alpha-7 noncompetitively in hippocampal primary cultures	2004	Bioorganic & medicinal chemistry letters, Apr-19, Volume: 14, Issue:8	Sensitivity of neuronal nicotinic acetylcholine receptors to the opiate antagonists naltrexone and naloxone: receptor blockade and up-regulation.
AID317858	Activity at human mu opioid receptor by [35S]GTPgammaS binding assay	2008	Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6	Synthesis and biological evaluation of alpha- and beta-6-amido derivatives of 17-cyclopropylmethyl-3, 14beta-dihydroxy-4, 5alpha-epoxymorphinan: potential alcohol-cessation agents.
AID149968	In vito concentration required to displace 9 (Kd = 1.6 nM and concentration is 1.8 nM) from opioid receptor kappa 1 in guinea brain membranes.	1992	Journal of medicinal chemistry, Jul-24, Volume: 35, Issue:15	Probes for narcotic receptor mediated phenomena. 18. Epimeric 6 alpha- and 6 beta-iodo-3,14-dihydroxy-17-(cyclopropylmethyl)-4,5 alpha-epoxymorphinans as potential ligands for opioid receptor single photon emission computed tomography: synthesis, evaluati
AID138326	Concentration required for antagonistic activity of normorphine in the mouse vas deferens at the dose ratio of 2.	1982	Journal of medicinal chemistry, Feb, Volume: 25, Issue:2	Common anionic receptor site hypothesis: its relevance to the antagonist action of naloxone.
AID603515	Selectivity ratio of Ki for delta opioid receptor in guinea pig forebrain homogenates to Ki for mu opioid receptor in guinea pig forebrain homogenates	2011	Bioorganic & medicinal chemistry letters, Jul-01, Volume: 21, Issue:13	Synthesis of novel triplet drugs with 1,3,5-trioxazatriquinane skeletons and their pharmacologies. 1: Synthesis of triplet drugs with morphinan skeletons.
AID239328	Inhibition of [3H]DAMGO binding to human Mu opioid receptor expressed in CHO cells	2004	Journal of medicinal chemistry, Oct-07, Volume: 47, Issue:21	Identification of a new scaffold for opioid receptor antagonism based on the 2-amino-1,1-dimethyl-7-hydroxytetralin pharmacophore.
AID149626	Inhibition of [3H]DPDPE binding to guinea pig brain membrane Opioid receptor delta 1 at 1.0 nM	1992	Journal of medicinal chemistry, Jun-26, Volume: 35, Issue:13	Electrophilic opioid ligands. Oxygen tethered alpha-methylene-gamma-lactone, acrylate, isothiocyanate, and epoxide derivatives of 6 beta-naltrexol.
AID298632	Displacement of [3H]U-69593 from human cloned kappa opioid receptor	2007	Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21	Cinnamoyl derivatives of 7alpha-aminomethyl-6,14-endo-ethanotetrahydrothebaine and 7alpha-aminomethyl-6,14-endo-ethanotetrahydrooripavine and related opioid ligands.
AID540216	Clearance in dog after iv administration	2005	Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7	Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure.
AID147087	Blockage of Nicotinic acetylcholine receptor alpha-7 noncompetitively in cultured hippocampal neurons	2004	Bioorganic & medicinal chemistry letters, Apr-19, Volume: 14, Issue:8	Sensitivity of neuronal nicotinic acetylcholine receptors to the opiate antagonists naltrexone and naloxone: receptor blockade and up-regulation.
AID111971	Percent analgesia of compound was measured in mice by using tail-flick assay	1980	Journal of medicinal chemistry, Jun, Volume: 23, Issue:6	Long-acting opiate agonists and antagonists: 14-hydroxydihydromorphinone hydrazones.
AID767591	Selectivity ratio of Ki for mouse kappa opioid receptor to Ki for mouse mu opioid receptor	2013	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 23, Issue:18	Structure activity relationship studies of 17-cyclopropylmethyl-3,14β-dihydroxy-4,5α-epoxy-6α-(isoquinoline-3'-carboxamido)morphinan (NAQ) analogues as potent opioid receptor ligands: preliminary results on the role of electronic characteristics for affin
AID317860	Activity at human kappa opioid receptor by [35S]GTPgammaS binding assay	2008	Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6	Synthesis and biological evaluation of alpha- and beta-6-amido derivatives of 17-cyclopropylmethyl-3, 14beta-dihydroxy-4, 5alpha-epoxymorphinan: potential alcohol-cessation agents.
AID1079941	Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID150029	Compound was evaluated for antagonist potency in guinea pig ileum preparation using morphine (Opioid receptor mu 1)	1991	Journal of medicinal chemistry, Jun, Volume: 34, Issue:6	An approach to the design of receptor-type-selective non-peptide antagonists of peptidergic receptors: delta opioid antagonists.
AID416817	Selectivity ratio of IC50 for human kappa opioid receptor to IC50 for human mu opioid receptor	2009	Bioorganic & medicinal chemistry letters, Apr-15, Volume: 19, Issue:8	Syntheses of novel high affinity ligands for opioid receptors.
AID1611794	Displacement of [3H]-DPN from recombinant human delta opioid receptor expressed in CHO-K1 cell membranes by radioligand binding assay	2019	ACS medicinal chemistry letters, Dec-12, Volume: 10, Issue:12	Discovery of Axelopran (TD-1211): A Peripherally Restricted μ-Opioid Receptor Antagonist.
AID274413	Displacement of [3H]diprenorphine from human cloned delta opioid receptor expressed in CHO cells	2006	Journal of medicinal chemistry, Dec-14, Volume: 49, Issue:25	Elucidation of the bioactive conformation of the N-substituted trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidine class of mu-opioid receptor antagonists.
AID588209	Literature-mined public compounds from Greene et al multi-species hepatotoxicity modelling dataset	2010	Chemical research in toxicology, Jul-19, Volume: 23, Issue:7	Developing structure-activity relationships for the prediction of hepatotoxicity.
AID148058	Inhibitory binding constant in guinea pig brain homogenate was reported at mu site at a temperature 25 degree Centigrade labeled with [3H](D-Ala2-MePhe4,Gly-ol5)enkephalin(1 nM)	1985	Journal of medicinal chemistry, Jul, Volume: 28, Issue:7	10-Ketonaltrexone and 10-ketooxymorphone.
AID149890	Binding affinity against Delta Opioid receptor in Guinea pig brain membranes using [3H]DAMGO+DADLE	1996	Journal of medicinal chemistry, Apr-26, Volume: 39, Issue:9	Opioid antagonist activity of naltrexone-derived bivalent ligands: importance of a properly oriented molecular scaffold to guide "address" recognition at kappa opioid receptors.
AID1194138	Selectivity ratio of EC50 for mouse DOR to EC50 for mouse MOR	2015	Bioorganic & medicinal chemistry, Apr-15, Volume: 23, Issue:8	Design, syntheses, and pharmacological characterization of 17-cyclopropylmethyl-3,14β-dihydroxy-4,5α-epoxy-6α-(isoquinoline-3'-carboxamido)morphinan analogues as opioid receptor ligands.
AID588219	FDA HLAED, gamma-glutamyl transferase (GGT) increase	2004	Current drug discovery technologies, Dec, Volume: 1, Issue:4	Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID625280	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID603731	Selectivity ratio of Ki for mu opioid receptor in guinea pig forebrain homogenate to Ki for kappa opioid receptor in guinea pig cerebellum homogenate	2011	Bioorganic & medicinal chemistry letters, Jul-01, Volume: 21, Issue:13	Synthesis of new opioid derivatives with a propellane skeleton and their pharmacology: part 1.
AID273130	Displacement of [3H]DAMGO from human recombinant mu opioid receptor expressed in CHO cells	2006	Journal of medicinal chemistry, Oct-05, Volume: 49, Issue:20	Structural determinants of opioid activity in derivatives of 14-aminomorphinones: effects of changes to the chain linking of the C14-amino group to the aryl ring.
AID149934	Opioid receptor delta 1 apparent binding constant from rat brain membranes using [3H]DADLE binding assay	1990	Journal of medicinal chemistry, Sep, Volume: 33, Issue:9	Photoactivatable opiate derivatives as irreversible probes of the mu-opioid receptor.
AID320424	Antagonist activity at mu opioid receptor in Swiss mouse vas deferens assessed as reversal of Sufentanil effect on electrically-induced driven twitch	2008	Bioorganic & medicinal chemistry, Jan-15, Volume: 16, Issue:2	The influence of esters and carboxylic acids as the N-substituent of opioids. Part 1: Benzomorphans.
AID148627	Displacement of [3H]bremazocine from opioid receptor of guinea pig membrane	1991	Journal of medicinal chemistry, Aug, Volume: 34, Issue:8	Electrophilic gamma-lactone kappa-opioid receptor probes. Analogues of 2'-hydroxy-2-tetrahydrofurfuryl-5,9-dimethyl-6,7-benzomorphan diastereomers.
AID274411	Displacement of [3H]diprenorphine from human cloned mu opioid receptor expressed in CHO cells	2006	Journal of medicinal chemistry, Dec-14, Volume: 49, Issue:25	Elucidation of the bioactive conformation of the N-substituted trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidine class of mu-opioid receptor antagonists.
AID152407	Inhibition of [3H]fluadom binding to opioid receptor	1989	Journal of medicinal chemistry, Feb, Volume: 32, Issue:2	Synthesis and biological evaluation of 14-alkoxymorphinans. 2. (-)-N-(cyclopropylmethyl)-4,14-dimethoxymorphinan-6-one, a selective mu opioid receptor antagonist.
AID484374	Displacement of [3H]DAMGO from mu opioid receptor in Hartley guinea pig forebrain by liquid scintillation counting	2010	Bioorganic & medicinal chemistry letters, Jun-15, Volume: 20, Issue:12	Investigation of Beckett-Casy model 2: synthesis of novel 15-16 nornaltrexone derivatives and their pharmacology.
AID149277	Binding affinity was determined in a crude membrane preparation from guinea pig brain by displacement of [3H]U-69593 from Opioid receptor kappa 1	1997	Journal of medicinal chemistry, Feb-28, Volume: 40, Issue:5	(E)- and (Z)-7-arylidenenaltrexones: synthesis and opioid receptor radioligand displacement assays.
AID588214	FDA HLAED, liver enzyme composite activity	2004	Current drug discovery technologies, Dec, Volume: 1, Issue:4	Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID269582	Reversal of stimulation of [35S]GTP-gamma-S binding to human recombinant DOR transfected in CHO cells relative to DPDPE	2006	Journal of medicinal chemistry, Aug-24, Volume: 49, Issue:17	Structural determinants of opioid activity in derivatives of 14-aminomorphinones: effect of substitution in the aromatic ring of cinnamoylaminomorphinones and codeinones.
AID312068	Antagonist activity at mu opioid receptor in NMRI mouse vas deferens assessed as effect on Tyr-(R)-spiro-Aba-Gly-Phe-NH2 induced muscle contraction	2008	Journal of medicinal chemistry, Jan-10, Volume: 51, Issue:1	Endomorphin-2 with a beta-turn backbone constraint retains the potent micro-opioid receptor agonist properties.
AID540213	Half life in human after iv administration	2008	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7	Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID26304	Partition coefficient (logD6.5)	2000	Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13	QSAR model for drug human oral bioavailability.
AID395297	Antagonist activity against delta opioid receptor in mouse vas deferens assessed as effect on DPDPE -induced contraction	2009	Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6	14 beta-O-cinnamoylnaltrexone and related dihydrocodeinones are mu opioid receptor partial agonists with predominant antagonist activity.
AID301036	Displacement of [3H]bremazocine from human delta opioid receptor expressed in CHO cells in presence of high sodium by SPA	2007	Bioorganic & medicinal chemistry letters, Oct-01, Volume: 17, Issue:19	Structure-activity relationship studies of carboxamido-biaryl ethers as opioid receptor antagonists (OpRAs). Part 1.
AID767590	Selectivity ratio of Ki for mouse delta opioid receptor to Ki for mouse mu opioid receptor	2013	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 23, Issue:18	Structure activity relationship studies of 17-cyclopropylmethyl-3,14β-dihydroxy-4,5α-epoxy-6α-(isoquinoline-3'-carboxamido)morphinan (NAQ) analogues as potent opioid receptor ligands: preliminary results on the role of electronic characteristics for affin
AID609328	Antimalarial activity against chloroquine-resistant Plasmodium chabaudi infected in mouse assessed as parasitemia at 10 mg/kg, po administered for 3 consecutive days	2011	Bioorganic & medicinal chemistry letters, Aug-15, Volume: 21, Issue:16	Opioid δ₁ receptor antagonist 7-benzylidenenaltrexone as an effective resistance reverser for chloroquine-resistant Plasmodium chabaudi.
AID228110	Selectivity ratio between kappa to that of mu opioid receptor	1996	Journal of medicinal chemistry, Apr-26, Volume: 39, Issue:9	Opioid antagonist activity of naltrexone-derived bivalent ligands: importance of a properly oriented molecular scaffold to guide "address" recognition at kappa opioid receptors.
AID232233	Selectivity given as ratio of mu receptor to delta receptor	2004	Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6	Identification of opioid ligands possessing mixed micro agonist/delta antagonist activity among pyridomorphinans derived from naloxone, oxymorphone, and hydromorphone [correction of hydropmorphone].
AID148025	Binding affinity against Opioid receptor mu 1 in Guinea pig brain membranes using [3H]DAMGO	1996	Journal of medicinal chemistry, Apr-26, Volume: 39, Issue:9	Opioid antagonist activity of naltrexone-derived bivalent ligands: importance of a properly oriented molecular scaffold to guide "address" recognition at kappa opioid receptors.
AID452922	Displacement of [3H]U69593 from guinea pig cerebellum kappa opioid receptor	2010	Bioorganic & medicinal chemistry letters, Jan-01, Volume: 20, Issue:1	Drug design and synthesis of a novel kappa opioid receptor agonist with an oxabicyclo[2.2.2]octane skeleton and its pharmacology.
AID1054691	Agonist activity at delta opioid receptor (unknown origin) expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrs	2013	Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22	Design, synthesis, and biological evaluation of 14-heteroaromatic-substituted naltrexone derivatives: pharmacological profile switch from mu opioid receptor selectivity to mu/kappa opioid receptor dual selectivity.
AID227058	Competitive inhibition of the DADLE on mouse vas deferens for the opioid receptor delta at 300 nM	1991	Journal of medicinal chemistry, May, Volume: 34, Issue:5	Role of spacer and address components in peptidomimetic delta opioid receptor antagonists related to naltrindole.
AID151148	Inhibition of Mu opioid receptor of mouse vas deferens	2004	Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3	Structure-activity study on the Phe side chain arrangement of endomorphins using conformationally constrained analogues.
AID232529	Effect of protecte expressed as morphine IC50 ratio (IC50 after treatment/control IC50) at 200 nM concentration	1983	Journal of medicinal chemistry, Oct, Volume: 26, Issue:10	Different receptor sites mediate opioid agonism and antagonism.
AID232962	Ke selectivity ratio (kappa/delta) of the compound	1991	Journal of medicinal chemistry, Jun, Volume: 34, Issue:6	An approach to the design of receptor-type-selective non-peptide antagonists of peptidergic receptors: delta opioid antagonists.
AID452923	Displacement of [3H]NTI from guinea pig forebrain delta opioid receptor	2010	Bioorganic & medicinal chemistry letters, Jan-01, Volume: 20, Issue:1	Drug design and synthesis of a novel kappa opioid receptor agonist with an oxabicyclo[2.2.2]octane skeleton and its pharmacology.
AID148970	Ke value was obtained from IC50 ratio values when compared with Opioid receptor kappa 1 agonist in Guinea pig Ileum using U-50488 as radioligand	1996	Journal of medicinal chemistry, Apr-26, Volume: 39, Issue:9	Opioid antagonist activity of naltrexone-derived bivalent ligands: importance of a properly oriented molecular scaffold to guide "address" recognition at kappa opioid receptors.
AID270159	Intrinsic activity at kappa opioid receptor in presence of 1 uM GDP	2006	Journal of medicinal chemistry, Sep-07, Volume: 49, Issue:18	Highly potent and selective phenylmorphan-based inverse agonists of the opioid delta receptor.
AID149283	Compound was evaluated for binding affinity of Opioid receptor kappa 1 in guinea pig brain membranes	1991	Journal of medicinal chemistry, Jun, Volume: 34, Issue:6	An approach to the design of receptor-type-selective non-peptide antagonists of peptidergic receptors: delta opioid antagonists.
AID588212	Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in rodents	2010	Chemical research in toxicology, Jan, Volume: 23, Issue:1	Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID1133436	Binding affinity to pig ileum opioid receptor	1978	Journal of medicinal chemistry, Jan, Volume: 21, Issue:1	Quantum chemical studies of N-substituent variation in the oxymorphone series of opiate narcotics.
AID147987	Displacement of [3H]U-69593 from human recombinant Opioid receptor kappa 1 on CHO cell membranes.	2003	Journal of medicinal chemistry, Apr-10, Volume: 46, Issue:8	14-amino, 14-alkylamino, and 14-acylamino analogs of oxymorphindole. Differential effects on opioid receptor binding and functional profiles.
AID123368	Narcotic antagonistic potency evaluated in morphine-induced Straub tail phenomenon in mice	1981	Journal of medicinal chemistry, Jul, Volume: 24, Issue:7	Allylprodine analogues as receptor probes. Evidence that phenolic and nonphenolic ligands interact with different subsites on identical opioid receptors.
AID603169	Displacement of [125I]-IBNtxA from MOR-1 expressed in CHO cells	2011	Bioorganic & medicinal chemistry letters, Jul-01, Volume: 21, Issue:13	Generation of novel radiolabeled opiates through site-selective iodination.
AID269583	Reversal of stimulation of [35S]GTPgammaS binding to human recombinant KOR transfected in CHO cells relative to U69593	2006	Journal of medicinal chemistry, Aug-24, Volume: 49, Issue:17	Structural determinants of opioid activity in derivatives of 14-aminomorphinones: effect of substitution in the aromatic ring of cinnamoylaminomorphinones and codeinones.
AID1611817	Peripheral selectivity index, ratio of ID50 for inhibition of morphine-induced delays in gastric emptying in ICR mouse to ID50 for inhibition of morphine-induced delays in intestinal transit in ICR mouse	2019	ACS medicinal chemistry letters, Dec-12, Volume: 10, Issue:12	Discovery of Axelopran (TD-1211): A Peripherally Restricted μ-Opioid Receptor Antagonist.
AID151909	Binding affinity for Opioid receptor mu 1 was determined by inhibition of binding of [3H]DAMGO (1.4-3 nM) to rat brain membranes	1999	Journal of medicinal chemistry, Sep-09, Volume: 42, Issue:18	Synthesis, opioid receptor binding, and biological activities of naltrexone-derived pyrido- and pyrimidomorphinans.
AID23449	Partition coefficient (logP)	1982	Journal of medicinal chemistry, Feb, Volume: 25, Issue:2	Common anionic receptor site hypothesis: its relevance to the antagonist action of naloxone.
AID148475	Inhibition of total opioid receptor by displacing 0.5 nM [3H]bremazocine in guinea pig brain membrane	1992	Journal of medicinal chemistry, Nov-27, Volume: 35, Issue:24	O3-(2-carbomethoxyallyl) ethers of opioid ligands derived from oxymorphone, naltrexone, etorphine, diprenorphine, norbinaltorphimine, and naltrindole. Unexpected O3-dealkylation in the opioid radioligand displacement assay.
AID150034	Inhibition of binding of [3H]DADLE to Opioid receptor delta 1 in guinea pig membranes	2003	Journal of medicinal chemistry, May-08, Volume: 46, Issue:10	2002 Medicinal Chemistry Division Award address: monoamine transporters and opioid receptors. Targets for addiction therapy.
AID1191372	Displacement of [3H]U69593 from rat recombinant kappa opioid receptor expressed in CHO cells after 60 mins	2015	European journal of medicinal chemistry, Jan-27, Volume: 90	Novel fluoroalkyl derivatives of selective kappa opioid receptor antagonist JDTic: Design, synthesis, pharmacology and molecular modeling studies.
AID415722	Displacement of [3H]NTI from delta opioid receptor expressed in CHO cells	2009	Bioorganic & medicinal chemistry letters, Mar-15, Volume: 19, Issue:6	14-O-Heterocyclic-substituted naltrexone derivatives as non-peptide mu opioid receptor selective antagonists: design, synthesis, and biological studies.
AID274390	Displacement of [3H]diprenorphine from human cloned mu opioid receptor expressed in CHO cells	2006	Journal of medicinal chemistry, Dec-14, Volume: 49, Issue:25	Synthesis and pharmacological evaluation of novel octahydro-1H-pyrido[1,2-a]pyrazine as mu-opioid receptor antagonists.
AID625286	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1079947	Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID347310	Displacement of [3H]NTI from monocloned delta opioid receptor expressed in CHO cells	2009	Journal of medicinal chemistry, Mar-12, Volume: 52, Issue:5	Design, synthesis, and biological evaluation of 6alpha- and 6beta-N-heterocyclic substituted naltrexamine derivatives as mu opioid receptor selective antagonists.
AID286303	Displacement of [3H]U-69593 from human opioid kappa receptor expressed in CHO cells	2007	Journal of medicinal chemistry, May-03, Volume: 50, Issue:9	Pharmacological properties of bivalent ligands containing butorphan linked to nalbuphine, naltrexone, and naloxone at mu, delta, and kappa opioid receptors.
AID150398	Inhibition of [3H]diprenorphine binding to rat brain membrane opioid receptors;(T= total opioid receptor family)	1990	Journal of medicinal chemistry, Sep, Volume: 33, Issue:9	Photoactivatable opiate derivatives as irreversible probes of the mu-opioid receptor.
AID417156	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	2009	Bioorganic & medicinal chemistry letters, Apr-15, Volume: 19, Issue:8	Syntheses of novel high affinity ligands for opioid receptors.
AID149546	Tested for binding affinity towards kappa receptor in presence of [3H]EKC radioligand	1994	Journal of medicinal chemistry, Jul-22, Volume: 37, Issue:15	Discovery of a potent, peripherally selective trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidine opioid antagonist for the treatment of gastrointestinal motility disorders.
AID149140	Binding affinity against Kappa Opioid receptor in Guinea pig brain membranes using [3H]-DAMGO+EKC	1996	Journal of medicinal chemistry, Apr-26, Volume: 39, Issue:9	Opioid antagonist activity of naltrexone-derived bivalent ligands: importance of a properly oriented molecular scaffold to guide "address" recognition at kappa opioid receptors.
AID1820198	Displacement of [3H]-naloxone from mouse MOR expressed in CHO cells incubated for 1.5 hrs by competitive radioligand binding assay	2021	Journal of medicinal chemistry, 06-10, Volume: 64, Issue:11	Structure-Based Design and Development of Chemical Probes Targeting Putative MOR-CCR5 Heterodimers to Inhibit Opioid Exacerbated HIV-1 Infectivity.
AID348693	Binding affinity to kappa opioid receptor in guinea pig cerebellum	2008	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 18, Issue:18	Synthesis of N-isobutylnoroxymorphone from naltrexone by a selective cyclopropane ring opening reaction.
AID311284	Selectivity for antagonist activity at human delta opioid receptor to kappa opioid receptor expressed in CHO cells by [35S]GTP-gamma-S assay	2007	Journal of natural products, Aug, Volume: 70, Issue:8	Flavonoids as opioid receptor ligands: identification and preliminary structure-activity relationships.
AID588218	FDA HLAED, lactate dehydrogenase (LDH) increase	2004	Current drug discovery technologies, Dec, Volume: 1, Issue:4	Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID348694	Binding affinity to delta opioid receptor in guinea pig forebrain	2008	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 18, Issue:18	Synthesis of N-isobutylnoroxymorphone from naltrexone by a selective cyclopropane ring opening reaction.
AID227076	Kappa opioid activity was evaluated on electrically stimulated guinea pig ileum by using ethylketazocine (EK) as standard.	1996	Journal of medicinal chemistry, Apr-26, Volume: 39, Issue:9	Opioid antagonist activity of naltrexone-derived bivalent ligands: importance of a properly oriented molecular scaffold to guide "address" recognition at kappa opioid receptors.
AID1121819	Antagonist activity at human mu opioid receptor expressed in Gqi5 transfected CHO cells assessed as inhibition of DAMGO-stimulated Ca2+ influx preincubated for 15 mins followed by DAMGO challenge	2013	MedChemComm, May-01, Volume: 4, Issue:5	A Bivalent Ligand Targeting the Putative Mu Opioid Receptor and Chemokine Receptor CCR5 Heterodimers: Binding Affinity versus Functional Activities.
AID148992	inhibition of 1.0 nM [3H]- DAGO binding to guinea pig brain membrane opioid receptor mu	1992	Journal of medicinal chemistry, Jun-26, Volume: 35, Issue:13	Electrophilic opioid ligands. Oxygen tethered alpha-methylene-gamma-lactone, acrylate, isothiocyanate, and epoxide derivatives of 6 beta-naltrexol.
AID320415	Antinociceptive activity in sc dosed mouse by tail flick method	2008	Bioorganic & medicinal chemistry, Jan-15, Volume: 16, Issue:2	The influence of esters and carboxylic acids as the N-substituent of opioids. Part 1: Benzomorphans.
AID148040	Binding affinity was measured by the displacement of [3H]- DAMGO in guinea pig brain membrane of Opioid receptor mu 1	1990	Journal of medicinal chemistry, Jun, Volume: 33, Issue:6	Design of peptidomimetic delta opioid receptor antagonists using the message-address concept.
AID151914	Binding constant for the antagonist state was measured for its ability to displace [3H]naloxone from opioid mu 1 receptor buffered homogenate of rat brain membranes	1988	Journal of medicinal chemistry, Mar, Volume: 31, Issue:3	Structure-activity relationships for drugs binding to the agonist and antagonist states of the primary morphine receptor.
AID23717	Partition coefficient (logP)	1988	Journal of medicinal chemistry, Mar, Volume: 31, Issue:3	Structure-activity relationships for drugs binding to the agonist and antagonist states of the primary morphine receptor.
AID624620	Specific activity of expressed human recombinant UGT2B7H	2000	Annual review of pharmacology and toxicology, , Volume: 40	Human UDP-glucuronosyltransferases: metabolism, expression, and disease.
AID1181420	Antagonist activity at human recombinant mu opioid receptor expressed in CHO cell membranes assessed as inhibition of DAMGO-induced response after 60 mins by [35S]GTPgammaS binding assay	2014	Bioorganic & medicinal chemistry, Aug-01, Volume: 22, Issue:15	Pyrrolo- and pyridomorphinans: non-selective opioid antagonists and delta opioid agonists/mu opioid partial agonists.
AID1054694	Selectivity ratio of Ki for delta opioid receptor (unknown origin) to Ki for mu opioid receptor (unknown origin)	2013	Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22	Design, synthesis, and biological evaluation of 14-heteroaromatic-substituted naltrexone derivatives: pharmacological profile switch from mu opioid receptor selectivity to mu/kappa opioid receptor dual selectivity.
AID148543	Dose ratio due to Antagonist Effect at a concentration of 100 nM by ethylketazocine, Opioid receptor kappa 1 in the guinea pig ileum longitudinal muscle myenteric plexus.	1985	Journal of medicinal chemistry, Jul, Volume: 28, Issue:7	10-Ketonaltrexone and 10-ketooxymorphone.
AID149910	Compound was evaluated for binding affinity at Opioid receptor delta 1 in guinea pig brain membranes	1991	Journal of medicinal chemistry, Jun, Volume: 34, Issue:6	An approach to the design of receptor-type-selective non-peptide antagonists of peptidergic receptors: delta opioid antagonists.
AID417157	Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding relative to basal level	2009	Bioorganic & medicinal chemistry letters, Apr-15, Volume: 19, Issue:8	Syntheses of novel high affinity ligands for opioid receptors.
AID149320	In vito concentration required to displace [3H]cyclofoxy (Kd = 0.8 nM and concentration is 1.3 nM) from mu and kappa2 receptor in rat brain membranes.	1992	Journal of medicinal chemistry, Jul-24, Volume: 35, Issue:15	Probes for narcotic receptor mediated phenomena. 18. Epimeric 6 alpha- and 6 beta-iodo-3,14-dihydroxy-17-(cyclopropylmethyl)-4,5 alpha-epoxymorphinans as potential ligands for opioid receptor single photon emission computed tomography: synthesis, evaluati
AID357091	Antinociceptive effect in NY1DD transgenic mouse assessed as partial agonist response at 8 nmol, icv by heat tail flick test	2007	Proceedings of the National Academy of Sciences of the United States of America, Apr-03, Volume: 104, Issue:14	Naloxone acts as a potent analgesic in transgenic mouse models of sickle cell anemia.
AID303910	Antagonist activity at cloned human delta opioid receptor expressed in CHO cells assessed as inhibition of agonist-stimulated GTPgammaS binding	2007	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24	Structure activity relationship studies of carboxamido-biaryl ethers as opioid receptor antagonists (OpRAs). Part 2.
AID395290	Displacement of [3H]DAMGO from mu opioid receptor in Hartley guinea pig brain membrane	2009	Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6	14 beta-O-cinnamoylnaltrexone and related dihydrocodeinones are mu opioid receptor partial agonists with predominant antagonist activity.
AID617024	Agonist activity against mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding at 100 nM relative to DAMGO	2011	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18	Structure selectivity relationship studies of 17-cyclopropylmethyl-3,14β-dihydroxy-4,5α-epoxy-6β-[(4'-pyridyl)carboxamido]morphinan derivatives toward the development of the mu opioid receptor antagonists.
AID1526731	Substrate activity at human OCT1 expressed in HEK293 cells assessed as increase in compound uptake at 0.05 uM incubated for 2 mins by LC-MS/MS analysis relative to control empty vector transfected cells	2019	Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21	Opioids as Substrates and Inhibitors of the Genetically Highly Variable Organic Cation Transporter OCT1.
AID482930	Solubility in 0.3 M acetate buffer at pH 5	2010	Bioorganic & medicinal chemistry letters, Jun-01, Volume: 20, Issue:11	Novel 3-O-pegylated carboxylate and 3-O-pegylated carbamate prodrugs of naltrexone for microneedle-enhanced transdermal delivery.
AID228107	Selectivity ratio between delta and mu opioid receptor from guinea pig brain membrane	1996	Journal of medicinal chemistry, Apr-26, Volume: 39, Issue:9	Opioid antagonist activity of naltrexone-derived bivalent ligands: importance of a properly oriented molecular scaffold to guide "address" recognition at kappa opioid receptors.
AID450018	Displacement of [3H]U69593 from kappa opioid receptor expressed in HEK293 cells by visible spectrophotometry	2009	Bioorganic & medicinal chemistry, Sep-15, Volume: 17, Issue:18	Synthesis and pharmacological evaluation of 6-naltrexamine analogs for alcohol cessation.
AID149420	In vito concentration required to displace 9 (Kd = 1.6 nM and concentration is 1.8 nM) from opioid receptor kappa 1 in guinea brain membranes.	1992	Journal of medicinal chemistry, Jul-24, Volume: 35, Issue:15	Probes for narcotic receptor mediated phenomena. 18. Epimeric 6 alpha- and 6 beta-iodo-3,14-dihydroxy-17-(cyclopropylmethyl)-4,5 alpha-epoxymorphinans as potential ligands for opioid receptor single photon emission computed tomography: synthesis, evaluati
AID223587	Binding affinity towards kappa-opioid receptor by displacement of [3H]-EKC at from guinea pig cortical tissue	1993	Journal of medicinal chemistry, Oct-01, Volume: 36, Issue:20	Structure-activity relationships of trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidine antagonists for mu- and kappa-opioid receptors.
AID147978	Binding affinity was measured by the displacement of [3H]- EK in guinea pig brain membrane of opioid receptor kappa	1990	Journal of medicinal chemistry, Jun, Volume: 33, Issue:6	Design of peptidomimetic delta opioid receptor antagonists using the message-address concept.
AID540220	Clearance in human after iv administration	2005	Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7	Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure.
AID298653	Antagonist activity at human kappa opioid receptor expressed in CHO cells assessed as effect on 35S]GTPgammaS binding	2007	Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21	Cinnamoyl derivatives of 7alpha-aminomethyl-6,14-endo-ethanotetrahydrothebaine and 7alpha-aminomethyl-6,14-endo-ethanotetrahydrooripavine and related opioid ligands.
AID149748	Inhibitory concentration was determined against delta-opioid receptor using [3H]- DPDPE radioligand	1995	Journal of medicinal chemistry, Feb-03, Volume: 38, Issue:3	Isothiocyanate-substituted benzyl ether opioid receptor ligands derived from 6 beta-naltrexol.
AID150018	Antagonistic activity for Opioid receptor mu 1 in guinea pig ileal longitudinal muscle at 100 nM	1988	Journal of medicinal chemistry, Apr, Volume: 31, Issue:4	Binaltorphimine-related bivalent ligands and their kappa opioid receptor antagonist selectivity.
AID1194125	Stimulation of mouse MOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assay relative to DAMGO	2015	Bioorganic & medicinal chemistry, Apr-15, Volume: 23, Issue:8	Design, syntheses, and pharmacological characterization of 17-cyclopropylmethyl-3,14β-dihydroxy-4,5α-epoxy-6α-(isoquinoline-3'-carboxamido)morphinan analogues as opioid receptor ligands.
AID128214	Narcotic agonistic activity in acetic acid mouse writhing assay after subcutaneous administration of the drug	1981	Journal of medicinal chemistry, Dec, Volume: 24, Issue:12	Analgesic narcotic antagonists. 8. 7 alpha-Alkyl-4,5 alpha-epoxymorphinan-6-ones.
AID588215	FDA HLAED, alkaline phosphatase increase	2004	Current drug discovery technologies, Dec, Volume: 1, Issue:4	Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID1079936	Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source]
AID622101	Displacement of [3H]U69,593 from guinea pig kappa opioid receptor in cerebellum	2011	Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20	Synthesis of novel triplet drugs with 1,3,5-trioxazatriquinane skeletons and their pharmacologies. Part 2: Synthesis of novel triplet drugs with the epoxymethano structure (capped homotriplet).
AID609329	Reversal of chloroquine-resistance in Plasmodium chabaudi infected in mouse at 10 mg/kg, po coadministered with chloroquine 3 mg/kg, iv administered for 3 consecutive days measured on day 4	2011	Bioorganic & medicinal chemistry letters, Aug-15, Volume: 21, Issue:16	Opioid δ₁ receptor antagonist 7-benzylidenenaltrexone as an effective resistance reverser for chloroquine-resistant Plasmodium chabaudi.
AID273133	Selectivity for human mu opioid receptor over delta opioid receptor	2006	Journal of medicinal chemistry, Oct-05, Volume: 49, Issue:20	Structural determinants of opioid activity in derivatives of 14-aminomorphinones: effects of changes to the chain linking of the C14-amino group to the aryl ring.
AID1079931	Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source]
AID1194132	Agonist activity at mouse KOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assay relative to (+/-)-trans-U50488	2015	Bioorganic & medicinal chemistry, Apr-15, Volume: 23, Issue:8	Design, syntheses, and pharmacological characterization of 17-cyclopropylmethyl-3,14β-dihydroxy-4,5α-epoxy-6α-(isoquinoline-3'-carboxamido)morphinan analogues as opioid receptor ligands.
AID149011	Binding affinity was measured by the displacement of [3H]- DAMGO in guinea pig brain membrane of opioid receptor mu	1990	Journal of medicinal chemistry, Jun, Volume: 33, Issue:6	Design of peptidomimetic delta opioid receptor antagonists using the message-address concept.
AID450029	Antagonist activity at mu opioid receptor expressed in HEK293 cells assessed as inhibition of compound 11-induced [35S]GTPgammaS binding	2009	Bioorganic & medicinal chemistry, Sep-15, Volume: 17, Issue:18	Synthesis and pharmacological evaluation of 6-naltrexamine analogs for alcohol cessation.
AID395292	Displacement of [3H]U69,593 from kappa opioid receptor in Hartley guinea pig brain membrane	2009	Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6	14 beta-O-cinnamoylnaltrexone and related dihydrocodeinones are mu opioid receptor partial agonists with predominant antagonist activity.
AID149266	Binding affinity was determined towards opioid receptor kappa 1 using [3H]U-69593 as radioligand	2003	Bioorganic & medicinal chemistry letters, Jun-02, Volume: 13, Issue:11	Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. Part 2: 8-formamidocyclazocine analogues.
AID88604	Increase in the charge carried by choline- induced currents in 68-day-old organotypic hippocampal cultures by naltrexone (0.3 uM)	2004	Bioorganic & medicinal chemistry letters, Apr-19, Volume: 14, Issue:8	Sensitivity of neuronal nicotinic acetylcholine receptors to the opiate antagonists naltrexone and naloxone: receptor blockade and up-regulation.
AID147960	Inhibition of opioid receptor kappa by displacing 0.5 nM [3H]bremazocine in guinea pig brain membrane	1992	Journal of medicinal chemistry, Nov-27, Volume: 35, Issue:24	O3-(2-carbomethoxyallyl) ethers of opioid ligands derived from oxymorphone, naltrexone, etorphine, diprenorphine, norbinaltorphimine, and naltrindole. Unexpected O3-dealkylation in the opioid radioligand displacement assay.
AID148132	Selectivity ratio is IC50 value of opioid receptor kappa to that of opioid receptor delta	1991	Journal of medicinal chemistry, May, Volume: 34, Issue:5	Role of spacer and address components in peptidomimetic delta opioid receptor antagonists related to naltrindole.
AID256843	Inhibition of DAMGO stimulated [35S]GTP-gamma-S binding to cloned human mu opioid receptor	2005	Journal of medicinal chemistry, Dec-29, Volume: 48, Issue:26	N-substituted cis-4a-(3-hydroxyphenyl)-8a-methyloctahydroisoquinolines are opioid receptor pure antagonists.
AID148289	Dose ratio due to Antagonist Effect at a concentration of 100 nM by ethylketazocine, Opioid receptor kappa 1 in mouse vas deferens.	1985	Journal of medicinal chemistry, Jul, Volume: 28, Issue:7	10-Ketonaltrexone and 10-ketooxymorphone.
AID224587	Binding affinity towards mu-opioid receptor by the displacement of [3H]Nal in rat brain homogenates	1993	Journal of medicinal chemistry, Oct-01, Volume: 36, Issue:20	3,4-Dimethyl-4-(3-hydroxyphenyl)piperidines: opioid antagonists with potent anorectant activity.
AID286302	Displacement of [3H]DAMGO from human opioid gamma receptor expressed in CHO cells	2007	Journal of medicinal chemistry, May-03, Volume: 50, Issue:9	Pharmacological properties of bivalent ligands containing butorphan linked to nalbuphine, naltrexone, and naloxone at mu, delta, and kappa opioid receptors.
AID273150	Selectivity for guinea pig mu opioid receptor over kappa opioid receptor	2006	Journal of medicinal chemistry, Oct-05, Volume: 49, Issue:20	Structural determinants of opioid activity in derivatives of 14-aminomorphinones: effects of changes to the chain linking of the C14-amino group to the aryl ring.
AID128019	Inhibition of acetic acid induced mouse writhing assay following s.c. administration.	1981	Journal of medicinal chemistry, Dec, Volume: 24, Issue:12	Analgesic narcotic antagonists. 9. 6-Methylene-8 beta-alkyl-N-(cycloalkylmethyl)-3-hydroxy- or -methoxymorphinans.
AID148961	Compound was evaluated for antagonist potency in guinea pig ileum preparation using ethylketazocine (Opioid receptor kappa 1)	1991	Journal of medicinal chemistry, Jun, Volume: 34, Issue:6	An approach to the design of receptor-type-selective non-peptide antagonists of peptidergic receptors: delta opioid antagonists.
AID1749823	Antinociceptive activity in iv dosed Sprague-Dawley rat assessed as hot plate latency compound administered as cumulative dose at 5 mins intervals in presence of naltrexone by Hot-plate test
AID286313	Agonist activity at human opioid gamma receptor expressed in CHO cells assessed as maximal inhibition of DAGO-stimulated [35S]GTP-gamma-S binding	2007	Journal of medicinal chemistry, May-03, Volume: 50, Issue:9	Pharmacological properties of bivalent ligands containing butorphan linked to nalbuphine, naltrexone, and naloxone at mu, delta, and kappa opioid receptors.
AID176828	Tested for concentration required to reduce the food consumption by 20 % subcutaneously; The maximum effect achievedwas approximately 20% and not dose related	1993	Journal of medicinal chemistry, Oct-01, Volume: 36, Issue:20	3,4-Dimethyl-4-(3-hydroxyphenyl)piperidines: opioid antagonists with potent anorectant activity.
AID416816	Selectivity ratio of IC50 for human delta opioid receptor to IC50 for human mu opioid receptor	2009	Bioorganic & medicinal chemistry letters, Apr-15, Volume: 19, Issue:8	Syntheses of novel high affinity ligands for opioid receptors.
AID1181416	Displacement of [3H]Cl-DPDPE from human recombinant delta opioid receptor expressed in CHO cell membranes after 60 mins by scintillation counting method	2014	Bioorganic & medicinal chemistry, Aug-01, Volume: 22, Issue:15	Pyrrolo- and pyridomorphinans: non-selective opioid antagonists and delta opioid agonists/mu opioid partial agonists.
AID274412	Displacement of [3H]diprenorphine from human cloned kappa opioid receptor expressed in CHO cells	2006	Journal of medicinal chemistry, Dec-14, Volume: 49, Issue:25	Elucidation of the bioactive conformation of the N-substituted trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidine class of mu-opioid receptor antagonists.
AID767588	Agonist activity at mouse mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrs relative to DAMGO	2013	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 23, Issue:18	Structure activity relationship studies of 17-cyclopropylmethyl-3,14β-dihydroxy-4,5α-epoxy-6α-(isoquinoline-3'-carboxamido)morphinan (NAQ) analogues as potent opioid receptor ligands: preliminary results on the role of electronic characteristics for affin
AID540209	Volume of distribution at steady state in human after iv administration	2008	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7	Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID148494	The IC50 value of agonist (ethylketazocine) in presence of antagonist (Compound 20 nM) divided by the control IC60 value with no antagonist in GPI (Guinea pig ileum)	1987	Journal of medicinal chemistry, Feb, Volume: 30, Issue:2	Bimorphinans as highly selective, potent kappa opioid receptor antagonists.
AID756074	Agonist activity at mu opioid receptor (unknown origin) expressed CHO cells assessed as stimulation of [35S]-GTP[gammaS] binding relative to DAMGO	2013	Bioorganic & medicinal chemistry letters, Jul-01, Volume: 23, Issue:13	Opioid receptor selectivity profile change via isosterism for 14-O-substituted naltrexone derivatives.
AID286314	Agonist activity at human opioid gamma receptor expressed in CHO cells assessed as inhibition of DAGO-stimulated [35S]GTPgammaS binding	2007	Journal of medicinal chemistry, May-03, Volume: 50, Issue:9	Pharmacological properties of bivalent ligands containing butorphan linked to nalbuphine, naltrexone, and naloxone at mu, delta, and kappa opioid receptors.
AID227052	Competitive inhibition of Morphine on Guinea pig ileal longitudinal muscle for the opioid receptor mu at 100 nM	1991	Journal of medicinal chemistry, May, Volume: 34, Issue:5	Role of spacer and address components in peptidomimetic delta opioid receptor antagonists related to naltrindole.
AID311281	Antagonist activity at human mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S assay	2007	Journal of natural products, Aug, Volume: 70, Issue:8	Flavonoids as opioid receptor ligands: identification and preliminary structure-activity relationships.
AID756075	Agonist activity at mu opioid receptor (unknown origin) expressed CHO cells assessed as stimulation of [35S]-GTP[gammaS] binding	2013	Bioorganic & medicinal chemistry letters, Jul-01, Volume: 23, Issue:13	Opioid receptor selectivity profile change via isosterism for 14-O-substituted naltrexone derivatives.
AID141506	Binding affinity was determined against Mu opioid receptor using [3H]naltrexone as radioligand	1998	Bioorganic & medicinal chemistry letters, Nov-17, Volume: 8, Issue:22	N-substituted octahydro-4a-(3-hydroxyphenyl)-10a-methyl-benzo[g]isoquinolines are opioid receptor pure antagonists.
AID1181415	Displacement of [3H]U69593 from human recombinant kappa opioid receptor expressed in CHO cell membranes after 60 mins by scintillation counting method	2014	Bioorganic & medicinal chemistry, Aug-01, Volume: 22, Issue:15	Pyrrolo- and pyridomorphinans: non-selective opioid antagonists and delta opioid agonists/mu opioid partial agonists.
AID1133438	Binding affinity to rat brain opioid receptor	1978	Journal of medicinal chemistry, Jan, Volume: 21, Issue:1	Quantum chemical studies of N-substituent variation in the oxymorphone series of opiate narcotics.
AID415719	Selectivity ratio of Ki for kappa opioid receptor to Ki for mu opioid receptor	2009	Bioorganic & medicinal chemistry letters, Mar-15, Volume: 19, Issue:6	14-O-Heterocyclic-substituted naltrexone derivatives as non-peptide mu opioid receptor selective antagonists: design, synthesis, and biological studies.
AID238974	Binding affinity against Opioid receptor mu 1 expressed in CHO cells using [3H]DAMGO as radioligand	2005	Bioorganic & medicinal chemistry letters, Apr-15, Volume: 15, Issue:8	Synthesis and opioid receptor binding properties of a highly potent 4-hydroxy analogue of naltrexone.
AID149124	Binding affinity at Opioid receptor kappa 1 by displacement of [3H]U-69593 in guinea pig brain membranes	2004	Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6	Identification of opioid ligands possessing mixed micro agonist/delta antagonist activity among pyridomorphinans derived from naloxone, oxymorphone, and hydromorphone [correction of hydropmorphone].
AID540212	Mean residence time in human after iv administration	2008	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7	Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID152204	Binding affinity against Opioid receptor mu 1 using [3H]naloxone as radioligand.	1998	Journal of medicinal chemistry, Oct-08, Volume: 41, Issue:21	N-Substituted 9beta-methyl-5-(3-hydroxyphenyl)morphans are opioid receptor pure antagonists.
AID148693	Opioid receptor kappa 1 antagonistic activity was measured by the displacement of ethylketazocine in the guinea pig ileum at a concentration of 100 nM	1990	Journal of medicinal chemistry, Jun, Volume: 33, Issue:6	Design of peptidomimetic delta opioid receptor antagonists using the message-address concept.
AID151597	Binding activity against Opioid receptor mu 1 using [3H]DAMGO as radioligand in rat brain membranes.	1998	Journal of medicinal chemistry, Oct-08, Volume: 41, Issue:21	N-Substituted 9beta-methyl-5-(3-hydroxyphenyl)morphans are opioid receptor pure antagonists.
AID1133437	Agonist activity at pig ileum opioid receptor	1978	Journal of medicinal chemistry, Jan, Volume: 21, Issue:1	Quantum chemical studies of N-substituent variation in the oxymorphone series of opiate narcotics.
AID148119	Selectivity ratio is Ki value of opioid receptor kappa to that of opioid receptor delta	1991	Journal of medicinal chemistry, May, Volume: 34, Issue:5	Role of spacer and address components in peptidomimetic delta opioid receptor antagonists related to naltrindole.
AID286309	Antagonist activity at human opioid kappa receptor expressed in CHO cells assessed as maximal inhibition of U-50488-stimulated [35S]GTP-gamma-S binding	2007	Journal of medicinal chemistry, May-03, Volume: 50, Issue:9	Pharmacological properties of bivalent ligands containing butorphan linked to nalbuphine, naltrexone, and naloxone at mu, delta, and kappa opioid receptors.
AID1447100	Displacement of [3H]DAMGO from mu opioid receptor in guinea pig brain membrane	2017	Bioorganic & medicinal chemistry letters, 05-01, Volume: 27, Issue:9	Synthesis and evaluation of a ligand targeting the μ and δ opioid receptors for drug delivery to lung cancer.
AID273146	Activity at human recombinant kappa opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding relative to U69593	2006	Journal of medicinal chemistry, Oct-05, Volume: 49, Issue:20	Structural determinants of opioid activity in derivatives of 14-aminomorphinones: effects of changes to the chain linking of the C14-amino group to the aryl ring.
AID311524	Oral bioavailability in human	2007	Bioorganic & medicinal chemistry, Dec-15, Volume: 15, Issue:24	Hologram QSAR model for the prediction of human oral bioavailability.
AID141511	Compound was tested for the inhibition of [35S]GTP-gamma-S, binding in Guinea pig Caudate stimulated by the opioid receptor agonist Mu-DAMGO	1998	Bioorganic & medicinal chemistry letters, Nov-17, Volume: 8, Issue:22	N-substituted octahydro-4a-(3-hydroxyphenyl)-10a-methyl-benzo[g]isoquinolines are opioid receptor pure antagonists.
AID417162	Antagonist activity against human mu opioid receptor expressed in CHO cells assessed as inhibition of DAMGO-stimulated [35S]GTPgammaS binding	2009	Bioorganic & medicinal chemistry letters, Apr-15, Volume: 19, Issue:8	Syntheses of novel high affinity ligands for opioid receptors.
AID42547	Increase in the charge carried by ACh- induced currents in CA1 pyramidal neurons of 2022-day-old cultures by naltrexone (0.3 uM)	2004	Bioorganic & medicinal chemistry letters, Apr-19, Volume: 14, Issue:8	Sensitivity of neuronal nicotinic acetylcholine receptors to the opiate antagonists naltrexone and naloxone: receptor blockade and up-regulation.
AID692550	Displacement of [3H]-DAMGO from mouse MOR expressed in HEK293 cells	2012	ACS medicinal chemistry letters, Aug-09, Volume: 3, Issue:8	Tuned-Affinity Bivalent Ligands for the Characterization of Opioid Receptor Heteromers.
AID416815	Displacement of [3H]U69,593 from human kappa opioid receptor expressed in CHO cells after 60 mins by scintillation counting	2009	Bioorganic & medicinal chemistry letters, Apr-15, Volume: 19, Issue:8	Syntheses of novel high affinity ligands for opioid receptors.
AID232429	Ratio of inhibition of binding to opioid receptor in the presence and absence of NaCl	1989	Journal of medicinal chemistry, Feb, Volume: 32, Issue:2	Synthesis and biological evaluation of 14-alkoxymorphinans. 2. (-)-N-(cyclopropylmethyl)-4,14-dimethoxymorphinan-6-one, a selective mu opioid receptor antagonist.
AID149760	Inhibition of [35S]GTP-gamma-S, binding in guines pig caudate stimulated by SNC-80 for Opioid receptor delta 1	2003	Journal of medicinal chemistry, May-08, Volume: 46, Issue:10	2002 Medicinal Chemistry Division Award address: monoamine transporters and opioid receptors. Targets for addiction therapy.
AID679758	TP_TRANSPORTER: increase in Calcein-AM intracellular accumulation (Calcein-AM: ? uM, Naltrexone: 100 uM) in MDR1-expressing MDCKII cells	2002	The Journal of pharmacology and experimental therapeutics, Dec, Volume: 303, Issue:3	Passive permeability and P-glycoprotein-mediated efflux differentiate central nervous system (CNS) and non-CNS marketed drugs.
AID624613	Specific activity of expressed human recombinant UGT1A10	2000	Annual review of pharmacology and toxicology, , Volume: 40	Human UDP-glucuronosyltransferases: metabolism, expression, and disease.
AID22293	Delta logD (logD6.5 - logD7.4)	2000	Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13	QSAR model for drug human oral bioavailability.
AID149550	Binding affinity for Opioid receptor kappa 1 was determined by inhibition of binding of [3H]U-69593 (1.2-2.2 nM) to guinea pig brain membranes	1999	Journal of medicinal chemistry, Sep-09, Volume: 42, Issue:18	Synthesis, opioid receptor binding, and biological activities of naltrexone-derived pyrido- and pyrimidomorphinans.
AID540211	Fraction unbound in human after iv administration	2008	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7	Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID233909	Selectivity ratio measured in terms of delta opioid receptor to the mu opioid receptor	1997	Journal of medicinal chemistry, Feb-28, Volume: 40, Issue:5	(E)- and (Z)-7-arylidenenaltrexones: synthesis and opioid receptor radioligand displacement assays.
AID1135662	Displacement of [3H]naloxone from opioid receptor (unknown origin) in brain homogenate measured after four washes	1978	Journal of medicinal chemistry, Jul, Volume: 21, Issue:7	6beta-[N,N-Bis(2-chloroethyl)amino]-17-(cyclopropylmethyl)-4,5alpha-epoxy-3,14-dihydroxymorphinan(chlornaltrexamine) a potent opioid receptor alkylating agent with ultralong narcotic antagonist actitivty.
AID1268024	Displacement of 2-((1E,3E,5E)-5-(1-Ethyl-3,3-dimethyl-5-sulfoindolin-2-ylidene)-penta-1,3-dien-1-yl)-1-(6-((6-((6S,7R,7aR,12bS)-9-hydroxy-7-methoxy-3-methyl-1,2,3,4,5,6,7,7a-octahydro-4a,7-ethano-4,12-methanobenzofuro[3,2-e]isoquinoline-6-carboxamido)hexy	2015	Journal of medicinal chemistry, Dec-24, Volume: 58, Issue:24	Synthesis, Biological Evaluation, and Utility of Fluorescent Ligands Targeting the μ-Opioid Receptor.
AID1181424	Agonist activity at human recombinant delta opioid receptor expressed in CHO cell membranes after 60 mins by [35S]GTPgammaS binding assay	2014	Bioorganic & medicinal chemistry, Aug-01, Volume: 22, Issue:15	Pyrrolo- and pyridomorphinans: non-selective opioid antagonists and delta opioid agonists/mu opioid partial agonists.
AID239386	Inhibition of [3H]U-69593 binding to human kappa opioid receptor expressed in CHO cells	2004	Journal of medicinal chemistry, Oct-07, Volume: 47, Issue:21	Identification of a new scaffold for opioid receptor antagonism based on the 2-amino-1,1-dimethyl-7-hydroxytetralin pharmacophore.
AID320425	Antagonist activity at kappa opioid receptor in Swiss mouse vas deferens assessed as reversal of U50488 effect on electrically-induced driven twitch	2008	Bioorganic & medicinal chemistry, Jan-15, Volume: 16, Issue:2	The influence of esters and carboxylic acids as the N-substituent of opioids. Part 1: Benzomorphans.
AID452924	Displacement of [3H]DAMGO from guinea pig forebrain mu opioid receptor	2010	Bioorganic & medicinal chemistry letters, Jan-01, Volume: 20, Issue:1	Drug design and synthesis of a novel kappa opioid receptor agonist with an oxabicyclo[2.2.2]octane skeleton and its pharmacology.
AID149795	Binding affinity was determined as ability to displace [3H]DADLE radioligand from Opioid receptor delta 1	1998	Bioorganic & medicinal chemistry letters, Nov-17, Volume: 8, Issue:22	N-substituted octahydro-4a-(3-hydroxyphenyl)-10a-methyl-benzo[g]isoquinolines are opioid receptor pure antagonists.
AID1726170	Antiviral activity against HIV1 3B infected in human TZM-bl cells assessed as reduction in viral entry by measuring Tat protein level at 1500 nM measured after 3 days in presence of IT1T and morphine by luciferase-based assay	2020	ACS medicinal chemistry letters, Nov-12, Volume: 11, Issue:11	Bivalent Ligand Aiming Putative Mu Opioid Receptor and Chemokine Receptor CXCR4 Dimers in Opioid Enhanced HIV-1 Entry.
AID146643	Blockage of Nicotinic acetylcholine receptor alpha4-beta2 noncompetitively in acute hippocampal slices	2004	Bioorganic & medicinal chemistry letters, Apr-19, Volume: 14, Issue:8	Sensitivity of neuronal nicotinic acetylcholine receptors to the opiate antagonists naltrexone and naloxone: receptor blockade and up-regulation.
AID149863	Inhibitory concentration was determined against Opioid receptor mu 1 using [3H]- DAMGO radioligand	1995	Journal of medicinal chemistry, Feb-03, Volume: 38, Issue:3	Isothiocyanate-substituted benzyl ether opioid receptor ligands derived from 6 beta-naltrexol.
AID229803	Ratio of Ki for delta receptor to that of kappa receptor	1998	Journal of medicinal chemistry, Dec-17, Volume: 41, Issue:26	Identification of an opioid kappa receptor subtype-selective N-substituent for (+)-(3R,4R)-dimethyl-4-(3-hydroxyphenyl)piperidine.
AID150032	Inhibition of [35S]GTP-gamma-S, binding in guinea pig caudate stimulated by SNC80 (Opioid receptor delta 1)	1998	Journal of medicinal chemistry, Oct-08, Volume: 41, Issue:21	N-Substituted 9beta-methyl-5-(3-hydroxyphenyl)morphans are opioid receptor pure antagonists.
AID148330	Percent stimulation of [35S]GTP-gamma-S, binding in recombinant human Opioid receptor mu 1 transfected into CHO cells	2003	Journal of medicinal chemistry, Apr-10, Volume: 46, Issue:8	14-amino, 14-alkylamino, and 14-acylamino analogs of oxymorphindole. Differential effects on opioid receptor binding and functional profiles.
AID148739	Binding affinity against Opioid receptor kappa 1 using [3H]ethylketocyclazocine as radioligand.	1998	Journal of medicinal chemistry, Oct-08, Volume: 41, Issue:21	N-Substituted 9beta-methyl-5-(3-hydroxyphenyl)morphans are opioid receptor pure antagonists.
AID148933	Ke value is obtained from IC50 ratio value when compared with delta opioid agonist in MVD preparations using DADLE as radioligand	1996	Journal of medicinal chemistry, Apr-26, Volume: 39, Issue:9	Opioid antagonist activity of naltrexone-derived bivalent ligands: importance of a properly oriented molecular scaffold to guide "address" recognition at kappa opioid receptors.
AID311283	Selectivity for antagonist activity at human mu opioid receptor to kappa opioid receptor expressed in CHO cells by [35S]GTP-gamma-S assay	2007	Journal of natural products, Aug, Volume: 70, Issue:8	Flavonoids as opioid receptor ligands: identification and preliminary structure-activity relationships.
AID767592	Displacement of [3H]-naltrindole from mouse delta opioid receptor expressed in CHO cells after 1.5 hrs	2013	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 23, Issue:18	Structure activity relationship studies of 17-cyclopropylmethyl-3,14β-dihydroxy-4,5α-epoxy-6α-(isoquinoline-3'-carboxamido)morphinan (NAQ) analogues as potent opioid receptor ligands: preliminary results on the role of electronic characteristics for affin
AID317855	Displacement of [3H]U69593 from human kappa opioid receptor expressed in CHO cells	2008	Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6	Synthesis and biological evaluation of alpha- and beta-6-amido derivatives of 17-cyclopropylmethyl-3, 14beta-dihydroxy-4, 5alpha-epoxymorphinan: potential alcohol-cessation agents.
AID410719	Displacement of [3H]Naltrindole form human delta opioid receptor expressed in CHO cells	2009	Bioorganic & medicinal chemistry letters, Jan-01, Volume: 19, Issue:1	Syntheses and opioid receptor binding properties of carboxamido-substituted opioids.
AID147908	Binding affinity determined on Opioid receptor mu 1 in Guinea pig brain membranes using radioligand [3H]DAMGO	1998	Journal of medicinal chemistry, Dec-17, Volume: 41, Issue:26	Identification of an opioid kappa receptor subtype-selective N-substituent for (+)-(3R,4R)-dimethyl-4-(3-hydroxyphenyl)piperidine.
AID141762	Tested for binding affinity towards mu receptor in presence of [3H]NAL radioligand	1994	Journal of medicinal chemistry, Jul-22, Volume: 37, Issue:15	Discovery of a potent, peripherally selective trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidine opioid antagonist for the treatment of gastrointestinal motility disorders.
AID286306	Ratio of Ki for human opioid kappa receptor to Ki for human opioid delta receptor	2007	Journal of medicinal chemistry, May-03, Volume: 50, Issue:9	Pharmacological properties of bivalent ligands containing butorphan linked to nalbuphine, naltrexone, and naloxone at mu, delta, and kappa opioid receptors.
AID624616	Specific activity of expressed human recombinant UGT2B15	2000	Annual review of pharmacology and toxicology, , Volume: 40	Human UDP-glucuronosyltransferases: metabolism, expression, and disease.
AID147958	Displacement of 0.5 nM [3H]bremazocine from guinea pig brain membrane opioid receptor kappa with 100 nM DAGO and 100 nM DPDPE	1992	Journal of medicinal chemistry, Jun-26, Volume: 35, Issue:13	Electrophilic opioid ligands. Oxygen tethered alpha-methylene-gamma-lactone, acrylate, isothiocyanate, and epoxide derivatives of 6 beta-naltrexol.
AID149262	Binding affinity towards guinea pig Opioid receptor kappa 1 using radioligand [3H]U-69593	2001	Bioorganic & medicinal chemistry letters, Jul-09, Volume: 11, Issue:13	3-Carboxamido analogues of morphine and naltrexone. synthesis and opioid receptor binding properties.
AID301032	Antagonist activity at human kappa opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay	2007	Bioorganic & medicinal chemistry letters, Oct-01, Volume: 17, Issue:19	Structure-activity relationship studies of carboxamido-biaryl ethers as opioid receptor antagonists (OpRAs). Part 1.
AID588210	Human drug-induced liver injury (DILI) modelling dataset from Ekins et al	2010	Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 38, Issue:12	A predictive ligand-based Bayesian model for human drug-induced liver injury.
AID227059	Delta opioid activity on Mouse vas deference using DADLE as standard	1996	Journal of medicinal chemistry, Apr-26, Volume: 39, Issue:9	Opioid antagonist activity of naltrexone-derived bivalent ligands: importance of a properly oriented molecular scaffold to guide "address" recognition at kappa opioid receptors.
AID417159	Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding relative to basal level	2009	Bioorganic & medicinal chemistry letters, Apr-15, Volume: 19, Issue:8	Syntheses of novel high affinity ligands for opioid receptors.
AID256845	Inhibition of U69,593 stimulated [35S]GTP-gamma-S binding to cloned human kappa opioid receptor	2005	Journal of medicinal chemistry, Dec-29, Volume: 48, Issue:26	N-substituted cis-4a-(3-hydroxyphenyl)-8a-methyloctahydroisoquinolines are opioid receptor pure antagonists.
AID1268040	Displacement of [3H]DAMGO from human MOR expressed in HEK293 cells preincubated for 1 hr followed by radioligand addition measured after 1 hr by liquid scintillation counting analysis	2015	Journal of medicinal chemistry, Dec-24, Volume: 58, Issue:24	Synthesis, Biological Evaluation, and Utility of Fluorescent Ligands Targeting the μ-Opioid Receptor.
AID150033	Inhibition of [35S]GTP-gamma-S, binding from Opioid receptor delta 1 in Guinea pig Caudate stimulated by SNC80	1998	Journal of medicinal chemistry, Dec-17, Volume: 41, Issue:26	Identification of an opioid kappa receptor subtype-selective N-substituent for (+)-(3R,4R)-dimethyl-4-(3-hydroxyphenyl)piperidine.
AID395294	Displacement of [3H]DPDPE from human delta opioid receptor expressed in CHO cells	2009	Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6	14 beta-O-cinnamoylnaltrexone and related dihydrocodeinones are mu opioid receptor partial agonists with predominant antagonist activity.
AID1054687	Selectivity ratio of Ki for kappa opioid receptor (unknown origin) to Ki for mu opioid receptor (unknown origin)	2013	Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22	Design, synthesis, and biological evaluation of 14-heteroaromatic-substituted naltrexone derivatives: pharmacological profile switch from mu opioid receptor selectivity to mu/kappa opioid receptor dual selectivity.
AID148748	In vito concentration required to displace [3H]BRM (Kd = 1.0 nM and concentration is 1.8 nM) from opioid receptor kappa 2 in guinea brain membranes.	1992	Journal of medicinal chemistry, Jul-24, Volume: 35, Issue:15	Probes for narcotic receptor mediated phenomena. 18. Epimeric 6 alpha- and 6 beta-iodo-3,14-dihydroxy-17-(cyclopropylmethyl)-4,5 alpha-epoxymorphinans as potential ligands for opioid receptor single photon emission computed tomography: synthesis, evaluati
AID231888	Compound was tested for ability to protect against the irreversible antagonism of morphine''s effects by beta-FNA in guinea pig ileum at 2 nM concentration	1983	Journal of medicinal chemistry, Oct, Volume: 26, Issue:10	Different receptor sites mediate opioid agonism and antagonism.
AID1054693	Agonist activity at mu opioid receptor (unknown origin) expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrs relative to DAMGO	2013	Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22	Design, synthesis, and biological evaluation of 14-heteroaromatic-substituted naltrexone derivatives: pharmacological profile switch from mu opioid receptor selectivity to mu/kappa opioid receptor dual selectivity.
AID149214	Antagonistic potency at opioid receptor delta (300 nM) (Ke =IC50 in the presence of antagonist divided by the control IC50 value)	1991	Journal of medicinal chemistry, May, Volume: 34, Issue:5	Role of spacer and address components in peptidomimetic delta opioid receptor antagonists related to naltrindole.
AID625281	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID311282	Antagonist activity at human delta opioid receptor expressed in CHO cells by [35S]GTPgammaS assay	2007	Journal of natural products, Aug, Volume: 70, Issue:8	Flavonoids as opioid receptor ligands: identification and preliminary structure-activity relationships.
AID149041	Inhibition of [3H]naloxone binding to opioid receptor in presence of NaCl	1989	Journal of medicinal chemistry, Feb, Volume: 32, Issue:2	Synthesis and biological evaluation of 14-alkoxymorphinans. 2. (-)-N-(cyclopropylmethyl)-4,14-dimethoxymorphinan-6-one, a selective mu opioid receptor antagonist.
AID270158	Intrinsic activity at mu opioid receptor in presence of 1 uM GDP	2006	Journal of medicinal chemistry, Sep-07, Volume: 49, Issue:18	Highly potent and selective phenylmorphan-based inverse agonists of the opioid delta receptor.
AID1194142	Antagonist activity at human MOR expressed in CHO cells assessed as inhibition of DAMGO-induced increase in intracellular Ca2+ level incubated for 15 mins prior to DAMGO addition by microplate reader analysis	2015	Bioorganic & medicinal chemistry, Apr-15, Volume: 23, Issue:8	Design, syntheses, and pharmacological characterization of 17-cyclopropylmethyl-3,14β-dihydroxy-4,5α-epoxy-6α-(isoquinoline-3'-carboxamido)morphinan analogues as opioid receptor ligands.
AID274417	Antagonist activity against human cloned mu opioid receptor expressed in CHO cells assessed as inhibition of loperamide-stimulated [35S]GTP-gamma-S binding	2006	Journal of medicinal chemistry, Dec-14, Volume: 49, Issue:25	Elucidation of the bioactive conformation of the N-substituted trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidine class of mu-opioid receptor antagonists.
AID1079943	Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID230901	Ratio of antagonistic activity at delta to kappa receptor	1988	Journal of medicinal chemistry, Jul, Volume: 31, Issue:7	Only one pharmacophore is required for the kappa opioid antagonist selectivity of norbinaltorphimine.
AID149279	Binding affinity was measured by the displacement of [3H]- EK in guinea pig brain membrane of Opioid receptor kappa 1	1990	Journal of medicinal chemistry, Jun, Volume: 33, Issue:6	Design of peptidomimetic delta opioid receptor antagonists using the message-address concept.
AID624608	Specific activity of expressed human recombinant UGT1A4	2000	Annual review of pharmacology and toxicology, , Volume: 40	Human UDP-glucuronosyltransferases: metabolism, expression, and disease.
AID1133442	Narcotic antagonist activity in sc dosed mouse assessed as inhibition of oxymorphone-induced nacrosis	1978	Journal of medicinal chemistry, Jan, Volume: 21, Issue:1	Quantum chemical studies of N-substituent variation in the oxymorphone series of opiate narcotics.
AID354073	Displacement of [3H]U69593 from kappa opioid receptor in guinea pig cerebellum	2009	Bioorganic & medicinal chemistry letters, May-01, Volume: 19, Issue:9	Synthesis of a new opioid ligand having the oxabicyclo[3.2.1]octane skeleton using a new rearrangement reaction.
AID169598	Antagonistic potency of compound after oral administration in rats	1982	Journal of medicinal chemistry, Feb, Volume: 25, Issue:2	Common anionic receptor site hypothesis: its relevance to the antagonist action of naloxone.
AID1447101	Displacement of [3H]DADLE from delta opioid receptor in guinea pig brain membrane	2017	Bioorganic & medicinal chemistry letters, 05-01, Volume: 27, Issue:9	Synthesis and evaluation of a ligand targeting the μ and δ opioid receptors for drug delivery to lung cancer.
AID150852	Binding affinity for human Opioid receptor mu 1 transfected into chinese hamster ovary cells by displacing [3H]DAMGO radioligand	2003	Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14	Opioid binding and in vitro profiles of a series of 4-hdroxy-3-methoxyindolomorphinans. Transformation of a delta-selective ligand into a high affinity kappa-selective ligand by introduction of a 5,14-substituted bridge.
AID395296	Antagonist activity against mu opioid receptor in mouse vas deferens assessed as effect on DAMGO-induced contraction	2009	Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6	14 beta-O-cinnamoylnaltrexone and related dihydrocodeinones are mu opioid receptor partial agonists with predominant antagonist activity.
AID450020	Selectivity ratio of Ki for kappa opioid receptor to Ki for mu opioid receptor	2009	Bioorganic & medicinal chemistry, Sep-15, Volume: 17, Issue:18	Synthesis and pharmacological evaluation of 6-naltrexamine analogs for alcohol cessation.
AID149300	In vito concentration required to displace [3H]DAGO (Kd = 0.7 nM and concentration is 1.7 nM) from opioid receptor mu in rat brain membranes.	1992	Journal of medicinal chemistry, Jul-24, Volume: 35, Issue:15	Probes for narcotic receptor mediated phenomena. 18. Epimeric 6 alpha- and 6 beta-iodo-3,14-dihydroxy-17-(cyclopropylmethyl)-4,5 alpha-epoxymorphinans as potential ligands for opioid receptor single photon emission computed tomography: synthesis, evaluati
AID301035	Displacement of [3H]diprenorphine from human kappa opioid receptor expressed in CHO cells in presence of high sodium by SPA	2007	Bioorganic & medicinal chemistry letters, Oct-01, Volume: 17, Issue:19	Structure-activity relationship studies of carboxamido-biaryl ethers as opioid receptor antagonists (OpRAs). Part 1.
AID1461674	Antagonist activity at OGFR in human SKOV3 cells assessed as cell growth inhibition at 10 uM treated as pulsed dose of 6 hrs every other day by hemacytometric method	2017	Bioorganic & medicinal chemistry, 08-15, Volume: 25, Issue:16	Selective opioid growth factor receptor antagonists based on a stilbene isostere.
AID1191374	Displacement of [3H]DADLE from human recombinant delta opioid receptor expressed in HEK cells after 60 mins	2015	European journal of medicinal chemistry, Jan-27, Volume: 90	Novel fluoroalkyl derivatives of selective kappa opioid receptor antagonist JDTic: Design, synthesis, pharmacology and molecular modeling studies.
AID148389	Antagonistic activity for Opioid receptor delta 1 in mouse vas deferens preparation at 100 nM	1988	Journal of medicinal chemistry, Apr, Volume: 31, Issue:4	Binaltorphimine-related bivalent ligands and their kappa opioid receptor antagonist selectivity.
AID149202	Compound was evaluated for the binding affinity to opioid receptor delta using [3H]DADLE as radioligand in guinea pig brain membrane	1991	Journal of medicinal chemistry, May, Volume: 34, Issue:5	Role of spacer and address components in peptidomimetic delta opioid receptor antagonists related to naltrindole.
AID1079944	Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID756080	Displacement of [3H]naloxone from mu opioid receptor (unknown origin) after 1.5 hrs	2013	Bioorganic & medicinal chemistry letters, Jul-01, Volume: 23, Issue:13	Opioid receptor selectivity profile change via isosterism for 14-O-substituted naltrexone derivatives.
AID149987	Agonistic activity towards Opioid receptor kappa 1	2003	Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14	Opioid binding and in vitro profiles of a series of 4-hdroxy-3-methoxyindolomorphinans. Transformation of a delta-selective ligand into a high affinity kappa-selective ligand by introduction of a 5,14-substituted bridge.
AID415724	Antagonist activity against mu opioid receptor expressed in CHO cells assessed as stimulation [35S]GTPgammaS binding relative to DAMGO	2009	Bioorganic & medicinal chemistry letters, Mar-15, Volume: 19, Issue:6	14-O-Heterocyclic-substituted naltrexone derivatives as non-peptide mu opioid receptor selective antagonists: design, synthesis, and biological studies.
AID149087	Displacement of [3H]- diprenorphine from delta-receptor expressed in HEK 293 cells	2001	Journal of medicinal chemistry, Mar-15, Volume: 44, Issue:6	Investigation of the selectivity of oxymorphone- and naltrexone-derived ligands via site-directed mutagenesis of opioid receptors: exploring the "address" recognition locus.
AID484376	Displacement of [3H]NTI from delta opioid receptor in Hartley guinea pig forebrain by liquid scintillation counter	2010	Bioorganic & medicinal chemistry letters, Jun-15, Volume: 20, Issue:12	Investigation of Beckett-Casy model 2: synthesis of novel 15-16 nornaltrexone derivatives and their pharmacology.
AID625284	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID238166	Antagonist potency towards human mu opioid receptor in [35S]GTP-gamma-S, assay	2004	Journal of medicinal chemistry, Oct-07, Volume: 47, Issue:21	Identification of a new scaffold for opioid receptor antagonism based on the 2-amino-1,1-dimethyl-7-hydroxytetralin pharmacophore.
AID1054698	Displacement of [3H]DPN from kappa opioid receptor (unknown origin) expressed in CHO cell membranes after 1.5 hrs	2013	Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22	Design, synthesis, and biological evaluation of 14-heteroaromatic-substituted naltrexone derivatives: pharmacological profile switch from mu opioid receptor selectivity to mu/kappa opioid receptor dual selectivity.
AID149543	Opioid receptor kappa 1 apparent binding constant from guinea pig cerebellum using [3H]diprenorphine binding assay	1990	Journal of medicinal chemistry, Sep, Volume: 33, Issue:9	Photoactivatable opiate derivatives as irreversible probes of the mu-opioid receptor.
AID1872814	Inhibition of LPS-induced NO production in mouse BV-2 microglia cells incubated for 24 hrs by 2,3-diaminonaphthalene assay	2022	European journal of medicinal chemistry, May-05, Volume: 235	Toll-like receptor 4 (TLR4) inhibitors: Current research and prospective.
AID625288	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID273145	Activity at human recombinant kappa opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding	2006	Journal of medicinal chemistry, Oct-05, Volume: 49, Issue:20	Structural determinants of opioid activity in derivatives of 14-aminomorphinones: effects of changes to the chain linking of the C14-amino group to the aryl ring.
AID149192	Binding affinity was measured by the displacement of [3H]- DADLE in guinea pig brain membrane of opioid receptor delta	1990	Journal of medicinal chemistry, Jun, Volume: 33, Issue:6	Design of peptidomimetic delta opioid receptor antagonists using the message-address concept.
AID223601	Antagonism of bremazocine induced kappa receptor diuresis in rats at a concentration of 0.08 mg/kg subcutaneously	1993	Journal of medicinal chemistry, Oct-01, Volume: 36, Issue:20	3,4-Dimethyl-4-(3-hydroxyphenyl)piperidines: opioid antagonists with potent anorectant activity.
AID1713965	Antagonist activity at human MOR transfected in CHO cells co-transfected with Gqi5 assessed as inhibition of DAMGO-induced calcium mobilization incubated for 15 mins prior to DAMGO addition and measured for 90 secs by Fluo-4AM dye based fluorescence analy	2016	Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22	Exploration of bivalent ligands targeting putative mu opioid receptor and chemokine receptor CCR5 dimerization.
AID148070	Stimulation of [35S]GTP-gamma-S, binding at human recombinant Opioid receptor delta 1 transfected into CHO cells.	2003	Journal of medicinal chemistry, Apr-10, Volume: 46, Issue:8	14-amino, 14-alkylamino, and 14-acylamino analogs of oxymorphindole. Differential effects on opioid receptor binding and functional profiles.
AID149718	Dose ratio due to Antagonist Effect at a concentration of 100 nM by normorphine, Opioid receptor mu 1 in the guinea pig ileum longitudinal muscle myenteric plexus.	1985	Journal of medicinal chemistry, Jul, Volume: 28, Issue:7	10-Ketonaltrexone and 10-ketooxymorphone.
AID148998	Opioid receptor mu antagonistic activity was measured by the displacement of morphine in the guinea pig ileum at a concentration of 100 nM	1990	Journal of medicinal chemistry, Jun, Volume: 33, Issue:6	Design of peptidomimetic delta opioid receptor antagonists using the message-address concept.
AID1123188	Displacement of [3H]-naloxone from opioid receptor in rat brain homogenate at 1x10'-8 M preincubated for 5 mins followed by washout measured after 15 mins by liquid scintillation counting analysis relative to control	1979	Journal of medicinal chemistry, Feb, Volume: 22, Issue:2	Synthesis and pharmacologic characterization of an alkylating analogue (chlornaltrexamine) of naltrexone with ultralong-lasting narcotic antagonist properties.
AID1222793	Dissociation constant, pKa of the compound	2013	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 41, Issue:5	Which metabolites circulate?
AID1123211	Effect on development of dependence to morphine in Swiss Webster mouse assessed as increase in naloxone ED50 for eliciting withdrawal jumping at 0.24 nmol, icv after 72 hrs relative to control	1979	Journal of medicinal chemistry, Feb, Volume: 22, Issue:2	Synthesis and pharmacologic characterization of an alkylating analogue (chlornaltrexamine) of naltrexone with ultralong-lasting narcotic antagonist properties.
AID148339	Effective concentration agonistic activity towards Opioid receptor mu 1	2003	Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14	Opioid binding and in vitro profiles of a series of 4-hdroxy-3-methoxyindolomorphinans. Transformation of a delta-selective ligand into a high affinity kappa-selective ligand by introduction of a 5,14-substituted bridge.
AID148838	Antagonistic activity at Opioid receptor kappa 1 in electrically stimulated Guinea pig ileum using ethylketazocine as the agonist at 100 nM concentration	1988	Journal of medicinal chemistry, Jul, Volume: 31, Issue:7	Only one pharmacophore is required for the kappa opioid antagonist selectivity of norbinaltorphimine.
AID417161	Agonist activity at human kappa opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding relative to basal level	2009	Bioorganic & medicinal chemistry letters, Apr-15, Volume: 19, Issue:8	Syntheses of novel high affinity ligands for opioid receptors.
AID301033	Antagonist activity at human delta opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay	2007	Bioorganic & medicinal chemistry letters, Oct-01, Volume: 17, Issue:19	Structure-activity relationship studies of carboxamido-biaryl ethers as opioid receptor antagonists (OpRAs). Part 1.
AID149750	Tested for the binding affinity against the Delta opioid receptor in guinea pig brain using [3H]DPDPE	1994	Journal of medicinal chemistry, Dec-09, Volume: 37, Issue:25	Synthesis and opioid receptor affinity of a series of aralkyl ethers of 6 alpha- and 6 beta-naltrexol.
AID150015	Antagonistic activity at Opioid receptor mu 1 in electrically stimulated Guinea pig ileum using morphine as the agonist at 100 nM concentration	1988	Journal of medicinal chemistry, Jul, Volume: 31, Issue:7	Only one pharmacophore is required for the kappa opioid antagonist selectivity of norbinaltorphimine.
AID149755	Antagonistic activity at Opioid receptor delta 1 in electrically stimulated Guinea pig ileum using DADLE as the agonist at 100 nM concentration	1988	Journal of medicinal chemistry, Jul, Volume: 31, Issue:7	Only one pharmacophore is required for the kappa opioid antagonist selectivity of norbinaltorphimine.
AID2954	Selectivity ratio of binding affinity towards mu to delta receptors of rat brain membranes	1999	Journal of medicinal chemistry, Sep-09, Volume: 42, Issue:18	Synthesis, opioid receptor binding, and biological activities of naltrexone-derived pyrido- and pyrimidomorphinans.
AID756076	Selectivity ratio of Ki for kappa opioid receptor (unknown origin) to Ki for mu opioid receptor (unknown origin)	2013	Bioorganic & medicinal chemistry letters, Jul-01, Volume: 23, Issue:13	Opioid receptor selectivity profile change via isosterism for 14-O-substituted naltrexone derivatives.
AID151128	Dose ratio due to Antagonist Effect at a concentration of 100 nM by normorphine, Opioid receptor mu 1 in mouse vas deferens.	1985	Journal of medicinal chemistry, Jul, Volume: 28, Issue:7	10-Ketonaltrexone and 10-ketooxymorphone.
AID354251	Displacement of [3H]DAMGO from mu opioid receptor in guinea pig forebrain	2009	Bioorganic & medicinal chemistry letters, May-01, Volume: 19, Issue:9	Synthesis of a new opioid ligand having the oxabicyclo[3.2.1]octane skeleton using a new rearrangement reaction.
AID1820200	Antagonist activity at mouse MOR expressed in CHO cells assessed as inhibition of DAMGO-induced calcium mobilization preincubated for 60 mins measured after 15 mins by calcium mobilization assay	2021	Journal of medicinal chemistry, 06-10, Volume: 64, Issue:11	Structure-Based Design and Development of Chemical Probes Targeting Putative MOR-CCR5 Heterodimers to Inhibit Opioid Exacerbated HIV-1 Infectivity.
AID1079933	Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is
AID692551	Displacement of [3H]-DAMGO from mouse MOR/DOR expressed in HEK293 cells	2012	ACS medicinal chemistry letters, Aug-09, Volume: 3, Issue:8	Tuned-Affinity Bivalent Ligands for the Characterization of Opioid Receptor Heteromers.
AID317857	Selectivity ratio of Ki for human mu opioid receptor over Ki for human kappa opioid receptor	2008	Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6	Synthesis and biological evaluation of alpha- and beta-6-amido derivatives of 17-cyclopropylmethyl-3, 14beta-dihydroxy-4, 5alpha-epoxymorphinan: potential alcohol-cessation agents.
AID174610	Duration of action of compound was determined at the AD99 dose level in rats	1982	Journal of medicinal chemistry, Feb, Volume: 25, Issue:2	Common anionic receptor site hypothesis: its relevance to the antagonist action of naloxone.
AID233860	Selectivity between kappa opioid receptor and delta opioid receptor.	2003	Journal of medicinal chemistry, Apr-10, Volume: 46, Issue:8	14-amino, 14-alkylamino, and 14-acylamino analogs of oxymorphindole. Differential effects on opioid receptor binding and functional profiles.
AID1194122	Selectivity ratio of Ki for mouse DOR to Ki for mouse MOR	2015	Bioorganic & medicinal chemistry, Apr-15, Volume: 23, Issue:8	Design, syntheses, and pharmacological characterization of 17-cyclopropylmethyl-3,14β-dihydroxy-4,5α-epoxy-6α-(isoquinoline-3'-carboxamido)morphinan analogues as opioid receptor ligands.
AID767589	Agonist activity at mouse mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrs	2013	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 23, Issue:18	Structure activity relationship studies of 17-cyclopropylmethyl-3,14β-dihydroxy-4,5α-epoxy-6α-(isoquinoline-3'-carboxamido)morphinan (NAQ) analogues as potent opioid receptor ligands: preliminary results on the role of electronic characteristics for affin
AID1121821	Displacement of [3H]-naloxone from human mu opioid receptor expressed in CHO cells after 1 hr	2013	MedChemComm, May-01, Volume: 4, Issue:5	A Bivalent Ligand Targeting the Putative Mu Opioid Receptor and Chemokine Receptor CCR5 Heterodimers: Binding Affinity versus Functional Activities.
AID698730	Displacement of [125I]-BNtxA from Mu-type opioid receptor exon 11-associated truncated six transmembrane domain splice variant in mouse brain membranes after 90 mins	2012	Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14	Synthesis and evaluation of aryl-naloxamide opiate analgesics targeting truncated exon 11-associated μ opioid receptor (MOR-1) splice variants.
AID17665	Compound was evaluated for equilibrium constant, Ke	1983	Journal of medicinal chemistry, Oct, Volume: 26, Issue:10	Different receptor sites mediate opioid agonism and antagonism.
AID273134	Selectivity for human mu opioid receptor over kappa opioid receptor	2006	Journal of medicinal chemistry, Oct-05, Volume: 49, Issue:20	Structural determinants of opioid activity in derivatives of 14-aminomorphinones: effects of changes to the chain linking of the C14-amino group to the aryl ring.
AID450019	Selectivity ratio of Ki for delta opioid receptor to Ki for mu opioid receptor	2009	Bioorganic & medicinal chemistry, Sep-15, Volume: 17, Issue:18	Synthesis and pharmacological evaluation of 6-naltrexamine analogs for alcohol cessation.
AID603514	Selectivity ratio of Ki for kappa opioid receptor in guinea pig cerebellum homogenates to Ki for mu opioid receptor in guinea pig forebrain homogenates	2011	Bioorganic & medicinal chemistry letters, Jul-01, Volume: 21, Issue:13	Synthesis of novel triplet drugs with 1,3,5-trioxazatriquinane skeletons and their pharmacologies. 1: Synthesis of triplet drugs with morphinan skeletons.
AID1194145	Reversal of morphine-induced antinociceptive activity in Swiss-Webster mouse assessed as wet-dog shakes at 1 mg/kg, sc measured immediately relative to control	2015	Bioorganic & medicinal chemistry, Apr-15, Volume: 23, Issue:8	Design, syntheses, and pharmacological characterization of 17-cyclopropylmethyl-3,14β-dihydroxy-4,5α-epoxy-6α-(isoquinoline-3'-carboxamido)morphinan analogues as opioid receptor ligands.
AID603511	Displacement of [3H]-DAMGO from mu opioid receptor in guinea pig forebrain homogenates	2011	Bioorganic & medicinal chemistry letters, Jul-01, Volume: 21, Issue:13	Synthesis of novel triplet drugs with 1,3,5-trioxazatriquinane skeletons and their pharmacologies. 1: Synthesis of triplet drugs with morphinan skeletons.
AID227972	Selectivity ratio between Ke value to that of DAMGO (using DADLE as agonist; delta agonist/DAMGO)	1996	Journal of medicinal chemistry, Apr-26, Volume: 39, Issue:9	Opioid antagonist activity of naltrexone-derived bivalent ligands: importance of a properly oriented molecular scaffold to guide "address" recognition at kappa opioid receptors.
AID149630	Inhibition of Opioid receptor delta 1 by displacing 1 nM [3H]DPDPE in guinea pig brain membrane	1992	Journal of medicinal chemistry, Nov-27, Volume: 35, Issue:24	O3-(2-carbomethoxyallyl) ethers of opioid ligands derived from oxymorphone, naltrexone, etorphine, diprenorphine, norbinaltorphimine, and naltrindole. Unexpected O3-dealkylation in the opioid radioligand displacement assay.
AID224588	Binding affinity was determined as ability to displace [3H]DAMGO radioligand from Mu opioid receptor	1998	Bioorganic & medicinal chemistry letters, Nov-17, Volume: 8, Issue:22	N-substituted octahydro-4a-(3-hydroxyphenyl)-10a-methyl-benzo[g]isoquinolines are opioid receptor pure antagonists.
AID227975	Selectivity ratio between Ke value to that of DAMGO (using U-50488 as agonist; k agonist/DAMGO)	1996	Journal of medicinal chemistry, Apr-26, Volume: 39, Issue:9	Opioid antagonist activity of naltrexone-derived bivalent ligands: importance of a properly oriented molecular scaffold to guide "address" recognition at kappa opioid receptors.
AID1461671	Antagonist activity at OGFR in African green monkey COS7 cells harboring OGF assessed as increase in cell growth at 1 uM after 72 hrs by hemacytometric method	2017	Bioorganic & medicinal chemistry, 08-15, Volume: 25, Issue:16	Selective opioid growth factor receptor antagonists based on a stilbene isostere.
AID625276	FDA Liver Toxicity Knowledge Base Benchmark Dataset (LTKB-BD) drugs of most concern for DILI	2011	Drug discovery today, Aug, Volume: 16, Issue:15-16	FDA-approved drug labeling for the study of drug-induced liver injury.
AID273137	Displacement of [3H]Cl-DPDPE from delta receptor in guinea pig brain homogenate	2006	Journal of medicinal chemistry, Oct-05, Volume: 49, Issue:20	Structural determinants of opioid activity in derivatives of 14-aminomorphinones: effects of changes to the chain linking of the C14-amino group to the aryl ring.
AID410722	Ratio of Ki for human delta opioid receptor to Ki for human kappa opioid receptor expressed in CHO cells	2009	Bioorganic & medicinal chemistry letters, Jan-01, Volume: 19, Issue:1	Syntheses and opioid receptor binding properties of carboxamido-substituted opioids.
AID1611816	Peripheral selectivity index, ratio of ID50 for inhibition of morphine-induced antinociceptive activity in ICR mouse to ID50 for inhibition of morphine-induced delays in intestinal transit in ICR mouse	2019	ACS medicinal chemistry letters, Dec-12, Volume: 10, Issue:12	Discovery of Axelopran (TD-1211): A Peripherally Restricted μ-Opioid Receptor Antagonist.
AID1611815	Inhibition of morphine-induced antinociceptive activity in po dosed ICR mouse administered via gavage pretreated with compound and 30 mins later injected with morphine and measured after 30 mins by hot plate test	2019	ACS medicinal chemistry letters, Dec-12, Volume: 10, Issue:12	Discovery of Axelopran (TD-1211): A Peripherally Restricted μ-Opioid Receptor Antagonist.
AID1694865	Displacement of [3H]-NLX from mouse MOR expressed in CHO cells incubated for 1.5 hrs by radioligand binding assay	2020	RSC medicinal chemistry, Jan-01, Volume: 11, Issue:1	Design and synthesis of a bivalent probe targeting the putative mu opioid receptor and chemokine receptor CXCR4 heterodimer.
AID29811	Oral bioavailability in human	2000	Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13	QSAR model for drug human oral bioavailability.
AID149435	Inhibition of binding of [3H]U69, 593 to Opioid receptor kappa 1 in guinea pig membranes	2003	Journal of medicinal chemistry, May-08, Volume: 46, Issue:10	2002 Medicinal Chemistry Division Award address: monoamine transporters and opioid receptors. Targets for addiction therapy.
AID286304	Displacement of [3H]naltrindole from human opioid delta receptor expressed in CHO cells	2007	Journal of medicinal chemistry, May-03, Volume: 50, Issue:9	Pharmacological properties of bivalent ligands containing butorphan linked to nalbuphine, naltrexone, and naloxone at mu, delta, and kappa opioid receptors.
AID148495	The IC50 value of agonist (morphine) in presence of antagonist (Compound 20 nM) divided by the control IC60 value with no antagonist in GPI (Guinea pig ileum)	1987	Journal of medicinal chemistry, Feb, Volume: 30, Issue:2	Bimorphinans as highly selective, potent kappa opioid receptor antagonists.
AID540218	Clearance in monkey after iv administration	2005	Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7	Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure.
AID539464	Solubility of the compound in 0.1 M phosphate buffer at 600 uM at pH 7.4 after 24 hrs by LC/MS/MS analysis	2010	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24	Experimental solubility profiling of marketed CNS drugs, exploring solubility limit of CNS discovery candidate.
AID1194137	Selectivity ratio of EC50 for mouse KOR to EC50 for mouse MOR	2015	Bioorganic & medicinal chemistry, Apr-15, Volume: 23, Issue:8	Design, syntheses, and pharmacological characterization of 17-cyclopropylmethyl-3,14β-dihydroxy-4,5α-epoxy-6α-(isoquinoline-3'-carboxamido)morphinan analogues as opioid receptor ligands.
AID138325	Concentration required for antagonistic activity of Met-enkephalin in the mouse vas deferens at the dose ratio of 2.	1982	Journal of medicinal chemistry, Feb, Volume: 25, Issue:2	Common anionic receptor site hypothesis: its relevance to the antagonist action of naloxone.
AID286305	Ratio of Ki for human opioid kappa receptor to Ki for human opioid gamma receptor	2007	Journal of medicinal chemistry, May-03, Volume: 50, Issue:9	Pharmacological properties of bivalent ligands containing butorphan linked to nalbuphine, naltrexone, and naloxone at mu, delta, and kappa opioid receptors.
AID149982	Percent stimulation of [35S]GTP-gamma-S, binding in recombinant human Opioid receptor kappa 1 transfected into CHO cells: Antagonist activity	2003	Journal of medicinal chemistry, Apr-10, Volume: 46, Issue:8	14-amino, 14-alkylamino, and 14-acylamino analogs of oxymorphindole. Differential effects on opioid receptor binding and functional profiles.
AID149276	Binding affinity was determined as ability to displace [3H]-U-69, radioligand from Opioid receptor kappa 1	1998	Bioorganic & medicinal chemistry letters, Nov-17, Volume: 8, Issue:22	N-substituted octahydro-4a-(3-hydroxyphenyl)-10a-methyl-benzo[g]isoquinolines are opioid receptor pure antagonists.
AID149346	In vito concentration required to displace [3H]DADLE (Kd = 1.6 nM and concentration is 1.9 nM) from high affinity delta-site in rat brain membranes.	1992	Journal of medicinal chemistry, Jul-24, Volume: 35, Issue:15	Probes for narcotic receptor mediated phenomena. 18. Epimeric 6 alpha- and 6 beta-iodo-3,14-dihydroxy-17-(cyclopropylmethyl)-4,5 alpha-epoxymorphinans as potential ligands for opioid receptor single photon emission computed tomography: synthesis, evaluati
AID273141	Activity at human recombinant mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding	2006	Journal of medicinal chemistry, Oct-05, Volume: 49, Issue:20	Structural determinants of opioid activity in derivatives of 14-aminomorphinones: effects of changes to the chain linking of the C14-amino group to the aryl ring.
AID624607	Specific activity of expressed human recombinant UGT1A3	2000	Annual review of pharmacology and toxicology, , Volume: 40	Human UDP-glucuronosyltransferases: metabolism, expression, and disease.
AID1079945	Animal toxicity known. [column 'TOXIC' in source]
AID1054699	Displacement of [3H]NLX from mu opioid receptor (unknown origin) expressed in CHO cell membranes after 1.5 hrs	2013	Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22	Design, synthesis, and biological evaluation of 14-heteroaromatic-substituted naltrexone derivatives: pharmacological profile switch from mu opioid receptor selectivity to mu/kappa opioid receptor dual selectivity.
AID320413	Antinociceptive activity in sc dosed mouse by hot plate method	2008	Bioorganic & medicinal chemistry, Jan-15, Volume: 16, Issue:2	The influence of esters and carboxylic acids as the N-substituent of opioids. Part 1: Benzomorphans.
AID149274	Binding affinity was determined against Opioid receptor kappa 1 using [3H]ethylketocyclazocine as radioligand	1998	Bioorganic & medicinal chemistry letters, Nov-17, Volume: 8, Issue:22	N-substituted octahydro-4a-(3-hydroxyphenyl)-10a-methyl-benzo[g]isoquinolines are opioid receptor pure antagonists.
AID1054692	Agonist activity at kappa opioid receptor (unknown origin) expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrs relative to U50488	2013	Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22	Design, synthesis, and biological evaluation of 14-heteroaromatic-substituted naltrexone derivatives: pharmacological profile switch from mu opioid receptor selectivity to mu/kappa opioid receptor dual selectivity.
AID79203	Opioid receptor antagonist activity as inhibiting binding of normorphine to guinea pig ileum	1981	Journal of medicinal chemistry, Feb, Volume: 24, Issue:2	Some 14 beta-substituted analogues of N-(cyclopropylmethyl)normorphine.
AID42548	Increase in the charge carried by choline- induced currents in CA1 pyramidal neurons of 2022-day-old cultures by naltrexone (0.3 uM)	2004	Bioorganic & medicinal chemistry letters, Apr-19, Volume: 14, Issue:8	Sensitivity of neuronal nicotinic acetylcholine receptors to the opiate antagonists naltrexone and naloxone: receptor blockade and up-regulation.
AID148966	Inhibition of [35S]GTP-gamma-S, binding in guines pig caudate stimulated by U69, 593 of Opioid receptor kappa 1	2003	Journal of medicinal chemistry, May-08, Volume: 46, Issue:10	2002 Medicinal Chemistry Division Award address: monoamine transporters and opioid receptors. Targets for addiction therapy.
AID147999	Binding affinity in recombinant human Opioid receptor kappa 1 transfected into chinese hamster ovary cells by displacing [3H]U-69593 radioligand	2003	Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14	Opioid binding and in vitro profiles of a series of 4-hdroxy-3-methoxyindolomorphinans. Transformation of a delta-selective ligand into a high affinity kappa-selective ligand by introduction of a 5,14-substituted bridge.
AID577293	Inverse agonist activity at mu opioid receptor by [35S]GTPgammaS binding assay	2011	Journal of medicinal chemistry, Feb-24, Volume: 54, Issue:4	Probes for narcotic receptor mediated phenomena. 41. Unusual inverse μ-agonists and potent μ-opioid antagonists by modification of the N-substituent in enantiomeric 5-(3-hydroxyphenyl)morphans.
AID231887	Compound was tested for ability to protect against the irreversible antagonism of morphine''s effects by beta-FNA in guinea pig ileum at 20 nM concentration	1983	Journal of medicinal chemistry, Oct, Volume: 26, Issue:10	Different receptor sites mediate opioid agonism and antagonism.
AID274391	Displacement of [3H]diprenorphine from human cloned kappa opioid receptor expressed in CHO cells	2006	Journal of medicinal chemistry, Dec-14, Volume: 49, Issue:25	Synthesis and pharmacological evaluation of novel octahydro-1H-pyrido[1,2-a]pyrazine as mu-opioid receptor antagonists.
AID625292	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID298631	Displacement of [3H]DAMGO from human cloned mu opioid receptor	2007	Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21	Cinnamoyl derivatives of 7alpha-aminomethyl-6,14-endo-ethanotetrahydrothebaine and 7alpha-aminomethyl-6,14-endo-ethanotetrahydrooripavine and related opioid ligands.
AID1461556	Antimicrobial activity against Trichomonas vaginalis after 48 hrs by neutral red staining based invert microscopic analysis	2017	Bioorganic & medicinal chemistry, 08-15, Volume: 25, Issue:16	Antitrichomonal activity of δ opioid receptor antagonists, 7-benzylidenenaltrexone derivatives.
AID1133439	Narcotic agonist activity in rat by writhing test	1978	Journal of medicinal chemistry, Jan, Volume: 21, Issue:1	Quantum chemical studies of N-substituent variation in the oxymorphone series of opiate narcotics.
AID540221	Volume of distribution at steady state in human after iv administration	2005	Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7	Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure.
AID1123189	Displacement of [3H]-naloxone from opioid receptor in rat brain homogenate at 1x10'-8 M preincubated for 5 mins measured after second washout by liquid scintillation counting analysis relative to control	1979	Journal of medicinal chemistry, Feb, Volume: 22, Issue:2	Synthesis and pharmacologic characterization of an alkylating analogue (chlornaltrexamine) of naltrexone with ultralong-lasting narcotic antagonist properties.
AID303905	Displacement of [3H]diprenorphine from cloned human mu opioid receptor expressed in CHO cells	2007	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24	Structure activity relationship studies of carboxamido-biaryl ethers as opioid receptor antagonists (OpRAs). Part 2.
AID152386	Displacement of [3H]- diprenorphine from mu-K303E-receptor expressed in HEK 293 cells	2001	Journal of medicinal chemistry, Mar-15, Volume: 44, Issue:6	Investigation of the selectivity of oxymorphone- and naltrexone-derived ligands via site-directed mutagenesis of opioid receptors: exploring the "address" recognition locus.
AID223596	Binding affinity towards kappa opioid receptor by displacement of [3H]EKC in guinea pig cortical tissue	1993	Journal of medicinal chemistry, Oct-01, Volume: 36, Issue:20	3,4-Dimethyl-4-(3-hydroxyphenyl)piperidines: opioid antagonists with potent anorectant activity.
AID228109	Selectivity ratio between kappa and mu opioid receptor from guinea pig brain membrane	1996	Journal of medicinal chemistry, Apr-26, Volume: 39, Issue:9	Opioid antagonist activity of naltrexone-derived bivalent ligands: importance of a properly oriented molecular scaffold to guide "address" recognition at kappa opioid receptors.
AID311280	Antagonist activity at human kappa opioid receptor expressed in CHO cells by [35S]GTP-gamma-S assay	2007	Journal of natural products, Aug, Volume: 70, Issue:8	Flavonoids as opioid receptor ligands: identification and preliminary structure-activity relationships.
AID227974	Selectivity ratio between Ke value to that of DAMGO (using EK as agonist; k agonist/DAMGO)	1996	Journal of medicinal chemistry, Apr-26, Volume: 39, Issue:9	Opioid antagonist activity of naltrexone-derived bivalent ligands: importance of a properly oriented molecular scaffold to guide "address" recognition at kappa opioid receptors.
AID320414	Antinociceptive activity in sc dosed mouse by phenylquinone antiwrithing assay	2008	Bioorganic & medicinal chemistry, Jan-15, Volume: 16, Issue:2	The influence of esters and carboxylic acids as the N-substituent of opioids. Part 1: Benzomorphans.
AID149901	Binding affinity was determined towards Opioid receptor delta 1 using [3H]naltrindole as radioligand	2003	Bioorganic & medicinal chemistry letters, Jun-02, Volume: 13, Issue:11	Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. Part 2: 8-formamidocyclazocine analogues.
AID1079932	Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID588211	Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in humans	2010	Chemical research in toxicology, Jan, Volume: 23, Issue:1	Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID1726158	Antagonist activity at human mu opioid receptor expressed in CHO cells co- expressing Gqi5 assessed as decrease in DAMGO-induced intracellular calcium mobilization incubated for 15 mins followed by DAMGO addition by Fluo-AM dye based fluorescence assay	2020	ACS medicinal chemistry letters, Nov-12, Volume: 11, Issue:11	Bivalent Ligand Aiming Putative Mu Opioid Receptor and Chemokine Receptor CXCR4 Dimers in Opioid Enhanced HIV-1 Entry.
AID450017	Displacement of [3H]DPDPE from delta opioid receptor expressed in HEK293 cells by visible spectrophotometry	2009	Bioorganic & medicinal chemistry, Sep-15, Volume: 17, Issue:18	Synthesis and pharmacological evaluation of 6-naltrexamine analogs for alcohol cessation.
AID1447102	Antitumor activity against human SQC cells xenografted in nude mouse model assessed as tumor growth inhibition at 0.1 mg/kg administered daily relative to control	2017	Bioorganic & medicinal chemistry letters, 05-01, Volume: 27, Issue:9	Synthesis and evaluation of a ligand targeting the μ and δ opioid receptors for drug delivery to lung cancer.
AID347311	Displacement of [3H]norBNI from monocloned kappa opioid receptor expressed in CHO cells	2009	Journal of medicinal chemistry, Mar-12, Volume: 52, Issue:5	Design, synthesis, and biological evaluation of 6alpha- and 6beta-N-heterocyclic substituted naltrexamine derivatives as mu opioid receptor selective antagonists.
AID1611798	Half life in rat liver microsomes at 3 uM	2019	ACS medicinal chemistry letters, Dec-12, Volume: 10, Issue:12	Discovery of Axelopran (TD-1211): A Peripherally Restricted μ-Opioid Receptor Antagonist.
AID151584	Binding constant for the agonist state was measured for its ability to displace [3H]naloxone from opioid mu 1 receptor buffered homogenate of rat brain membranes	1988	Journal of medicinal chemistry, Mar, Volume: 31, Issue:3	Structure-activity relationships for drugs binding to the agonist and antagonist states of the primary morphine receptor.
AID312067	Antagonist activity at mu opioid receptor in NMRI mouse vas deferens assessed as effect on DAMGO-induced muscle contraction	2008	Journal of medicinal chemistry, Jan-10, Volume: 51, Issue:1	Endomorphin-2 with a beta-turn backbone constraint retains the potent micro-opioid receptor agonist properties.
AID540217	Volume of distribution at steady state in dog after iv administration	2005	Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7	Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure.
AID149164	Compound was evaluated for the binding affinity to Opioid receptor mu using [3H]DAMGO as radioligand in guinea pig brain membrane	1991	Journal of medicinal chemistry, May, Volume: 34, Issue:5	Role of spacer and address components in peptidomimetic delta opioid receptor antagonists related to naltrindole.
AID456915	Displacement of [3H]NTI from delta opioid receptor in guinea pig forebrain	2010	Bioorganic & medicinal chemistry letters, Feb-01, Volume: 20, Issue:3	Investigation of Beckett-Casy model 1: synthesis of novel 16,17-seco-naltrexone derivatives and their pharmacology.
AID148122	Antagonistic potency at opioid receptor kappa (100 nM) (Ke =IC50 in the presence of antagonist divided by the control IC50 value)	1991	Journal of medicinal chemistry, May, Volume: 34, Issue:5	Role of spacer and address components in peptidomimetic delta opioid receptor antagonists related to naltrindole.
AID317854	Displacement of [3H]DPDPE from human delta opioid receptor expressed in CHO cells	2008	Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6	Synthesis and biological evaluation of alpha- and beta-6-amido derivatives of 17-cyclopropylmethyl-3, 14beta-dihydroxy-4, 5alpha-epoxymorphinan: potential alcohol-cessation agents.
AID148930	Compound was evaluated for antagonist potency in the mouse vas deferens preparation using [D-Ala2,D-Leu5]enkephalin (Opioid receptor delta 1)	1991	Journal of medicinal chemistry, Jun, Volume: 34, Issue:6	An approach to the design of receptor-type-selective non-peptide antagonists of peptidergic receptors: delta opioid antagonists.
AID149927	Inhibition of [3H]-DADLE binding to Opioid receptor delta 1 of rat brain membranes	1998	Journal of medicinal chemistry, May-21, Volume: 41, Issue:11	Investigation of the N-substituent conformation governing potency and mu receptor subtype-selectivity in (+)-(3R, 4R)-dimethyl-4-(3-hydroxyphenyl)piperidine opioid antagonists.
AID147964	Opioid receptor kappa antagonistic activity was measured by the displacement of ethylketazocine in the guinea pig ileum at a concentration of 100 nM	1990	Journal of medicinal chemistry, Jun, Volume: 33, Issue:6	Design of peptidomimetic delta opioid receptor antagonists using the message-address concept.
AID146642	Blockage of Nicotinic acetylcholine receptor alpha4-beta2 noncompetitively in CA1 stratum radiatum interneurons	2004	Bioorganic & medicinal chemistry letters, Apr-19, Volume: 14, Issue:8	Sensitivity of neuronal nicotinic acetylcholine receptors to the opiate antagonists naltrexone and naloxone: receptor blockade and up-regulation.
AID1474166	Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index	2016	Drug discovery today, Apr, Volume: 21, Issue:4	DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID227077	Mu opioid activity was evaluated on electrically stimulated guinea pig ileum by using morphine(M) as standard.	1996	Journal of medicinal chemistry, Apr-26, Volume: 39, Issue:9	Opioid antagonist activity of naltrexone-derived bivalent ligands: importance of a properly oriented molecular scaffold to guide "address" recognition at kappa opioid receptors.
AID395295	Displacement of [3H]U69,593 from human kappa opioid receptor expressed in CHO cells	2009	Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6	14 beta-O-cinnamoylnaltrexone and related dihydrocodeinones are mu opioid receptor partial agonists with predominant antagonist activity.
AID273149	Selectivity for guinea pig mu opioid receptor over delta opioid receptor	2006	Journal of medicinal chemistry, Oct-05, Volume: 49, Issue:20	Structural determinants of opioid activity in derivatives of 14-aminomorphinones: effects of changes to the chain linking of the C14-amino group to the aryl ring.
AID1194123	Selectivity ratio of Ki for mouse KOR to Ki for mouse MOR	2015	Bioorganic & medicinal chemistry, Apr-15, Volume: 23, Issue:8	Design, syntheses, and pharmacological characterization of 17-cyclopropylmethyl-3,14β-dihydroxy-4,5α-epoxy-6α-(isoquinoline-3'-carboxamido)morphinan analogues as opioid receptor ligands.
AID76379	Tested for potent reversible agonist activity on electrically stimulated guinea pig ileal longitudinal muscle preparation	1980	Journal of medicinal chemistry, Mar, Volume: 23, Issue:3	A novel opioid receptor site directed alkylating agent with irreversible narcotic antagonistic and reversible agonistic activities.
AID1726157	Agonist activity at mu opioid receptor (unknown origin) assessed as maximum efficacy by [35S]-GTPgammaS binding assay relative to DAMGO	2020	ACS medicinal chemistry letters, Nov-12, Volume: 11, Issue:11	Bivalent Ligand Aiming Putative Mu Opioid Receptor and Chemokine Receptor CXCR4 Dimers in Opioid Enhanced HIV-1 Entry.
AID148969	Ke value was obtained from IC50 ratio values when compared with Opioid receptor kappa 1 agonist in Guinea pig Ileum using EK as radioligand	1996	Journal of medicinal chemistry, Apr-26, Volume: 39, Issue:9	Opioid antagonist activity of naltrexone-derived bivalent ligands: importance of a properly oriented molecular scaffold to guide "address" recognition at kappa opioid receptors.
AID149944	Binding affinity for Opioid receptor delta 1 was determined by inhibition of binding of [3H]DADLE (1.3-2.0 nM) to rat brain membranes	1999	Journal of medicinal chemistry, Sep-09, Volume: 42, Issue:18	Synthesis, opioid receptor binding, and biological activities of naltrexone-derived pyrido- and pyrimidomorphinans.
AID148585	Displacement of [3H]diprenorphine from k-Y312A-receptor expressed in HEK 293 cells	2001	Journal of medicinal chemistry, Mar-15, Volume: 44, Issue:6	Investigation of the selectivity of oxymorphone- and naltrexone-derived ligands via site-directed mutagenesis of opioid receptors: exploring the "address" recognition locus.
AID270160	Inverse agonist activity at human cloned delta opioid receptor expressed in CHO cells assessed as inhibition of DPDPE-stimulated [35S]GTP-gamma-S binding in presence of 1 uM GDP	2006	Journal of medicinal chemistry, Sep-07, Volume: 49, Issue:18	Highly potent and selective phenylmorphan-based inverse agonists of the opioid delta receptor.
AID148057	Inhibition of binding of [3H]DAMGO to Opioid receptor mu 1 in guinea pig membranes	2003	Journal of medicinal chemistry, May-08, Volume: 46, Issue:10	2002 Medicinal Chemistry Division Award address: monoamine transporters and opioid receptors. Targets for addiction therapy.
AID1054682	Reduction of morphine-induced antinociceptive activity in sc dosed Swiss-Webster mouse assessed as dose required to antagonize morphine effect by warm-water tail-flick assay	2013	Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22	Design, synthesis, and biological evaluation of 14-heteroaromatic-substituted naltrexone derivatives: pharmacological profile switch from mu opioid receptor selectivity to mu/kappa opioid receptor dual selectivity.
AID223599	Antagonist activity towards U50 488 induced kappa opioid receptor by mouse writhing assay at 2.5 mg/kg subcutaneously	1993	Journal of medicinal chemistry, Oct-01, Volume: 36, Issue:20	3,4-Dimethyl-4-(3-hydroxyphenyl)piperidines: opioid antagonists with potent anorectant activity.
AID756077	Selectivity ratio of Ki for delta opioid receptor (unknown origin) to Ki for mu opioid receptor (unknown origin)	2013	Bioorganic & medicinal chemistry letters, Jul-01, Volume: 23, Issue:13	Opioid receptor selectivity profile change via isosterism for 14-O-substituted naltrexone derivatives.
AID150044	The compound was tested for antagonist activity by selective inhibition of [35S]GTP-gamma-S, binding in Guinea pig caudate stimulated by SMC-80 (Opioid receptor delta 1)	1998	Journal of medicinal chemistry, May-21, Volume: 41, Issue:11	Investigation of the N-substituent conformation governing potency and mu receptor subtype-selectivity in (+)-(3R, 4R)-dimethyl-4-(3-hydroxyphenyl)piperidine opioid antagonists.
AID148810	Antagonist potency was determined as the ratio of [antagonist] to (IC50 ratio-1) for opioid receptor delta 1	1990	Journal of medicinal chemistry, Jun, Volume: 33, Issue:6	Design of peptidomimetic delta opioid receptor antagonists using the message-address concept.
AID303906	Displacement of [3H]diprenorphine from cloned human kappa opioid receptor expressed in CHO cells	2007	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24	Structure activity relationship studies of carboxamido-biaryl ethers as opioid receptor antagonists (OpRAs). Part 2.
AID152389	Displacement of [3H]- diprenorphine from mu-receptor expressed in HEK 293 cells	2001	Journal of medicinal chemistry, Mar-15, Volume: 44, Issue:6	Investigation of the selectivity of oxymorphone- and naltrexone-derived ligands via site-directed mutagenesis of opioid receptors: exploring the "address" recognition locus.
AID149897	Binding affinity towards Opioid receptor delta 1 of guinea pig brain membranes using radioligand 0.2 nM [3H]Naltrindole	2001	Bioorganic & medicinal chemistry letters, Jul-09, Volume: 11, Issue:13	3-Carboxamido analogues of morphine and naltrexone. synthesis and opioid receptor binding properties.
AID450030	Antagonist activity at delta opioid receptor expressed in HEK293 cells assessed as inhibition of compound 14-induced [35S]GTPgammaS binding	2009	Bioorganic & medicinal chemistry, Sep-15, Volume: 17, Issue:18	Synthesis and pharmacological evaluation of 6-naltrexamine analogs for alcohol cessation.
AID450032	Antagonist activity at NOP expressed in HEK293 cells assessed as inhibition of compound 15-induced [35S]GTPgammaS binding	2009	Bioorganic & medicinal chemistry, Sep-15, Volume: 17, Issue:18	Synthesis and pharmacological evaluation of 6-naltrexamine analogs for alcohol cessation.
AID150239	Inhibitory concentration was determined against Opioid receptors using [3H]- bremazocine radioligand	1995	Journal of medicinal chemistry, Feb-03, Volume: 38, Issue:3	Isothiocyanate-substituted benzyl ether opioid receptor ligands derived from 6 beta-naltrexol.
AID117734	Percent reduction of analgesia induced by U-50,488 at 15 mg/kg after sc administration was measured in mice	1989	Journal of medicinal chemistry, Feb, Volume: 32, Issue:2	Synthesis and biological evaluation of 14-alkoxymorphinans. 2. (-)-N-(cyclopropylmethyl)-4,14-dimethoxymorphinan-6-one, a selective mu opioid receptor antagonist.
AID1726156	Agonist activity at mu opioid receptor (unknown origin) by [35S]-GTPgammaS binding assay	2020	ACS medicinal chemistry letters, Nov-12, Volume: 11, Issue:11	Bivalent Ligand Aiming Putative Mu Opioid Receptor and Chemokine Receptor CXCR4 Dimers in Opioid Enhanced HIV-1 Entry.
AID540219	Volume of distribution at steady state in monkey after iv administration	2005	Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7	Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure.
AID76582	Opioid agonistic activity was measured in guinea pig ileum	1981	Journal of medicinal chemistry, Feb, Volume: 24, Issue:2	Some 14 beta-substituted analogues of N-(cyclopropylmethyl)normorphine.
AID395291	Displacement of [3H]DAMGO from delta opioid receptor in Hartley guinea pig brain membrane	2009	Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6	14 beta-O-cinnamoylnaltrexone and related dihydrocodeinones are mu opioid receptor partial agonists with predominant antagonist activity.
AID151601	Binding affinity at Opioid receptor mu 1 by displacement of [3H]DAMGO in rat brain membrane	2004	Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6	Identification of opioid ligands possessing mixed micro agonist/delta antagonist activity among pyridomorphinans derived from naloxone, oxymorphone, and hydromorphone [correction of hydropmorphone].
AID603727	Selectivity ratio of Ki for delta opioid receptor in guinea pig forebrain homogenate to Ki for kappa opioid receptor in guinea pig cerebellum homogenate	2011	Bioorganic & medicinal chemistry letters, Jul-01, Volume: 21, Issue:13	Synthesis of new opioid derivatives with a propellane skeleton and their pharmacology: part 1.
AID354252	Displacement of [3H]NTI from delta opioid receptor in guinea pig forebrain	2009	Bioorganic & medicinal chemistry letters, May-01, Volume: 19, Issue:9	Synthesis of a new opioid ligand having the oxabicyclo[3.2.1]octane skeleton using a new rearrangement reaction.
AID152226	Binding affinity was determined towards opioid receptor mu1 using [3H]DAMGO as radioligand	2003	Bioorganic & medicinal chemistry letters, Jun-02, Volume: 13, Issue:11	Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. Part 2: 8-formamidocyclazocine analogues.
AID229805	Ratio of Ki for mu receptor to that of kappa receptor	1998	Journal of medicinal chemistry, Dec-17, Volume: 41, Issue:26	Identification of an opioid kappa receptor subtype-selective N-substituent for (+)-(3R,4R)-dimethyl-4-(3-hydroxyphenyl)piperidine.
AID415720	Selectivity ratio of Ki for delta opioid receptor to Ki for mu opioid receptor	2009	Bioorganic & medicinal chemistry letters, Mar-15, Volume: 19, Issue:6	14-O-Heterocyclic-substituted naltrexone derivatives as non-peptide mu opioid receptor selective antagonists: design, synthesis, and biological studies.
AID117735	Percent reduction of analgesia induced by morphine at 10 mg/kg after sc administration was measured in mice	1989	Journal of medicinal chemistry, Feb, Volume: 32, Issue:2	Synthesis and biological evaluation of 14-alkoxymorphinans. 2. (-)-N-(cyclopropylmethyl)-4,14-dimethoxymorphinan-6-one, a selective mu opioid receptor antagonist.
AID1194119	Displacement of [3H]naloxane from mouse MOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assay	2015	Bioorganic & medicinal chemistry, Apr-15, Volume: 23, Issue:8	Design, syntheses, and pharmacological characterization of 17-cyclopropylmethyl-3,14β-dihydroxy-4,5α-epoxy-6α-(isoquinoline-3'-carboxamido)morphinan analogues as opioid receptor ligands.
AID1079948	Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID416814	Displacement of [3H]naltrindole from human delta opioid receptor expressed in CHO cells after 3 hrs by scintillation counting	2009	Bioorganic & medicinal chemistry letters, Apr-15, Volume: 19, Issue:8	Syntheses of novel high affinity ligands for opioid receptors.
AID312066	Antagonist activity at mu opioid receptor in NMRI mouse vas deferens assessed as effect on endomorphin 2-induced muscle contraction	2008	Journal of medicinal chemistry, Jan-10, Volume: 51, Issue:1	Endomorphin-2 with a beta-turn backbone constraint retains the potent micro-opioid receptor agonist properties.
AID232232	Selectivity given as ratio of kappa receptor to delta receptor	2004	Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6	Identification of opioid ligands possessing mixed micro agonist/delta antagonist activity among pyridomorphinans derived from naloxone, oxymorphone, and hydromorphone [correction of hydropmorphone].
AID152388	Displacement of [3H]- diprenorphine from mu-W318A-receptor expressed in HEK 293 cells	2001	Journal of medicinal chemistry, Mar-15, Volume: 44, Issue:6	Investigation of the selectivity of oxymorphone- and naltrexone-derived ligands via site-directed mutagenesis of opioid receptors: exploring the "address" recognition locus.
AID256844	Inhibition of DPDPE stimulated [35S]GTP-gamma-S binding to cloned human delta opioid receptor	2005	Journal of medicinal chemistry, Dec-29, Volume: 48, Issue:26	N-substituted cis-4a-(3-hydroxyphenyl)-8a-methyloctahydroisoquinolines are opioid receptor pure antagonists.
AID1135663	Displacement of [3H]naloxone from opioid receptor (unknown origin) in brain homogenate at 10 nM	1978	Journal of medicinal chemistry, Jul, Volume: 21, Issue:7	6beta-[N,N-Bis(2-chloroethyl)amino]-17-(cyclopropylmethyl)-4,5alpha-epoxy-3,14-dihydroxymorphinan(chlornaltrexamine) a potent opioid receptor alkylating agent with ultralong narcotic antagonist actitivty.
AID298652	Antagonist activity at human mu opioid receptor expressed in CHO cells assessed as effect on [35S]GTP-gamma-S binding	2007	Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21	Cinnamoyl derivatives of 7alpha-aminomethyl-6,14-endo-ethanotetrahydrothebaine and 7alpha-aminomethyl-6,14-endo-ethanotetrahydrooripavine and related opioid ligands.
AID239162	Binding affinity against Opioid receptor delta 1 expressed in CHO cells using [3H]Naltrindole as radioligand	2005	Bioorganic & medicinal chemistry letters, Apr-15, Volume: 15, Issue:8	Synthesis and opioid receptor binding properties of a highly potent 4-hydroxy analogue of naltrexone.
AID603512	Displacement of [3H]-NTI from delta opioid receptor in guinea pig forebrain homogenates	2011	Bioorganic & medicinal chemistry letters, Jul-01, Volume: 21, Issue:13	Synthesis of novel triplet drugs with 1,3,5-trioxazatriquinane skeletons and their pharmacologies. 1: Synthesis of triplet drugs with morphinan skeletons.
AID1054690	Agonist activity at delta opioid receptor (unknown origin) expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrs relative to SNC80	2013	Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22	Design, synthesis, and biological evaluation of 14-heteroaromatic-substituted naltrexone derivatives: pharmacological profile switch from mu opioid receptor selectivity to mu/kappa opioid receptor dual selectivity.
AID148665	Opioid receptor delta 1 antagonistic activity was measured by the displacement of DADLE in the mouse vas deferens at tha concentration of 300 nM	1990	Journal of medicinal chemistry, Jun, Volume: 33, Issue:6	Design of peptidomimetic delta opioid receptor antagonists using the message-address concept.
AID347313	Selectivity ratio of Ki for monocloned kappa opioid receptor to Ki for monocloned mu opioid receptor	2009	Journal of medicinal chemistry, Mar-12, Volume: 52, Issue:5	Design, synthesis, and biological evaluation of 6alpha- and 6beta-N-heterocyclic substituted naltrexamine derivatives as mu opioid receptor selective antagonists.
AID681116	TP_TRANSPORTER: transepithelial transport (basal to apical) in MDR1-expressing MDCKII cells	2002	The Journal of pharmacology and experimental therapeutics, Dec, Volume: 303, Issue:3	Passive permeability and P-glycoprotein-mediated efflux differentiate central nervous system (CNS) and non-CNS marketed drugs.
AID1194144	Reversal of morphine-induced antinociceptive activity in Swiss-Webster mouse assessed as escape jumps at 1 mg/kg, sc measured immediately relative to control	2015	Bioorganic & medicinal chemistry, Apr-15, Volume: 23, Issue:8	Design, syntheses, and pharmacological characterization of 17-cyclopropylmethyl-3,14β-dihydroxy-4,5α-epoxy-6α-(isoquinoline-3'-carboxamido)morphinan analogues as opioid receptor ligands.
AID149209	Opioid receptor delta antagonistic activity was measured by the displacement of DADLE in the mouse vas deferens at tha concentration of 300 nM	1990	Journal of medicinal chemistry, Jun, Volume: 33, Issue:6	Design of peptidomimetic delta opioid receptor antagonists using the message-address concept.
AID149431	Inhibition of [3H]U-69593 binding to Opioid receptor kappa 1 of guinea pig membranes	1998	Journal of medicinal chemistry, May-21, Volume: 41, Issue:11	Investigation of the N-substituent conformation governing potency and mu receptor subtype-selectivity in (+)-(3R, 4R)-dimethyl-4-(3-hydroxyphenyl)piperidine opioid antagonists.
AID1526732	Substrate activity at human OCT1 expressed in HEK293 cells assessed as increase in compound uptake at 0.1 uM incubated for 2 mins by LC-MS/MS analysis relative to control empty vector transfected cells	2019	Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21	Opioids as Substrates and Inhibitors of the Genetically Highly Variable Organic Cation Transporter OCT1.
AID149321	In vito concentration required to displace [3H]cyclofoxy (Kd = 0.8 nM and concentration is 1.3 nM) from mu and kappa2 receptor in rat brain membranes.	1992	Journal of medicinal chemistry, Jul-24, Volume: 35, Issue:15	Probes for narcotic receptor mediated phenomena. 18. Epimeric 6 alpha- and 6 beta-iodo-3,14-dihydroxy-17-(cyclopropylmethyl)-4,5 alpha-epoxymorphinans as potential ligands for opioid receptor single photon emission computed tomography: synthesis, evaluati
AID148624	Inhibition of 0.5 nM [3H]bremazocine binding to guinea pig brain membrane opioid receptors	1992	Journal of medicinal chemistry, Jun-26, Volume: 35, Issue:13	Electrophilic opioid ligands. Oxygen tethered alpha-methylene-gamma-lactone, acrylate, isothiocyanate, and epoxide derivatives of 6 beta-naltrexol.
AID149125	Binding affinity determined on Opioid receptor kappa 1 in Guinea pig brain membranes using radioligand [3H]U-69593	1998	Journal of medicinal chemistry, Dec-17, Volume: 41, Issue:26	Identification of an opioid kappa receptor subtype-selective N-substituent for (+)-(3R,4R)-dimethyl-4-(3-hydroxyphenyl)piperidine.
AID148586	Displacement of [3H]diprenorphine from opioid receptor kappa 1 expressed in HEK 293 cells	2001	Journal of medicinal chemistry, Mar-15, Volume: 44, Issue:6	Investigation of the selectivity of oxymorphone- and naltrexone-derived ligands via site-directed mutagenesis of opioid receptors: exploring the "address" recognition locus.
AID227049	Competitive inhibition of Ethylketazocine on Guinea pig ileal longitudinal muscle for the opioid receptor kappa at 100 nM	1991	Journal of medicinal chemistry, May, Volume: 34, Issue:5	Role of spacer and address components in peptidomimetic delta opioid receptor antagonists related to naltrindole.
AID125752	Antagonist activity against morphine was determined in vitro in mice using tail flick assay	1990	Journal of medicinal chemistry, Feb, Volume: 33, Issue:2	Conjugate addition ligands of opioid antagonists. Methacrylate esters and ethers of 6 alpha- and 6 beta-naltrexol.
AID150394	Inhibition of stereospecific [3H]diprenorphine binding to opioid receptors of rat brain homogenates by 50% in the presence of Na	1982	Journal of medicinal chemistry, Feb, Volume: 25, Issue:2	Common anionic receptor site hypothesis: its relevance to the antagonist action of naloxone.
AID595127	Antagonist activity at human kappa opioid receptor expressed in CHO cells assessed as inhibition of U69,593 stimulated [35S]GTPgammaS binding	2010	ACS medicinal chemistry letters, Oct-14, Volume: 1, Issue:7	1-Substituted 4-(3-Hydroxyphenyl)piperazines Are Pure Opioid Receptor Antagonists.
AID395298	Antagonist activity against kappa opioid receptor in mouse vas deferens assessed as effect on U69593-induced contraction	2009	Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6	14 beta-O-cinnamoylnaltrexone and related dihydrocodeinones are mu opioid receptor partial agonists with predominant antagonist activity.
AID148182	The compound was tested for antagonist activity by selective inhibition of [35S]GTP-gamma-S, binding to Opioid receptor mu 1 in Guinea pig caudate stimulated by DAMGO[mu]	1998	Journal of medicinal chemistry, May-21, Volume: 41, Issue:11	Investigation of the N-substituent conformation governing potency and mu receptor subtype-selectivity in (+)-(3R, 4R)-dimethyl-4-(3-hydroxyphenyl)piperidine opioid antagonists.
AID1054700	Induction of withdrawal symptoms in chronic morphine-exposed Swiss-Webster mouse assessed as decrease in wet dog shakes at 1 mg/kg, sc measured over 20 mins	2013	Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22	Design, synthesis, and biological evaluation of 14-heteroaromatic-substituted naltrexone derivatives: pharmacological profile switch from mu opioid receptor selectivity to mu/kappa opioid receptor dual selectivity.
AID169772	Antagonistic potency of compound after subcutaneous administration in rats	1982	Journal of medicinal chemistry, Feb, Volume: 25, Issue:2	Common anionic receptor site hypothesis: its relevance to the antagonist action of naloxone.
AID1611813	Inhibition of morphine-induced delays in intestinal transit in po dosed ICR mouse administered via gavage pretreated with compound and 30 mins later injected with morphine followed 5 mins later by ingestion of test meal and measured after 60 mins	2019	ACS medicinal chemistry letters, Dec-12, Volume: 10, Issue:12	Discovery of Axelopran (TD-1211): A Peripherally Restricted μ-Opioid Receptor Antagonist.
AID386623	Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells at 100 uM by confocal microscopy	2008	Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19	Structural requirements for drug inhibition of the liver specific human organic cation transport protein 1.
AID270157	Agonist activity at delta opioid receptor at 31.6 uM	2006	Journal of medicinal chemistry, Sep-07, Volume: 49, Issue:18	Highly potent and selective phenylmorphan-based inverse agonists of the opioid delta receptor.
AID767594	Displacement of [3H]-naloxone from mouse mu opioid receptor expressed in CHO cells after 1.5 hrs	2013	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 23, Issue:18	Structure activity relationship studies of 17-cyclopropylmethyl-3,14β-dihydroxy-4,5α-epoxy-6α-(isoquinoline-3'-carboxamido)morphinan (NAQ) analogues as potent opioid receptor ligands: preliminary results on the role of electronic characteristics for affin
AID125760	Compound was evaluated for antagonist activity only at subagonistic dose levels by mouse hotplate procedure	1981	Journal of medicinal chemistry, Jul, Volume: 24, Issue:7	Allylprodine analogues as receptor probes. Evidence that phenolic and nonphenolic ligands interact with different subsites on identical opioid receptors.
AID274396	Antagonist activity assessed as inhibition of loperamide-stimulated [35S]GTPgammaS binding to human mu opioid receptor expressed in CHO cells	2006	Journal of medicinal chemistry, Dec-14, Volume: 49, Issue:25	Synthesis and pharmacological evaluation of novel octahydro-1H-pyrido[1,2-a]pyrazine as mu-opioid receptor antagonists.
AID149848	Selectivity ratio of binding affinity towards kappa of guinea pig brain membrane to delta receptors of rat brain membranes	1999	Journal of medicinal chemistry, Sep-09, Volume: 42, Issue:18	Synthesis, opioid receptor binding, and biological activities of naltrexone-derived pyrido- and pyrimidomorphinans.
AID167701	Percent change of rate in the respiratory activity was measured in rabbit at 0.1 mg/kg dose given intravenously	1989	Journal of medicinal chemistry, Feb, Volume: 32, Issue:2	Synthesis and biological evaluation of 14-alkoxymorphinans. 2. (-)-N-(cyclopropylmethyl)-4,14-dimethoxymorphinan-6-one, a selective mu opioid receptor antagonist.
AID149415	Compound was tested for the inhibition of [35S]GTP-gamma-S, binding to Opioid receptor kappa 1	1998	Bioorganic & medicinal chemistry letters, Nov-17, Volume: 8, Issue:22	N-substituted octahydro-4a-(3-hydroxyphenyl)-10a-methyl-benzo[g]isoquinolines are opioid receptor pure antagonists.
AID625289	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver disease	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID273135	Displacement of [3H]DAMGO from mu opioid receptor in guinea pig brain homogenate	2006	Journal of medicinal chemistry, Oct-05, Volume: 49, Issue:20	Structural determinants of opioid activity in derivatives of 14-aminomorphinones: effects of changes to the chain linking of the C14-amino group to the aryl ring.
AID149409	Binding affinity against Opioid receptor kappa 1 of guinea pig brain membranes using 1 nM of (-)-[3H]ethylketazocine as radioligand	1986	Journal of medicinal chemistry, Jul, Volume: 29, Issue:7	Peptides as receptor selectivity modulators of opiate pharmacophores.
AID540214	Clearance in rat after iv administration	2005	Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7	Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure.
AID625290	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1191373	Displacement of [3H]diprenorphine from human recombinant mu opioid receptor expressed in HEK cells after 60 mins	2015	European journal of medicinal chemistry, Jan-27, Volume: 90	Novel fluoroalkyl derivatives of selective kappa opioid receptor antagonist JDTic: Design, synthesis, pharmacology and molecular modeling studies.
AID233705	Selectivity ratio was determined from Ke value of Opioid receptor kappa 1 and Opioid receptor delta 1	1990	Journal of medicinal chemistry, Jun, Volume: 33, Issue:6	Design of peptidomimetic delta opioid receptor antagonists using the message-address concept.
AID1079937	Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID239076	Binding affinity against Opioid receptor kappa 1 expressed in CHO cells using [3H]U-69593 as radioligand	2005	Bioorganic & medicinal chemistry letters, Apr-15, Volume: 15, Issue:8	Synthesis and opioid receptor binding properties of a highly potent 4-hydroxy analogue of naltrexone.
AID622102	Selectivity ratio of Ki for guinea pig kappa opioid receptor to mouse mu opioid receptor	2011	Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20	Synthesis of novel triplet drugs with 1,3,5-trioxazatriquinane skeletons and their pharmacologies. Part 2: Synthesis of novel triplet drugs with the epoxymethano structure (capped homotriplet).
AID1347107	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347098	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347108	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347083	qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen	2020	Antiviral research, 01, Volume: 173	A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347105	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347154	Primary screen GU AMC qHTS for Zika virus inhibitors	2020	Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49	Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID651635	Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1347082	qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal	2020	Antiviral research, 01, Volume: 173	A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347106	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347095	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347424	RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)	2019	The Journal of biological chemistry, 11-15, Volume: 294, Issue:46	Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347094	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347086	qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal	2020	Antiviral research, 01, Volume: 173	A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347407	qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection	2020	ACS chemical biology, 07-17, Volume: 15, Issue:7	High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347092	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1745845	Primary qHTS for Inhibitors of ATXN expression
AID1508630	Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay	2021	Cell reports, 04-27, Volume: 35, Issue:4	A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347093	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347425	Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)	2019	The Journal of biological chemistry, 11-15, Volume: 294, Issue:46	Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347104	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1159550	Human Phosphogluconate dehydrogenase (6PGD) Inhibitor Screening	2015	Nature cell biology, Nov, Volume: 17, Issue:11	6-Phosphogluconate dehydrogenase links oxidative PPP, lipogenesis and tumour growth by inhibiting LKB1-AMPK signalling.
AID1159607	Screen for inhibitors of RMI FANCM (MM2) intereaction	2016	Journal of biomolecular screening, Jul, Volume: 21, Issue:6	A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
AID1347411	qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary	2020	ACS chemical biology, 07-17, Volume: 15, Issue:7	High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	1386 (16.72)	18.7374
1990's	1960 (23.65)	18.2507
2000's	2081 (25.11)	29.6817
2010's	2136 (25.77)	24.3611
2020's	725 (8.75)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Publication Type	This drug (%)	All Drugs (%)
Trials	1,228 (14.04%)	5.53%
Reviews	830 (9.49%)	6.00%
Case Studies	318 (3.64%)	4.05%
Observational	13 (0.15%)	0.25%
Other	6,356 (72.68%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (418)

Trial Overview

Trial	Phase	Enrollment	Study Type	Start Date	Status
Naltrexone and Cognitive-Behavioral Therapy for Patients With Alcoholism and Post-Traumatic Stress Disorder [NCT00006489]	Phase 4	165 participants (Actual)	Interventional	2000-12-31	Completed
A Proof-of-Concept, Multicenter, Randomized, Double-Blind, Parallel Study of Naltrexone Sustained-Release (SR) and/or Fluoxetine Therapy in the Treatment of Subjects With Obsessive-Compulsive Disorder (OCD) [NCT00758966]	Phase 2	8 participants (Actual)	Interventional	2008-09-30	Terminated(stopped due to Sponsor Decision- Financial Considerations)
Naltrexone and CBT for Problem-Drinking MSM [NCT01115894]	Phase 3	200 participants (Actual)	Interventional	2007-02-28	Active, not recruiting
Comparing Treatments for HIV-Infected Opioid Users in an Integrated Care Effectiveness Study (CHOICES) Scale-Up [NCT03275350]	Phase 2/Phase 3	114 participants (Actual)	Interventional	2018-02-05	Completed
Opioid Modulation of the Effect of Alcohol on the Dopaminergic Reward System: a [18F]-Fallypride- and [18F]-Fluoro-DOPA-PET Study. [NCT03854942]	Phase 1	43 participants (Actual)	Interventional	2011-08-30	Terminated(stopped due to Recruitment rate could not be met in the study period, review group was dissolved before regular end of study. Recruitment was therefore terminated.)
Opioid Modulation of Two Models of Pain Inhibition in Healthy Controls and Patients With Temporomandibular Disorder (TMD) [NCT01327326]		0 participants (Actual)	Interventional	2011-12-31	Withdrawn
Naltrexone Effects on Alcohol Intake Using a Laboratory Bar in Asp40 Positive and Negative Alcohol Users Characterized by fMRI and Genetic Screening [NCT00254670]		0 participants	Interventional	2005-02-28	Completed
IC PaIN Trial: Interstitial Cystitis Pain Improvement With Naltrexone, the Effect of Low Dose Naltrexone on Symptoms and Pain of Patients With Interstitial Cystitis/Painful Bladder Syndrome a Randomized Placebo-controlled Prospective Trial [NCT04313972]	Phase 4	2 participants (Actual)	Interventional	2021-09-07	Completed
Phase 2 Comparison of Low-Dose Naltrexone vs ARV Effectiveness in HIV+ Progression [NCT01174914]	Phase 2	171 participants (Actual)	Interventional	2008-03-31	Completed
Long-acting Injectable Naltrexone Induction: A Randomized Trial of Outpatient Opioid Detoxification With Naltrexone vs. Buprenorphine [NCT01377610]	Phase 1	150 participants (Actual)	Interventional	2011-06-30	Completed
Naltrexone-induced Blockade of Neural Responses Induced by Fast-Acting Antidepressant Effects [NCT04322526]	Phase 4	25 participants (Actual)	Interventional	2017-07-01	Completed
Trial Evaluating Effectiveness of Contrave (Naltrexone HCl / Bupropion HCl) for Weight Maintenance in Adults With BMI ≥ 27 Kg/m2, After 6 Month Intensive Behavior Modification Program: Contrave Obesity Trials (COR) Weight Maintenance Study [NCT04589130]	Phase 4	89 participants (Actual)	Interventional	2021-02-01	Active, not recruiting
A Randomized Controlled Trial Evaluating the Effectiveness of Contrave (Naltrexone HCl and Bupropion HCl) in Patients Who Have Weight Recidivism Following Bariatric Surgery: Contrave Obesity Trials (COR) Weight Regain Study [NCT04587843]	Phase 4	18 participants (Actual)	Interventional	2021-04-01	Active, not recruiting
Naltrexone Plus Ketamine for the Rapid Treatment of Major Depressive Disorder and Alcohol Use Disorder [NCT03658330]	Phase 2	5 participants (Actual)	Interventional	2016-05-31	Completed
Naltrexone in the Treatment of Dissociative Symptoms in Patients With Borderline Personality Disorder [NCT01133301]	Phase 2	30 participants (Actual)	Interventional	1998-08-31	Completed
An fMRI Study of Opioid-related Changes in Neural Activity [NCT02818036]		82 participants (Actual)	Interventional	2016-08-31	Completed
Low-Dose Naltrexone for the Treatment of Painful Diabetic Neuropathy, a Small, Randomized, Double-blind, Placebo-controlled Crossover Trial [NCT04678895]	Phase 2	35 participants (Anticipated)	Interventional	2020-12-22	Recruiting
Phase 1 Study of Interactions Between Oral Naltrexone and Bupropion and Intravenous Methamphetamine in Methamphetamine Experienced Volunteers [NCT01359930]	Phase 1	16 participants (Anticipated)	Interventional	2011-08-31	Completed
An Open-Label, Phase I Study of the Pharmacokinetics and Bioavailability of Single, Ascending Subcutaneous Doses of Methylnaltrexone Versus Intravenous Dose in Normal, Healthy Male Volunteers [NCT01367496]	Phase 1	6 participants (Actual)	Interventional	2002-06-30	Completed
A Phase 1, Single-Center, Dose-Escalation Study to Determine the Safety and Pharmacokinetics of a Single Oral Dose of PF614 in Healthy Subjects Compared to OxyContin® [NCT02454712]	Phase 1	64 participants (Actual)	Interventional	2016-11-16	Completed
A Randomized, Double-Blind, Placebo/Positive Controlled, Evaluation of the Effects of MNTX on ECG Parameters and Cardiac Repolarization in Normal Volunteers [NCT01363323]	Phase 1	546 participants (Actual)	Interventional	2004-11-30	Completed
A Phase I, Randomized, Open-Label, Active- and Placebo-Controlled Parallel Group Study of the Effect of Subcutaneous and Intravenous Methylnaltrexone on CYP450 2D6 Activity in Healthy Extensive Metabolizers of Dextromethorphan [NCT01367535]	Phase 1	54 participants (Actual)	Interventional	2006-03-31	Completed
A Phase 3, Randomized, Double-blind, Placebo-controlled, Parallel Group Study to Evaluate the Safety, Tolerability, and Efficacy of Naltrexone for Use in Conjunction With Buprenorphine in Adults With Opioid Use Disorder Transitioning From Buprenorphine Ma [NCT02696434]	Phase 3	101 participants (Actual)	Interventional	2016-04-30	Completed
Biomarkers of Disease and Response to Treatment in Opioid Addiction [NCT02324725]	Phase 4	32 participants (Actual)	Interventional	2011-10-31	Completed
Oral Naltrexone for Improved Medication Compliance Among HIV-infected Men With Alcohol Use Disorder [NCT01377168]	Phase 4	159 participants (Actual)	Interventional	2014-05-31	Completed
Buprenorphine as Adjunct to Outpatient Induction Onto Vivitrol [NCT03113409]	Phase 2/Phase 3	10 participants (Actual)	Interventional	2017-06-01	Terminated(stopped due to no funding available to continue)
Fibromyalgia and Naltrexone: The FINAL Study [NCT04270877]	Phase 2	99 participants (Actual)	Interventional	2021-01-06	Completed
A Phase 3b Efficacy and Safety Study of Adjunctive ALKS 5461 in Treatment Refractory Major Depressive Disorder [NCT03188185]	Phase 3	278 participants (Actual)	Interventional	2017-06-12	Completed
Comparing Medication Maintenance in Comprehensive Community and Pharmacy Settings to Enhance Engagement [NCT03766893]	Early Phase 1	11 participants (Actual)	Interventional	2018-09-01	Completed
Pilot Study of Opioid-receptor Antagonists to Reduce Pain and Inflammation Among HIV-Infected Persons With Alcohol Problems [NCT04052139]	Phase 2	45 participants (Actual)	Interventional	2021-01-25	Completed
A Randomized, Double-Blind, Placebo- and Moxifloxacin Positive-Controlled (Open-Label), Cross-Over Study to Evaluate the Potential Effect of Naltrexone and Bupropion Extended-Release Combination on Cardiac Repolarization in Healthy Subjects [NCT02735603]	Phase 1	84 participants (Actual)	Interventional	2016-04-30	Completed
A Pilot Study of Low Dose Naltrexone Use in Patients With Postural Orthostatic Tachycardia Syndrome [NCT05363514]	Phase 4	80 participants (Anticipated)	Interventional	2024-01-31	Not yet recruiting
Opioid Modulation and Neural Reward Activation in Healthy Adults [NCT04854551]	Phase 1/Phase 2	13 participants (Actual)	Interventional	2021-05-01	Completed
12-month Randomized, Double-blind, Placebo-controlled, Pharmacological Clinical Trial to Evaluate the Effectiveness, Cost-utility and Neurobiological Effects of Low-dose Naltrexone in Patients With Fibromyalgia (INNOVA Project) [NCT04739995]	Phase 4	120 participants (Anticipated)	Interventional	2022-06-01	Enrolling by invitation
Single-Dose, Open-Label, Two-Period, Two-Treatment, Two-Sequence Crossover Exploratory Bioavailability Study of Subsys® (Fentanyl Sublingual Spray), 400 mcg, and Fentanyl Citrate Injection 2 mL x 0.05 mg/mL (Total Dose 100 mcg) Under Fasted Conditions [NCT02138396]		12 participants (Actual)	Interventional	2014-01-31	Completed
An Open Label, Single Dose, Randomized, Two Way Crossover Study to Estimate Oxycodone Relative Bioavailability in Healthy Volunteers Following Administration of PF 00345439 Formulation K 40 Mg Under Fasting Conditions With 40% Ethanol Compared With Water [NCT02165930]	Phase 1	17 participants (Actual)	Interventional	2014-07-31	Completed
The Evaluation of Safety and Tolerance of Commercially Available Naltrexone Administered Daily - Assessment for CBRN Operations [NCT03879460]	Phase 1	15 participants (Actual)	Interventional	2019-03-18	Completed
CURE Addiction Center of Excellence: Brain Mechanisms of Relapse and Recovery - Prescription Opiates/Medication [NCT01587196]	Phase 2	72 participants (Anticipated)	Interventional	2012-01-31	Completed
Novel Interventions to Reduce Stress Induced Non-homeostatic Eating [NCT01175512]	Early Phase 1	42 participants (Actual)	Interventional	2010-07-31	Completed
A Single Dose Study to Evaluate the Pharmacokinetics of Oxycodone and PF614 When PF614 Solution is Co-Administered With Nafamostat, as an Immediate Release Solution and/or Extended Release (ER) Capsule Formulations in Healthy Subjects [NCT05090280]	Phase 1	111 participants (Actual)	Interventional	2021-12-01	Active, not recruiting
Naltrexone Sustained Release (SR) 32 mg and Bupropion Sustained Release (SR) 360 mg Combination Therapy in Functional Magnetic Resonance Imaging (fMRI) Changes in Overweight or Obese Subjects [NCT00711477]	Phase 2	46 participants (Actual)	Interventional	2008-09-30	Completed
Effect of Naltrexone and Bupropion Combination on Weight Loss and Smoking Cessation in Obese, Cigarette-smoking Patients With Schizophrenia [NCT02736474]	Phase 4	22 participants (Actual)	Interventional	2016-05-31	Completed
Pilot Study Into Low Dose Naltrexone (LDN) and Nicotinamide Adenine Dinucleotide (NAD+) for Treatment of Patients With Post-COVID-19 Syndrome (Long-COVID19) [NCT04604704]	Phase 2	36 participants (Actual)	Interventional	2021-01-28	Completed
Treatment of Chronic Itch in Atopic Dermatitis With Oral Clonidine and Oral Naltrexone: Nerve Function [NCT02268448]	Phase 1	8 participants (Actual)	Interventional	2015-07-31	Completed
Treatment of Chronic Itch in Atopic Dermatitis With Opioid Antagonist Naltrexone and Effects on Skin Circadian Rhythm [NCT04325802]	Phase 2	0 participants (Actual)	Interventional	2022-12-31	Withdrawn(stopped due to Covid-19 pandemic)
A Phase 1b, Randomized 2-Part Single-Center Study to Evaluate the PK and Safety of Multiple Ascending Oral Doses of PF614 and the Food Effect and BA/BE of Single Oral Doses of PF614 Relative to OxyContin in Healthy Adult Subjects [NCT05043766]	Phase 1	84 participants (Actual)	Interventional	2021-09-08	Completed
A Randomized Placebo-Controlled, Crossover-Design Study of the Effects of Low Dose Naltrexone on Quality of Life as Measured by the Multiple Sclerosis Quality of Life Inventory (MSQLI54) [NCT00501696]	Phase 3	80 participants (Actual)	Interventional	2007-02-28	Completed
A Feasibility Study for Testing the Effects of Extended-release Naltrexone (Vivitrol) on Recidivism and Other Participant Outcomes in Drug Court Settings [NCT02978417]	Phase 4	14 participants (Actual)	Interventional	2017-09-21	Completed
The Comparison of Stress Response to Rapid Opioid Detoxification Applying Different Methods of Opioid Antagonism With Naltrexone and Sedation [NCT02362256]		60 participants (Actual)	Interventional	2014-05-31	Completed
Emergency Department-Initiated Medications for Alcohol Use Disorder [NCT05827159]	Phase 3	240 participants (Anticipated)	Interventional	2023-11-30	Not yet recruiting
Trial of Naltrexone and Dextromethorphan for Gulf War Veterans Illnesses [NCT02206490]	Phase 2	60 participants (Actual)	Interventional	2012-01-31	Completed
VIVITROL® (Naltrexone for Extended Release Injectable Suspension (XR-NTX)) for Opioid Dependent Inmates Released From Prison [NCT01563718]	Phase 4	26 participants (Actual)	Interventional	2012-03-31	Completed
Two-Period, Two-Treatment, Randomized Crossover Study of the Pharmacokinetics of Nalmefene by Intranasal and Intramuscular Administration in Healthy Volunteers [NCT04759768]	Phase 1	68 participants (Actual)	Interventional	2021-02-08	Completed
Study of Immunomodulation Using Naltrexone and Ketamine for COVID-19 [NCT04365985]	Phase 2	70 participants (Actual)	Interventional	2020-04-29	Terminated(stopped due to Because of the decrease in COVID cases, enrollment is extremely low. Given the current study design, it is not possible to gather data necessary to answer the question about whether study treatment reduces mortality)
Single-dose Interventions to Reduce Re-admissions for Hospitalized Patients With Refractory Alcohol Use Disorder: A Randomized Pilot Feasibility Study. [NCT04562779]	Early Phase 1	44 participants (Actual)	Interventional	2021-01-19	Completed
Promoting Medications for Alcohol Use Disorder on the General Medicine Service at Yale New Haven Hospital: a Pilot Study [NCT04287790]		67 participants (Actual)	Observational	2020-01-01	Terminated(stopped due to COVID-19 disrupted recruitment)
A Breath-based Naltrexone Adherence Tool to Manage Narcotic-addicted HIV Patients. [NCT02194764]		8 participants (Actual)	Interventional	2014-06-30	Completed
Cognitive-Behavioral and Pharmacologic Treatment of Binge-Eating Disorder and Obesity [NCT03946111]	Phase 2/Phase 3	40 participants (Anticipated)	Interventional	2019-08-07	Recruiting
Effectiveness of Low-doses of Naltrexone (LDN) on Pain Perception and Quality of Life in Women With Vulvodynia [NCT05955313]	Phase 2	300 participants (Anticipated)	Interventional	2023-05-31	Recruiting
A Multicenter, Randomized, Double-Blind, Placebo-Controlled Study Comparing the Safety and Efficacy of Naltrexone Sustained Release (SR)/Bupropion SR and Placebo in Subjects With Obesity Participating in a Behavior Modification Program [NCT00456521]	Phase 3	793 participants (Actual)	Interventional	2007-03-31	Completed
A Double Blind Randomized Trial of Low-dose Naltrexone for Post-COVID Fatigue Syndrome [NCT05430152]	Phase 2	160 participants (Anticipated)	Interventional	2023-12-31	Not yet recruiting
An Open-Label Study Assessing the Safety and Efficacy of Naltrexone Sustained Release (SR)/Bupropion Sustained Release (SR) in Overweight or Obese Subjects With Major Depression [NCT00624858]	Phase 2	25 participants (Anticipated)	Interventional	2008-01-31	Completed
OLANI PK/Safety Study in Healthy Volunteers [NCT03810495]	Phase 1	20 participants (Actual)	Interventional	2019-04-11	Completed
Phase IV Pragmatic Randomized Controlled Study to Assess the Effect of Naltrexone Hydrochloride Extended Release (ER) and Bupropion Hydrochloride ER Combination (Contrave®/Mysimba®) on the Occurrence of Major Adverse Cardiovascular Events [NCT06098079]	Phase 4	8,400 participants (Anticipated)	Interventional	2024-01-31	Not yet recruiting
Naltrexone Treatment for Prolonged Grief Disorder: A Pilot Study [NCT04547985]	Phase 4	9 participants (Actual)	Interventional	2021-01-05	Terminated(stopped due to We are terminating the study due to low accrual.)
Efficacy and Mechanisms of Naltrexone+Bupropion for Binge Eating Disorder [NCT03539900]	Phase 2/Phase 3	89 participants (Actual)	Interventional	2018-04-17	Completed
Naltrexone Treatment for Prolonged Grief Disorder: A Proof of Concept Study [NCT06140420]	Phase 4	48 participants (Anticipated)	Interventional	2023-08-01	Recruiting
Defining the Clinical Role of Topiramate in the Treatment of Alcohol Dependence in Australia [NCT03479086]	Phase 3	180 participants (Anticipated)	Interventional	2017-06-20	Recruiting
The Safety and Efficacy of Naltrexone and Scopolamine Utilized in Combination in the Treatment of Major Depression: A Double Blinded, Randomized, Controlled Pilot Study [NCT03386448]	Phase 4	14 participants (Actual)	Interventional	2018-01-01	Completed
Adherence to HIV Therapy in Heroin Addicts: Oral vs. Extended Release Naltrexone [NCT01101815]	Phase 2	200 participants (Actual)	Interventional	2010-06-30	Completed
Pharmacokinetic Evaluation of Intranasal Naltrexone and Naloxone Administered Separately and in Combination in Healthy Volunteers [NCT03851731]	Phase 1	12 participants (Actual)	Interventional	2015-10-05	Completed
Collaborative Care for Alcohol Use Disorders in the Patient-centered Medical Home [NCT02885311]	Phase 1/Phase 2	27 participants (Actual)	Interventional	2017-01-31	Completed
Brain Imaging Study on the Effects of Treatment With Naltrexone on Cue-induced Craving and Brain's Metabolic Changes in Alcohol and Cannabis-dependent Patients [NCT01560013]		24 participants (Anticipated)	Interventional	2012-10-31	Not yet recruiting
Impact of Colchicine and Low-dose Naltrexone on COVID-19 Disease Progression and Clinical Course in Hospitalized Patients [NCT04756128]	Phase 2	142 participants (Actual)	Interventional	2021-01-25	Completed
Naltrexone and Behavioral Drug and HIV Risk Reduction Counseling in Russia [NCT01389167]	Phase 3	320 participants (Anticipated)	Interventional	2011-09-30	Completed
Phase 1, Double-blind, Randomized, 2-Period, 2-Treatment Crossover Study to Evaluate the Safety of SP-104 Compared to Immediate Release Naltrexone Capsules in Healthy Adult Subjects [NCT04958876]	Phase 1	52 participants (Actual)	Interventional	2021-10-04	Completed
Alcohol Dependence: Study of the Possible Reduction of Compulsion by Association of Naltrexone With Poly-unsaturated Fatty Acids (PUFAs) [NCT01211769]	Phase 3	80 participants (Actual)	Interventional	2006-02-28	Completed
Effective Treatment for Prescription Opioid Abuse [NCT00719095]	Phase 2	105 participants (Actual)	Interventional	2006-04-30	Completed
Validation of a Test System for Development of Medications for Alcoholism [NCT02652585]	Phase 3	46 participants (Actual)	Interventional	2016-02-29	Completed
Naltrexone Treatment in Pathologic Gambling Disorder [NCT00053677]	Phase 3	83 participants (Actual)	Interventional	2002-12-31	Completed
Medication-Assisted Treatment for Youth With Substance Use Disorders [NCT02593474]	Phase 1	11 participants (Actual)	Interventional	2015-09-30	Completed
Efficacy of Naltrexone in Women's Smoking Cessation [NCT00271024]	Phase 2	333 participants (Actual)	Interventional	2005-12-31	Completed
Effects of Low Dose Naltrexone in Fibromyalgia [NCT00568555]		53 participants (Actual)	Interventional	2007-06-30	Completed
Efficacy of Low Dose Naltrexone in Psoriasis; Clinical Trial in a Tertiary Care Hospital of Karachi. [NCT04250792]	Phase 1	42 participants (Actual)	Interventional	2019-01-01	Completed
Defining an Endopheneotype for Alcohol Treatment With Naltrexone [NCT00817089]	Phase 4	24 participants (Actual)	Interventional	2007-12-31	Completed
Delivering Transcutaneous Auricular Neurostimulation to Improve Relapse Prevention in Opioid Use Disorder [NCT05053503]		168 participants (Anticipated)	Interventional	2022-05-25	Recruiting
Low Dose Naltrexone for Treatment of Pain in Patients With Fibromyalgia - Effect Via a Central Mechanism? A Randomized, Double-blinded, Placebo-controlled, Crossover Study. [NCT02806440]	Phase 4	140 participants (Anticipated)	Interventional	2016-06-30	Recruiting
A Single-Center, Randomized, Double-Blind, Active- and Placebo-Controlled Crossover Study to Evaluate the Subjective Effects of PTI-801 in Non-Physically Dependent Subjects With a History of Drug Abuse [NCT00734461]	Phase 2	14 participants (Actual)	Interventional	2007-08-31	Completed
An Open-Label Study Assessing the Safety and Efficacy of Naltrexone Sustained Release (SR) in Combination With Bupropion Sustained Release (SR) in Overweight and Obese, Nicotine-Dependent Subjects [NCT00563563]	Phase 2	30 participants (Actual)	Interventional	2007-10-31	Completed
A Single-Center, Open-Label Study to Evaluate the Absorption, Metabolism, and Excretion of Single Doses of [14c]-Samidorphan in Healthy Male Subjects [NCT02504463]	Phase 1	10 participants (Actual)	Interventional	2015-06-30	Completed
Prevention of Stimulant-Induced Euphoria With an Opioid Receptor Antagonist [NCT01673594]	Phase 4	37 participants (Actual)	Interventional	2012-09-30	Completed
Long Acting Naltrexone for Opioid Addiction: the Importance of Mental, Physical and Societal Factors for Sustained Abstinence and Recovery [NCT03647774]	Phase 4	317 participants (Actual)	Interventional	2018-08-01	Completed
Assessing Changes in the Brain Melanocortin System and Sensory Processing in Response to Alcohol to Advance Our Understanding of the Pathophysiology and Psychopharmacology of Binge Drinking [NCT02842073]	Phase 2	12 participants (Actual)	Interventional	2016-11-01	Completed
A Single Site, Phase 2B, Randomized, Double-Blind, Study to Assess the Efficacy, Safety, and Tolerability of Low-Dose Naltrexone and Acetaminophen Combination vs. Placebo in the Treatment of Chronic Low Back Pain (ANODYNE-4) [NCT03201393]	Phase 2	12 participants (Actual)	Interventional	2017-08-15	Completed
Improving Outcomes of Opioid Addicted Prisoners With Extended-Release Injectable Naltrexone (Vivitrol) Before vs. After Reentry [NCT02617628]	Phase 2/Phase 3	146 participants (Actual)	Interventional	2016-01-01	Completed
A Randomized Controlled Trial Comparing Buprenorphine/Naloxone With Naltrexone for Treatment in Opioid Dependent Adolescents and Young Adults [NCT01015066]	Phase 4	0 participants (Actual)	Interventional	2009-11-30	Withdrawn(stopped due to Study personnel left institution, anticipated funding did not occur)
A Double-blind, Placebo-controlled Study of Naltrexone in Trichotillomania [NCT00775229]	Phase 2	51 participants (Actual)	Interventional	2008-08-31	Completed
A Pilot Trial of Naltrexone for Methamphetamine Addiction - Role of the A118G SNP [NCT00984360]	Phase 2	22 participants (Actual)	Interventional	2009-09-30	Completed
Association of Genetic Variations and Weight Loss Response to Naltrexone/Bupropion [NCT05919797]	Phase 4	120 participants (Anticipated)	Interventional	2023-06-08	Recruiting
Exploring the Pharmacokinetic Characteristics of Different Doses of Naltrexone Implants in Patients With Alcohol Use Disorders [NCT05919017]	Phase 1	60 participants (Anticipated)	Interventional	2023-06-16	Recruiting
A Multi-Center, Randomized, Double-Blind, Placebo-Controlled Phase III Study to Assess the Efficacy and Safety of PXT3003 in Charcot-Marie-Tooth Type 1A (CMT1A) Treated 15 Months [NCT05092841]	Phase 3	176 participants (Anticipated)	Interventional	2021-09-28	Recruiting
Pharmacokinetic Evaluation of Intranasal, Intramuscular, and Oral Naltrexone in Healthy Volunteers [NCT02750748]	Phase 1	14 participants (Actual)	Interventional	2016-07-31	Completed
A Phase 1, Open-Label, Sequential Design Study to Evaluate the Potential Effect of Multiple Oral Doses of Extended-Release Combination of Naltrexone and Bupropion on the Pharmacokinetics of a Single Oral Dose of Metformin in Healthy Subjects [NCT02745912]	Phase 1	30 participants (Actual)	Interventional	2016-04-30	Completed
Use of TNF-blocking Therapy in Combination With DMARDs in Patients With Early Rheumatoid Arthritis [NCT00908089]	Phase 4	100 participants (Actual)	Interventional	2003-03-31	Active, not recruiting
Effect of Naltrexone in Achieving and Maintaining Abstinence From Alcohol in Patients With Cirrhosis- A Double Blind Randomized Controlled Trial. [NCT04391764]		100 participants (Actual)	Interventional	2020-12-06	Completed
Effects of Low-dose Naltrexone in Combination With a Range of Smoked Marijuana [NCT00743145]	Phase 2	23 participants (Actual)	Interventional	2008-05-31	Completed
Feasibility and Tolerability of a Combination of Naltrexone and Baclofen for Alcohol Dependence: A Pilot Study. [NCT00614328]	Phase 1	40 participants (Actual)	Interventional	2007-07-31	Completed
A Randomized, Double-Blind, Phase 4 Study to Evaluate the Efficacy of Naltrexone HCl/Bupropion HCl Extended Release Versus Placebo for Treatment of Weight Regain in Patients Post Bariatric Surgery [NCT02616315]	Phase 4	0 participants (Actual)	Interventional	2016-02-29	Withdrawn
Vivitrol for Reducing Driving While Impaired Behavior Among Repeat Offenders-a Pilot Study [NCT00537745]	Phase 4	14 participants (Actual)	Interventional	2007-04-30	Completed
The Effects of VIVITROL® on Alcohol-Related Cue-Induced Craving and BOLD [Blood Oxygen-level-dependent] Functional Magnetic Resolution Imaging (fMRI) Signal Activation Patterns [NCT00511836]	Phase 4	31 participants (Actual)	Interventional	2007-07-31	Completed
Use of Mysimba in Patients With Weight Regain After Bariatric Surgery [NCT04902625]	Phase 4	116 participants (Anticipated)	Interventional	2023-03-21	Recruiting
Phase 1, Open Label, Randomized, Single-dose, 3-Period, 3-Treatment Crossover Study to Evaluate the Pharmacokinetics of SP-104 Under Fasting and Fed Conditions and to Compare to Naltrexone Hydrochloride Tablets USP in Healthy Adult Subjects [NCT05002946]	Phase 1	18 participants (Actual)	Interventional	2022-01-11	Completed
Low-dose Naltrexone for Bladder Pain Syndrome: A Randomized Placebo-controlled Prospective Pilot Trial [NCT04450316]	Phase 2	40 participants (Anticipated)	Interventional	2020-10-08	Suspended(stopped due to Study temporarily suspended awaiting research personnel to resume recruitment)
Relapse Prevention in Stimulant Use Disorder [NCT04553263]	Early Phase 1	0 participants (Actual)	Interventional	2023-06-11	Withdrawn(stopped due to Study never initiated)
Revisiting Safety Signals: Examining a Separate Safety Mechanism for Social Support Figures [NCT04166071]	Early Phase 1	60 participants (Anticipated)	Interventional	2021-12-13	Enrolling by invitation
Naltrexone & SSRI in Alcoholics With Depression/PTSD [NCT00338962]	Phase 3	88 participants (Actual)	Interventional	2001-10-31	Completed
A Multicenter, Randomized, Double Blind, Placebo Controlled Study Comparing the Safety and Efficacy of Naltrexone 32 mg Sustained Release (SR)/Bupropion 360 mg Sustained Release (SR) and Placebo in Obese Subjects With Type 2 Diabetes Mellitus [NCT00474630]	Phase 3	505 participants (Actual)	Interventional	2007-05-31	Completed
Dronabinol Naltrexone Treatment for Opioid Dependence [NCT01024335]	Phase 2/Phase 3	60 participants (Actual)	Interventional	2010-01-31	Completed
An Open-label, Randomized, Single-dose, Parallel-group Study to Investigate the PK Profile of Single Dose Buprenorphine Transdermal Patch 20 mg Applied for 3 Days, 40 mg for 3 Days and 40 mg for 4 Days in Chinese Subjects With Chronic Pain [NCT03975010]	Phase 1	45 participants (Anticipated)	Interventional	2019-05-13	Recruiting
Open Label Comparison of Injectable Buprenorphine ( Brixadi®) and Naltrexone (Vivitrol®) for Opioid Use Disorder [NCT05596955]	Phase 2	60 participants (Anticipated)	Interventional	2023-01-12	Recruiting
A Multi-Center, Primary Care-Based, Open-Label Study to Assess the Success of Converting Opioid-Experienced Patients, With Chronic, Moderate to Severe Pain, to EMBEDA Using a Standardized Conversion Guide, and to Identify Behaviors Related to Prescription [NCT01179191]	Phase 4	684 participants (Actual)	Interventional	2010-08-31	Terminated(stopped due to See termination reason in detailed description.)
Non-Response to Naltrexone (NTX): Next Steps in Managing Alcoholism [NCT00115037]	Phase 4	302 participants (Actual)	Interventional	2003-09-30	Completed
Behavioral and Pharmacologic Treatment of Binge Eating and Obesity [NCT03045341]	Phase 2/Phase 3	136 participants (Actual)	Interventional	2017-02-27	Completed
Injectable Naltrexone Treatment of Alcohol Dependence in Serious Mental Illness (SMI): An Open Prospective Pilot Trial [NCT00453609]	Phase 4	15 participants (Actual)	Interventional	2007-04-30	Completed
Treatment of Chronic Itch in Atopic Dermatitis With Topical Naltrexone as Well as the Influence of Circadian Rhythm [NCT04154033]	Phase 2	0 participants (Actual)	Interventional	2020-10-01	Withdrawn(stopped due to Funding)
Dopamine D2/3- and μ-opioid Receptor Antagonists Reduce Cue-induced Reward Responding and Reward Impulsivity in Healthy Volunteers [NCT02557984]		121 participants (Actual)	Interventional	2014-02-28	Completed
[NCT00234689]		0 participants	Interventional	2002-01-31	Completed
Combined Pharmacotherapies for Alcoholism [NCT00768508]	Phase 3	300 participants (Actual)	Interventional	2008-09-30	Completed
COMBINE: Effect of Combined Pharmacotherapies and Behavioral Interventions [NCT00006206]	Phase 3	1,375 participants	Interventional	1997-08-31	Completed
Open-Label Study of the Safety and Tolerability of VIVITROL Administered to Health Care Professionals Participating in an Extended Outpatient Treatment Program for Opioid Dependence [NCT00834080]	Phase 3	38 participants (Actual)	Interventional	2009-03-31	Completed
An Exploratory Study of Naltrexone Plus Aripiprazole for Alcohol Dependence [NCT00667875]	Phase 2	65 participants (Actual)	Interventional	2008-04-30	Completed
The Effects of Naltrexone in Active Crohn's Disease [NCT00663117]	Phase 2	40 participants (Actual)	Interventional	2006-09-30	Completed
Attenuation of Pain in Men and Women: Mechanisms of Exercise-Induced Analgesia [NCT01220414]		60 participants (Actual)	Interventional	2010-09-30	Completed
Pharmacokinetics of Naltrexone Hydrochloride (HCl) Following Intravenous (i.v.) and Oral Routes of Administration in Healthy Subjects [NCT00714584]	Phase 1	18 participants (Actual)	Interventional	2003-05-31	Completed
A Long-Term, Open-Label Safety Study of ALO-01 (Morphine Sulfate Plus Naltrexone Hydrochloride Extended-Release) Capsules in Subjects With Chronic Moderate to Severe Nonmalignant Pain [NCT00415597]	Phase 3	467 participants (Actual)	Interventional	2006-12-31	Completed
The Impact of Intravenous Heroin Use on Immune Activation in Treated HIV [NCT03976258]		190 participants (Actual)	Observational	2017-07-14	Completed
Pharmacotherapy for HIV Infected Patients With Alcohol Problems [NCT00854230]	Phase 4	0 participants (Actual)	Interventional	2009-01-31	Withdrawn(stopped due to We expanded to a bigger, multi-site study & decided to close this study.)
Effect of Naltrexone on Craving and Ethanol-Induced Brain Activity [NCT00667771]	Early Phase 1	70 participants (Actual)	Interventional	2008-04-22	Completed
Pilot Study of Depot Naltrexone in Alcohol-Dependent, Homeless Veterans [NCT01155869]	Phase 4	7 participants (Actual)	Interventional	2010-08-31	Terminated(stopped due to Poor enrollment)
Naltrexone in Treatment of Cocaine Dependence [NCT00015080]	Phase 2	0 participants	Interventional	1995-05-31	Completed
Genetic and Brain Mechanisms of Naltrexone?s Treatment Efficacy for Alcoholism [NCT00920829]	Phase 4	358 participants (Actual)	Interventional	2009-06-30	Completed
Depot Naltrexone Treatment of Opioid Dependent Parolees [NCT00756990]		61 participants (Actual)	Interventional	2005-11-30	Completed
Predicting Response to Naltrexone With Eye Tracking in Videogame Disorder [NCT04649892]	Phase 2	40 participants (Anticipated)	Interventional	2021-01-31	Not yet recruiting
Methylnaltrexone for the Reversal of Opiate-Induced Constipation in the Intensive Care Unit [NCT01050595]	Phase 3	80 participants (Anticipated)	Interventional	2009-12-31	Recruiting
Understanding How Opioids Affect the Experiential and Neural Signatures of Social Experiences [NCT05007561]	Early Phase 1	210 participants (Anticipated)	Interventional	2021-11-16	Recruiting
Treatment of Pathological Gambling With Naltrexone Pharmacotherapy and Brief Intervention - a Placebo Controlled Trial [NCT01528007]	Phase 4	100 participants (Actual)	Interventional	2011-01-31	Completed
An Open-label, Non-randomized [11C]Carfentanil PET Study in Healthy Male Subjects to Investigate Brain Mu-opioid Receptor Occupancy, Pharmacokinetics, and Pharmacodynamics of Single Oral Doses of GSK1521498 and Naltrexone. [NCT00976066]	Phase 1	26 participants (Actual)	Interventional	2009-06-15	Completed
Neurocomputational Mechanisms of Mood Improvement [NCT04276259]	Phase 4	120 participants (Anticipated)	Interventional	2020-10-19	Recruiting
Combining Medications for the Treatment of Alcohol Dependence: An Inpatient Preliminary Study [NCT00769158]	Phase 1	4 participants (Actual)	Interventional	2008-10-31	Completed
Naltrexone for At-Risk and Problem Drinking in Smoking Cessation Treatment [NCT00938886]	Phase 2	150 participants (Actual)	Interventional	2009-10-31	Completed
A Multicenter, Randomized, Double Blind, Placebo Controlled Study Comparing the Safety and Efficacy of Naltrexone Sustained Release (SR)/Bupropion Sustained Release (SR) and Placebo in Obese Subjects [NCT00567255]	Phase 3	1,496 participants (Actual)	Interventional	2007-12-31	Completed
In Hospital Administration of Extended-Release Naltrexone for Alcohol Use Disorder: A Pilot Study of Feasibility and Acceptability [NCT05087771]	Phase 4	0 participants (Actual)	Interventional	2022-03-31	Withdrawn(stopped due to no longer randomized, drug being offered to all patients)
A Randomized, Double-Blind, Triple-Dummy, Single-Dose, Four-Way Crossover Study to Determine the Relative Bioavailability, Pharmacodynamic Effects, and Safety of Equivalent Doses of Whole and Crushed ALO-01 Versus Morphine IR in Opioid Experienced, Non-De [NCT00751478]	Phase 1/Phase 2	32 participants (Actual)	Interventional	2007-03-31	Completed
A Phase 2, Multicenter, Randomized, Double-Blind, Placebo-Controlled, Full-Factorial, Parallel-Group Study Evaluating Safety and Efficacy of Naltrexone-Acetaminophen Combination in Acute Migraine Treatment in Adults, With Exploratory Focus on Co-Occurring [NCT05685225]	Phase 2	300 participants (Anticipated)	Interventional	2024-03-01	Not yet recruiting
Low Dose Naltrexone for Chronic Pain in Osteoarthritis and Inflammatory Arthritis [NCT04115020]	Phase 2	0 participants (Actual)	Interventional	2020-01-31	Withdrawn(stopped due to A pilot study was negative.)
The Efficacy of Low Dose Naltrexone Therapy in Children With Crohn's Disease [NCT00715117]	Phase 2	14 participants (Actual)	Interventional	2008-07-31	Completed
Pilot Trial of Naltrexone for Obesity in Women With Schizophrenia [NCT00793780]		24 participants (Actual)	Interventional	2008-12-31	Completed
Opioid Relapse & HIV Risk: 48 Versus 24 Weeks of Injectable Extended Release Naltrexone [NCT01882361]	Phase 2/Phase 3	77 participants (Actual)	Interventional	2013-06-30	Completed
Low Dose Naltrexone for the Treatment of Juvenile Primary Fibromyalgia Syndrome [NCT00855972]		0 participants (Actual)	Interventional	2010-08-31	Withdrawn(stopped due to The FDA IND application is paused due to additional required testing. The IRB protocol was closed prior to research starting.)
Comparison of Cognitive Behavioral Therapy and Motivational Enhancement Therapy Plus Naltrexone for Alcoholism [NCT00000456]	Phase 4	160 participants (Actual)	Interventional	1992-09-30	Completed
Naltrexone and Psychosocial Treatments for the Treatment of Cocaine Dependence Complicated by Alcohol Dependence [NCT00167232]	Phase 3	164 participants (Actual)	Interventional	1998-01-31	Completed
Naltrexone Treatment of Alcohol Abuse in Schizophrenia [NCT00145847]	Phase 4	90 participants (Actual)	Interventional	2003-04-30	Completed
Double-Blind, Cross-Over Trial of Ketamine Therapy Plus or Minus Naltrexone in Treatment Resistant Depression (TRD) [NCT02911597]	Phase 1	16 participants (Actual)	Interventional	2016-09-30	Completed
Alcohol Research Center Grant. Component #1. COMBINING MEDICATIONS: ALCOHOL REACTIVITY AND CONSUMPTION [NCT00183222]	Phase 2	160 participants	Interventional	2005-05-31	Completed
Naltrexone for Heavy Drinking in Young Adults [NCT00568958]	Phase 4	140 participants (Actual)	Interventional	2008-02-29	Completed
A Double-Blind, Placebo-Controlled Study of Naltrexone in Compulsive Sexual Behavior [NCT00467558]	Phase 2	7 participants (Actual)	Interventional	2007-05-31	Completed
Pharmacogenetic Investigation of Naltrexone [NCT00270231]	Phase 2	64 participants (Actual)	Interventional	2004-03-31	Completed
Gabapentin as an Adjunct to Naltrexone for Alcoholism [NCT00183196]	Phase 3	150 participants (Actual)	Interventional	2003-01-31	Completed
Comparison of Anti-TNF Therapy Plus Methotrexate, Combination Therapy of DMARDs, and Methotrexate Alone in Very Early Polyarticular Juvenile Idiopathic Arthritis. A National Randomized Multicenter Clinical Trial. [NCT01015547]	Phase 3	60 participants (Actual)	Interventional	2003-05-31	Completed
Endogenous Modulation and Central Sensitization in New Daily Persistent Headache ( NDPH ) in Children [NCT03447782]	Phase 1/Phase 2	45 participants (Actual)	Interventional	2018-07-23	Completed
Naltrexone Augmentation of Nicotine Patch Therapy [NCT00218153]	Phase 3	200 participants	Interventional	2000-11-30	Completed
Naltrexone and Psychosocial Treatments for the Treatment of Cocaine Dependence Complicated by Alcohol Dependence [NCT00218660]	Phase 3	164 participants (Actual)	Interventional	1998-04-30	Completed
Long-Acting Injectable Naltrexone Treatment of Alcohol Dependence in Primary Care vs. in Specialized Chemical Dependence Treatment: A Pilot Trial [NCT00461890]	Phase 4	20 participants (Anticipated)	Interventional	2006-10-31	Terminated
Interventional, Randomized, Double-blind, Cross-over, Placebo-controlled Study to Investigate the Effects of Nalmefene After Single Dose on the Blood Oxygen Level Dependent (BOLD) Functional Magnetic Resonance Imaging (fMRI) Signal in the Ventral Striatum [NCT01969617]	Phase 1	22 participants (Actual)	Interventional	2013-11-30	Completed
Low Dose Naltrexone to Improve Physical Health in Patients With Vasculitis [NCT03482479]	Phase 2	36 participants (Anticipated)	Interventional	2019-02-04	Recruiting
General Evaluation of Eligibility for Substance Abuse/Dependence Research [NCT00439049]		7,500 participants (Anticipated)	Observational	2005-10-31	Recruiting
Augmenting Zyprexa With Naltrexone: Normalization of the Weight Gain Side Effect and the CNS Reward and Sensory Function [NCT00567034]	Phase 1	30 participants (Actual)	Interventional	2006-12-31	Completed
Double Blind 12-week Controlled Experiment With Two Groups of Pathological Gamblers, One Taking Active Drug (Naltrexone) and the Other Receiving Placebo.Patters Patterns of Visual Tracking Will be Acessed on Both Groups Prior and During Tratment in Order [NCT04738773]	Phase 2	40 participants (Anticipated)	Interventional	2021-06-01	Not yet recruiting
Extended-Release Naltrexone for Opioid Relapse Prevention Following Release From Jail [NCT01180647]	Phase 3	48 participants (Actual)	Interventional	2010-05-31	Completed
Effects of Mu-opiate Receptor Engagement on Microbial Translocation and Residual Immune Activation in HIV-infected, ART Suppressed Opioid Use Disorder Patients Initiating Medication-assisted Treatment [NCT04480554]	Phase 2	225 participants (Anticipated)	Interventional	2023-01-30	Recruiting
Combined Pharmacotherapy in Depressed Alcoholics [NCT00006204]	Phase 4	106 participants	Interventional	2000-03-31	Completed
Vivitrol Associated With Behavioural-Relapse Prevention Strategy as Treatment for Cannabis Use Disorder [NCT04139668]	Phase 2	10 participants (Anticipated)	Interventional	2020-09-30	Not yet recruiting
Pilot Study Into the Use of Metformin and Low Dose Naltrexone (LDN) for Patients With Coronavirus Disease 2019 (COVID-19) - Assessment of Short and Long Term Effects [NCT04604678]	Phase 2	0 participants (Actual)	Interventional	2021-02-28	Withdrawn(stopped due to Unable to recruit participants due to restrictive inclusion/exclusion criteria. Will update protocol with IRB & begin anew after approval.)
Cardiovascular and Metabolic Effects of Drugs for the Treatment of Obesity [NCT04575194]	Phase 4	40 participants (Anticipated)	Interventional	2020-09-08	Recruiting
Development of a Pharmacodynamic Biomarker of Opioid Antagonism in Adolescents With Eating Disorders [NCT05509257]	Early Phase 1	60 participants (Anticipated)	Interventional	2022-09-17	Recruiting
A Randomized, Double-Blind, Placebo- and Active-Controlled, 3-Way Crossover Study to Determine the Abuse Potential of Oral Administration of Crushed EMBEDA Relative to Crushed Controlled-Release Morphine Sulfate and Placebo in Non Dependent, Recreational [NCT01380093]	Phase 1	80 participants (Actual)	Interventional	2011-02-28	Completed
A Single-Center, Randomized, Double-Blind, Two-Way Crossover Study to Evaluate Whether a Single-Dose Administration of Crushed and Whole EMBEDA Induces Clinical Opiate Withdrawal Signs and Symptoms in Opioid-Dependent Patients With Chronic, Non-Cancer Pai [NCT01100437]	Phase 4	14 participants (Actual)	Interventional	2010-04-30	Terminated(stopped due to See termination reason in detailed description.)
Pharmacokinetics of Fentanyl Citrate Following Intravenous (i.v.) and Oral Routes of Administration in Healthy Subjects [NCT00714558]	Phase 1	18 participants (Actual)	Interventional	2003-04-30	Completed
Attenuation of Opioid Effects of Three Different Doses of Sublingual Buprenorphine / Naloxone by Oral Naltrexone in Healthy Volunteers [NCT00733720]	Phase 1	8 participants (Anticipated)	Interventional	2008-08-31	Completed
Behavioral Naltrexone Therapy (BNT) for Promoting Adherence to Oral Naltrexone (BNT-oral) vs Extended Release Injectable Depot Naltrexone (Depot-BNT); a Randomized Trial [NCT00577408]	Phase 3	60 participants (Actual)	Interventional	2007-09-30	Completed
Reducing Heavy Drinking to Optimize HIV/AIDS Treatment and Prevention [NCT01227044]	Phase 2/Phase 3	51 participants (Actual)	Interventional	2011-04-30	Completed
Evaluation of Naltrexone as a Treatment for Self-Injurious Behavior [NCT02726035]	Phase 4	0 participants (Actual)	Interventional	2014-02-22	Withdrawn(stopped due to PI deceased)
Effectiveness of Alcohol Interventions Among TB Patients in Tomsk Oblast, Russia [NCT00675961]		400 participants (Actual)	Interventional	2007-01-31	Completed
The Impact of the Opiate Antagonist Naltrexone on the Emotional Valence of Dreams [NCT02792140]	Phase 4	32 participants (Actual)	Interventional	2016-03-31	Completed
Safety Evaluation of D-TRANS Fentanyl With Naltrexone HCL in Opioid Tolerant Patients (ALZA C-2002-022) [NCT00650182]	Phase 2	406 participants (Actual)	Interventional	2003-01-31	Completed
Extended Release Naltrexone for Treating Amphetamine Dependence in Iceland [NCT01100853]	Phase 3	100 participants (Actual)	Interventional	2010-05-31	Completed
Glutamatergic Modulation to Facilitate Naltrexone Initiation in Opioid Dependence [NCT02437344]	Phase 2	16 participants (Actual)	Interventional	2015-01-31	Completed
An Open-Label Evaluation of the Independent Effect of Coadministration of a High Fat Meal and Naltrexone Blockade on the Pharmacokinetic Profile of Dilaudid OROS (Hydromorphone HCL) 16 mg [NCT00399295]	Phase 1	30 participants (Actual)	Interventional		Completed
A Proof-of-Concept, Randomized, Double-Blind and Placebo Controlled Clinical Trial With Naltrexone and Clonidine Combination (ATNC05) Compared With Placebo in the Treatment of Chronic Back Pain [NCT01415895]	Phase 2	78 participants (Actual)	Interventional	2011-07-31	Completed
A Randomized Double-Blind Placebo-Controlled Trial to Assess the Effectiveness of Low-Dose Naltrexone in Combination With Standard Treatment in Women With Chronic Pelvic Pain Secondary to Endometriosis [NCT03970330]	Phase 3	9 participants (Actual)	Interventional	2020-01-16	Terminated(stopped due to Original PI left institution, lack of funding to continue)
An ObEsity-centric Approach With and Without Anti-obesity Medications ComPared to the Usual-care ApprOach to Management of Patients With Obesity and Type 2 Diabetes in an Employer Setting: A Pragmatic Randomized Controlled Trial [NCT04531176]	Phase 4	69 participants (Actual)	Interventional	2020-09-01	Active, not recruiting
A Randomized, Open Label, Single Dose Pharmacokinetic and Safety Study of Implantable Long Acting 3-month Naltrexone Subcutaneous Pellets Compared to Naltrexone IM Injection (Vivitrol) in Healthy Volunteers [NCT04828694]	Phase 1	24 participants (Actual)	Interventional	2022-06-17	Completed
Naltrexone, Craving, and Drinking: Ecological Assessment [NCT00006203]	Phase 4	186 participants	Interventional		Completed
Extended-release Naltrexone (Vivitrol) for the Treatment of Alcohol Dependence in Urban Primary Care: a Feasibility Study [NCT00620750]	Phase 4	72 participants (Actual)	Interventional	2007-07-31	Completed
A Multicenter, Randomized, Double Blind, Placebo Controlled Study Comparing the Safety and Efficacy of Two Doses of Naltrexone Sustained Release (SR)/Bupropion Sustained Release (SR) and Placebo in Obese Subjects [NCT00532779]	Phase 3	1,742 participants (Actual)	Interventional	2007-10-31	Completed
Naltrexone & Bupropion to Stop Smoking With Less Weight Gain [NCT00129246]	Phase 1/Phase 2	40 participants (Actual)	Interventional	2004-12-31	Completed
Double-Blind Placebo-Controlled Investigation of Naltrexone for Pathological Gambling [NCT01057862]	Phase 2	9 participants (Actual)	Interventional	2009-02-28	Completed
A Randomized, Double-Blind, Placebo-Controlled, 3 Way Crossover Study Evaluating The Relative Abuse Potential Of Crushed Embeda Compared To Morphine Sulfate Controlled Release Tablets (Crushed) And Placebo In Non-Dependent, Recreational Opioid Users Follo [NCT01595867]	Phase 1	33 participants (Actual)	Interventional	2010-08-31	Completed
Naltrexone Implants Compared to Methadone Maintenance Treatment (MMT) Among Inmates About to be Released From Prison - a Randomized Controlled Trial [NCT00204243]	Phase 2	46 participants (Actual)	Interventional	2005-05-31	Completed
Assessment of and Treatment Applied to Food Addiction to Encourage Self-Management of Obesity in a Rural Healthy Behaviors Clinic [NCT03431831]	Phase 4	83 participants (Actual)	Interventional	2017-07-01	Completed
Naltrexone and CBT for Problem-drinking MSM [NCT00444418]	Phase 3	200 participants (Actual)	Interventional	2006-04-30	Completed
A Multi-site Study to Disseminate and Evaluate Pharmacotherapy for Alcohol Dependence in Convicted Drinking Drivers [NCT01638377]	Phase 4	2 participants (Actual)	Interventional	2012-08-31	Terminated(stopped due to Recruitment proved to be extremely difficult.)
Science-Based Treatment for Opioid-Dependent Adolescents [NCT00182572]	Phase 2	80 participants (Anticipated)	Interventional	2005-07-31	Recruiting
A Randomized, Double-Blind, Multiple-Dose, Parallel Group Study to Evaluate the Potential of Withdrawal Effects Following Administration of Oxycodone/Naltrexone Capsules and Oxycodone in Methadone-Maintained Opioid-Dependent Subjects [NCT02391571]	Phase 3	26 participants (Actual)	Interventional	2015-02-28	Completed
Naltrexone Treatment for Alcoholism: Predicting Outcome [NCT00000438]	Phase 4	192 participants	Interventional		Completed
Nalmefene Maintenance Treatment of Alcoholism [NCT00000450]	Phase 4	159 participants (Actual)	Interventional	1997-04-10	Completed
Feasibility, Mechanism of Action and Potential Side Effects of Extended Release Depot Naltrexone in Opioid Dependent Patients [NCT01471145]	Phase 4	40 participants (Anticipated)	Interventional	2013-01-31	Completed
Injectable Versus Oral Naltrexone Treatment of Alcohol Dependence In Serious Mental Illness (SMI): A Pilot Study [NCT00453804]	Phase 4	15 participants	Interventional	2006-07-31	Completed
An Open-Label, Multi-Center Study to Evaluate the Long-Term Safety of Medisorb® Naltrexone [NCT00156936]	Phase 3	108 participants (Actual)	Interventional	2004-08-31	Terminated(stopped due to Business decision)
Posttreatment Effects of Naltrexone [NCT00523133]	Phase 2	185 participants (Actual)	Interventional	2000-09-30	Completed
An Open Label Evaluation of the Dose Proportionality of Dilaudid SR (OROS� Hydromorphone HCL) Tablets 8mg, 16mg, 32mg, and 64mg [NCT00398957]	Phase 1	32 participants (Actual)	Interventional		Completed
Place of Low-Dose Naltrexone in Opiate Detoxification [NCT00135759]	Phase 2	174 participants (Actual)	Interventional	2005-04-30	Completed
Randomized, Placebo-Controlled Trial of Extended-Release Naltrexone and Monthly Extended-Release Buprenorphine for Cocaine Use Disorder (CURB-2) [NCT05262270]	Phase 2	426 participants (Anticipated)	Interventional	2023-04-18	Recruiting
Pilot Study of Opioid-receptor Antagonists to Reduce Pain and Inflammation Among HIV-Infected Persons With Alcohol Problems [NCT03278886]	Phase 1/Phase 2	11 participants (Actual)	Interventional	2018-07-03	Completed
Sertraline for Alcohol Dependence and Depression [NCT00004554]	Phase 4	171 participants (Actual)	Interventional	2000-01-31	Completed
Targeted Naltrexone for Problem Drinkers [NCT00369408]	Phase 4	163 participants (Actual)	Interventional	2003-06-30	Completed
An Investigation of the Effects of Opioid Receptor Blockade on Changes in Self-esteem and Attentional Bias Toward Social Cues [NCT04757506]		35 participants (Actual)	Interventional	2012-07-09	Completed
Behavioral and Biochemical Mechanisms of Self-Injury [NCT00065936]	Phase 3	37 participants	Interventional	1997-07-31	Active, not recruiting
Eating Disorder Individualized Therapeutics-Naltrexone Neuroimaging (EDIT-N2) [NCT04935931]	Early Phase 1	13 participants (Actual)	Interventional	2021-07-16	Completed
Evaluation of the Efficacy of the Opioid Antagonist Naltrexone on the Incidence and Intensity of Flashbacks and Dissociative States in Patients With Borderline Personality Disorder [NCT00124839]	Phase 3	48 participants (Anticipated)	Interventional	2005-10-31	Terminated(stopped due to Difficulties in recruiting enough subjects)
Phase II Randomized, Double-Blind Trial of Bupropion Versus Bupropion + Naltrexone for Smoking Cessation [NCT00419731]	Phase 2/Phase 3	120 participants (Anticipated)	Interventional	2006-11-30	Recruiting
Effects of Naltrexone on Nocturnal Breathing Patterns at Altitude [NCT05037032]	Phase 4	16 participants (Actual)	Interventional	2021-08-08	Completed
A Double-Blind, Placebo-Controlled Study of Naltrexone in Kleptomania [NCT00332579]	Phase 2	25 participants (Actual)	Interventional	2006-05-01	Completed
Two Medications, Disulfiram and Naltrexone, in the Treatment of Patients With Both Cocaine and Alcohol Dependence [NCT00142844]	Phase 2	208 participants (Actual)	Interventional	1999-09-30	Completed
Targeted Naltrexone for Early Problem Drinkers [NCT00000455]	Phase 4	160 participants	Interventional		Completed
Study of the Effect of Naltrexone on Cerebral Blood Flow and Hypoglycemia in Type 1 Diabetes Mellitus [NCT01053078]	Phase 1/Phase 2	29 participants (Actual)	Interventional	2009-10-31	Completed
A Randomized, Single-Dose Opiate Challenge Study of Medisorb® Naltrexone in Opioid-Using Adults [NCT01218984]	Phase 2	27 participants (Actual)	Interventional	2002-03-31	Completed
A Double-Blind Placebo-Controlled Evaluation of Effectiveness of Oral Naltrexone in Management of Adolescent Eating Disorders [NCT05073679]	Phase 2/Phase 3	60 participants (Anticipated)	Interventional	2022-04-22	Enrolling by invitation
Naltrexone for Bipolar Disorder and Alcohol Dependence [NCT00223275]	Phase 4	50 participants (Anticipated)	Interventional	2005-05-31	Completed
Opiate Dependence: Combined Naltrexone/Behavior Therapy [NCT00238914]	Phase 2	12 participants (Actual)	Interventional	1999-08-31	Completed
A Phase II Single Arm Adaptive Weight Loss Study in Women With Early Stage Breast Cancer [NCT04499950]	Phase 2	55 participants (Actual)	Interventional	2021-02-08	Active, not recruiting
Study Behavioral Naltrexone Therapy: A Novel Treatment for Heroin Dependence [NCT00332228]	Phase 2	125 participants (Actual)	Interventional	2002-06-30	Completed
Comparing Treatments for HIV-Infected Opioid and Alcohol Users in an Integrated Care Effectiveness Study [NCT01908062]	Phase 3	51 participants (Actual)	Interventional	2014-06-30	Completed
A Double-Blind, Placebo-Controlled Study of Naltrexone in Pyromania [NCT00467454]	Phase 2	0 participants (Actual)	Interventional	2007-06-30	Withdrawn(stopped due to Funding allocation to different clinical trials.)
Testing the Effectiveness of Low Dose Naltrexone for Smoking Cessation and Minimization of Post-cessation Weight Gain [NCT00105482]	Phase 2	172 participants (Actual)	Interventional	2005-01-31	Completed
Naltrexone Naltrexone Implants as an Aid in Preventing Relapse Following Inpatient Treatment for Opioid Addiction - a Randomised Study [NCT00521157]	Phase 2/Phase 3	56 participants (Actual)	Interventional	2006-01-31	Completed
[NCT00000452]	Phase 4	240 participants	Interventional		Completed
Naltrexone for Opioid Dependent Released Human Immunodeficiency Virus Positive (HIV+) Criminal Justice Populations [NCT01246401]	Phase 1/Phase 2	151 participants (Actual)	Interventional	2011-03-31	Completed
Post-Treatment Effects of Naltrexone [NCT00006449]	Phase 4	160 participants	Interventional	2000-09-30	Completed
A Double-Blind Placebo-Controlled Study of Methylnaltrexone (MNTX) for the Relief of Constipation Due to Chronic Opioid Therapy in Patients With Advanced Medical Illness [NCT00401362]	Phase 3	154 participants (Actual)	Interventional	2003-02-28	Completed
The Role of Pharmacotherapy in Prevention of Relapse in Alcohol Dependence [NCT00120601]	Phase 4	200 participants	Interventional	2003-03-31	Active, not recruiting
[NCT00027079]	Phase 2	360 participants	Interventional	2001-09-30	Completed
Naltrexone and Nicotine Replacement Effects on Cue Reactivity of Smokers [NCT00018213]		0 participants	Interventional	1998-04-30	Completed
HIV Risk Reduction and Drug Abuse Treatment in Iran [NCT00398008]	Phase 2	0 participants (Actual)	Interventional	2004-10-31	Withdrawn(stopped due to Study was never able to start in IRAN)
The Use of Naltrexone Hydrochloride to Promote Healing in Patients With Resistant Non-infectious Corneal Ulcer [NCT05924893]		50 participants (Actual)	Interventional	2021-01-01	Completed
Lemborexant Augmentation of Naltrexone for Alcohol Craving and Sleep: A Randomized, Double-Blind, Placebo- Controlled Study [NCT05458609]	Phase 3	14 participants (Anticipated)	Interventional	2023-02-09	Enrolling by invitation
Heroin Addiction Treatment: Naltrexone and Adrenergic Agents [NCT00142948]	Phase 2	301 participants (Actual)	Interventional	2006-02-28	Completed
The Treatment of Late Life Major Depression Complication by Alcohol [NCT00018824]	Phase 4	74 participants (Actual)	Interventional	1999-10-31	Completed
Combined Treatment for Cocaine-Alcohol Dependence [NCT00218569]	Phase 2	87 participants (Actual)	Interventional	2003-04-30	Completed
Effects of Alpha-2 Adrenergic and Opiate Receptor Blockade on Sexual Function in Healthy Male Volunteers [NCT00042536]		40 participants	Observational	2002-07-31	Completed
Pharmacogenetic Response to Naltrexone for Alcohol Dependence [NCT00831272]	Phase 4	221 participants (Actual)	Interventional	2009-01-05	Completed
Screening Medications for Cocaine Cessation and Relapse Prevention [NCT00218023]	Phase 2	101 participants (Actual)	Interventional	2006-03-31	Completed
Opioid Antagonism Enhances Marijuana's Effects in Heavy Marijuana Smokers [NCT00403117]	Phase 2	49 participants (Actual)	Interventional	2006-12-31	Completed
The Effects of Low Dose Naltrexone (LDN) on Diseases of Aging - A Retrospective Cross-sectional Study Into Off-label Use of LDN [NCT05307627]		2,500 participants (Anticipated)	Observational	2022-03-14	Suspended(stopped due to Technological barriers are affecting the participant response experience.)
Efficacy and Safety of VIVITROL® in Adults Completing Inpatient Treatment for Alcohol Dependence [NCT00501631]	Phase 3	300 participants (Actual)	Interventional	2007-07-31	Completed
Effects of Mediterranean Diet and Naltrexone/Bupropion Treatment on Body Weight and Metabolic Risk Factors in Obese Breast Cancer Patients After Breast Cancer Treatment [NCT03581630]		72 participants (Actual)	Interventional	2017-07-29	Completed
Employment-Based Depot Naltrexone Clinical Trial II [NCT00684775]	Phase 2	38 participants (Actual)	Interventional	2008-05-31	Completed
Control of Cognition: Naltrexone, Methylphenidate, and ADHD Study [NCT01993108]	Phase 4	23 participants (Actual)	Interventional	2013-10-31	Completed
CTN-0054 Accelerated Development of Additive Pharmacotherapy Treatment (ADAPT) for Methamphetamine Use Disorder [NCT01982643]	Phase 1/Phase 2	49 participants (Actual)	Interventional	2013-11-30	Completed
The ION+EMI Study: Intermittent Oral Naltrexone Enhanced With an Ecological Momentary Intervention for Methamphetamine-using MSM [NCT04791969]	Phase 2	54 participants (Anticipated)	Interventional	2021-12-14	Recruiting
Addiction Treatment in Russia: Oral and Depot Naltrexone [NCT00218426]	Phase 2/Phase 3	306 participants (Actual)	Interventional	2006-07-31	Completed
Low Dose Naltrexone for Metastatic Melanoma, Castrate Resistant Prostate Cancer and Renal Cancer: A Phase II Brown University Oncology Group Research Project [NCT01650350]	Phase 2	7 participants (Actual)	Interventional	2012-11-30	Terminated(stopped due to Study stopped 10/24/13 secondary to lack of patients/slow enrollment)
Pharmacological and Behavioral Treatments to Treat Loss-of-Control Eating and Improve Weight Outcomes After Bariatric Surgery: Maintenance Treatment (Stage 2a) [NCT04605081]	Phase 2/Phase 3	100 participants (Anticipated)	Interventional	2022-01-10	Enrolling by invitation
Pharmacological and Behavioral Treatments to Treat Loss-of-Control Eating and Improve Weight Outcomes After Bariatric Surgery: Acute (Stage 1) [NCT04599478]	Phase 2/Phase 3	160 participants (Anticipated)	Interventional	2021-06-29	Recruiting
Pharmacotherapeutic Intervention to Improve Treatment Engagement Among Alcohol-dependent Veterans After Hospital Discharge [NCT01856712]	Phase 3	54 participants (Actual)	Interventional	2013-05-31	Completed
Long-acting Naltrexone for Pre-release Prisoners: A Randomized Trial of Mobile Treatment [NCT02867124]	Phase 3	240 participants (Anticipated)	Interventional	2017-01-31	Recruiting
Linking Infectious and Narcology Care-Part II [NCT03290391]	Phase 4	225 participants (Actual)	Interventional	2018-09-19	Completed
Naltrexone Implants as an Aid in Preventing Relapse Following Inpatient Treatment for Opioid Addiction. [NCT00269607]	Phase 2/Phase 3	12 participants (Actual)	Interventional	2005-05-31	Terminated(stopped due to Recruitment difficulties. Reframed as pilot study)
Testing the Reward-Drinker Hypothesis of Naltrexone Using an Extended-Release Formulation [NCT05028062]	Phase 4	60 participants (Anticipated)	Interventional	2022-03-07	Recruiting
A Bioequivalence Study Comparing Vivitrol and O'Neil Long Acting Naltrexone Implant (OLANI) in Healthy Participants [NCT04716881]	Phase 1	9 participants (Actual)	Interventional	2021-01-25	Completed
Individually Adapted Therapy of Alcoholism: Clinical Studies [NCT00317031]	Phase 4	435 participants (Actual)	Interventional	2002-11-30	Completed
Randomized Double-Blind Trial of Low-Dose Naltrexone for Children With PDD [NCT00318162]	Phase 1/Phase 2	50 participants (Anticipated)	Interventional		Not yet recruiting
Treatment Strategy for Alcohol Use Disorders in Veterans With TBI [NCT01342549]	Phase 3	62 participants (Actual)	Interventional	2011-09-30	Completed
Depot Pharmacotherapies for Opioid-Dependent Offenders: Outcomes and Costs [NCT02110264]	Phase 3	151 participants (Actual)	Interventional	2015-06-30	Completed
A Double-Blind Comparison of Naltrexone and Placebo in Adults With Attention Deficit Hyperactivity Disorder [NCT01721330]	Phase 4	3 participants (Actual)	Interventional	2012-11-30	Terminated(stopped due to Competing studies)
A Multicenter, Randomized, Double-Blind, Placebo-Controlled, Phase 4 Study to Assess the Effect of Naltrexone Hydrochloride and Bupropion Hydrochloride Extended Release Combination on the Occurrence of Major Adverse Cardiovascular Events in Overweight and [NCT02638129]	Phase 4	67 participants (Actual)	Interventional	2016-01-31	Terminated
Neural Correlates of Food Reward in Native American Women [NCT01623440]		69 participants (Actual)	Observational	2009-11-30	Completed
Sertraline and Naltrexone for Alcohol Dependents [NCT00000440]	Phase 2	124 participants	Interventional		Completed
Low Dose Naltrexone (LDN) for the Treatment of Chronic Neuropathic Pain in Patients With Human Immunodeficiency Virus (HIV), a Prospective, Pragmatic, Open Label Clinical Trial [NCT05537935]	Phase 4	60 participants (Anticipated)	Interventional	2023-04-28	Suspended(stopped due to Recruitment has been temporarily paused for IRB review)
A Multi-center, Randomized, Double-blind, Placebo Controlled Phase III Study to Assess the Efficacy, Safety, and Tolerability of PXT3003 in Charcot-Marie-Tooth Type 1A (CMT1A) [NCT04762758]	Phase 3	350 participants (Anticipated)	Interventional	2021-03-30	Active, not recruiting
Pharmacotherapy for Hazardous Drinking in HIV Infected Women: Randomized Trial [NCT01245647]	Phase 2	19 participants (Actual)	Interventional	2010-11-30	Completed
Medication Development in Protracted Abstinence in Alcoholism: Acamprosate Versus Naltrexone [NCT00656630]	Phase 2	68 participants (Actual)	Interventional	2007-12-31	Completed
Methylnaltrexone Versus Naloxegol in the Treatment of Opioid-Induced Constipation in the Emergency Department [NCT03523520]	Phase 4	15 participants (Actual)	Interventional	2020-12-23	Completed
Prevention of Relapse to Opioid Addiction Using Depot Naltrexone [NCT00781898]	Phase 2/Phase 3	308 participants (Actual)	Interventional	2008-06-30	Completed
A Multicenter Double-Blind Extension of Alkermes Study ALK21-003 to Evaluate the Long-Term Safety of Medisorb® Naltrexone [NCT01218971]	Phase 3	332 participants (Actual)	Interventional	2002-08-31	Completed
A Phase II, Randomized, Double-Blind Pilot Trial of VIVITROL® (Naltrexone for Extended-Release Injectable Suspension) for the Treatment of Cocaine and Alcohol Dependence [NCT00777062]	Phase 2	80 participants (Actual)	Interventional	2009-07-31	Completed
Optimal Prevention of Overdose Deaths and Opioid Relapse Following Discharge: A Multi-Center RCT of Naltrexone Versus Buprenorphine in Norway [NCT01717963]	Phase 3	166 participants (Actual)	Interventional	2012-10-31	Completed
An Open-Label Study of Naltrexone in Adults With Attention Deficit Hyperactivity Disorder. [NCT01873729]	Phase 4	3 participants (Actual)	Interventional	2013-11-30	Completed
A Randomized, Double-blind, Placebo-controlled, Crossover Study to Evaluate the Influence of the A118G Polymorphism in the mu Opioid Receptor Gene (OPRM1) on Effects of GSK1521498 and Naltrexone on Physiological and Behavioural Markers of Brain Function i [NCT01738867]	Phase 1	56 participants (Actual)	Interventional	2012-12-12	Completed
Pharmacokinetic Characterization of the Active, Separated System With PK Controller (Fentanyl Iontophoretic Transdermal System, 40 Mcg Fentanyl Per Activation). [NCT01750060]	Phase 1	54 participants (Actual)	Interventional	2012-12-31	Completed
The Mechanism of Human Non-Shivering Thermogenesis and Basal Metabolic Rate [NCT01950520]	Phase 2	134 participants (Anticipated)	Interventional	2014-02-07	Recruiting
Kappa Opioid Receptor Antagonism for the Treatment of Alcohol Use Disorder (AUD) and Comorbid Post-Traumatic Stress Disorder (PTSD) [NCT03852628]	Phase 2	69 participants (Actual)	Interventional	2019-05-20	Terminated(stopped due to Futility analysis)
A Single-dose Crossover Study of Fentanyl Sublingual Spray 400 Mcg Versus Actiq® 400 Mcg Versus Fentanyl Citrate Injection (iv) 100 Mcg Under Fasted Conditions [NCT01780233]	Phase 1	40 participants (Actual)	Interventional	2007-04-30	Completed
Low Dose Naltrexone in Symptomatic Inflammatory Bowel Disease [NCT01810185]	Phase 2	0 participants (Actual)	Interventional	2013-03-31	Withdrawn(stopped due to Low patient enrollment)
A Randomized, Single-Dose, Placebo-Controlled, Double-Blind, 3-Way Crossover Study to Determine the Relative Abuse Potential of Intravenous Oxycodone Hydrochloride Alone or in Combination With Intravenous Naltrexone Hydrochloride in Opioid Experienced Non [NCT01825447]	Phase 1	89 participants (Actual)	Interventional	2013-07-31	Completed
Oral v. Injection Naltrexone in Hospital: Comparative Effectiveness for Alcoholism [NCT02478489]	Phase 4	248 participants (Actual)	Interventional	2016-06-30	Completed
A Phase I Study to Evaluate the Safety of Naltrexone and Propranolol in Combination With Standard of Care Ipilimumab and Nivolumab in Patients With Advanced Melanoma [NCT05968690]	Phase 1	12 participants (Anticipated)	Interventional	2023-09-11	Recruiting
Combining Varenicline and Naltrexone for Smoking Cessation and Drinking Reduction [NCT02698215]	Phase 2	165 participants (Actual)	Interventional	2016-05-31	Completed
Randomized, Proof-Of-Concept Trial of Augmentation of Antidepressants by Low Dose Naltrexone (LDN) for Patients With Breakthrough Symptoms of Major Depressive Disorder on Antidepressant Therapy [NCT01874951]	Phase 2	12 participants (Actual)	Interventional	2013-06-30	Completed
NIDA (National Institute on Drug Abuse) CTN (Clinical Trials Network) Protocol 0068: Accelerated Development of Additive Pharmacotherapy Treatment (ADAPT-2) for Methamphetamine Use Disorder [NCT03078075]	Phase 3	403 participants (Actual)	Interventional	2017-05-05	Completed
A Comparative Effectiveness Trial of Extended Release Naltrexone Versus Extended Release Buprenorphine With Individuals Leaving Jail [NCT04408313]	Phase 2/Phase 3	240 participants (Anticipated)	Interventional	2020-10-28	Recruiting
CTN-0051: Extended-Release Naltrexone vs. Buprenorphine for Opioid Treatment [NCT02032433]	Phase 4	570 participants (Actual)	Interventional	2014-01-29	Completed
[NCT01895036]	Phase 1/Phase 2	6 participants (Actual)	Interventional	2011-02-28	Completed
Naltrexone and Varenicline: Weight Gain and Tolerability in Smokers [NCT00502216]	Phase 1/Phase 2	40 participants (Actual)	Interventional	2007-07-31	Completed
Neurobiology of Opioid Dependence: 4 [NCT00000195]	Phase 2	0 participants (Actual)	Interventional	1993-01-31	Withdrawn
Emergency Department Initiated Oral Naltrexone for Patients With Moderate to Severe Alcohol Use Disorder: A Pilot Feasibility Study [NCT04817410]	Phase 1	21 participants (Actual)	Interventional	2021-09-28	Completed
Behavioral/Pharmacological Treatments for Alcohol-Nicotine Dependence [NCT00000447]	Phase 4	200 participants	Interventional	1998-09-30	Completed
Feasibility of Emergency Department Initiated Extended-Release Naltrexone and Case Management Services for the Treatment of Alcohol Use Disorder [NCT04094584]	Phase 4	179 participants (Actual)	Interventional	2020-08-14	Terminated(stopped due to 12 month follow up data not collected due to pandemic disruptions)
Extended-Release Naltrexone (XR-NTX, VIVITROL) for the Treatment of Actively-Using Methamphetamine-Dependent Men Who Have Sex With Men [NCT01449565]	Phase 2	100 participants (Actual)	Interventional	2012-09-30	Completed
An Open-Label, Single-Dose, Randomized, Three-Way Crossover Study in Healthy Volunteers to Estimate the Effects of Food and of Sprinkling ALO-02 Pellets on Applesauce on the Bioavailability of Oxycodone and Naltrexone/6- Β -Naltrexol From a Extended Relea [NCT01456507]	Phase 1	24 participants (Actual)	Interventional	2011-10-31	Completed
A Randomized, Open Label, Long-Term, Multi-Center Study of the Safety of Medisorb® Naltrexone [NCT01218997]	Phase 3	436 participants (Actual)	Interventional	2003-08-31	Completed
Neurobiology of Opioid Dependence: 5 [NCT00000196]	Phase 2	0 participants (Actual)	Interventional	1993-01-31	Withdrawn
Etiology and Treatment of Alcohol Dependence [NCT00000442]	Phase 4	57 participants	Interventional		Completed
Naltrexone: Consummatory Behaviors in Alcoholic Women [NCT00000448]	Phase 4	160 participants (Actual)	Interventional	1995-10-31	Completed
Randomized, Double-blind, Placebo-controlled Study of Naltrexone for Impulse Control Disorders in Parkinson's Disease [NCT01052831]	Phase 4	50 participants (Actual)	Interventional	2009-11-30	Completed
N-acetylcysteine Plus Naltrexone for the Treatment of Alcohol Dependence [NCT01214083]	Phase 2	111 participants (Actual)	Interventional	2010-10-15	Completed
Oxytocin and Naltrexone: Investigation of Combined Effects on Stress- and Alcohol Cue-induced Craving in Alcohol Use Disorder - a Randomized Double-blind Placebo-controlled Parallel-group Trial [NCT05093296]	Phase 2/Phase 3	62 participants (Anticipated)	Interventional	2021-12-02	Recruiting
A Clinical Trial to Assess a Single Dose of Low-Dose Naltrexone and Acetaminophen Combination and Its Components in the Acute Treatment of Migraine [NCT03061734]	Phase 2	92 participants (Actual)	Interventional	2017-02-18	Completed
A Double-Blind Study of N-Acetyl Cysteine Plus Naltrexone in the Treatment of Methamphetamine Dependence [NCT00332605]	Phase 2	45 participants (Actual)	Interventional	2006-06-30	Completed
Evaluation of NMDA Antagonist for Opiate Dependence [NCT00125515]	Phase 2	81 participants (Actual)	Interventional	2005-06-30	Completed
A Multi-Center Extension of Alkermes' Study ALK21-003-EXT (NCT01218971) to Evaluate the Long-Term Safety of Medisorb® Naltrexone [NCT00156923]	Phase 3	108 participants (Actual)	Interventional	2003-10-31	Completed
Treatment With Naltrexone/Buprpion (Mysimba) to Optimize Weight Outcomes After Bariatric Surgery [NCT04399395]	Phase 4	0 participants (Actual)	Interventional	2020-11-01	Withdrawn(stopped due to Covid-pandemic)
Defining an Endophenotype for Alcohol Misuse: A Focus On Minority Populations [NCT00256451]	Phase 4	43 participants (Actual)	Interventional	2005-11-30	Completed
An Open Label, Flexible Dose Study of Very Low Doses of Naltrexone-Buprenorphine Transfer to Extend-Release Naltrexone (VIVITROL®) in Opioid Addiction [NCT01690546]	Phase 2	38 participants (Actual)	Interventional	2012-09-30	Completed
Individualized Pharmacological Approach to Obesity Management: A Randomized Clinical Trial [NCT03374956]	Phase 3	193 participants (Actual)	Interventional	2017-12-11	Completed
Neuropharmacological Basis of Social Connection: The Role of Opioids [NCT01672723]		34 participants (Actual)	Interventional	2012-10-31	Completed
Novel Interventions for Alcohol Dependent Frequent Emergency Department Users: Phase IV, Randomized, Open-label, Non-placebo-controlled Study of Extended-release Naltrexone and Care Management on Healthcare Use, Drinking, & Quality of Life [NCT02445339]	Phase 4	50 participants (Actual)	Interventional	2015-07-31	Completed
Comparing Medication Maintenance in Comprehensive Community and Pharmacy Settings to Enhance Engagement [NCT04139213]	Phase 2/Phase 3	250 participants (Anticipated)	Interventional	2019-07-25	Active, not recruiting
Low Dose Naltrexone for Chronic Pain in Osteoarthritis and Inflammatory Arthritis [NCT03008590]	Phase 2	29 participants (Actual)	Interventional	2018-05-01	Completed
A Phase 1, Randomized, Open-Label, Exploratory, Parallel, Pharmacokinetic Single Dose Study of IVL3004 Versus Vivitrol® (Naltrexone) LAI in Healthy Subjects [NCT05620940]	Phase 1	30 participants (Anticipated)	Interventional	2023-10-01	Not yet recruiting
Behavioral and Pharmacologic Treatment of Binge Eating and Obesity [NCT03047005]	Phase 2/Phase 3	68 participants (Actual)	Interventional	2017-08-28	Completed
An Open-label, Single-dose and Multiple-dose, Randomized, Crossover Study to Evaluate Pharmacokinetics, Safety and Tolerability After Administration of ALO-02 40 Mg Twice Daily Compared to ALO-02 80 Mg Once Daily and to Oxycontin 40 Mg Twice Daily in Heal [NCT01557257]	Phase 1	13 participants (Actual)	Interventional	2012-03-31	Completed
Effects of Low Dose Naltrexone on Quality of Life in High Grade Glioma Patients: A Placebo-Controlled, Double-Blind Randomized Trial [NCT01303835]	Phase 2	110 participants (Actual)	Interventional	2011-05-31	Completed
Effects of 500 mg Immediate Release and Extended Release Methylnaltrexone on Loperamide-induced Delay of the Oro-cecal and Whole-gut Transit Time in Healthy Subjects [NCT01596777]	Phase 1	15 participants (Actual)	Interventional	2010-01-31	Completed
A Phase II, Double-blind, Placebo-Controlled, Pilot Trial of the Combination of Modafinil and Naltrexone for the Treatment of Cocaine and Alcohol Dependence [NCT00142818]	Phase 2	164 participants (Actual)	Interventional	2006-02-28	Completed
Assessment of the Effect of Naltrexone on Lofexidine Single Dose Pharmacokinetics in Healthy Subjects [NCT02446002]	Phase 1	25 participants (Actual)	Interventional	2015-05-31	Completed
A Phase 3, Multicenter, Randomized, Double-Blind, Placebo-Controlled Study of the Efficacy and Safety of Medisorb® Naltrexone in Alcohol-Dependent Adults [NCT01218958]	Phase 3	624 participants (Actual)	Interventional	2002-02-28	Completed
A Randomized, Double-Blind, Placebo-Controlled Trial of Naltrexone in the Treatment of Concurrent Alcohol Dependence and Pathological Gambling [NCT00326807]		50 participants	Interventional	2001-06-30	Completed
Sweet Preference and Alcohol Craving Predict Naltrexone Response in Alcoholism [NCT01296646]	Phase 2	80 participants (Actual)	Interventional	2010-01-31	Completed
Investigating Glutamate and Opioid Mechanisms of Antidepressant Response to Ketamine [NCT04977674]	Early Phase 1	27 participants (Actual)	Interventional	2021-09-27	Completed
Naltrexone as an Adjunct in Alcoholic Cocaine Dependent Patients [NCT00000307]	Phase 2	0 participants	Interventional	2003-04-30	Completed
Effectiveness of Naltrexone in a Community Setting [NCT00000445]	Phase 4	300 participants	Interventional		Completed
Naltrexone and SSRI Therapy for Alcohol Dependence in Alaska Natives [NCT00000451]	Phase 2	198 participants (Actual)	Interventional	2003-01-31	Completed
A Phase 3 Efficacy and Safety Study of ALKS 5461 for the Adjunctive Treatment of Major Depressive Disorder (the FORWARD-4 Study) [NCT02158533]	Phase 3	385 participants (Actual)	Interventional	2014-05-31	Completed
Risky Decision Making in Methamphetamine Users: The Role of Opioid Blockade [NCT01822132]		76 participants (Actual)	Interventional	2013-05-31	Completed
Pharmacotherapy for Alcohol Consumption in HIV Infected Women: Randomized Trial [NCT01625091]	Phase 3	194 participants (Actual)	Interventional	2012-12-31	Completed
Nalmefene in Nicotine and Alcohol Dependence [NCT00000437]	Phase 4	60 participants (Actual)	Interventional	1997-09-26	Completed
Coping, Exposure, and Naltrexone Treatment With Alcoholics [NCT00000449]	Phase 4	160 participants	Interventional		Completed
HIV Risk Reduction and Drug Abuse Treatment in Malaysia [NCT00383045]	Phase 2	180 participants	Interventional	2003-04-30	Completed
A Feasibility Assessment of a Decentralized Platform Adaptive Double-Blind, Randomized Controlled Trial Investigating Repurposed Drugs in the Treatment of Post-Acute Sequelae of Coronavirus-19 (PASC) [NCT05946551]	Phase 3	36 participants (Anticipated)	Interventional	2024-01-31	Not yet recruiting
Phase 2, Multicenter, Randomized, Double Blind, Placebo Controlled Study of Combination Therapy for Safety and Efficacy in Subjects With Uncomplicated Obesity [NCT00364871]	Phase 2	410 participants (Actual)	Interventional	2005-04-30	Completed
NIDA-CTN-0100: Optimizing Retention, Duration and Discontinuation Strategies for Opioid Use Disorder Pharmacotherapy (RDD) [NCT04464980]	Phase 2	2,190 participants (Anticipated)	Interventional	2021-06-08	Recruiting
A Pilot Trial of Naltrexone-Bupropion Combination Versus Placebo Combined With Bupropion for Weight Loss in Comorbid Schizophrenia [NCT03132571]	Phase 2	5 participants (Actual)	Interventional	2017-06-01	Terminated(stopped due to Study discontinued due to funding.)
Alcohol Pharmacotherapy for HIV+ Prisoners With Alcohol Dependence and Problem Drinking [NCT01077310]		100 participants (Actual)	Interventional	2010-08-31	Completed
Optimizing Pharmacotherapy for Bipolar Alcoholics [NCT00302133]	Phase 1/Phase 2	88 participants (Actual)	Interventional	2006-05-31	Completed
Phase II Study of Naltrexone for the Treatment of Hormone-Refractory, Metastatic Breast Cancer [NCT00379197]	Phase 2	13 participants (Actual)	Interventional	2006-07-31	Terminated(stopped due to slow accrual)
Randomized, Double-Blind, Study to Assess Low-Dose Naltrexone and Acetaminophen Combination in the Prevention of Episodic Migraine in Adults [NCT03194555]	Phase 2	12 participants (Actual)	Interventional	2017-08-25	Completed
An Open-label Study To Evaluate The Pharmacokinetics And Safety Of Alo-02 (Oxycodone Hydrochloride And Naltrexone Hydrochloride) Extended-release Capsules In Children And Adolescents 7-17 Years Of Age Who Require Opioid Analgesia [NCT02680847]	Phase 4	32 participants (Actual)	Interventional	2016-01-21	Terminated(stopped due to The trial was terminated on 08FEB2018. Pfizer has decided to withdraw the New Drug Application and has notified FDA. There are no efficacy or safety concerns.)
Randomized, Double-Blind, and Placebo-Controlled Study to Assess a Single Dose of Low-Dose Naltrexone and Acetaminophen Combination Versus Sumatriptan in the Acute Treatment of Migraine With Nausea [NCT03185143]	Phase 2/Phase 3	36 participants (Actual)	Interventional	2017-06-27	Completed
Low Dose Naltrexone (LDN) Immune Monitoring [NCT02107014]		9 participants (Actual)	Interventional	2014-03-31	Completed
Participant(s) With Autism and High Pain Tolerance Treated With High Dose Naltrexone [NCT05100563]		1 participants (Actual)	Observational	2018-10-01	Completed
Behavioral and Pharmacological Treatments to Enhance Weight Outcomes After Metabolic and Bariatric Surgery [NCT05157698]	Phase 2/Phase 3	160 participants (Anticipated)	Interventional	2022-01-13	Recruiting
A Randomized, Triple-blind, Placebo- and Positive-Controlled, Parallel Group Study of the Effect of Buprenorphine Delivered by the Buprenorphine Transdermal System (BTDS) at Doses up to 80 mcg/Hour and Naltrexone on ECG Intervals in Healthy Adult Subjects [NCT01999114]	Phase 1	328 participants (Actual)	Interventional	2012-03-31	Completed
Say When: Targeting Heavy Alcohol Use With Naltrexone Among MSM [NCT02330419]	Phase 2	120 participants (Actual)	Interventional	2015-04-30	Completed
A Multicenter, 12-month, Open-label, Single-arm, Safety Study Of Oxycodone Hydrochloride And Naltrexone Hydrochloride Extended-release Capsules In Subjects With Moderate To Severe Chronic Noncancer Pain [NCT01428583]	Phase 3	395 participants (Actual)	Interventional	2010-12-31	Completed
A Multi-center, Randomized, Multiple-dose, Double-blind, Placebo-controlled, Parallel Group, Phase 3 Study to Evaluate the Efficacy and Safety of Abuse-deterrent Capsules Oxycodone Hydrochloride Plus Naltrexone Hydrochloride (a) or Oxycodone Hydrochloride [NCT02401750]	Phase 3	163 participants (Actual)	Interventional	2015-06-30	Completed
Naltrexone for Antipsychotic-Induced Weight Gain [NCT01866098]		144 participants (Actual)	Interventional	2013-05-31	Completed
Optimizing Naltrexone for Individuals of East Asian Descent [NCT02026011]	Phase 2	87 participants (Actual)	Interventional	2013-12-31	Completed
A Phase 2, Randomized, Multicenter, Safety, Tolerability, and Dose-Ranging Study of Samidorphan, a Component of ALKS 3831, in Adults With Schizophrenia Treated With Olanzapine [NCT01903837]	Phase 2	347 participants (Actual)	Interventional	2013-06-30	Completed
The Immune Effects of Low-dose Naltrexone in People With Myalgic Encephalopathy/Chronic Fatigue Syndrome (ME/CFS) [NCT02965768]		0 participants (Actual)	Interventional	2016-01-31	Withdrawn(stopped due to Study was temporarily suspended to focus on other projects, but was never resumed. No participants were determined eligible and none started the protocol.)
Improving Treatment Outcomes for Prescription Opioid Dependence [NCT02543944]	Phase 2/Phase 3	117 participants (Actual)	Interventional	2016-02-29	Completed
Treatment of Binge Eating Disorder in Obesity: Naltrexone/ Bupropion Combination Versus Placebo [NCT02317744]		22 participants (Actual)	Interventional	2014-12-31	Completed
The Effect of Opiate Blockade With Naltrexone on Counterregulatory Mechanisms in Hypoglycemia [NCT01462227]		17 participants (Actual)	Interventional	2011-08-31	Completed
Placebo Controlled Study of Memantine as an Adjunct to Naltrexone in the Treatment of Opioid Dependence [NCT00476242]	Phase 2/Phase 3	82 participants (Actual)	Interventional	2008-06-30	Completed
Alcohol Research Center Grant. Component #1: Naltrexone Effects on Alcohol Reactivity and Consumption, Evaluating the Genetic Variability of Naltrexone Response [NCT00366626]	Phase 4	83 participants (Actual)	Interventional	2006-04-30	Completed
Examining Mu Opioid Mechanisms of Ketamine's Rapid Effects in OCD (MKET2) [NCT05940324]	Phase 2	150 participants (Anticipated)	Interventional	2023-11-30	Not yet recruiting
Efficacy and Safety of VIVITROL® (Naltrexone for Extended-release Injectable Suspension) in Adults With Opioid Dependence [NCT00678418]	Phase 3	250 participants (Actual)	Interventional	2008-06-30	Completed
The Effect of Naltrexone and Varenicline on Alcohol-Mediated Smoking Lapse [NCT00773422]	Phase 2	30 participants (Actual)	Interventional	2008-01-31	Completed
A Randomized, Double-blind, Double-dummy, Placebo Controlled, Single-dose, 6-way Crossover Study To Determine The Relative Abuse Potential Of Alo-02 (Oxycodone Hydrochloride And Naltrexone Hydrochloride Extended-release Capsules) Compared To Oxycodone Imm [NCT01746901]	Phase 1	81 participants (Actual)	Interventional	2013-02-28	Completed
Randomized, Open-label Clinical Trial of Extended-Release vs. Oral Naltrexone for Alcohol Treatment in Primary Care. [NCT01893827]	Phase 4	237 participants (Actual)	Interventional	2014-06-30	Completed
Effect of Methylnaltrexone on Gastrointestinal and Colonic Transit in Health [NCT01055704]	Phase 4	48 participants (Actual)	Interventional	2009-11-30	Completed
A Single-Center, Randomized, Double Masked, Placebo Controlled Clinical Study to Assess the Safety and Efficacy of Topical Naltrexone Ophthalmic Solution on the Signs and Symptoms of Dry Eye in Diabetic Subjects [NCT03660475]	Phase 2	60 participants (Actual)	Interventional	2018-07-31	Completed
A Multicenter, Randomized, Double-Blind, Placebo-Controlled, Phase 3 Efficacy Study of Kadian NT (Morphine Sulfate Plus Naltrexone Hydrochloride Extended-Release) Capsules in Subjects With Moderate to Severe Chronic Pain Due to Osteoarthritis of the Hip o [NCT00420992]	Phase 3	547 participants (Actual)	Interventional	2006-12-31	Completed
The Separate and Combined Effects of Vivitrol and Opiate Abstinence Reinforcement in the Treatment of Opioid Dependence [NCT01556425]	Phase 2	84 participants (Actual)	Interventional	2012-05-31	Completed
Glutamate-opioid Interactions in Alcohol Drinking Behaviors [NCT01519063]	Phase 2	75 participants (Actual)	Interventional	2012-01-31	Completed
Extended-Release Naltrexone Opioid Treatment at Jail Re-Entry [NCT01999946]	Phase 4	217 participants (Actual)	Interventional	2014-06-27	Completed
Cocaine Use Reduction With Buprenorphine (CURB) [NCT01402492]	Phase 2/Phase 3	302 participants (Actual)	Interventional	2011-09-30	Completed
A Phase II Multi-Center Safety Study Examining the Use of the O'Neil Long Acting Naltrexone Implant (OLANI) in Opioid Dependent Persons Receiving Repeat Dosing [NCT05382091]	Phase 2	250 participants (Anticipated)	Interventional	2023-10-15	Not yet recruiting
A Novel Human Laboratory Model for Screening Medications for Alcohol Use Disorder [NCT04249882]	Phase 2	53 participants (Actual)	Interventional	2020-01-28	Completed
[NCT01723384]	Phase 2	30 participants (Actual)	Interventional	2013-05-31	Completed
A Randomized, Double-blind, Placebo Controlled, Single-dose, 4-way Crossover Study To Determine The Relative Abuse Potential Of Alo-02 (Oxycodone Hydrochloride And Naltrexone Hydrochloride Extended Release Capsules) Compared To Oxycodone Immediate Release [NCT01775189]	Phase 1	45 participants (Actual)	Interventional	2013-02-28	Completed
Open-Label Study in Healthy Volunteers to Evaluate the Safety, Tolerability, and Pharmacokinetics of Switching From Oral Naltrexone HCL to DLP-160 (Naltrexone Implant) to Intramuscular Vivitrol® [NCT05304364]	Phase 1	10 participants (Actual)	Interventional	2022-03-22	Completed
Opioid-Induced Swallowing Dysfunction - The Impact of Bolus Volume: a Randomized, Double-Blind Study in Healthy Volunteers [NCT03283020]	Phase 4	20 participants (Anticipated)	Interventional	2017-11-11	Recruiting
Ketamine for The Rapid Treatment of Major Depression and Alcohol Use Disorder [NCT02461927]	Phase 1/Phase 2	65 participants (Actual)	Interventional	2015-01-01	Completed
A Phase 4, Pilot, Open-label Study of VIVITROL in the Prevention of Re-arrest and Re-incarceration [NCT01453374]	Phase 4	27 participants (Actual)	Interventional	2011-01-31	Completed
A Phase 1 Bioequivalence Study of Naltrexone SR/Bupropion SR Combination Trilayer Tablets From Two Manufacturers in Healthy Subjects [NCT02259179]	Phase 1	80 participants (Actual)	Interventional	2014-09-30	Completed
Naltrexone Randomized Controlled Trial for Treatment-Emergent Fatigue in Patients Receiving Radiation Therapy for Breast Cancer [NCT02137252]	Phase 2	3 participants (Actual)	Interventional	2014-05-31	Terminated(stopped due to no enough patients)
Effectiveness of Semaglutide 2.4 mg vs. Commercially Available Medications for Chronic Weight Management in Participants With Obesity in a Multi-employer Setting in The US - a Pragmatic Clinical Study [NCT05579249]	Phase 4	500 participants (Anticipated)	Interventional	2023-01-19	Recruiting
The Effect of Regular Naltrexone Dosing on Disordered Gamblers: An Examination of Neural Activation, Gambling Urges, and Gambling Behaviour [NCT02537197]	Phase 1	35 participants (Actual)	Interventional	2016-04-30	Completed
Oral Low-Dose Naltrexone in the Treatment of Lichen Planopilaris and Frontal Fibrosing Alopecia; an Uncontrolled Open-label Prospective Study [NCT04409041]	Phase 2	43 participants (Actual)	Interventional	2019-09-01	Completed
Association of Low Doses of Naltrexone and Transcranial Direct Current Stimulation in Fibromyalgia: Randomized Clinical Trial, Blind, Controlled With Placebo [NCT04502251]	Phase 2/Phase 3	92 participants (Actual)	Interventional	2018-08-01	Completed
Bridging ED to Outpatient AUD Therapy With Naltrexone [NCT05228418]	Phase 4	20 participants (Anticipated)	Interventional	2022-03-31	Not yet recruiting
Kappa-PET Imaging and Naltrexone in Alcohol Drinking Behaviors [NCT01625611]	Phase 1	59 participants (Actual)	Interventional	2011-02-28	Completed
Health Services Research: Extended Release Naltrexone for Opioid-Dependent Youth [NCT01843023]	Phase 4	288 participants (Actual)	Interventional	2013-06-30	Completed
Open-Label Pilot Study of Long-Acting Injectable Naltrexone Treatment for Cannabis Dependence [NCT02088177]	Phase 1/Phase 2	12 participants (Actual)	Interventional	2014-10-31	Completed
Brain Mechanisms of Cognitive Response to Pharmacotherapy in Opioid Use Disorder [NCT04454411]	Phase 2	200 participants (Anticipated)	Interventional	2025-02-01	Not yet recruiting
Effect of Prazosin and Naltrexone on Personalized Script-Induced Alcohol Craving in Individuals With Alcohol Use Disorders With and Without Comorbid PTSD [NCT02322047]	Phase 2	31 participants (Actual)	Interventional	2015-03-03	Completed
A Multicenter, 12 Week, Double-blind, Placebo-controlled, Randomized Withdrawal Study To Determine The Efficacy And Safety Of Alo-02 (Oxycodone Hydrochloride And Naltrexone Hydrochloride) Extended-release Capsules In Subjects With Moderate To Severe Chron [NCT01571362]	Phase 3	410 participants (Actual)	Interventional	2012-06-30	Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

Trial	Outcome
NCT00006489 (3) [back to overview]	Drinking Timeline Follow-back Interview (TFBI)
NCT00006489 (3) [back to overview]	Penn Alcohol Cravings Scale
NCT00006489 (3) [back to overview]	Posttraumatic Stress Disorder (PTSD) Symptom Scale - Interview (PSS-I-IV)
NCT00053677 (1) [back to overview]	Yale-Brown Obsessive Compulsive Scale for Pathological Gambling (PG-YBOCS)
NCT00105482 (5) [back to overview]	Cigarettes Smoked Per Day.
NCT00105482 (5) [back to overview]	Point Prevalence Smoking Abstinence at 26 Weeks.
NCT00105482 (5) [back to overview]	Point Prevalence Smoking Abstinence at 6 Weeks
NCT00105482 (5) [back to overview]	Weight Gain at 26 Weeks.
NCT00105482 (5) [back to overview]	Weight Gain at 6 Weeks.
NCT00115037 (2) [back to overview]	Percentage of Heavy Drinking Days
NCT00115037 (2) [back to overview]	Count of Responders and Non-responders in Phase 1
NCT00125515 (1) [back to overview]	Retention in Treatment
NCT00129246 (4) [back to overview]	Weight Gain
NCT00129246 (4) [back to overview]	Weight Gain Abstinent Participants
NCT00129246 (4) [back to overview]	Point Prevalence Abstinence
NCT00129246 (4) [back to overview]	Smoking Cessation
NCT00142818 (2) [back to overview]	Percent Days of Heavy Drinking (Measured by Timeline Follow Back Starting at Week Two Through Week 14
NCT00142818 (2) [back to overview]	Cocaine Use (Measured by Timeline Follow Back and Urine Screen From Week 2-week 14)
NCT00156923 (1) [back to overview]	Number of Participants Reporting at Least 1 Treatment-emergent Adverse Event (TEAE)
NCT00156936 (1) [back to overview]	Number of Subjects Who Reported at Least 1 Treatment-emergent Adverse Event (TEAE) While on Study.
NCT00183196 (1) [back to overview]	Time to Relapse to Drinking
NCT00218023 (2) [back to overview]	Mean Percentage of Cocaine-positive Urines Over Course of 12 Week Treatment in Subgroup Achieving Abstinence at Baseline
NCT00218023 (2) [back to overview]	Mean Percentage of Cocaine-positive Urines Over Course of 12 Week Treatment in Subgroup NOT Achieving Abstinence at Baseline
NCT00218426 (11) [back to overview]	Cocaine Drug Use
NCT00218426 (11) [back to overview]	Amphetamine Drug Use
NCT00218426 (11) [back to overview]	Benzodiazepine Drug Use
NCT00218426 (11) [back to overview]	Composite Score of Psychiatric Problems
NCT00218426 (11) [back to overview]	Global Assessment Form (GAF)
NCT00218426 (11) [back to overview]	HIV Risk (Baseline)
NCT00218426 (11) [back to overview]	Marijuana Drug Use
NCT00218426 (11) [back to overview]	Number of Subjects Who Dropped Out of Treatment
NCT00218426 (11) [back to overview]	Positive Opioid Urine Test
NCT00218426 (11) [back to overview]	Retention Without Relapse to Heroin Addiction (Measured at Month 6)
NCT00218426 (11) [back to overview]	Use of Alcohol
NCT00256451 (5) [back to overview]	Profile of Mood States - Vigor
NCT00256451 (5) [back to overview]	Subjective High From Alcohol Scale
NCT00256451 (5) [back to overview]	Profile of Mood States - Fatigue Scale
NCT00256451 (5) [back to overview]	Biphasic Alcohol Effects Scale - Stimulation
NCT00256451 (5) [back to overview]	Biphasic Alcohol Effects Scale - Sedation
NCT00270231 (1) [back to overview]	Number of Nicotine Cigarette Choices Taken During the Cigarette Choice Procedure.
NCT00271024 (10) [back to overview]	7-Day Point Prevalence Smoking Abstinence: 12 Weeks Post Quit-Date
NCT00271024 (10) [back to overview]	7-Day Point Prevalence Smoking Abstinence: 4 Weeks Post Quit-Date
NCT00271024 (10) [back to overview]	7-Day Point Prevalence Smoking Abstinence: 26 Weeks Post Quit-Date
NCT00271024 (10) [back to overview]	7-Day Point Prevalence Smoking Abstinence: 52 Weeks Post Quit-Date
NCT00271024 (10) [back to overview]	Prolonged Smoking Abstinence: 12 Weeks Post Quit-Date
NCT00271024 (10) [back to overview]	Prolonged Smoking Abstinence: 4 Weeks Post Quit-Date
NCT00271024 (10) [back to overview]	Weight Change at End of Treatment (Regardless of Quit Status)
NCT00271024 (10) [back to overview]	Weight Change at End of Treatment (Smoking Abstinent Only)
NCT00271024 (10) [back to overview]	Opioid Antagonist Reported Side Effects: 1-Week Post Quit Date
NCT00271024 (10) [back to overview]	Opioid Antagonist Reported Side Effects: 4-Weeks Post Quit Date
NCT00302133 (2) [back to overview]	Mean Number of Standard Drinks Per Drinking Day During the Last 4 Weeks of the Trial
NCT00302133 (2) [back to overview]	% Subjects Abstinent
NCT00332579 (1) [back to overview]	Yale Brown Obsessive Compulsive Scale Modified for Kleptomania (K-YBOCS)
NCT00332605 (1) [back to overview]	Penn Craving Scale
NCT00338962 (4) [back to overview]	Mean Number of Side Effects
NCT00338962 (4) [back to overview]	Mean Self-report Weekly Craving Via Obsessive Compulsive Drinking Scale (OCDS)
NCT00338962 (4) [back to overview]	Hamilton Depression Rating Scale (HAM-D)
NCT00338962 (4) [back to overview]	Clinician-Administered PTSD Scale (CAPS)
NCT00366626 (2) [back to overview]	Limited Access Alcohol Consumption Paradigm; Total Number of Drinks Consumed
NCT00366626 (2) [back to overview]	"Natural Alcohol Consumption Period; Average Number of Drinks Per Day Consumed During the 5 Day Natural (Usual Environment) Drinking Observation Period"
NCT00379197 (2) [back to overview]	Median Time to Event
NCT00379197 (2) [back to overview]	Disease Response
NCT00403117 (3) [back to overview]	Change in Mean Heart Rate as a Function of Marijuana Strength and Naltrexone Dose.
NCT00403117 (3) [back to overview]	Change in Mean Psychomotor Task Performance as a Function of Marijuana Strength and Naltrexone Dose
NCT00403117 (3) [back to overview]	Change in Mean Subjective Mood Scores as a Function of Marijuana Strength and Naltrexone Dose.
NCT00415597 (3) [back to overview]	Subjects With Treatment Emergent Adverse Events
NCT00415597 (3) [back to overview]	Mean Percent Change From Baseline to 52 Weeks in Brief Pain Inventory Score (BPI) of Average Pain
NCT00415597 (3) [back to overview]	Mean Percent Change From Baseline to 12 Weeks in Brief Pain Inventory Score (BPI) of Average Pain
NCT00420992 (1) [back to overview]	Mean Change From Randomization to 12 Weeks Following Randomization in Diary Brief Pain Inventory Score of Average Pain (Daily Scores of Average Pain Averaged Over 7 Days)
NCT00456521 (18) [back to overview]	Change in IWQOL-Lite Total Scores
NCT00456521 (18) [back to overview]	Change in Question 19 From 21-Item COE (Control of Eating) Questionnaire
NCT00456521 (18) [back to overview]	Change in Systolic Blood Pressure
NCT00456521 (18) [back to overview]	Change in Waist Circumference
NCT00456521 (18) [back to overview]	Co-primary: Body Weight- Mean Percent Change
NCT00456521 (18) [back to overview]	Co-primary: Body Weight- Proportion of Subjects With ≥5% Decrease
NCT00456521 (18) [back to overview]	Body Weight- Proportion of Subjects With ≥10% Decrease
NCT00456521 (18) [back to overview]	Change in Diastolic Blood Pressure
NCT00456521 (18) [back to overview]	Change in Fasting Blood Glucose Levels
NCT00456521 (18) [back to overview]	Change in Fasting HDL Cholesterol Levels
NCT00456521 (18) [back to overview]	Change in Fasting Insulin Levels, Using Log-transformed Data
NCT00456521 (18) [back to overview]	Change in Fasting LDL Cholesterol
NCT00456521 (18) [back to overview]	Change in Fasting Triglycerides Levels, Using Log-transformed Data
NCT00456521 (18) [back to overview]	Change in Food Craving Inventory Carbohydrates Subscale Scores
NCT00456521 (18) [back to overview]	Change in Food Craving Inventory Sweets Subscale Scores
NCT00456521 (18) [back to overview]	Change in High-sensitivity C Reactive Protein (Hs-CRP) Levels, Using Log-transformed Data
NCT00456521 (18) [back to overview]	Change in HOMA-IR Levels, Using Log-transformed Data
NCT00456521 (18) [back to overview]	Change in IDS-SR Total Scores
NCT00467558 (2) [back to overview]	Clinical Global Impression Scale - Severity
NCT00467558 (2) [back to overview]	Yale Brown Obsessive Compulsive Scale Modified for Compulsive Sexual Behavior (YBOCS)
NCT00474630 (25) [back to overview]	Change in High-sensitivity C Reactive Protein (Hs-CRP) Levels, Using Log-transformed Data
NCT00474630 (25) [back to overview]	Change in Fasting Insulin Levels, Using Log-transformed Data
NCT00474630 (25) [back to overview]	Change in Fasting HDL Cholesterol Levels
NCT00474630 (25) [back to overview]	Change in HbA1c Levels
NCT00474630 (25) [back to overview]	Change in Food Craving Inventory Sweets Subscale Score
NCT00474630 (25) [back to overview]	Change in IWQOL-Lite Total Scores
NCT00474630 (25) [back to overview]	Change in Question 19 From 21-Item COE (Control of Eating) Questionnaire
NCT00474630 (25) [back to overview]	Change in Food Craving Inventory Carbohydrates Subscale Score
NCT00474630 (25) [back to overview]	Change in Fasting Triglycerides Levels, Using Log-transformed Data
NCT00474630 (25) [back to overview]	Change in Fasting LDL Cholesterol Levels
NCT00474630 (25) [back to overview]	HbA1c- Proportion of Subjects With HbA1c <7% at Endpoint
NCT00474630 (25) [back to overview]	Percent of Subjects With Dose Reduction in Oral Antidiabetes Medications
NCT00474630 (25) [back to overview]	Percent of Subjects With Dose Increase in Oral Antidiabetes Medications
NCT00474630 (25) [back to overview]	Percent of Subjects Requiring Rescue Medications for Diabetes
NCT00474630 (25) [back to overview]	Change in Fasting Blood Glucose Levels
NCT00474630 (25) [back to overview]	Change in Diastolic Blood Pressure
NCT00474630 (25) [back to overview]	Body Weight- Proportion of Subjects With ≥10% Decrease
NCT00474630 (25) [back to overview]	Change in Systolic Blood Pressure
NCT00474630 (25) [back to overview]	Percent of Subjects Discontinuing Due to Poor Glycemic Control
NCT00474630 (25) [back to overview]	Change in Waist Circumference
NCT00474630 (25) [back to overview]	Co-primary: Body Weight- Mean Percent Change
NCT00474630 (25) [back to overview]	Co-primary: Body Weight- Proportion of Subjects With ≥5% Decrease
NCT00474630 (25) [back to overview]	Change in IDS-SR Total Scores
NCT00474630 (25) [back to overview]	Change in HOMA-IR Levels, Using Log-transformed Data
NCT00474630 (25) [back to overview]	HbA1c- Proportion of Subjects With HbA1c <6.5% at Endpoint
NCT00476242 (3) [back to overview]	Retention in Treatment The Primary Outcome Measure Will be the Dichotomous Measure Retention in Treatment (Whether the Patient Completes the 12 Week Trial, Yes/no).
NCT00476242 (3) [back to overview]	Opiate Use Measured by Urine Toxicology Results
NCT00476242 (3) [back to overview]	Opiate Craving Based on Heroin Craving Scale
NCT00501631 (1) [back to overview]	Cumulative Percentage of Participants by Heavy Drinking Rate
NCT00502216 (3) [back to overview]	Weight Gain in Treatment Completers
NCT00502216 (3) [back to overview]	Weight Gain in Participants Who Are Continuously Abstinent for the Last 4 Weeks of Treatment
NCT00502216 (3) [back to overview]	Tolerability of the Combination of 25 mg Naltrexone and 2 mg Varenicline
NCT00511836 (5) [back to overview]	Change From Baseline in Daily Craving Score in Alcohol-dependent Subjects (Actiwatch Data)
NCT00511836 (5) [back to overview]	Change From Baseline in Obsessive-Compulsive Drinking Scale (OCDS) Score in Alcohol-dependent Subjects
NCT00511836 (5) [back to overview]	Change From Baseline in BOLD Signal Activation Values in the Reward Circuitry
NCT00511836 (5) [back to overview]	Change From Baseline in Blood Oxygen-level-dependent (BOLD) Signal Activation Values Detected in the Reward Circuitry of the Brain in Alcohol-dependent Subjects After Presentation of Alcohol-related Cues.
NCT00511836 (5) [back to overview]	Change From Baseline in BOLD Signal Activation Values for the Inferior Frontal Gyrus
NCT00532779 (18) [back to overview]	Change in Fasting Triglycerides Levels, Using Log-transformed Data
NCT00532779 (18) [back to overview]	Change in Fasting Insulin Levels, Using Log-transformed Data
NCT00532779 (18) [back to overview]	Change in Fasting HDL Cholesterol Levels
NCT00532779 (18) [back to overview]	Body Weight- Proportion of Subjects With ≥10% Decrease
NCT00532779 (18) [back to overview]	Co-primary: Body Weight- Mean Percent Change
NCT00532779 (18) [back to overview]	Change in Diastolic Blood Pressure
NCT00532779 (18) [back to overview]	Change in Fasting Blood Glucose Levels
NCT00532779 (18) [back to overview]	Co-primary: Body Weight- Proportion of Subjects With ≥5% Decrease
NCT00532779 (18) [back to overview]	Change in Waist Circumference
NCT00532779 (18) [back to overview]	Change in Food Craving Inventory Carbohydrates Subscale Score
NCT00532779 (18) [back to overview]	Change in Food Craving Inventory Sweets Subscale Score
NCT00532779 (18) [back to overview]	Change in High-sensitivity C Reactive Protein (Hs-CRP) Levels, Using Log-transformed Data
NCT00532779 (18) [back to overview]	Change in HOMA-IR Levels, Using Log-transformed Data
NCT00532779 (18) [back to overview]	Change in IDS-SR Total Scores
NCT00532779 (18) [back to overview]	Change in IWQOL-Lite Total Scores
NCT00532779 (18) [back to overview]	Change in Question 19 From 21-Item COE (Control of Eating) Questionnaire
NCT00532779 (18) [back to overview]	Change in Systolic Blood Pressure
NCT00532779 (18) [back to overview]	Change in Fasting LDL Cholesterol Levels
NCT00537745 (2) [back to overview]	Evidence of Attempts to Drive After Drinking
NCT00537745 (2) [back to overview]	% Days w/1+Interlock Test Failures
NCT00567255 (20) [back to overview]	Change in Diastolic Blood Pressure
NCT00567255 (20) [back to overview]	Change in Fasting Blood Glucose Levels
NCT00567255 (20) [back to overview]	Change in Fasting Insulin Levels, Using Log-transformed Data
NCT00567255 (20) [back to overview]	Co-primary: Body Weight- Proportion of Subjects With ≥5% Decrease From Baseline to Week 28
NCT00567255 (20) [back to overview]	Change in Waist Circumference
NCT00567255 (20) [back to overview]	Change in Systolic Blood Pressure
NCT00567255 (20) [back to overview]	Change in Question 19 From 21-Item COE (Control of Eating) Questionnaire
NCT00567255 (20) [back to overview]	Change in IDS-SR Total Score
NCT00567255 (20) [back to overview]	Change in HOMA-IR Levels, Using Log-transformed Data
NCT00567255 (20) [back to overview]	Change in High-sensitivity C Reactive Protein (Hs-CRP) Levels, Using Log-transformed Data
NCT00567255 (20) [back to overview]	Change in Food Craving Inventory Sweets Subscale Score
NCT00567255 (20) [back to overview]	Change in Fasting LDL Cholesterol Levels
NCT00567255 (20) [back to overview]	Change in Fasting Triglycerides Levels, Using Log-transformed Data
NCT00567255 (20) [back to overview]	Co-primary: Body Weight- Mean Percent Change From Baseline to Week 28
NCT00567255 (20) [back to overview]	Change in Food Craving Inventory Carbohydrates Subscale Score
NCT00567255 (20) [back to overview]	Change in IWQOL-Lite Total Scores
NCT00567255 (20) [back to overview]	Body Weight- Proportion of Subjects With ≥10% Decrease From Baseline to Week 28
NCT00567255 (20) [back to overview]	Change in Fasting HDL Cholesterol Levels
NCT00567255 (20) [back to overview]	Body Weight- Mean Percent Change From Baseline to Week 56
NCT00567255 (20) [back to overview]	Body Weight- Proportion of Subjects With ≥5% Decrease From Baseline to Week 56
NCT00568555 (5) [back to overview]	Percent Change in Heat Pain Sensitivity Between Baseline and End of Placebo Treatment and Between Baseline to End of LDN Treatment.
NCT00568555 (5) [back to overview]	Percent Change in Pain Scores Between Baseline to End of Placebo Treatment and Between Baseline to End of LDN Treatment.
NCT00568555 (5) [back to overview]	Percent Change in Sleep Quality Scores Between Baseline to End of Placebo Treatment and Between Baseline to End of LDN Treatment.
NCT00568555 (5) [back to overview]	Percent Change in Pressure Pain Threshold Between Baseline and End of Placebo Treatment and Between Baseline to End of LDN Treatment.
NCT00568555 (5) [back to overview]	Percent Change in Fatigue Scores Between Baseline to End of Placebo Treatment and Between Baseline to End of LDN Treatment.
NCT00568958 (7) [back to overview]	Number of Drinks Per Drinking Day
NCT00568958 (7) [back to overview]	Frequency of Heavy Episodic Drinking
NCT00568958 (7) [back to overview]	Frequency of Heavy Episodic Drinking
NCT00568958 (7) [back to overview]	Number of Drinks Per Drinking Day
NCT00568958 (7) [back to overview]	Percent Days Abstinent From Drinking
NCT00568958 (7) [back to overview]	Percent Days Abstinent From Drinking
NCT00568958 (7) [back to overview]	Percentage of Drinking to an Estimated Blood Alcohol Concentration (BAC) of .08 or Higher
NCT00577408 (1) [back to overview]	Treatment Retention
NCT00620750 (1) [back to overview]	Percent of Patients Initiating Vivitrol Treatment Who Receive 3 Consecutive Monthly Vivitrol Injections
NCT00656630 (5) [back to overview]	Change From Baseline in Standard Drinks Per Week at 1 Week
NCT00656630 (5) [back to overview]	Change From Screening in Craving on the Alcohol Craving Questionnaire-Short Form (ACQ-SF) Total Score at Week 1
NCT00656630 (5) [back to overview]	Change From Baseline in Sleep Quality on the Pittsburgh Sleep Quality Index (PSQI) Total Score at Week 1
NCT00656630 (5) [back to overview]	Change From Baseline in Mood on the Beck Depression Inventory (BDI-II) at Week 1
NCT00656630 (5) [back to overview]	Visual Analog Scale of Craving to Drink at 1 Week Following Administration of Acamprosate or Naltrexone or Placebo During the Double-Blind Period
NCT00663117 (4) [back to overview]	Histology Inflammatory Score by Colon Biopsies
NCT00663117 (4) [back to overview]	Percentage Change From Baseline of Quality of Life IBDQ (Inflammatory Bowel Disease Quality of Life Survey)
NCT00663117 (4) [back to overview]	Percentage of Patients With a 5 Point Drop in CDEIS Score by Endoscopy
NCT00663117 (4) [back to overview]	Percentage of Subjects Achieving a 70-point Decline in CDAI Scores (Crohn's Disease Activity Index) Scores;
NCT00667875 (4) [back to overview]	Percent Heavy Drinking Days
NCT00667875 (4) [back to overview]	Percent Riboflavin Positive Urine Samples as a Measure of Medication Compliance
NCT00667875 (4) [back to overview]	Drinks Per Drinking Day
NCT00667875 (4) [back to overview]	Pill Counts During Treatment
NCT00678418 (5) [back to overview]	Percentage (%) of Opioid-free Weeks Per Subject in Double-blind Period (Part A)
NCT00678418 (5) [back to overview]	Incidence of Subjects Who Relapsed to Physiologic Opioid Dependence During the 24-week Treatment Period (Part A)
NCT00678418 (5) [back to overview]	Change in Percentage of Self-reported Opioid-free Days From Baseline to Week 24
NCT00678418 (5) [back to overview]	Craving Score: Change From Baseline
NCT00678418 (5) [back to overview]	Days to Discontinuation During Part A
NCT00684775 (7) [back to overview]	Time to the First Missed Dose
NCT00684775 (7) [back to overview]	Average Percentage of 30-day Urine Samples Negative for Cocaine
NCT00684775 (7) [back to overview]	HIV Risk Behaviors
NCT00684775 (7) [back to overview]	Naltrexone Injections Received
NCT00684775 (7) [back to overview]	Percentage of 30-day Urine Samples Negative for Opiates
NCT00684775 (7) [back to overview]	Percentage of M-W-F Samples Negative for Cocaine
NCT00684775 (7) [back to overview]	Percentage of M,W,F Urine Samples Negative for Opiates
NCT00711477 (12) [back to overview]	Dutch Eating Behavior Questionnaire - Change in Restrained Eating Subscale Score
NCT00711477 (12) [back to overview]	Dutch Eating Behavior Questionnaire - Change in External Eating Subscale Score
NCT00711477 (12) [back to overview]	Dutch Eating Behavior Questionnaire - Change in Emotional Eating B Subscale Score
NCT00711477 (12) [back to overview]	Dutch Eating Behavior Questionnaire - Change in Emotional Eating A Subscale Score
NCT00711477 (12) [back to overview]	Percent Change in Body Weight
NCT00711477 (12) [back to overview]	Response to Food Related Cues Using Functional Magnetic Resonance Imaging - Anterior Cingulate
NCT00711477 (12) [back to overview]	Response to Food Related Cues Using Functional Magnetic Resonance Imaging - Hippocampal Region 1
NCT00711477 (12) [back to overview]	Response to Food Related Cues Using Functional Magnetic Resonance Imaging - Hippocampal Region 2
NCT00711477 (12) [back to overview]	Response to Food Related Cues Using Functional Magnetic Resonance Imaging - Posterior Insula
NCT00711477 (12) [back to overview]	Response to Food Related Cues Using Functional Magnetic Resonance Imaging - Superior Frontal
NCT00711477 (12) [back to overview]	Response to Food Related Cues Using Functional Magnetic Resonance Imaging - Superior Parietal
NCT00711477 (12) [back to overview]	Change in Question 19 From 21-Item COE (Control of Eating) Questionnaire
NCT00715117 (3) [back to overview]	Pediatric Crohn's Disease Activity Index Score (PCDAI)
NCT00715117 (3) [back to overview]	Change in Quality of Life Scores From Baseline to After 8 Weeks of Naltrexone Therapy
NCT00715117 (3) [back to overview]	Number of Patients Reporting Side Effects
NCT00743145 (1) [back to overview]	Subjective Marijuana Effects
NCT00773422 (2) [back to overview]	Latency to Initiate Ad-lib Smoking Session
NCT00773422 (2) [back to overview]	Number of Cigarettes Smoked During the Ad-lib Period
NCT00775229 (3) [back to overview]	Liver Function Tests
NCT00775229 (3) [back to overview]	National Institute of Mental Health Trichotillomania Symptom Severity Scale
NCT00775229 (3) [back to overview]	Massachusetts General Hospital Hairpulling Scale
NCT00777062 (2) [back to overview]	Urine Assay for Benzoylecgonine (BE), the Primary Metabolite of Cocaine.
NCT00777062 (2) [back to overview]	Time Line Follow Back -Reported Days of Abstinence From Drinking
NCT00781898 (1) [back to overview]	Relapse
NCT00793780 (6) [back to overview]	Change in Body Weight From Baseline
NCT00793780 (6) [back to overview]	LDL Cholesterol
NCT00793780 (6) [back to overview]	Fasting Serum Glucose Lab Values
NCT00793780 (6) [back to overview]	Insulin Levels
NCT00793780 (6) [back to overview]	PANSS- Positive and Negative Symptom Scale
NCT00793780 (6) [back to overview]	Change in Questionnaire on Craving for Sweet or Rich Foods Score
NCT00817089 (2) [back to overview]	Adrenocorticotropic Hormone (ACTH) Levels
NCT00817089 (2) [back to overview]	Biphasic Alcohol Effects Scale:Total Mood
NCT00831272 (1) [back to overview]	Clinical Response to Naltrexone, as Measured by a Reduction in the Percent Days of Heavy Drinking Days (as Defined by >5 Drinks/Day for Males; >4 for Females) During the 12 Weeks of the Trial.
NCT00834080 (1) [back to overview]	Number of Subjects Reporting at Least 1 Treatment-emergent Adverse Event (TEAE) While on Study.
NCT00920829 (1) [back to overview]	Percent Heavy Drinking Days by mu Opioid Receptor Gene
NCT00938886 (2) [back to overview]	7-day Point Prevalence Smoking Abstinence
NCT00938886 (2) [back to overview]	Percent Heavy Drinking Days
NCT01024335 (2) [back to overview]	Opiate Withdrawal Measured by the Subjective Opiate Withdrawal Scale (SOWS) .
NCT01024335 (2) [back to overview]	Retention
NCT01052831 (2) [back to overview]	Percentage of Participants Assessed as Very Much Improved or Much Improved Based on the Clinical Global Impression-Improvement (CGI-I) Scale
NCT01052831 (2) [back to overview]	Questionnaire for Impulsive-Compulsive Disorders in Parkinson's Disease - Rating Scale (QUIP-RS)
NCT01053078 (2) [back to overview]	Cerebral Blood Flow
NCT01053078 (2) [back to overview]	Hypoglycemia Symptom Score
NCT01055704 (8) [back to overview]	T1/2 of Gastric Emptying of Solid
NCT01055704 (8) [back to overview]	Colonic Geometric Center at 4 Hours
NCT01055704 (8) [back to overview]	Colonic Filling at 6 Hours
NCT01055704 (8) [back to overview]	Colonic Geometric Center at 24 Hours
NCT01055704 (8) [back to overview]	Colonic Geometric Center at 48 Hours
NCT01055704 (8) [back to overview]	Stool Consistency as Reported From the Bristol Stool Scale
NCT01055704 (8) [back to overview]	Stool Frequency
NCT01055704 (8) [back to overview]	T1/2 of Ascending Colon Emptying
NCT01057862 (2) [back to overview]	Gambling Symptom Assessment Scale (G-SAS)
NCT01057862 (2) [back to overview]	Yale Brown Obsessive Compulsive Scale Modified for Pathological Gambling (YBOCS-PG)
NCT01077310 (4) [back to overview]	Alcohol Treatment Outcome: Change in Percent of Heavy Drinking Days
NCT01077310 (4) [back to overview]	Alcohol Treatment Outcome: Change in Average Drinks Per Drinking Day
NCT01077310 (4) [back to overview]	Alcohol Treatment Outcome: Time to Alcohol Relapse
NCT01077310 (4) [back to overview]	Percentage of Those Maintain or Improve to HIV RNA-1 Viral Load Less Then 400 Copies/mL
NCT01100437 (16) [back to overview]	Plasma Decay Half-Life (t1/2) During the Treatment Phase
NCT01100437 (16) [back to overview]	Time to Reach Maximum Observed Plasma Concentration (Tmax) During the Treatment Phase
NCT01100437 (16) [back to overview]	Volume of Distribution (Vd/F)During the Treatment Phase
NCT01100437 (16) [back to overview]	Maximum Observed Plasma Concentration (Cmax) During the Treatment Phase
NCT01100437 (16) [back to overview]	Apparent Oral Clearance (CL/F) During the Treatment Phase
NCT01100437 (16) [back to overview]	Time to First Occurrence of a COWS Score ≥ 13 for Each Treatment During the Treatment Phase
NCT01100437 (16) [back to overview]	Number of Participants With Clinical Opiate Withdrawal Scale (COWS) Score Greater Than or Equal to (≥) 13 in the Treatment Phase
NCT01100437 (16) [back to overview]	Morphine Plasma Concentration at First COWS ≥ 13 in the Treatment Phase
NCT01100437 (16) [back to overview]	Maximum Post-dose COWS in the Treatment Phase
NCT01100437 (16) [back to overview]	6-β-Naltrexone Plasma Concentration at First COWS ≥ 13 in Treatment Phase
NCT01100437 (16) [back to overview]	Area Under the Curve From Time Zero to End of Dosing Interval (AUC0-τ) During the Treatment Phase
NCT01100437 (16) [back to overview]	Area Under the Curve From Time Zero to Extrapolated Infinite Time [AUC (0 - ∞)] During the Treatment Phase
NCT01100437 (16) [back to overview]	Area Under the Curve From Time Zero to the Time of Last Measurable Concentration (AUC0-last) During the Treatment Phase
NCT01100437 (16) [back to overview]	Average Numeric Pain Rating Scale (NPRS) in Titration/Stabilization and Maintenance Phases
NCT01100437 (16) [back to overview]	Naltrexone Plasma Concentration at First COWS ≥ 13 in the Treatment Phase
NCT01100437 (16) [back to overview]	Minimum Observed Plasma Concentration (Cmin) During the Treatment Phase
NCT01100853 (6) [back to overview]	Amphetamine Craving Scale
NCT01100853 (6) [back to overview]	Beck Depression Inventory
NCT01100853 (6) [back to overview]	Number Negative Urines (Proportion Negative Urines)
NCT01100853 (6) [back to overview]	Number Negative Urines (Proportion Negative Urines) Amphetamine
NCT01100853 (6) [back to overview]	Risk Assessment Battery
NCT01100853 (6) [back to overview]	Prior Admissions to Vogur Hospital
NCT01155869 (2) [back to overview]	Treatment Participation
NCT01155869 (2) [back to overview]	Mean Weekly Self-reported Alcohol Consumption
NCT01179191 (14) [back to overview]	Number of Participants With Aberrant Behaviors
NCT01179191 (14) [back to overview]	Number of Participants With Urine Drug Test Results Positive for Unaccounted Opioids
NCT01179191 (14) [back to overview]	Number of Titration Steps to Achieve Stable Dose
NCT01179191 (14) [back to overview]	Percentage of Participants Achieving Stable Dose of EMBEDA Within 6 Weeks Titration Phase
NCT01179191 (14) [back to overview]	Percentage of Participants With Rescue Medications Usage During Titration
NCT01179191 (14) [back to overview]	Change From Baseline in Brief Pain Inventory (BPI) at Visit 3 (First Visit After Successful Titration)
NCT01179191 (14) [back to overview]	Duration to Titrate Participants to Stable Dose Stratified by Prior Opioid Therapy
NCT01179191 (14) [back to overview]	Number of Participants With Abnormal Urine Drug Test Results
NCT01179191 (14) [back to overview]	Number of Participants With Greater Than or Equal to One Urine Drug Test Results Negative for Expected Opioid
NCT01179191 (14) [back to overview]	Number of Titration Steps to Achieve Stable Dose Stratified by Prior Opioid Therapy
NCT01179191 (14) [back to overview]	Percentage of Participants Achieving Stable Dose of EMBEDA Within 6 Weeks Titration Phase Stratified by Prior Opioid Therapy
NCT01179191 (14) [back to overview]	Duration to Titrate Participants to Stable Dose
NCT01179191 (14) [back to overview]	Number of Participants With Urine Drug Test Results Positive for Illicit Substances
NCT01179191 (14) [back to overview]	Investigator's Level of Satisfaction With the EMBEDA Conversion Guide
NCT01180647 (6) [back to overview]	Post-Release Opioid Relapse
NCT01180647 (6) [back to overview]	Accidental Drug Overdose
NCT01180647 (6) [back to overview]	Adverse Events and Serious Adverse Events
NCT01180647 (6) [back to overview]	Injection Drug Use Post-release
NCT01180647 (6) [back to overview]	Any Opioid Use Post-release
NCT01180647 (6) [back to overview]	Participation in Community Drug Treatment Post-release
NCT01211769 (3) [back to overview]	"Drinking Days in the Previous Month"
NCT01211769 (3) [back to overview]	Short Alcohol Dependence Data Questionnaire (SADD)
NCT01211769 (3) [back to overview]	Obsessive Compulsive Drinking Scale (OCDS)
NCT01214083 (9) [back to overview]	Liver Function Tests (ALT)
NCT01214083 (9) [back to overview]	Drinks Per Drinking Days
NCT01214083 (9) [back to overview]	Clinical Global Impression (CGI)
NCT01214083 (9) [back to overview]	Liver Function Tests (AST)
NCT01214083 (9) [back to overview]	Quality of Life Enjoyment and Satisfaction Questionnaire (Q-LES-Q)
NCT01214083 (9) [back to overview]	Percentage of Heavy Drinking Days
NCT01214083 (9) [back to overview]	Percentage of Drinking Days
NCT01214083 (9) [back to overview]	Penn Alcohol Craving Scale (PACS)
NCT01214083 (9) [back to overview]	Obsessive Compulsive Drinking Scale (OCDS)
NCT01218958 (2) [back to overview]	Percentage of Heavy Drinking Days Over the Treatment Period
NCT01218958 (2) [back to overview]	Number of Participants Reporting at Least 1 Treatment-emergent Adverse Event (TEAE)
NCT01218971 (1) [back to overview]	Number of Participants Reporting at Least 1 Treatment-emergent Adverse Event (TEAE) While in Study
NCT01218984 (1) [back to overview]	Slope Change From Baseline for Pupil Size
NCT01218997 (1) [back to overview]	Number of Subjects Reporting at Least 1 Treatment-emergent Adverse Event (TEAE) While on Study
NCT01220414 (1) [back to overview]	Time for Subject to Reach Pain Threshold
NCT01227044 (2) [back to overview]	HAART Adherence
NCT01227044 (2) [back to overview]	Heavy Drinking Days
NCT01245647 (5) [back to overview]	CD4 Count (Mean)
NCT01245647 (5) [back to overview]	HIV Medication Adherence (95% or Better)
NCT01245647 (5) [back to overview]	HIV Viral Load Suppressed
NCT01245647 (5) [back to overview]	Number of Drinks Per Week
NCT01245647 (5) [back to overview]	Risky Sexual Behaviors
NCT01246401 (9) [back to overview]	Antiretroviral Therapy (ART) Adherence 100%
NCT01246401 (9) [back to overview]	ART Adherence for 4 or More Injections XR-NTX Versus Placebo and 3 or Less Injections of XR-NTX
NCT01246401 (9) [back to overview]	Opioid Abstinence at 6 Months for Those With More Than 4 Injections
NCT01246401 (9) [back to overview]	Participants Who Had Undetectable HIV-1 RNA Levels at Less Than 400 Copies/mL at Six Month
NCT01246401 (9) [back to overview]	Particpants Who Had Undetectable HIV-1 RNA Levels at Less Than 50 Copies/mL
NCT01246401 (9) [back to overview]	Time to Opioid Relapse or End of Intervention
NCT01246401 (9) [back to overview]	CD4 Cell Count (Cells/mL)
NCT01246401 (9) [back to overview]	Participants With Opiate Abstinence Via By Doing Urine Toxicology Test
NCT01246401 (9) [back to overview]	Addiction Severity
NCT01296646 (2) [back to overview]	Percent Days Abstinent
NCT01296646 (2) [back to overview]	Percent Heavy Drinking Days
NCT01303835 (3) [back to overview]	Effects of Low-dose Naltrexone Versus Placebo on Change in Functional Capacity From Baseline
NCT01303835 (3) [back to overview]	Effects of Low-dose Naltrexone Versus Placebo on Change in Neurocognitive Function From Baseline
NCT01303835 (3) [back to overview]	Effects of Low-dose Naltrexone Versus Placebo on Change in Quality of Life (QoL) in High-grade Glioma Patients Undergoing Standard Chemoradiation From Baseline
NCT01342549 (1) [back to overview]	Time to Relapse to Heavy Drinking as Defined by Having 5 or More Drinks in a Sitting for Men and Will be Assessed Using the Time Line Follow Back for Recent Drinking Method. A Structured Questionnaire Will Review Alcohol Consumed on the Previous Week.
NCT01380093 (109) [back to overview]	Sleepy: Area Under Effect Curve (AUE) From 0-2 Hours
NCT01380093 (109) [back to overview]	Bad Effects: Area Under Effect Curve (AUE) From 0-8 Hours
NCT01380093 (109) [back to overview]	Bad Effects: Peak Effect (Emax)
NCT01380093 (109) [back to overview]	Bad Effects: Time to Maximum (Peak) Effect (TEmax)
NCT01380093 (109) [back to overview]	Dizzy: Area Under Effect Curve (AUE) From 0-1 Hour
NCT01380093 (109) [back to overview]	Dizzy: Area Under Effect Curve (AUE) From 0-12 Hours
NCT01380093 (109) [back to overview]	Dizzy: Area Under Effect Curve (AUE) From 0-2 Hours
NCT01380093 (109) [back to overview]	Dizzy: Area Under Effect Curve (AUE) From 0-24 Hours
NCT01380093 (109) [back to overview]	Dizzy: Area Under Effect Curve (AUE) From 0-4 Hours
NCT01380093 (109) [back to overview]	Dizzy: Area Under Effect Curve (AUE) From 0-8 Hours
NCT01380093 (109) [back to overview]	Dizzy: Peak Effect (Emax)
NCT01380093 (109) [back to overview]	Dizzy: Time to Maximum (Peak) Effect (TEmax)
NCT01380093 (109) [back to overview]	Drug Liking: Area Under Effect Curve (AUE) From 0-1 Hour
NCT01380093 (109) [back to overview]	Drug Liking: Area Under Effect Curve (AUE) From 0-12 Hours
NCT01380093 (109) [back to overview]	Drug Liking: Area Under Effect Curve (AUE) From 0-2 Hours
NCT01380093 (109) [back to overview]	Drug Liking: Area Under Effect Curve (AUE) From 0-24 Hours
NCT01380093 (109) [back to overview]	Drug Liking: Area Under Effect Curve (AUE) From 0-4 Hours
NCT01380093 (109) [back to overview]	Drug Liking: Area Under Effect Curve (AUE) From 0-8 Hours
NCT01380093 (109) [back to overview]	Drug Liking: Peak Effect (Emax)
NCT01380093 (109) [back to overview]	Drug Liking: Time to Maximum (Peak) Effect (TEmax)
NCT01380093 (109) [back to overview]	Area Under the Curve From Time Zero to Last Quantifiable Concentration [AUC (0-4)] of Naltrexone
NCT01380093 (109) [back to overview]	Feel Sick: Area Under Effect Curve (AUE) From 0-1 Hour
NCT01380093 (109) [back to overview]	Area Under the Curve From Time Zero to Last Quantifiable Concentration [AUC (0-4)] of Naltrexone Metabolite (6-beta-naltrexol)
NCT01380093 (109) [back to overview]	Area Under the Curve From Time Zero to Last Quantifiable Concentration [AUC (0-8)] of Morphine
NCT01380093 (109) [back to overview]	Area Under the Curve From Time Zero to Last Quantifiable Concentration [AUC (0-8)] of Naltrexone
NCT01380093 (109) [back to overview]	Area Under the Curve From Time Zero to Last Quantifiable Concentration [AUC (0-8)] of Naltrexone Metabolite (6-beta-naltrexol)
NCT01380093 (109) [back to overview]	Bad Effects: Area Under Effect Curve (AUE) From 0-1 Hour
NCT01380093 (109) [back to overview]	Bad Effects: Area Under Effect Curve (AUE) From 0-12 Hours
NCT01380093 (109) [back to overview]	Bad Effects: Area Under Effect Curve (AUE) From 0-24 Hours
NCT01380093 (109) [back to overview]	Bad Effects: Area Under Effect Curve (AUE) From 0-4 Hours
NCT01380093 (109) [back to overview]	Feel Sick: Area Under Effect Curve (AUE) From 0-12 Hours
NCT01380093 (109) [back to overview]	Feel Sick: Area Under Effect Curve (AUE) From 0-2 Hours
NCT01380093 (109) [back to overview]	Feel Sick: Area Under Effect Curve (AUE) From 0-24 Hours
NCT01380093 (109) [back to overview]	Feel Sick: Area Under Effect Curve (AUE) From 0-4 Hours
NCT01380093 (109) [back to overview]	Feel Sick: Area Under Effect Curve (AUE) From 0-8 Hours
NCT01380093 (109) [back to overview]	Feel Sick: Peak Effect (Emax)
NCT01380093 (109) [back to overview]	Feel Sick: Time to Maximum (Peak) Effect (TEmax)
NCT01380093 (109) [back to overview]	Good Effects: Area Under Effect Curve (AUE) From 0-1 Hour
NCT01380093 (109) [back to overview]	Good Effects: Area Under Effect Curve (AUE) From 0-12 Hours
NCT01380093 (109) [back to overview]	Good Effects: Area Under Effect Curve (AUE) From 0-2 Hours
NCT01380093 (109) [back to overview]	Good Effects: Area Under Effect Curve (AUE) From 0-24 Hours
NCT01380093 (109) [back to overview]	Good Effects: Area Under Effect Curve (AUE) From 0-4 Hours
NCT01380093 (109) [back to overview]	Good Effects: Area Under Effect Curve (AUE) From 0-8 Hours
NCT01380093 (109) [back to overview]	Good Effects: Peak Effect (Emax)
NCT01380093 (109) [back to overview]	Good Effects: Time to Maximum (Peak) Effect (TEmax)
NCT01380093 (109) [back to overview]	High: Area Under Effect Curve (AUE) From 0-1 Hour
NCT01380093 (109) [back to overview]	High: Area Under Effect Curve (AUE) From 0-12 Hours
NCT01380093 (109) [back to overview]	High: Area Under Effect Curve (AUE) From 0-2 Hours
NCT01380093 (109) [back to overview]	High: Area Under Effect Curve (AUE) From 0-24 Hours
NCT01380093 (109) [back to overview]	High: Area Under Effect Curve (AUE) From 0-4 Hours
NCT01380093 (109) [back to overview]	High: Area Under Effect Curve (AUE) From 0-8 Hours
NCT01380093 (109) [back to overview]	High: Peak Effect (Emax)
NCT01380093 (109) [back to overview]	High: Time to Maximum (Peak) Effect (TEmax)
NCT01380093 (109) [back to overview]	Maximum Observed Plasma Concentration (Cmax) of Morphine
NCT01380093 (109) [back to overview]	Maximum Observed Plasma Concentration (Cmax) of Naltrexone
NCT01380093 (109) [back to overview]	Maximum Observed Plasma Concentration (Cmax) of Naltrexone Metabolite (6-beta-naltrexol)
NCT01380093 (109) [back to overview]	Nausea: Area Under Effect Curve (AUE) From 0-1 Hour
NCT01380093 (109) [back to overview]	Nausea: Area Under Effect Curve (AUE) From 0-12 Hours
NCT01380093 (109) [back to overview]	Nausea: Area Under Effect Curve (AUE) From 0-2 Hours
NCT01380093 (109) [back to overview]	Nausea: Area Under Effect Curve (AUE) From 0-24 Hours
NCT01380093 (109) [back to overview]	Nausea: Area Under Effect Curve (AUE) From 0-4 Hours
NCT01380093 (109) [back to overview]	Nausea: Area Under Effect Curve (AUE) From 0-8 Hours
NCT01380093 (109) [back to overview]	Nausea: Peak Effect (Emax)
NCT01380093 (109) [back to overview]	Nausea: Time to Maximum (Peak) Effect (TEmax)
NCT01380093 (109) [back to overview]	Overall Drug Liking Effect at 24 Hours
NCT01380093 (109) [back to overview]	Pupillometry: Area Under Effect Curve (AUE) From 0-1 Hour
NCT01380093 (109) [back to overview]	Pupillometry: Area Under Effect Curve (AUE) From 0-12 Hours
NCT01380093 (109) [back to overview]	Pupillometry: Area Under Effect Curve (AUE) From 0-2 Hours
NCT01380093 (109) [back to overview]	Pupillometry: Area Under Effect Curve (AUE) From 0-24 Hours
NCT01380093 (109) [back to overview]	Pupillometry: Area Under Effect Curve (AUE) From 0-4 Hours
NCT01380093 (109) [back to overview]	Pupillometry: Area Under Effect Curve (AUE) From 0-8 Hours
NCT01380093 (109) [back to overview]	Pupillometry: Peak Effect (Emax)
NCT01380093 (109) [back to overview]	Bad Effects: Area Under Effect Curve (AUE) From 0-2 Hours
NCT01380093 (109) [back to overview]	Pupillometry: Time to Maximum (Peak) Effect (TEmax)
NCT01380093 (109) [back to overview]	Sleepy: Area Under Effect Curve (AUE) From 0-1 Hour
NCT01380093 (109) [back to overview]	Sleepy: Area Under Effect Curve (AUE) From 0-12 Hours
NCT01380093 (109) [back to overview]	Sleepy: Area Under Effect Curve (AUE) From 0-24 Hours
NCT01380093 (109) [back to overview]	Sleepy: Area Under Effect Curve (AUE) From 0-4 Hours
NCT01380093 (109) [back to overview]	Sleepy: Area Under Effect Curve (AUE) From 0-8 Hours
NCT01380093 (109) [back to overview]	Sleepy: Peak Effect (Emax)
NCT01380093 (109) [back to overview]	Sleepy: Time to Maximum (Peak) Effect (TEmax)
NCT01380093 (109) [back to overview]	Take Drug Again Effect at 24 Hours
NCT01380093 (109) [back to overview]	Time to Reach Maximum Observed Plasma Concentration (Tmax) of Morphine
NCT01380093 (109) [back to overview]	Time to Reach Maximum Observed Plasma Concentration (Tmax) of Naltrexone
NCT01380093 (109) [back to overview]	Time to Reach Maximum Observed Plasma Concentration (Tmax) of Naltrexone Metabolite (6-beta-naltrexol)
NCT01380093 (109) [back to overview]	Any Effects: Area Under Effect Curve (AUE) From 0-1 Hour
NCT01380093 (109) [back to overview]	Any Effects: Area Under Effect Curve (AUE) From 0-12 Hours
NCT01380093 (109) [back to overview]	Any Effects: Area Under Effect Curve (AUE) From 0-2 Hours
NCT01380093 (109) [back to overview]	Any Effects: Area Under Effect Curve (AUE) From 0-24 Hours
NCT01380093 (109) [back to overview]	Any Effects: Area Under Effect Curve (AUE) From 0-4 Hours
NCT01380093 (109) [back to overview]	Any Effects: Area Under Effect Curve (AUE) From 0-8 Hours
NCT01380093 (109) [back to overview]	Any Effects: Peak Effect (Emax)
NCT01380093 (109) [back to overview]	Any Effects: Time to Maximum (Peak) Effect (TEmax)
NCT01380093 (109) [back to overview]	Area Under the Curve From Time Zero to Extrapolated Infinite Time [AUC (0 - ∞)] of Morphine
NCT01380093 (109) [back to overview]	Area Under the Curve From Time Zero to Extrapolated Infinite Time [AUC (0 - ∞)] of Naltrexone
NCT01380093 (109) [back to overview]	Area Under the Curve From Time Zero to Extrapolated Infinite Time [AUC (0 - ∞)] of Naltrexone Metabolite (6-beta-naltrexol)
NCT01380093 (109) [back to overview]	Area Under the Curve From Time Zero to Last Quantifiable Concentration [AUC (0-1)] of Morphine
NCT01380093 (109) [back to overview]	Area Under the Curve From Time Zero to Last Quantifiable Concentration [AUC (0-1)] of Naltrexone
NCT01380093 (109) [back to overview]	Area Under the Curve From Time Zero to Last Quantifiable Concentration [AUC (0-1)] of Naltrexone Metabolite (6-beta-naltrexol)
NCT01380093 (109) [back to overview]	Area Under the Curve From Time Zero to Last Quantifiable Concentration [AUC (0-12)] of Morphine
NCT01380093 (109) [back to overview]	Area Under the Curve From Time Zero to Last Quantifiable Concentration [AUC (0-12)] of Naltrexone
NCT01380093 (109) [back to overview]	Area Under the Curve From Time Zero to Last Quantifiable Concentration [AUC (0-12)] of Naltrexone Metabolite (6-beta-naltrexol)
NCT01380093 (109) [back to overview]	Area Under the Curve From Time Zero to Last Quantifiable Concentration [AUC (0-2)] of Morphine
NCT01380093 (109) [back to overview]	Area Under the Curve From Time Zero to Last Quantifiable Concentration [AUC (0-2)] of Naltrexone
NCT01380093 (109) [back to overview]	Area Under the Curve From Time Zero to Last Quantifiable Concentration [AUC (0-2)] of Naltrexone Metabolite (6-beta-naltrexol)
NCT01380093 (109) [back to overview]	Area Under the Curve From Time Zero to Last Quantifiable Concentration [AUC (0-24)] of Morphine
NCT01380093 (109) [back to overview]	Area Under the Curve From Time Zero to Last Quantifiable Concentration [AUC (0-24)] of Naltrexone
NCT01380093 (109) [back to overview]	Area Under the Curve From Time Zero to Last Quantifiable Concentration [AUC (0-24)] of Naltrexone Metabolite (6-beta-naltrexol)
NCT01380093 (109) [back to overview]	Area Under the Curve From Time Zero to Last Quantifiable Concentration [AUC (0-4)] of Morphine
NCT01402492 (1) [back to overview]	Cocaine Use Days as Measured by Self-report, Corroborated by Thrice-weekly Urine Drug Screens
NCT01428583 (14) [back to overview]	Percentage of Participants With Current Opioid Misuse Measure (COMM) Score of 9 or Above
NCT01428583 (14) [back to overview]	Percentage of Participants With Clinical Opiate Withdrawal Scale (COWS) Score
NCT01428583 (14) [back to overview]	Participants Global Assessment of Treatment Satisfaction
NCT01428583 (14) [back to overview]	Number of Participants With Treatment-Emergent Adverse Events (AEs) and Adverse Reactions
NCT01428583 (14) [back to overview]	Number of Participants With Treatment Emergent (TE) Adverse Events (AEs) Based on Intensity
NCT01428583 (14) [back to overview]	Number of Participants With Rescue Medication (Acetaminophen Tablets)
NCT01428583 (14) [back to overview]	Mean Daily Dose of Study Medication (Oxycodone Component)
NCT01428583 (14) [back to overview]	Mean Change From Baseline in Worst Pain Score at Weeks 1, 4, Months 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 12 or Early Termination
NCT01428583 (14) [back to overview]	Mean Change From Baseline in Pain Right Now Score at Weeks 1, 4, Months 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 12 or Early Termination
NCT01428583 (14) [back to overview]	Mean Change From Baseline in Average Pain Score at Weeks 1, 4, Months 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 12 or Early Termination
NCT01428583 (14) [back to overview]	Time to Stabilization of Study Medication
NCT01428583 (14) [back to overview]	Duration of Exposure to Study Medication
NCT01428583 (14) [back to overview]	Subjective Opiate Withdrawal Scale (SOWS) Score
NCT01428583 (14) [back to overview]	Percentage of Participants With Response to Urine Drug Test
NCT01453374 (9) [back to overview]	Criminal Activity
NCT01453374 (9) [back to overview]	Cocaine Use
NCT01453374 (9) [back to overview]	Opioid Craving
NCT01453374 (9) [back to overview]	Retention in the Community
NCT01453374 (9) [back to overview]	Opioid Overdose
NCT01453374 (9) [back to overview]	Incidence of Subject Re-incarceration
NCT01453374 (9) [back to overview]	Opioid Use
NCT01453374 (9) [back to overview]	Incidence of Subject Re-arrest
NCT01453374 (9) [back to overview]	Drug Abuse Treatment Program Entry
NCT01462227 (6) [back to overview]	Norepinephrine (pg/mL)
NCT01462227 (6) [back to overview]	Glucose Infusion Rate (mg/kg.Min)
NCT01462227 (6) [back to overview]	Glucose (mg/dL)
NCT01462227 (6) [back to overview]	Glucagon (pg/mL)
NCT01462227 (6) [back to overview]	Epinephrine (pg/mL)
NCT01462227 (6) [back to overview]	Cortisol (ug/dL)
NCT01519063 (7) [back to overview]	Stimulation Response to Alcohol: Priming Dose Phase
NCT01519063 (7) [back to overview]	Stimulation Response to Alcohol at Lab Session
NCT01519063 (7) [back to overview]	Sedation Response to Alcohol: Priming Dose Phase
NCT01519063 (7) [back to overview]	Sedation Response to Alcohol at Lab Session
NCT01519063 (7) [back to overview]	Number of Drinks Consumed at Lab Session (Day 7)
NCT01519063 (7) [back to overview]	Craving AUC: Priming Dose Phase
NCT01519063 (7) [back to overview]	Craving AUC: Adlib Drinking Phase
NCT01556425 (2) [back to overview]	Percent of Weekly Urine Samples Negative for Opiates
NCT01556425 (2) [back to overview]	Percent of Weekly Urine Samples Negative for Cocaine
NCT01571362 (101) [back to overview]	Change From Screening Period to the End of Open-Label Titration Period in Participant Assessment of Overall Health State Using the EQ-5D VAS
NCT01571362 (101) [back to overview]	Change From Screening Period to the End of Open-Label Titration Period in Participant Assessment of Overall Health State Using the EuroQol 5-Dimensions (EQ-5D) Summary Index
NCT01571362 (101) [back to overview]	Change From Screening Period to the End of Open-Label Titration Period in Short Form-36v2 (SF-36v2) Health Survey Score
NCT01571362 (101) [back to overview]	Change From Screening to End of Double-Blind Weeks 2, 4, 8, and 12 (or Final Visit) in BPI-sf Scores of Average Pain
NCT01571362 (101) [back to overview]	Change From Screening to End of Double-Blind Weeks 2, 4, 8, and 12 (or Final Visit) in BPI-sf Scores of Least Pain
NCT01571362 (101) [back to overview]	Change From Screening to End of Double-Blind Weeks 2, 4, 8, and 12 (or Final Visit) in BPI-sf Scores of Pain Interference Index
NCT01571362 (101) [back to overview]	Change From Screening to End of Double-Blind Weeks 2, 4, 8, and 12 (or Final Visit) in BPI-sf Scores of Pain Right Now
NCT01571362 (101) [back to overview]	Change From Screening to End of Double-Blind Weeks 2, 4, 8, and 12 (or Final Visit) in BPI-sf Scores of Pain Severity Index
NCT01571362 (101) [back to overview]	Change From Screening to End of Double-Blind Weeks 2, 4, 8, and 12 (or Final Visit) in BPI-sf Scores of Worst Pain
NCT01571362 (101) [back to overview]	Change From Screening to End of Open-Label Titration Period in HRU Questionnaire: Money Spent on Physical Treatments in Past 4 Weeks
NCT01571362 (101) [back to overview]	Change From Screening to End of Open-Label Titration Period in HRU Questionnaire: Nights Stayed in Hospital
NCT01571362 (101) [back to overview]	Change From Screening to End of Open-Label Titration Period in HRU Questionnaire: Number of Office Visits Directly Related or Any Medication Used for Chronic Low Back Pain
NCT01571362 (101) [back to overview]	Change From Screening to Randomization Baseline in HRU Questionnaire: Money Spent on Physical Treatments in Past 4 Weeks
NCT01571362 (101) [back to overview]	Change From Screening to Randomization Baseline in HRU Questionnaire: Nights Stayed in Hospital
NCT01571362 (101) [back to overview]	Change From Screening to Randomization Baseline in HRU Questionnaire: Number of Office Visits Directly Related or Any Medication Used for Chronic Low Back Pain
NCT01571362 (101) [back to overview]	Clinical Opiate Withdrawal Scale (COWS) Total Score During the Open-Label Titration Period
NCT01571362 (101) [back to overview]	COWS Total Score During the Double-Blind Treatment Period
NCT01571362 (101) [back to overview]	COWS Total Score During the Post-Treatment Period
NCT01571362 (101) [back to overview]	Median Time to 20%, 30%, 40%, or 50% Analgesic Response From Screening Period to End of Open-Label Treatment
NCT01571362 (101) [back to overview]	Median Time to 20%, 30%, 40%, or 50% Analgesic Response From Screening Period to Randomization Baseline
NCT01571362 (101) [back to overview]	Median Time to 20%, 30%, 40%, or 50% Loss of Analgesic Response From Baseline During the Double-Blind Treatment Period
NCT01571362 (101) [back to overview]	Naltrexone and 6-β-naltrexol Observed Steady-State Plasma Concentration During the Double Blind Treatment Period
NCT01571362 (101) [back to overview]	Naltrexone and 6-β-naltrexol Observed Steady-State Plasma Concentration During the Titration Period
NCT01571362 (101) [back to overview]	Oxycodone and Noroxycodone Observed Steady-State Plasma Concentration During the Double-Blind Treatment Period
NCT01571362 (101) [back to overview]	Oxycodone and Noroxycodone Observed Steady-State Plasma Concentration During the Titration Period
NCT01571362 (101) [back to overview]	Percentage (%) of Participants With Shift in Patient Global Assessment (PGA) by Category With Baseline PGA Score of Very Good (1), Good (2), Fair (3), Poor (4), Very Poor (5) From Randomization Baseline to End of Double-Blind Week 12 (or Final Visit).
NCT01571362 (101) [back to overview]	Percentage of Participants Who Reported Being Satisfied/Very Satisfied With Treatment on the Satisfaction With Treatment Questionnaire During the Double-Blind Treatment Period
NCT01571362 (101) [back to overview]	Percentage of Participants With a 20%, 30%, 40%, or 50% Analgesic Response From Screening Period to End of Open-Label Treatment
NCT01571362 (101) [back to overview]	Percentage of Participants With a 20%, 30%, 40%, or 50% Analgesic Response From Screening Period to Randomization Baseline
NCT01571362 (101) [back to overview]	Percentage of Participants With a 20%, 30%, 40%, or 50% Loss of Analgesic Response From Randomization Baseline During the Double-Blind Treatment Period
NCT01571362 (101) [back to overview]	Percentage of Participants With Opiate Withdrawal During Post-Treatment by COWS Category
NCT01571362 (101) [back to overview]	Percentage of Participants With Opiate Withdrawal During the Double-Blind Treatment Period by COWS Category
NCT01571362 (101) [back to overview]	Percentage of Participants With Opiate Withdrawal During the Open-Label Titration Period by COWS Category
NCT01571362 (101) [back to overview]	Percentage of Participants With Shift From Randomization Baseline to End of Double-Blind Week 4 in PGA of Low Back Pain by Category in Participants With Randomization Baseline PGA Score of Very Good, Good, Fair, Poor, Very Poor
NCT01571362 (101) [back to overview]	Percentage of Participants With Shift From Randomization Baseline to End of Double-Blind Week 8 in PGA of Low Back Pain by Category in Participants With Randomization Baseline PGA Score of Very Good , Good, Fair, Poor, Very Poor
NCT01571362 (101) [back to overview]	Percentage of Participants With Shift From Randomization Baseline to End of Double-Blind Weeks 4, 8, and 12 (or Final Visit) in Hospitalization Because of Low Back Pain as Assessed Using the HRU Questionnaire
NCT01571362 (101) [back to overview]	Percentage of Participants With Shift From Screening Period to End of Open-Label Titration Period in Hospitalization Because of Low Back Pain as Assessed Using the Healthcare Resource Use (HRU) Questionnaire
NCT01571362 (101) [back to overview]	Percentage of Participants With Shift From Screening Period to Randomization Baseline in Hospitalization Because of Low Back Pain as Assessed Using the HRU Questionnaire
NCT01571362 (101) [back to overview]	Percentage of Participants With Shift From Screening Period to the End of Double-Blind Weeks 4, 8 and 12 (or Final Visit) in Hospitalization Because of Low Back Pain as Assessed Using the HRU Questionnaire
NCT01571362 (101) [back to overview]	Percentage of Participants With Shift From Screening to Randomization Baseline in PGA of Low Back Pain by Category in Participants With Screening PGA Score of Very Good, Good, Fair, Poor, Very Poor
NCT01571362 (101) [back to overview]	Percentage of Participants With Shift From Screening to the End of the Open-Label Titration Period in PGA of Low Back Pain by Category in Participants With Screening PGA Score of Very Good, Good, Fair, Poor, Very Poor
NCT01571362 (101) [back to overview]	Satisfaction With Treatment at Randomization Baseline
NCT01571362 (101) [back to overview]	Satisfaction With Treatment at the End of Open-Label Titration Period for All Participants
NCT01571362 (101) [back to overview]	SOWS Total Score During the Double-Blind Treatment Period
NCT01571362 (101) [back to overview]	SOWS Total Score During the Post-Treatment Period
NCT01571362 (101) [back to overview]	Change From Randomization Baseline to End of Double-Blind Weeks 2, 4, 8, and 12 (or Final Visit) in BPI-sf Scores of Pain Severity Index
NCT01571362 (101) [back to overview]	Area Under the Curve (AUC) of eDiary NRS-Pain Scores From Randomization Baseline to Final 2 Weeks of the Double-Blind Treatment Period (Weeks 11 and 12)
NCT01571362 (101) [back to overview]	Average Daily Use of Rescue Acetaminophen (Milligrams Per Day [mg/Day]) During the Double-Blind Treatment Period
NCT01571362 (101) [back to overview]	Change From Randomization Baseline to End of Double-Blind Week 12 (or Final Visit) in Participant Assessment of Overall Health State Using EQ-5D Summary Index
NCT01571362 (101) [back to overview]	Change From Randomization Baseline to End of Double-Blind Week 12 (or Final Visit) in Participant Assessment of Overall Health State Using the EQ-5D VAS
NCT01571362 (101) [back to overview]	Change From Screening Period to End of Double-Blind Week 12 (or Final Visit) in Participant Assessment of Overall Health State Using EQ-5D Summary Index
NCT01571362 (101) [back to overview]	Change From Screening Period to End of Double-Blind Week 12 (or Final Visit) in Participant Assessment of Overall Health State Using EQ-5D VAS
NCT01571362 (101) [back to overview]	Change in Roland-Morris Disability Questionnaire (RMDQ) Total Score From Randomization Baseline to the End of Double-Blind Week 12 (or Final Visit).
NCT01571362 (101) [back to overview]	Change in Weekly Average Electronic Diary (eDiary) Numeric Rating Scale -Pain (NRS-Pain) Score From Randomization Baseline to Final 2 Weeks (Average of Weeks 11 and 12)
NCT01571362 (101) [back to overview]	Mean Oxycodone Average Daily Dose During the Double-Blind Treatment Period
NCT01571362 (101) [back to overview]	Mean Oxycodone Average Daily Dose During the Open-Label Titration Period
NCT01571362 (101) [back to overview]	Mean Oxycodone Duration of Titration During the Open-Label Titration Period
NCT01571362 (101) [back to overview]	Mean Oxycodone Duration of Treatment During the Double-Blind Treatment Period
NCT01571362 (101) [back to overview]	Median Oxycodone Average Daily Dose During the Double-Blind Treatment Period
NCT01571362 (101) [back to overview]	Median Oxycodone Average Daily Dose During the Open-Label Titration Period
NCT01571362 (101) [back to overview]	Median Oxycodone Duration of Titration During the Open-Label Titration Period
NCT01571362 (101) [back to overview]	Median Oxycodone Duration of Treatment During the Double-Blind Treatment Period
NCT01571362 (101) [back to overview]	Median Time to Treatment Discontinuation for Investigator-Reported Lack of Efficacy During the Double-Blind Treatment Period
NCT01571362 (101) [back to overview]	Percentage of Participants Discontinuing Treatment for Investigator-Reported Lack of Efficacy
NCT01571362 (101) [back to overview]	Percentage of Participants With Improvement in Weekly Average eDiary NRS-Pain Scores From Screening to Final 2 Weeks of the Double-Blind Treatment Period (Average of Weeks 11 and 12) by Cumulative Percent Reduction ≥30%
NCT01571362 (101) [back to overview]	Percentage of Participants With Improvement in Weekly Average eDiary NRS-Pain Scores From Screening to Final 2 Weeks of the Double-Blind Treatment Period (Average of Weeks 11 and 12) by Cumulative Percent Reduction ≥40%
NCT01571362 (101) [back to overview]	Percentage of Participants With Improvement in Weekly Average eDiary NRS-Pain Scores From Screening to Final 2 Weeks of the Double-Blind Treatment Period (Average of Weeks 11 and 12) by Cumulative Percent Reduction ≥50%
NCT01571362 (101) [back to overview]	Percentage of Participants With Improvement in Weekly Average eDiary NRS-Pain Scores From Screening to Final 2 Weeks of the Double-Blind Treatment Period (Average of Weeks 11 and 12) by Cumulative Percent Reduction of Greater or Equal to (≥) 20%
NCT01571362 (101) [back to overview]	Change From Randomization Baseline to End of Double-Blind Weeks 2, 4, 8, and 12 (or Final Visit) in BPI-sf Scores of Average Pain
NCT01571362 (101) [back to overview]	Change From Randomization Baseline to End of Double-Blind Weeks 2, 4, 8, and 12 (or Final Visit) in BPI-sf Scores of Least Pain
NCT01571362 (101) [back to overview]	Change From Randomization Baseline to End of Double-Blind Weeks 2, 4, 8, and 12 (or Final Visit) in BPI-sf Scores of Pain Interference Index
NCT01571362 (101) [back to overview]	Change From Randomization Baseline to End of Double-Blind Weeks 2, 4, 8, and 12 (or Final Visit) in BPI-sf Scores of Pain Right Now
NCT01571362 (101) [back to overview]	Change From Randomization Baseline to End of Double-Blind Weeks 2, 4, 8, and 12 (or Final Visit) in BPI-sf Scores of Worst Pain
NCT01571362 (101) [back to overview]	Change From Randomization Baseline to End of Double-Blind Weeks 4, 8 and 12 (or Final Visit) in HRU Questionnaire: Money Spent on Treatments
NCT01571362 (101) [back to overview]	Change From Randomization Baseline to End of Double-Blind Weeks 4, 8 and 12 (or Final Visit) in HRU Questionnaire: Nights Spent in Hospital
NCT01571362 (101) [back to overview]	Change From Randomization Baseline to End of Double-Blind Weeks 4, 8 and 12 (or Final Visit) in HRU Questionnaire: Number of Office Visits Related to or Medications Used for Chronic Low Back Pain
NCT01571362 (101) [back to overview]	Change From Randomization Baseline to End of Double-Blind Weeks 4, 8, and 12 (or Final Visit) in WPAI:SHP Percent Activity Impairment Due to Low Back Pain
NCT01571362 (101) [back to overview]	Change From Randomization Baseline to End of Double-Blind Weeks 4, 8, and 12 (or Final Visit) in WPAI:SHP Percent Impairment Due to Low Back Pain
NCT01571362 (101) [back to overview]	Subjective Opiate Withdrawal Scale (SOWS) During the Open-Label Titration Period
NCT01571362 (101) [back to overview]	Change From Randomization Baseline to End of Double-Blind Weeks 4, 8, and 12 (or Final Visit) in WPAI:SHP Percent Overall Work Impairment Due to Low Back Pain
NCT01571362 (101) [back to overview]	Change From Randomization Baseline to End of Double-Blind Weeks 4, 8, and 12 (or Final Visit) in WPAI:SHP Percent Work Time Missed Due to Low Back Pain
NCT01571362 (101) [back to overview]	Change From Randomization Baseline to the End of Double-Blind Week 12 (or Final Visit) in SF-36v2 Health Survey
NCT01571362 (101) [back to overview]	Change From Randomization Baseline to the End of Double-Blind Weeks 2, 4, and 8 in RMDQ Total Score
NCT01571362 (101) [back to overview]	Change From Screening Period to End of Double-Blind Week 12 (or Final Visit) in SF-36v2 Health Survey
NCT01571362 (101) [back to overview]	Change From Screening Period to End of Double-Blind Weeks 2, 4, 8, and 12 (or Final Visit) in RMDQ Total Score
NCT01571362 (101) [back to overview]	Change From Screening Period to End of Double-Blind Weeks 4, 8 and 12 (or Final Visit) in HRU Questionnaire: Money Spent on Treatment for Chronic Low Back Pain
NCT01571362 (101) [back to overview]	Change From Screening Period to End of Double-Blind Weeks 4, 8 and 12 (or Final Visit) in HRU Questionnaire: Nights in Hospital for Chronic Low Back Pain
NCT01571362 (101) [back to overview]	Change From Screening Period to End of Double-Blind Weeks 4, 8 and 12 (or Final Visit) in HRU Questionnaire: Number of Office Visits Related or Medication Used for Chronic Low Back Pain
NCT01571362 (101) [back to overview]	Change From Screening Period to End of Double-Blind Weeks 4, 8, and 12 (or Final Visit) in WPAI:SHP Percent Activity Impairment Due to Low Back Pain
NCT01571362 (101) [back to overview]	Change From Screening Period to End of Double-Blind Weeks 4, 8, and 12 (or Final Visit) in WPAI:SHP Percent Impairment Due to Low Back Pain
NCT01571362 (101) [back to overview]	Change From Screening Period to End of Double-Blind Weeks 4, 8, and 12 (or Final Visit) in WPAI:SHP Percent Overall Work Impairment Due to Low Back Pain
NCT01571362 (101) [back to overview]	Change From Screening Period to End of Double-Blind Weeks 4, 8, and 12 (or Final Visit) in WPAI:SHP Percent Work Time Missed Due to Low Back Pain
NCT01571362 (101) [back to overview]	Change From Screening Period to End of Open-Label in Work Productivity and Activity Impairment Questionnaire: Specific Health Problem (WPAI:SHP): % Work Time Missed, % Impairment, % Overall Work Impairment, % Activity Impairment Due to Low Back Pain
NCT01571362 (101) [back to overview]	Change From Screening Period to End of Open-Label Titration Period in Roland-Morris Disability Questionnaire (RMDQ) Total Score for All Participants
NCT01571362 (101) [back to overview]	Change From Screening Period to End of Open-Label Treatment in Brief Pain Inventory - Short Form (BPI-sf): Worst Pain, Least Pain, Average Pain, Pain Right Now, Pain Severity Index, Pain Interference Index
NCT01571362 (101) [back to overview]	Change From Screening Period to Randomization Baseline in BPI-sf: Worst Pain, Least Pain, Average Pain, Pain Right Now, Pain Severity Index, Pain Interference Index
NCT01571362 (101) [back to overview]	Change From Screening Period to Randomization Baseline in Participant Assessment of Overall Health State Using the EQ-5D Summary Index
NCT01571362 (101) [back to overview]	Change From Screening Period to Randomization Baseline in Participant Assessment of Overall Health State Using the EQ-5D VAS
NCT01571362 (101) [back to overview]	Change From Screening Period to Randomization Baseline in RMDQ Total Score
NCT01571362 (101) [back to overview]	Change From Screening Period to Randomization Baseline in SF-36v2 Health Survey Score
NCT01571362 (101) [back to overview]	Change From Screening Period to Randomization Baseline in WPAI:SHP: Percent Work Time Missed, Percent Impairment, Percent Overall Work Impairment, Percent Activity Impairment Due to Low Back Pain
NCT01625091 (4) [back to overview]	Craving for Alcohol
NCT01625091 (4) [back to overview]	Drinking Problems (SIP-2R Score)
NCT01625091 (4) [back to overview]	Number of Binge Drinking Days
NCT01625091 (4) [back to overview]	Number of Participants Who Quit Hazardous Drinking
NCT01625611 (3) [back to overview]	Baseline KOR Differences
NCT01625611 (3) [back to overview]	Occupancy of KOR by NTX and Drinking
NCT01625611 (3) [back to overview]	Relationship Between NTX Responsivity and Occupancy of KOR
NCT01650350 (2) [back to overview]	To Assess the Toxicity Associated With Low Dose Naltrexone for Melanoma, CRPC and Renal Cancer.
NCT01650350 (2) [back to overview]	Number of Responses to Low Dose Naltrexone for Patients With Advanced Melanoma, Castrate Refractory Prostate Cancer (CRPC) or Renal Cancer Via RECIST
NCT01672723 (3) [back to overview]	Changes in Self-reported Feelings of Connection During Naltrexone (vs. Placebo)
NCT01672723 (3) [back to overview]	Daily Self-reported Feelings of Social Connection
NCT01672723 (3) [back to overview]	Self-reported Physical Symptoms
NCT01673594 (2) [back to overview]	Safety
NCT01673594 (2) [back to overview]	Change in Score on AISRS From Baseline to Week 6
NCT01690546 (10) [back to overview]	Craving
NCT01690546 (10) [back to overview]	Percentage of Participants Who Adhered to Study Visits.
NCT01690546 (10) [back to overview]	Percentage of Participants With Adherence to Medication (Naltrexone)
NCT01690546 (10) [back to overview]	Retention in Treatment
NCT01690546 (10) [back to overview]	Use of Ancillary Medications.
NCT01690546 (10) [back to overview]	Withdrawal Intensity as Measured by the Clinical Opiate Withdrawal Scale (COWS)
NCT01690546 (10) [back to overview]	Withdrawal Intensity as Measured by the Subjective Opiate Withdrawal Scale (SOWS)
NCT01690546 (10) [back to overview]	Illicit Drug Use, Measured by Urine Drug Testing
NCT01690546 (10) [back to overview]	Number of Participants That Self Reported Illicit Drug Use
NCT01690546 (10) [back to overview]	Satisfaction With Treatment, Measured by a Treatment Satisfaction Questionnaire
NCT01721330 (1) [back to overview]	Change in Adult Investigator Symptom Rating Scale (AISRS) Score
NCT01723384 (3) [back to overview]	Feasibility of Retaining Participants in Trial
NCT01723384 (3) [back to overview]	Tolerability to Study Drug, as Measured by Adverse Events
NCT01723384 (3) [back to overview]	Acceptability to Taking Medication
NCT01746901 (52) [back to overview]	Time to Reach Maximum Observed Plasma Concentration (Tmax) of Oxycodone, Oxymorphone and Noroxycodone
NCT01746901 (52) [back to overview]	Time to Reach Maximum Observed Plasma Concentration (Tmax) of Naltrexone and 6-beta-naltrexol
NCT01746901 (52) [back to overview]	Take Drug Again Effect at Hours 12, 24 and 36
NCT01746901 (52) [back to overview]	Sleepy: Area Under Effect Curve (AUE) From 0-1 Hour, 0-2 Hour, 0-8 Hour, 0-12 Hour, 0-24 Hour and 0-36 Hour
NCT01746901 (52) [back to overview]	Pupillometry: Area Under Effect Curve (AUE) From 0-1 Hour, 0-2 Hour, 0-8 Hour, 0-12 Hour, 0-24 Hour and 0-36 Hour
NCT01746901 (52) [back to overview]	Overall Drug Liking Effect at Hours 12, 24 and 36
NCT01746901 (52) [back to overview]	Number of Participants With Treatment-Emergent Adverse Events (AEs) or Serious Adverse Events (SAEs)
NCT01746901 (52) [back to overview]	Nausea: Area Under Effect Curve (AUE) From 0-1 Hour, 0-2 Hour, 0-8 Hour, 0-12 Hour, 0-24 Hour and 0-36 Hour
NCT01746901 (52) [back to overview]	Maximum Observed Plasma Concentration (Cmax) of Naltrexone and 6-beta-naltrexol
NCT01746901 (52) [back to overview]	High: Area Under Effect Curve (AUE) From 0-1 Hour, 0-8 Hour, 0-12 Hour, 0-24 Hour and 0-36 Hour
NCT01746901 (52) [back to overview]	Good Drug Effects: Area Under Effect Curve (AUE) From 0-1 Hour, 0-2 Hour, 0-8 Hour, 0-12 Hour, 0-24 Hour and 0-36 Hour
NCT01746901 (52) [back to overview]	Feel Sick: Area Under Effect Curve (AUE) From 0-1 Hour, 0-2 Hour, 0-8 Hour, 0-12 Hour, 0-24 Hour and 0-36 Hour
NCT01746901 (52) [back to overview]	Drug Liking: Area Under Effect Curve (AUE) From 0-1 Hour, 0-8 Hour, 0-12 Hour, 0-24 Hour and 0-36 Hour
NCT01746901 (52) [back to overview]	Dose Normalized Maximum Observed Plasma Concentration (Cmax[dn]) of Oxycodone, Oxymorphone and Noroxycodone
NCT01746901 (52) [back to overview]	Dizzy: Area Under Effect Curve (AUE) From 0-1 Hour, 0-2 Hour, 0-8 Hour, 0-12 Hour, 0-24 Hour and 0-36 Hour
NCT01746901 (52) [back to overview]	Area Under the Concentration-Time Curve (AUC) From 0-1 Hour, 0-2 Hour, 0-8 Hour 0-12 Hour and 0-24 Hour of Oxycodone
NCT01746901 (52) [back to overview]	Any Drug Effects: Area Under Effect Curve (AUE) From 0-1 Hour, 0-2 Hour, 0-8 Hour, 0-12 Hour, 0-24 Hour and 0-36 Hour
NCT01746901 (52) [back to overview]	Take Drug Again: Peak Effect (Emax)
NCT01746901 (52) [back to overview]	Take Drug Again: Minimum Effect (Emin)
NCT01746901 (52) [back to overview]	Take Drug Again: Mean Effect (Emean)
NCT01746901 (52) [back to overview]	Sleepy: Time to Maximum (Peak) Effect (TEmax)
NCT01746901 (52) [back to overview]	Sleepy: Peak Effect (Emax)
NCT01746901 (52) [back to overview]	Pupillometry: Time to Maximum (Peak) Effect (TEmax)
NCT01746901 (52) [back to overview]	Pupillometry: Peak Effect (Emax)
NCT01746901 (52) [back to overview]	Plasma Terminal Half-Life (t1/2) of Oxycodone
NCT01746901 (52) [back to overview]	Overall Drug Liking: Peak Effect (Emax)
NCT01746901 (52) [back to overview]	Overall Drug Liking: Minimum Effect (Emin)
NCT01746901 (52) [back to overview]	Overall Drug Liking: Mean Effect (Emean)
NCT01746901 (52) [back to overview]	Number of Participants With Clinically Significant Change in Vital Sign Examinations
NCT01746901 (52) [back to overview]	Number of Participants With Clinically Significant Change in Oxygen Saturation of Hemoglobin (SpO2)
NCT01746901 (52) [back to overview]	Number of Participants With Clinically Significant Change in End Tidal Carbon Dioxide (EtCO2)
NCT01746901 (52) [back to overview]	Nausea: Time to Maximum (Peak) Effect (TEmax)
NCT01746901 (52) [back to overview]	Nausea: Peak Effect (Emax)
NCT01746901 (52) [back to overview]	High: Time to Maximum (Peak) Effect (TEmax)
NCT01746901 (52) [back to overview]	High: Area Under Effect Curve (AUE) From 0-2 Hour
NCT01746901 (52) [back to overview]	Good Drug Effects: Time to Maximum (Peak) Effect (TEmax)
NCT01746901 (52) [back to overview]	Good Drug Effects: Peak Effect (Emax)
NCT01746901 (52) [back to overview]	Feel Sick: Time to Maximum (Peak) Effect (TEmax)
NCT01746901 (52) [back to overview]	Feel Sick: Peak Effect (Emax)
NCT01746901 (52) [back to overview]	Drug Liking: Time to Maximum (Peak) Effect (TEmax)
NCT01746901 (52) [back to overview]	Drug Liking: Peak Effect (Emax)
NCT01746901 (52) [back to overview]	Bad Drug Effects: Area Under Effect Curve (AUE) From 0-1 Hour, 0-2 Hour, 0-8 Hour, 0-12 Hour, 0-24 Hour and 0-36 Hour
NCT01746901 (52) [back to overview]	Dose Normalized Area Under the Curve From Time Zero to Extrapolated Infinite Time [AUC (0 - ∞)dn] of Oxycodone
NCT01746901 (52) [back to overview]	Dizzy: Time to Maximum (Peak) Effect (TEmax)
NCT01746901 (52) [back to overview]	Dizzy: Peak Effect (Emax)
NCT01746901 (52) [back to overview]	Bad Drug Effects: Time to Maximum (Peak) Effect (TEmax)
NCT01746901 (52) [back to overview]	Bad Drug Effects: Peak Effect (Emax)
NCT01746901 (52) [back to overview]	Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUClast) of Oxycodone
NCT01746901 (52) [back to overview]	Any Drug Effects: Time to Maximum (Peak) Effect (TEmax)
NCT01746901 (52) [back to overview]	Any Drug Effects: Peak Effect (Emax)
NCT01746901 (52) [back to overview]	High: Peak Effect (Emax)
NCT01746901 (52) [back to overview]	Drug Liking: Area Under Effect Curve (AUE) From 0-2 Hour
NCT01775189 (58) [back to overview]	Area Under the Curve From Time Zero to Extrapolated Infinite Time [AUC (0 - ∞)] of Oxycodone, Oxymorphone and Noroxycodone
NCT01775189 (58) [back to overview]	High: Time to Maximum (Peak) Effect (TEmax)
NCT01775189 (58) [back to overview]	Bad Drug Effects: Area Under Effect Curve (AUE) From 0-1 Hour, 0-2 Hour, 0-8 Hour and 0-24 Hour
NCT01775189 (58) [back to overview]	Area Under the Curve From Time Zero to Extrapolated Infinite Time [AUC (0 - ∞)] of Naltrexone and 6-beta-naltrexol
NCT01775189 (58) [back to overview]	Area Under the Concentration-Time Curve (AUC) From 0-1 Hour, 0-2 Hour and 0-8 Hour of Oxycodone, Oxymorphone and Noroxycodone
NCT01775189 (58) [back to overview]	Area Under the Concentration-Time Curve (AUC) From 0-1 Hour, 0-2 Hour and 0-8 Hour of Naltrexone and 6-beta-naltrexol
NCT01775189 (58) [back to overview]	Any Drug Effects: Area Under Effect Curve (AUE) From 0-1 Hour, 0-2 Hour, 0-8 Hour and 0-24 Hour
NCT01775189 (58) [back to overview]	Take Drug Again: Peak Effect (Emax)
NCT01775189 (58) [back to overview]	Sleepy: Time to Maximum (Peak) Effect (TEmax)
NCT01775189 (58) [back to overview]	Sleepy: Peak Effect (Emax)
NCT01775189 (58) [back to overview]	Pupillometry: Time to Maximum (Peak) Effect (TEmax)
NCT01775189 (58) [back to overview]	Pupillometry: Peak Effect (Emax)
NCT01775189 (58) [back to overview]	Percentage of Dose (Drug Powder) Insufflated
NCT01775189 (58) [back to overview]	Overall Drug Liking: Peak Effect (Emax)
NCT01775189 (58) [back to overview]	Overall Drug Liking: Mean Effect (Emean)
NCT01775189 (58) [back to overview]	Number of Participants With Clinically Significant Change in Vital Sign Examinations
NCT01775189 (58) [back to overview]	Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUClast) of Oxycodone, Oxymorphone and Noroxycodone
NCT01775189 (58) [back to overview]	Number of Participants With Clinically Significant Change in Oxygen Saturation of Hemoglobin (SpO2)
NCT01775189 (58) [back to overview]	Number of Participants With Clinically Significant Change in End Tidal Carbon Dioxide (EtCO2)
NCT01775189 (58) [back to overview]	Nausea: Time to Maximum (Peak) Effect (TEmax)
NCT01775189 (58) [back to overview]	Nausea: Peak Effect (Emax)
NCT01775189 (58) [back to overview]	Dizzy: Area Under Effect Curve (AUE) From 0-1 Hour, 0-2 Hour, 0-8 Hour and 0-24 Hour
NCT01775189 (58) [back to overview]	Drug Liking: Area Under Effect Curve (AUE) From 0-1 Hour, 0-8 Hour and 0-24 Hour
NCT01775189 (58) [back to overview]	Feel Sick: Area Under Effect Curve (AUE) From 0-1 Hour, 0-2 Hour, 0-8 Hour and 0-24 Hour
NCT01775189 (58) [back to overview]	Good Drug Effects: Area Under Effect Curve (AUE) From 0-1 Hour, 0-2 Hour, 0-8 Hour and 0-24 Hour
NCT01775189 (58) [back to overview]	High: Area Under Effect Curve (AUE) From 0-1 Hour, 0-8 Hour and 0-24 Hours
NCT01775189 (58) [back to overview]	Maximum Observed Plasma Concentration (Cmax) of Naltrexone and 6-beta-naltrexol
NCT01775189 (58) [back to overview]	Any Drug Effects: Peak Effect (Emax)
NCT01775189 (58) [back to overview]	Any Drug Effects: Time to Maximum (Peak) Effect (TEmax)
NCT01775189 (58) [back to overview]	Bad Drug Effects: Peak Effect (Emax)
NCT01775189 (58) [back to overview]	Bad Drug Effects: Time to Maximum (Peak) Effect (TEmax)
NCT01775189 (58) [back to overview]	Dizzy: Peak Effect (Emax)
NCT01775189 (58) [back to overview]	Dizzy: Time to Maximum (Peak) Effect (TEmax)
NCT01775189 (58) [back to overview]	Drug Liking: Area Under Effect Curve (AUE) From 0-2 Hour
NCT01775189 (58) [back to overview]	Drug Liking: Peak Effect (Emax)
NCT01775189 (58) [back to overview]	Drug Liking: Time to Maximum (Peak) Effect (TEmax)
NCT01775189 (58) [back to overview]	Feel Sick: Peak Effect (Emax)
NCT01775189 (58) [back to overview]	Feel Sick: Time to Maximum (Peak) Effect (TEmax)
NCT01775189 (58) [back to overview]	Good Drug Effects: Peak Effect (Emax)
NCT01775189 (58) [back to overview]	Take Drug Again: Mean Effect (Emean)
NCT01775189 (58) [back to overview]	Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUClast) of Naltrexone and 6-beta-naltrexol
NCT01775189 (58) [back to overview]	Good Drug Effects: Time to Maximum (Peak) Effect (TEmax)
NCT01775189 (58) [back to overview]	High: Area Under Effect Curve (AUE) From 0-2 Hour
NCT01775189 (58) [back to overview]	High: Peak Effect (Emax)
NCT01775189 (58) [back to overview]	Time to Reach Maximum Observed Plasma Concentration (Tmax) of Oxycodone, Oxymorphone and Noroxycodone
NCT01775189 (58) [back to overview]	Time to Reach Maximum Observed Plasma Concentration (Tmax) of Naltrexone and 6-beta-naltrexol
NCT01775189 (58) [back to overview]	Take Drug Again Effect at Hours 12 and 24
NCT01775189 (58) [back to overview]	Overall Drug Liking Effect at Hours 12 and 24
NCT01775189 (58) [back to overview]	Subject Rating Scale for Nasal Effects: Time to Maximum (Peak) Effect (TEmax)
NCT01775189 (58) [back to overview]	Subject Rating Scale for Nasal Effects: Peak Effect (Emax)
NCT01775189 (58) [back to overview]	Subject Rating Scale for Nasal Effects: Area Under Effect Curve (AUE) From 0-1 Hour and 0-2 Hour
NCT01775189 (58) [back to overview]	Sleepy: Area Under Effect Curve (AUE) From 0-1 Hour, 0-2 Hour, 0-8 Hour and 0-24 Hour
NCT01775189 (58) [back to overview]	Pupillometry: Area Under Effect Curve (AUE) From 0-1 Hour, 0-2 Hour, 0-8 Hour and 0-24 Hour
NCT01775189 (58) [back to overview]	Plasma Decay Half-Life (t1/2) of Oxycodone, Oxymorphone and Noroxycodone
NCT01775189 (58) [back to overview]	Plasma Decay Half-Life (t1/2) of Naltrexone and 6-beta-naltrexol
NCT01775189 (58) [back to overview]	Number of Participants With Treatment-Emergent Adverse Events (AEs) or Serious Adverse Events (SAEs)
NCT01775189 (58) [back to overview]	Nausea: Area Under Effect Curve (AUE) From 0-1 Hour, 0-2 Hour, 0-8 Hour and 0-24 Hour
NCT01775189 (58) [back to overview]	Maximum Observed Plasma Concentration (Cmax) of Oxycodone, Oxymorphone and Noroxycodone
NCT01822132 (5) [back to overview]	Risk Assessment Battery (RAB)
NCT01822132 (5) [back to overview]	Barrat Impulsiveness Scale (BIS)
NCT01822132 (5) [back to overview]	Discounting Tasks: Sexual Probability Discounting (SexPD)
NCT01822132 (5) [back to overview]	Discounting Tasks: Standard Delay Discounting (DD)
NCT01822132 (5) [back to overview]	Methamphetamine Use
NCT01843023 (4) [back to overview]	Treatment Retention
NCT01843023 (4) [back to overview]	Opioid Use at 6 Month Follow-up
NCT01843023 (4) [back to overview]	Monetized Healthcare Utilization
NCT01843023 (4) [back to overview]	HIV Sex Risk Behaviors
NCT01856712 (4) [back to overview]	Ongoing Alcohol Consumption
NCT01856712 (4) [back to overview]	Percentage of Participants Adhered to Medication
NCT01856712 (4) [back to overview]	Percentage of Patients Attended Recommended Outpatient Substance Abuse Treatment
NCT01856712 (4) [back to overview]	Retention Rate: Percentage of Participants Attended an Initial Behavioral Treatment Visit Within 2 Weeks of Hospital Discharge.
NCT01866098 (8) [back to overview]	Change in Weight From Baseline
NCT01866098 (8) [back to overview]	Changes in Fasting Glucose From Baseline
NCT01866098 (8) [back to overview]	Percent of Subjects Who Lost More Than 5% of Body Weight From Baseline
NCT01866098 (8) [back to overview]	Changes in Total Cholesterol From Baseline
NCT01866098 (8) [back to overview]	Changes in LDL From Baseline
NCT01866098 (8) [back to overview]	Changes in Insulin From Baseline
NCT01866098 (8) [back to overview]	Changes in HDL From Baseline
NCT01866098 (8) [back to overview]	Changes in Glycosylated Hemoglobin (HbA1c) From Baseline
NCT01873729 (2) [back to overview]	Change in Adult Investigator Symptom Rating Scale (AISRS) Scores From Baseline
NCT01873729 (2) [back to overview]	Clinical Global Impression (CGI)
NCT01874951 (8) [back to overview]	Change in HAM-D28 Total Score
NCT01874951 (8) [back to overview]	Response Rate
NCT01874951 (8) [back to overview]	Remission Rate
NCT01874951 (8) [back to overview]	Change in MADRS-15 Total Score
NCT01874951 (8) [back to overview]	Change in HAM-D-17 Total Score
NCT01874951 (8) [back to overview]	Change in CGI-S Total Score
NCT01874951 (8) [back to overview]	Change in MADRS-10 Total Score
NCT01874951 (8) [back to overview]	Final CGI-I Score
NCT01893827 (1) [back to overview]	Percentage of Participants With Alcohol Abstinence or Moderate Drinking
NCT01895036 (1) [back to overview]	Successful Discontinuation of Buprenorphine
NCT01903837 (5) [back to overview]	Percentage of Subjects Exhibiting Significant Weight Gain at Day 92
NCT01903837 (5) [back to overview]	Change in Clinical Global Impressions - Severity (CGI-S) From Baseline to Day 92
NCT01903837 (5) [back to overview]	Absolute Change in Total Positive and Negative Syndrome Scale (PANSS) Score
NCT01903837 (5) [back to overview]	Absolute Change in Body Weight (kg) From Baseline to Day 92
NCT01903837 (5) [back to overview]	Percent Change in Body Weight (Kilogram) From Baseline to Day 92
NCT01908062 (11) [back to overview]	Number of Participants With Urine Drug Screen (UDS) Positive for Opioids
NCT01908062 (11) [back to overview]	Number of Participants Successfully Retained on Pharmacotherapy Treatment at 16 Weeks
NCT01908062 (11) [back to overview]	HIV Viral Suppression at 16 Weeks
NCT01908062 (11) [back to overview]	Number of Participants With Successful Initiation of Treatment Within 4 Weeks of Randomization
NCT01908062 (11) [back to overview]	Participant Safety: Precipitated Withdrawal
NCT01908062 (11) [back to overview]	HIV Care Engagement
NCT01908062 (11) [back to overview]	Mean Days of Alcohol Use in Past 30 Days
NCT01908062 (11) [back to overview]	Mean Days of Opioid Use in Past 30 Days
NCT01908062 (11) [back to overview]	Number of Participants With Urine Ethyl Glucuronide (EtG) Positive for Alcohol
NCT01908062 (11) [back to overview]	Participant Safety: Any Fatal or Non-fatal Overdose Between Baseline and Week 16
NCT01908062 (11) [back to overview]	Participant Safety: Change in Liver Enzymes Between Baseline and Week 16
NCT01982643 (1) [back to overview]	"Participants Categorized as Responders"
NCT01993108 (4) [back to overview]	Accuracy on the Multi-Source Interference Task
NCT01993108 (4) [back to overview]	Characterize the Effects of Methylphenidate and Naltrexone on Neural Circuits in Prefrontal Cortex Associated With Top-down Control.
NCT01993108 (4) [back to overview]	Reaction Time on the Multi-Source Interference Task
NCT01993108 (4) [back to overview]	Reaction Time Variability on the Multi-Source Interference Task
NCT01999114 (12) [back to overview]	The Maximum Time-matched Change From Baseline in QT Data Corrected for Heart Rate (QTc), Placebo-corrected, Based on an Individual Correction (QTcI) Method (ΔΔQTcI)
NCT01999114 (12) [back to overview]	QTcF and QTcB for Historical Purposes, PR Interval, QRS Interval, and Uncorrected QT Interval
NCT01999114 (12) [back to overview]	Heart Rate (HR)
NCT01999114 (12) [back to overview]	ECG Morphology
NCT01999114 (12) [back to overview]	ECG Morphology
NCT01999114 (12) [back to overview]	Heart Rate (HR)
NCT01999114 (12) [back to overview]	Heart Rate (HR)
NCT01999114 (12) [back to overview]	The Maximum Time-matched Change From Baseline in QT Data Corrected for Heart Rate (QTc), Placebo-corrected, Based on an Individual Correction (QTcI) Method (ΔΔQTcI)
NCT01999114 (12) [back to overview]	QTcF and QTcB for Historical Purposes, PR Interval, QRS Interval, and Uncorrected QT Interval
NCT01999114 (12) [back to overview]	QTcF and QTcB for Historical Purposes, PR Interval, QRS Interval, and Uncorrected QT Interval
NCT01999114 (12) [back to overview]	The Maximum Time-matched Change From Baseline in QT Data Corrected for Heart Rate (QTc), Placebo-corrected, Based on an Individual Correction (QTcI) Method (ΔΔQTcI)
NCT01999114 (12) [back to overview]	ECG Morphology
NCT01999946 (1) [back to overview]	Time-to-Relapse: XRNTX vs. ETAU Following Release From Jail
NCT02026011 (5) [back to overview]	Alcohol Self-administration - Number of Drinks
NCT02026011 (5) [back to overview]	Neural Response to Alcohol Cues
NCT02026011 (5) [back to overview]	Subjective Response - Craving for Alcohol
NCT02026011 (5) [back to overview]	Subjective Response - Sedation
NCT02026011 (5) [back to overview]	Subjective Response - Stimulation
NCT02032433 (58) [back to overview]	Score on Color Word Card of Stoop Test
NCT02032433 (58) [back to overview]	Score on Subjective Opiate Withdrawal Scale (SOWS)
NCT02032433 (58) [back to overview]	Score on Subjective Opiate Withdrawal Scale (SOWS)
NCT02032433 (58) [back to overview]	Score on Trail Making Test Part A
NCT02032433 (58) [back to overview]	Score on Trail Making Test Part A
NCT02032433 (58) [back to overview]	Score on Trail Making Test Part B
NCT02032433 (58) [back to overview]	Score on Trail Making Test Part B
NCT02032433 (58) [back to overview]	Score on Word Card of Stoop Test
NCT02032433 (58) [back to overview]	Score on Word Card of Stoop Test
NCT02032433 (58) [back to overview]	Opioid Abstinence Over Time While on Study Medication (Objective)
NCT02032433 (58) [back to overview]	Time to Relapse (Intent to Treat Population)
NCT02032433 (58) [back to overview]	Time to Relapse (Per Protocol Population)
NCT02032433 (58) [back to overview]	Score of Medical Status Subscale Within Addiction Severity Index (ASI) Scale
NCT02032433 (58) [back to overview]	Opioid Craving Over Time W0
NCT02032433 (58) [back to overview]	Cigarette Smoking, W0 0
NCT02032433 (58) [back to overview]	Cigarette Smoking
NCT02032433 (58) [back to overview]	Alcohol Use Over Time, Drinks Per Day, Past 30 Days, W0
NCT02032433 (58) [back to overview]	Alcohol Use Over Time, Drinks Per Day
NCT02032433 (58) [back to overview]	Adverse Events Related to Study Medications
NCT02032433 (58) [back to overview]	Other Drug Use Over Time, Cocaine, W0
NCT02032433 (58) [back to overview]	Number Successfully Inducted Onto Assigned Study Medication
NCT02032433 (58) [back to overview]	Cigarette Smoking, W24 31 or More
NCT02032433 (58) [back to overview]	Cigarette Smoking, W24 21-30
NCT02032433 (58) [back to overview]	Cigarette Smoking, W24 11-20
NCT02032433 (58) [back to overview]	Cigarette Smoking, W24 0
NCT02032433 (58) [back to overview]	Cigarette Smoking, W0, 10 or Less
NCT02032433 (58) [back to overview]	Cigarette Smoking, W0 31 or More
NCT02032433 (58) [back to overview]	Cigarette Smoking, W0 21-30
NCT02032433 (58) [back to overview]	Cigarette Smoking, W0 11-20
NCT02032433 (58) [back to overview]	Other Drug Use Over Time, Cannabis, W0
NCT02032433 (58) [back to overview]	Other Drug Use Over Time, Cannabis, W24
NCT02032433 (58) [back to overview]	Opioid Abstinence Over Time While on Study Medication (Subjective)
NCT02032433 (58) [back to overview]	Other Drug Use Over Time, Cocaine, W24
NCT02032433 (58) [back to overview]	Other Drug Use Over Time, Stimulant, W0
NCT02032433 (58) [back to overview]	Other Drug Use Over Time, Stimulant, W24
NCT02032433 (58) [back to overview]	Score of Alcohol Subscale Within Addiction Severity Index (ASI) Scale
NCT02032433 (58) [back to overview]	Score of Alcohol Subscale Within Addiction Severity Index (ASI) Scale
NCT02032433 (58) [back to overview]	Score of Condom Use Subscale Within HIV Risk-Taking Behavior Scale (HRBS)
NCT02032433 (58) [back to overview]	Score of Condom Use Subscale Within HIV Risk-Taking Behavior Scale (HRBS)
NCT02032433 (58) [back to overview]	Score of Drug Use Subscale Within Addiction Severity Index (ASI) Scale
NCT02032433 (58) [back to overview]	Score of Drug Use Subscale Within Addiction Severity Index (ASI) Scale
NCT02032433 (58) [back to overview]	Score of Family / Social Relationship Subscale Within Addiction Severity Index (ASI) Scale
NCT02032433 (58) [back to overview]	Score of Legal Status Subscale Within Addiction Severity Index (ASI) Scale
NCT02032433 (58) [back to overview]	Score of Legal Status Subscale Within Addiction Severity Index (ASI) Scale
NCT02032433 (58) [back to overview]	Score of Medical Status Subscale Within Addiction Severity Index (ASI) Scale
NCT02032433 (58) [back to overview]	Score of Psychiatric Status Subscale Within Addiction Severity Index (ASI) Scale
NCT02032433 (58) [back to overview]	Score of Psychiatric Status Subscale Within Addiction Severity Index (ASI) Scale
NCT02032433 (58) [back to overview]	Score of Sexual Behavior Subscale Within HIV Risk-Taking Behavior Scale (HRBS)
NCT02032433 (58) [back to overview]	Score of Sexual Behavior Subscale Within HIV Risk-Taking Behavior Scale (HRBS)
NCT02032433 (58) [back to overview]	Score of Social Relationship Subscale Within Addiction Severity Index (ASI) Scale
NCT02032433 (58) [back to overview]	Score of Subacute Withdrawal Symptoms Subscale Within Hamilton Depression (HAM-D) Rating Scale
NCT02032433 (58) [back to overview]	Score of Subacute Withdrawal Symptoms Subscale Within Hamilton Depression (HAM-D) Rating Scale
NCT02032433 (58) [back to overview]	Score on Color Card of Stoop Test
NCT02032433 (58) [back to overview]	Score on Color Card of Stoop Test
NCT02032433 (58) [back to overview]	Score on Color Word Card of Stoop Test
NCT02032433 (58) [back to overview]	Score on EuroQOL EQ-5D Questionnaire
NCT02032433 (58) [back to overview]	Score on EuroQOL EQ-5D Questionnaire
NCT02032433 (58) [back to overview]	Score on Opioid Craving Scale (OCS)
NCT02088177 (2) [back to overview]	Number of Participants Receiving the Second Injection of Study Medication
NCT02088177 (2) [back to overview]	Change in Marijuana Use
NCT02107014 (65) [back to overview]	Change in PDGF-BB From Baseline.
NCT02107014 (65) [back to overview]	Change in MIP-1α From Baseline.
NCT02107014 (65) [back to overview]	Change in EGF From Baseline.
NCT02107014 (65) [back to overview]	Change in ENA-78 From Baseline.
NCT02107014 (65) [back to overview]	Change in CD40L From Baseline.
NCT02107014 (65) [back to overview]	Change in BDNF From Baseline.
NCT02107014 (65) [back to overview]	Change in Eotaxin From Baseline.
NCT02107014 (65) [back to overview]	Change in FaSL From Baseline.
NCT02107014 (65) [back to overview]	Change in LIF From Baseline.
NCT02107014 (65) [back to overview]	Change in FGF-β From Baseline.
NCT02107014 (65) [back to overview]	Change in G-CSF From Baseline.
NCT02107014 (65) [back to overview]	Change in VEGF From Baseline.
NCT02107014 (65) [back to overview]	Change in VEGF-D From Baseline.
NCT02107014 (65) [back to overview]	Change in RANTES From Baseline.
NCT02107014 (65) [back to overview]	Change in PIGF-1 From Baseline.
NCT02107014 (65) [back to overview]	Change in Pain From Baseline.
NCT02107014 (65) [back to overview]	Change in PAI-1 From Baseline.
NCT02107014 (65) [back to overview]	Change in Overall Fibromyalgia Symptoms From Baseline.
NCT02107014 (65) [back to overview]	Change in NGF From Baseline.
NCT02107014 (65) [back to overview]	Change in MIP-1β From Baseline.
NCT02107014 (65) [back to overview]	Change in VCAM-1 From Baseline.
NCT02107014 (65) [back to overview]	Change in MIG From Baseline.
NCT02107014 (65) [back to overview]	Change in MCP-3 From Baseline.
NCT02107014 (65) [back to overview]	Change in MCP-1 From Baseline.
NCT02107014 (65) [back to overview]	Change in TRAIL From Baseline.
NCT02107014 (65) [back to overview]	Change in TNF-β From Baseline.
NCT02107014 (65) [back to overview]	Change in TNF-α From Baseline.
NCT02107014 (65) [back to overview]	Change in TGF-β From Baseline.
NCT02107014 (65) [back to overview]	Change in TGF-α From Baseline.
NCT02107014 (65) [back to overview]	Change in SDF-1α From Baseline.
NCT02107014 (65) [back to overview]	Change in SCF From Baseline.
NCT02107014 (65) [back to overview]	Change in Resistin From Baseline.
NCT02107014 (65) [back to overview]	Change in M-CSF From Baseline.
NCT02107014 (65) [back to overview]	Change in IL-27 From Baseline.
NCT02107014 (65) [back to overview]	Change in Leptin From Baseline.
NCT02107014 (65) [back to overview]	Change in IP-10 From Baseline.
NCT02107014 (65) [back to overview]	Change in IL-9 From Baseline.
NCT02107014 (65) [back to overview]	Change in IL-8 From Baseline.
NCT02107014 (65) [back to overview]	Change in IL-18 From Baseline.
NCT02107014 (65) [back to overview]	Change in IL-17F From Baseline.
NCT02107014 (65) [back to overview]	Change in IL-17A From Baseline.
NCT02107014 (65) [back to overview]	Change in IL-15 From Baseline.
NCT02107014 (65) [back to overview]	Change in IL-13 From Baseline.
NCT02107014 (65) [back to overview]	Change in IL-12p70 From Baseline.
NCT02107014 (65) [back to overview]	Change in IL-12p40 From Baseline.
NCT02107014 (65) [back to overview]	Change in IL-10 From Baseline.
NCT02107014 (65) [back to overview]	Change in IFN-γ From Baseline.
NCT02107014 (65) [back to overview]	Change in IFN-β From Baseline.
NCT02107014 (65) [back to overview]	Change in IFN-α From Baseline.
NCT02107014 (65) [back to overview]	Change in ICAM-1 From Baseline.
NCT02107014 (65) [back to overview]	Change in IL-7 From Baseline.
NCT02107014 (65) [back to overview]	Change in IL-6 From Baseline.
NCT02107014 (65) [back to overview]	Change in IL-5 From Baseline.
NCT02107014 (65) [back to overview]	Change in HGF From Baseline.
NCT02107014 (65) [back to overview]	Change in GROa From Baseline.
NCT02107014 (65) [back to overview]	Change in GM-CSF From Baseline.
NCT02107014 (65) [back to overview]	Change in IL-4 From Baseline.
NCT02107014 (65) [back to overview]	Change in IL-31 From Baseline.
NCT02107014 (65) [back to overview]	Change in IL-23 From Baseline.
NCT02107014 (65) [back to overview]	Change in IL-22 From Baseline.
NCT02107014 (65) [back to overview]	Change in IL-21 From Baseline.
NCT02107014 (65) [back to overview]	Change in IL-2 From Baseline.
NCT02107014 (65) [back to overview]	Change in IL-1β From Baseline.
NCT02107014 (65) [back to overview]	Change in IL-1α From Baseline.
NCT02107014 (65) [back to overview]	Change in IL-1Ra From Baseline.
NCT02110264 (2) [back to overview]	Opioid Use
NCT02110264 (2) [back to overview]	Opioid Use Disorder
NCT02158533 (2) [back to overview]	Change From Baseline to Week 5 in the Montgomery Asberg Depression Rating Scale (MADRS) Total Score
NCT02158533 (2) [back to overview]	Number of Subjects With Adverse Events (AEs)
NCT02317744 (4) [back to overview]	Body Mass Index (BMI)
NCT02317744 (4) [back to overview]	Body Mass Index (BMI)
NCT02317744 (4) [back to overview]	Binge Eating Frequency (Continuous)
NCT02317744 (4) [back to overview]	Binge Eating Frequency (Continuous)
NCT02322047 (4) [back to overview]	Change in Mean Drinks Per Day of Drinking (Visit 8 - Visit 2)
NCT02322047 (4) [back to overview]	Change in Alcohol Craving (Visit 8 PACS - Visit 2 PACS)
NCT02322047 (4) [back to overview]	Change in Percent Heavy Drinking Days (PHDD) (Visit 8 PHDD - Visit 2 PHDD)
NCT02322047 (4) [back to overview]	Change in Percent Drinking Days (PDD) (Visit 8 PDD - Visit 2 PDD)
NCT02437344 (2) [back to overview]	Withdrawal: Subjective Opioid Withdrawal Scale (SOWS) Scores at Baseline and Administered Subsequently
NCT02437344 (2) [back to overview]	Successful Naltrexone Initiation
NCT02445339 (15) [back to overview]	Gamma-glutamyl Transferase (GGT) Levels
NCT02445339 (15) [back to overview]	EuroQoL-5 Dimensions (EQ-5D) Score
NCT02445339 (15) [back to overview]	EuroQoL-5 Dimensions (EQ-5D) Score
NCT02445339 (15) [back to overview]	Gamma-glutamyl Transferase (GGT) Levels
NCT02445339 (15) [back to overview]	Gamma-glutamyl Transferase (GGT) Levels
NCT02445339 (15) [back to overview]	Number of Heavy Drinking Days
NCT02445339 (15) [back to overview]	Short Inventory of Problems Related to Alcohol (SIP-2R) Score
NCT02445339 (15) [back to overview]	Number of Heavy Drinking Days
NCT02445339 (15) [back to overview]	Carbohydrate-deficient Transferrin (CDT) Levels
NCT02445339 (15) [back to overview]	Number of Heavy Drinking Days
NCT02445339 (15) [back to overview]	Carbohydrate-deficient Transferrin (CDT) Levels
NCT02445339 (15) [back to overview]	Carbohydrate-deficient Transferrin (CDT) Levels
NCT02445339 (15) [back to overview]	EuroQoL-5 Dimensions (EQ-5D) Score
NCT02445339 (15) [back to overview]	Short Inventory of Problems Related to Alcohol (SIP-2R) Score
NCT02445339 (15) [back to overview]	Short Inventory of Problems Related to Alcohol (SIP-2R) Score
NCT02478489 (1) [back to overview]	Change in Percent Heavy Drinking Days (%HDDs) Over the Past 30 Days From Baseline to 3 Month Follow-up, Assessed Using the Timeline Follow-Back
NCT02543944 (4) [back to overview]	Vivitrol Injection Receivers
NCT02543944 (4) [back to overview]	NTX Transition Initiation
NCT02543944 (4) [back to overview]	Detoxification Phase: Changes in Percent of Illicit Opioid-positive Urine Samples Over Time
NCT02543944 (4) [back to overview]	Detox Phase Completers
NCT02617628 (2) [back to overview]	Reincarceration
NCT02617628 (2) [back to overview]	Relapse to Opioid Use in Subjects by Month 3
NCT02680847 (6) [back to overview]	Number of Participants With All-causality and Treatment-related Serious Adverse Events (SAEs)
NCT02680847 (6) [back to overview]	Number of All-causality and Treatment-related AEs, by Intensity
NCT02680847 (6) [back to overview]	Number of Participants With All-causality and Treatment-related Adverse Events (AEs)
NCT02680847 (6) [back to overview]	Number of Participants With Maximum Changes in Vital Signs (Blood Pressure, Heart Rate, Respiratory Rate) Meeting Categorical Summarization Criteria
NCT02680847 (6) [back to overview]	Number of Participants With Laboratory (Lab) Abnormalities (Hematology and Chemistry)
NCT02680847 (6) [back to overview]	Number of Participants With Clinical Opiate Withdrawal Scale (COWS)
NCT02696434 (7) [back to overview]	Mean Peak COWS Scores During the Treatment Period (Days 1/1a-7)
NCT02696434 (7) [back to overview]	Proportion of Days With COWS Peak Score
NCT02696434 (7) [back to overview]	Proportion of Post-VIVITROL Days (Days 9-11) in Which Subjects in Each Group Demonstrate Mild Opioid Withdrawal
NCT02696434 (7) [back to overview]	Proportion of Subjects Who Receive and Tolerate a VIVITROL Injection on Day 8
NCT02696434 (7) [back to overview]	"Mean Score for Desire for Opioids Visual Analog Scale (VAS) During the Treatment Period and VIVITROL Induction and Post-VIVITROL Observation Period"
NCT02696434 (7) [back to overview]	Area Under the Curve (AUC) for COWS Scores During the Treatment Period and VIVITROL Induction and Post-VIVITROL Observation Period
NCT02696434 (7) [back to overview]	Incidence of Adverse Events (AEs)
NCT02698215 (2) [back to overview]	Number of Participants With Expired Carbon Monoxide Level <=5ppm
NCT02698215 (2) [back to overview]	Drinks Per Drinking Day
NCT02736474 (15) [back to overview]	Change in Fasting Insulin Levels
NCT02736474 (15) [back to overview]	Change in Leptin
NCT02736474 (15) [back to overview]	Waist Circumference
NCT02736474 (15) [back to overview]	Numbers of Participants Who Quit Smoking
NCT02736474 (15) [back to overview]	Depression Status Assessed by Self-rating Depression Scale（SDS）
NCT02736474 (15) [back to overview]	Clinical Symptoms Assessed by the Positive and Negative Syndrome Scale (PANSS)
NCT02736474 (15) [back to overview]	Changes From Baseline Craving for Nicotine Assessed by Visual Analog Scales (VAS) at 24 Weeks
NCT02736474 (15) [back to overview]	Change in Glycosylated Hemoglobin
NCT02736474 (15) [back to overview]	Change in Ghrelin
NCT02736474 (15) [back to overview]	Change in Fasting Triglycerides Levels
NCT02736474 (15) [back to overview]	Change in Fasting LDL Cholesterol
NCT02736474 (15) [back to overview]	Change in Fasting HDL Cholesterol Levels
NCT02736474 (15) [back to overview]	Change in Fasting Blood Glucose Levels
NCT02736474 (15) [back to overview]	Change From Baseline in Weight at 24 Weeks
NCT02736474 (15) [back to overview]	Anxiety Status Assessed by Self-Rating Anxiety Scale（SAS）
NCT02818036 (2) [back to overview]	Self-reported Feelings of Connection in Response to the Scanner Tasks
NCT02818036 (2) [back to overview]	Bold Oxygen-level Dependent (BOLD) Activations in Prespecified ROIs
NCT02842073 (5) [back to overview]	Number of Binge Drinking Days During Treatment
NCT02842073 (5) [back to overview]	Number of Participants Discontinuing Subsequent to Defined Intolerance
NCT02842073 (5) [back to overview]	Number of Participants With Treatment-Associated Adverse Events
NCT02842073 (5) [back to overview]	Final Penn Alcohol Craving Scale (PACS) Score
NCT02842073 (5) [back to overview]	Mean Number of Drinks/Binge Drinking Day During Treatment
NCT02885311 (1) [back to overview]	Weekly Change in Drinking
NCT02978417 (13) [back to overview]	Number of Participants Who Reported Improvement in Substance Use
NCT02978417 (13) [back to overview]	Number of Participants With New Arrests
NCT02978417 (13) [back to overview]	Number of Sanctions Imposed by the Court
NCT02978417 (13) [back to overview]	Treatment Participation (Non-Vivitrol)
NCT02978417 (13) [back to overview]	Treatment Satisfaction Score
NCT02978417 (13) [back to overview]	Vivitrol Participation
NCT02978417 (13) [back to overview]	Change in Medication-assisted Treatment (MAT) Attitudes
NCT02978417 (13) [back to overview]	Number of Positive Drug Screens
NCT02978417 (13) [back to overview]	Number of Participants With New Incarcerations
NCT02978417 (13) [back to overview]	Number of Missed Court Appointments
NCT02978417 (13) [back to overview]	Number of Participants Who Reported Illegal Behavior
NCT02978417 (13) [back to overview]	Number of Participants Who Reported Improvement in Subjective Functioning: Employment/Support Status
NCT02978417 (13) [back to overview]	Number of Participants Who Reported Improvement in Subjective Functioning: Family/Social Relationships
NCT03008590 (7) [back to overview]	Brief Pain Inventory - Pain Severity
NCT03008590 (7) [back to overview]	Clinical Global Impression of Improvement (CGI-I)
NCT03008590 (7) [back to overview]	Clinical Global Impression of Severity (CGI-S)
NCT03008590 (7) [back to overview]	painDETECT
NCT03008590 (7) [back to overview]	Beck Depression Inventory-II
NCT03008590 (7) [back to overview]	Brief Fatigue Inventory
NCT03008590 (7) [back to overview]	Brief Pain Inventory - Pain Interference
NCT03045341 (3) [back to overview]	Binge Eating Frequency (Continuous)
NCT03045341 (3) [back to overview]	Body Mass Index (Percent Weight Loss)
NCT03045341 (3) [back to overview]	Number of Participants Meeting Response Criteria
NCT03047005 (2) [back to overview]	Change in Body Mass Index
NCT03047005 (2) [back to overview]	Binge Eating Frequency (Continuous)
NCT03078075 (26) [back to overview]	Mean Change of Methamphetamine Craving at Stage 2
NCT03078075 (26) [back to overview]	Mean Change of Overall Functioning as Measured by Treatment Effectiveness Assessment (TEA) at Stage 1
NCT03078075 (26) [back to overview]	Mean Change of Overall Functioning as Measured by Treatment Effectiveness Assessment (TEA) at Stage 2
NCT03078075 (26) [back to overview]	Mean Number of Abstinent Days of Participants Who Used Other Substance Measured by UDS at Stage 2
NCT03078075 (26) [back to overview]	Mean Number of Abstinent Days of Participants Who Used Other Substance Measured by UDS at Stage 1
NCT03078075 (26) [back to overview]	Mean Change of Quality of Life (QOL) by PhenX Core Tier 1 Instrument at Stage 2
NCT03078075 (26) [back to overview]	Mean Change of Quality of Life (QOL) by PhenX Core Tier 1 Instrument at Stage 1
NCT03078075 (26) [back to overview]	Mean Change of Proportion of Other Substance Abstinent Days Measured by Self-report at Stage 2
NCT03078075 (26) [back to overview]	Mean Change Percentage of Methamphetamine Abstinent Days Measured by Self-report at Stage 2
NCT03078075 (26) [back to overview]	Mean Change of Percentage of Methamphetamine Abstinent Days Measured by Self-report at Stage 1
NCT03078075 (26) [back to overview]	Mean Change in Number of Other Substance Use by Self-report at Stage 1
NCT03078075 (26) [back to overview]	Mean Number of Study Weeks With Two Methamphetamine-negative UDS at Stage 2
NCT03078075 (26) [back to overview]	Treatment Effectiveness Score of Participants at Stage 1
NCT03078075 (26) [back to overview]	Mean Change in Number of Other Substance Use by Self-report at Stage 2
NCT03078075 (26) [back to overview]	Mean Change of Proportion of Other Substance Abstinent Days Measured by Self-report at Stage 1
NCT03078075 (26) [back to overview]	Mean Number of Study Weeks With Two Methamphetamine-negative UDS at Stage 1
NCT03078075 (26) [back to overview]	Number of Participants Who Completed the Visit in Week 12
NCT03078075 (26) [back to overview]	Percentage of Participants Who Used Methamphetamine in the Pre-evaluation Period
NCT03078075 (26) [back to overview]	Mean Change of Depression Symptom Score by PHQ-9 at Stage 2
NCT03078075 (26) [back to overview]	Treatment Effectiveness Score of Participants at Stage 2
NCT03078075 (26) [back to overview]	Mean Change of Methamphetamine Craving at Stage 1
NCT03078075 (26) [back to overview]	Mean Maximum Number of Consecutive Visits Negative UDS at Stage 2
NCT03078075 (26) [back to overview]	Change in Proportion of E-cigarettes Abstinent Days by Self-report at Stage 1
NCT03078075 (26) [back to overview]	Change in Proportion of E-cigarettes Abstinent Days by Self-report at Stage 2
NCT03078075 (26) [back to overview]	Mean Change of Depression Symptom Score by PHQ-9 at Stage 1
NCT03078075 (26) [back to overview]	Mean Maximum Number of Consecutive Visits Negative UDS at Stage 1
NCT03113409 (1) [back to overview]	Percentage of Patients Who Receive the Second Injection of XR-NTX.
NCT03132571 (3) [back to overview]	BMI
NCT03132571 (3) [back to overview]	Waist Circumference (Inches)
NCT03132571 (3) [back to overview]	Weight (kg)
NCT03188185 (1) [back to overview]	Change From Baseline to the End of Treatment (EOT) in the Montgomery Asberg Depression Rating Scale-10 (MADRS-10) Scores
NCT03275350 (13) [back to overview]	Number of Participants With HIV Viral Suppression, Complete Case
NCT03275350 (13) [back to overview]	Number of Participants Who Had Unprotected Sex in Past 30 Days
NCT03275350 (13) [back to overview]	CD4 Count
NCT03275350 (13) [back to overview]	Engagement in HIV Care: 100% Antiretroviral Therapy Adherence
NCT03275350 (13) [back to overview]	Engagement in HIV Care: Quality of Life
NCT03275350 (13) [back to overview]	Engagement in HIV Care: Antiretroviral Therapy Prescribed
NCT03275350 (13) [back to overview]	Number of Participants With at Least 1 HIV Care Visit in Past 12 Weeks
NCT03275350 (13) [back to overview]	Average Number of Self-Reported Days of Opioid Use in Last 30 Days
NCT03275350 (13) [back to overview]	Veterans Aging Cohort Study (VACS) Index
NCT03275350 (13) [back to overview]	Number of Participants With Multiple Sex Partners in Past 30 Days
NCT03275350 (13) [back to overview]	Number of Participants With HIV Viral Suppression, Per-protocol
NCT03275350 (13) [back to overview]	Number of Participants Who Test Positive for Opioids at 24 Weeks
NCT03275350 (13) [back to overview]	Number of Participants With HIV Viral Suppression, Missing Imputed as Unsuppressed
NCT03278886 (8) [back to overview]	Treatment Discontinuation Defined as Patient Self-report of Stopping Medication Anytime During the Treatment Period
NCT03278886 (8) [back to overview]	Reported Side Effects Using a Symptom Checklist, Plus an Open-ended Question
NCT03278886 (8) [back to overview]	Medication Satisfaction Defined as a Score From 0-100 Measured Via the Treatment Satisfaction Questionnaire for Medication (TSQM), With Higher Scores Corresponding to Higher Treatment Satisfaction.
NCT03278886 (8) [back to overview]	Severe Hepatotoxicity Defined as AST/ALT >10X the Level of Normal
NCT03278886 (8) [back to overview]	Number of Participants With Adherence Assessed Via Riboflavin in the Urine Confirming Adherence
NCT03278886 (8) [back to overview]	Medication Tolerability Measured Via a 0-100 Visual Analog Scale
NCT03278886 (8) [back to overview]	Change in Alcohol Use Defined as a Change in the Mean Number of Grams of Pure Ethanol Consumed Per Day From Baseline to 8 Weeks
NCT03278886 (8) [back to overview]	Adherence to Medication Defined as Self-report of Percentage of Study Medication Taken in the Past Two Weeks
NCT03290391 (5) [back to overview]	Undetectable HIV Viral Load at 6 Months
NCT03290391 (5) [back to overview]	Change in Mean CD4 Count From Baseline to 12 Months
NCT03290391 (5) [back to overview]	Initiation of Antiretroviral Therapy (ART)
NCT03290391 (5) [back to overview]	Retention in HIV Care
NCT03290391 (5) [back to overview]	Undetectable HIV Viral Load at 12 Months
NCT03374956 (3) [back to overview]	Change in Total Body Weight
NCT03374956 (3) [back to overview]	Percentage of Responders
NCT03374956 (3) [back to overview]	Percentage of Responders
NCT03386448 (1) [back to overview]	Response to Medications as Assessed by Change in Score on Modified MDRS Scale From Baseline to End of Study Period
NCT03447782 (3) [back to overview]	Functional Disability
NCT03447782 (3) [back to overview]	Pain Intensity
NCT03447782 (3) [back to overview]	Self- Perceived Pain Sensitivity
NCT03539900 (2) [back to overview]	Change in Binge Eating Frequency
NCT03539900 (2) [back to overview]	Percent BMI Change
NCT03660475 (17) [back to overview]	Visual Acuity Measured by Assessing Average Change in LogMAR Units for Both Eyes at Day 29. LogMAR Units Range From 0-1.0, With the Higher the Number Indicating a Worsening in Vision.
NCT03660475 (17) [back to overview]	Total Ocular Surface Disease Index
NCT03660475 (17) [back to overview]	Tear Osmolarity
NCT03660475 (17) [back to overview]	Visual Analog Scale for Pain
NCT03660475 (17) [back to overview]	Lissamine Green Staining
NCT03660475 (17) [back to overview]	Number of Participants With Treatment-related Adverse Events
NCT03660475 (17) [back to overview]	Tear Film Break-up Time
NCT03660475 (17) [back to overview]	Cochet-Bonnet Corneal Sensitivity Test
NCT03660475 (17) [back to overview]	Conjunctival Redness
NCT03660475 (17) [back to overview]	Dilated Fundoscopy
NCT03660475 (17) [back to overview]	Fluorescein Staining
NCT03660475 (17) [back to overview]	Intraocular Pressure
NCT03660475 (17) [back to overview]	Matrix Metalloprotienase-9 (MMP-9) is a Marker of Inflammation.
NCT03660475 (17) [back to overview]	Ocular Discomfort (Scale 1)
NCT03660475 (17) [back to overview]	Ocular Discomfort (Scale 2)
NCT03660475 (17) [back to overview]	Schirmer's Test
NCT03660475 (17) [back to overview]	Slit-lamp Biomicroscopy
NCT03810495 (9) [back to overview]	AUC of 6β-naltrexol
NCT03810495 (9) [back to overview]	Incidence of Adverse Events (AEs)
NCT03810495 (9) [back to overview]	Tmax of Naltrexone
NCT03810495 (9) [back to overview]	Time>Minimum Effective Concentration
NCT03810495 (9) [back to overview]	Percentage of Participants That Maintain MEC
NCT03810495 (9) [back to overview]	Median Tmax of 6β-naltrexol
NCT03810495 (9) [back to overview]	Median Cmax of Naltrexone
NCT03810495 (9) [back to overview]	Median Cmax of 6β-naltrexol
NCT03810495 (9) [back to overview]	AUC of Naltrexone
NCT03852628 (3) [back to overview]	Number of Participants With a Reduction in CAPS-5 Total Symptom Severity Score (TSSS) of 10 or More Points
NCT03852628 (3) [back to overview]	Composite Outcome Measure for a Reduction in Both Alcohol Use Disorder (AUD) and Post-Traumatic Stress Disorder (PTSD) Symptoms
NCT03852628 (3) [back to overview]	Number of Participants With a Reduction in Alcohol Use Disorder (AUD), With TLFB Tool
NCT03970330 (7) [back to overview]	PGIC Score (Nonmenstrual Pelvic Pain)
NCT03970330 (7) [back to overview]	PGIC Score (Dyspareunia)
NCT03970330 (7) [back to overview]	Pain Score Area Under the Curve (AUC)
NCT03970330 (7) [back to overview]	Ibuprofen Use
NCT03970330 (7) [back to overview]	EHP-30 Score
NCT03970330 (7) [back to overview]	PGIC Score (Painful Periods)
NCT03970330 (7) [back to overview]	Oxycodone Use
NCT04052139 (10) [back to overview]	Change in Biomarker IL-10
NCT04052139 (10) [back to overview]	Change in IL-1beta
NCT04052139 (10) [back to overview]	Number of Participants With a Change in HIV Viral Load Suppression Status
NCT04052139 (10) [back to overview]	Change in TNF-alpha
NCT04052139 (10) [back to overview]	Change in Percentage of Past Month Heavy Drinking Days
NCT04052139 (10) [back to overview]	Change in Past Week Pain Severity
NCT04052139 (10) [back to overview]	Change in Past Week Pain Interference
NCT04052139 (10) [back to overview]	Change in Cold Pain Tolerance
NCT04052139 (10) [back to overview]	Change in CD4 Count
NCT04052139 (10) [back to overview]	Change in Biomarker IL-6
NCT04094584 (7) [back to overview]	Change in Daily Total Alcohol Consumption From Baseline at 3 Months
NCT04094584 (7) [back to overview]	Change in Alcohol Related Life Consequences (Short Inventory of Problems Scale, Version 2R: SIP-2R)
NCT04094584 (7) [back to overview]	Change in Quality of Life Score at 3 Months
NCT04094584 (7) [back to overview]	Receipt of All Study Naltrexone Injections
NCT04094584 (7) [back to overview]	Participants Retained in Study at 3 Months
NCT04094584 (7) [back to overview]	Continued Naltrexone Use After Intervention Period
NCT04094584 (7) [back to overview]	Change in WHO Drinking Risk Level
NCT04249882 (3) [back to overview]	Cue-induced Craving
NCT04249882 (3) [back to overview]	# of Drinks Per Drinking Day
NCT04249882 (3) [back to overview]	Percentage of Days Abstinent
NCT04322526 (2) [back to overview]	BOLD Responses in the rACC Cortex During the Processing of Contextual Cues at Baseline (Post-placebo)
NCT04322526 (2) [back to overview]	Naltrexone-induced Changes in BOLD Responses in the rACC Cortex During the Processing of Contextual Cues (Placebo vs. Naltrexone)
NCT04365985 (11) [back to overview]	Intensive Care Unit (ICU) Duration
NCT04365985 (11) [back to overview]	Intubation
NCT04365985 (11) [back to overview]	Intubation Duration
NCT04365985 (11) [back to overview]	Length of Hospital Stay
NCT04365985 (11) [back to overview]	Liver Failure
NCT04365985 (11) [back to overview]	Progression of Oxygenation Needs
NCT04365985 (11) [back to overview]	COVID Mortality
NCT04365985 (11) [back to overview]	Renal Failure
NCT04365985 (11) [back to overview]	Cytokine Storm
NCT04365985 (11) [back to overview]	Intensive Care Unit (ICU) Admission
NCT04365985 (11) [back to overview]	Time Until Recovery
NCT04409041 (4) [back to overview]	Patient Reported Burning/Pain
NCT04409041 (4) [back to overview]	Change in Patient-Reported Itch
NCT04409041 (4) [back to overview]	Change in Investigator Rated Erythema
NCT04409041 (4) [back to overview]	Change in Investigator Rated Scale
NCT04716881 (23) [back to overview]	Median Ctrough of Naltrexone (After 1st Dose)
NCT04716881 (23) [back to overview]	Median Ctrough of Naltrexone (After 6th Dose)
NCT04716881 (23) [back to overview]	Median Tmax of 6β-naltrexol (After 1st Dose)
NCT04716881 (23) [back to overview]	Median Tmax of Naltrexone (After 1st Dose)
NCT04716881 (23) [back to overview]	Median Tmax of 6β-naltrexol (After th Dose)
NCT04716881 (23) [back to overview]	Median Cmax of 6β-naltrexol (After First Dose)
NCT04716881 (23) [back to overview]	Median Cmax of Naltrexone (After 1st Dose)
NCT04716881 (23) [back to overview]	Median Cmax of 6β-naltrexol (After 6th Dose)
NCT04716881 (23) [back to overview]	Median AUC0-inf of Naltrexone (After 6th Dose)
NCT04716881 (23) [back to overview]	Median AUC0-inf of Naltrexone (After 1st Dose)
NCT04716881 (23) [back to overview]	Median AUC0-inf of 6β-naltrexol (After 6th Dose)
NCT04716881 (23) [back to overview]	Median AUC0-inf of 6β-naltrexol (After 1st Dose)
NCT04716881 (23) [back to overview]	Adverse Events (AEs)
NCT04716881 (23) [back to overview]	6β-naltrexol Accumulation Ratio (AR) for Ctrough
NCT04716881 (23) [back to overview]	6β-naltrexol Accumulation Ratio (AR) for AUC0-inf
NCT04716881 (23) [back to overview]	6β-naltrexol Accumulation Ratio (AR) for Cmax
NCT04716881 (23) [back to overview]	Median Ctrough of 6β-naltrexol (After 6th Dose)
NCT04716881 (23) [back to overview]	Naltrexone Accumulation Ratio (AR) for Ctrough
NCT04716881 (23) [back to overview]	Naltrexone Accumulation Ratio (AR) for Cmax
NCT04716881 (23) [back to overview]	Naltrexone Accumulation Ratio (AR) for AUC0-inf
NCT04716881 (23) [back to overview]	Median Tmax of Naltrexone (After 6th Dose)
NCT04716881 (23) [back to overview]	Median Cmax of Naltrexone (After 6th Dose)
NCT04716881 (23) [back to overview]	Median Ctrough of 6β-naltrexol (After 1st Dose)
NCT04756128 (9) [back to overview]	Total Duration of Hospitalization (From First Dose of Study Drug to Discharge)
NCT04756128 (9) [back to overview]	In Patients Hospitalized With Moderate COVID-19, Subjects Who Required Remdesivir
NCT04756128 (9) [back to overview]	In Patients Hospitalized With Moderate COVID-19, Subjects Who Required Corticosteroids
NCT04756128 (9) [back to overview]	In Patients Hospitalized With Moderate COVID-19, Patients Who Required ICU or ICU Stepdown Cares
NCT04756128 (9) [back to overview]	In Patients Hospitalized With Moderate COVID-19, The Need for High Flow Nasal Cannula (HFNC) or Non-Invasive Positive Pressure Ventilation (NIPPV)
NCT04756128 (9) [back to overview]	The Number of Doses of Remdesivir Required In Patients Hospitalized With Moderate COVID-19
NCT04756128 (9) [back to overview]	Total Duration of Hospitalization
NCT04756128 (9) [back to overview]	In Patients Hospitalized With Moderate COVID-19, the Impact of Colchicine and LDN, Alone or in Combination, on Achieving Disease Recovery by Day 5.
NCT04756128 (9) [back to overview]	The Dosage Amount (in Milligrams) of Corticosteroids Required In Patients Hospitalized With Moderate COVID-19
NCT04854551 (3) [back to overview]	Brain Activation to Emotion Regulation
NCT04854551 (3) [back to overview]	Change in Brain Activation to Reward Between Placebo and Active Medication
NCT04854551 (3) [back to overview]	Alcohol Value
NCT04935931 (3) [back to overview]	Exposure
NCT04935931 (3) [back to overview]	Change in % Blood Oxygenation Level Dependent Change (%BOLD) in the Nucleus Accumbens
NCT04935931 (3) [back to overview]	Change in % Blood Oxygenation Level Dependent Change (%BOLD) in the Dorsal Anterior Cingulate Cortex

Drinking Timeline Follow-back Interview (TFBI)

The TFBI is an interview that utilizes a calendar method to assess when and how much alcohol was consumed by the participant. At Week 0 (Pretreatment), Week 24 (Posttreatment), and Week 52 (Follow-up), alcohol consumed in the past 90 days was assessed. This measure was then used to calculate the percentage of days drinking in the past 90 days at each time point. Higher scores for percentage of days drinking indicate worse drinking outcomes. (NCT00006489)
Timeframe: Week 0 (Pretreatment), Week 24 (Posttreatment), Week 52 (Follow-up)

,,,

Intervention	percentage of days (Mean)
	Pretreatment (Week 0)	Posttreatmwent (Week 24)	Follow-up (Week 52)
Naltrexone + CBT (Prolonged Exposure Therapy)	71.2	7.3	8.8
Naltrexone + Supportive Counseling	75.4	3.5	21.5
Placebo + CBT (Prolonged Exposure Therapy)	78.6	13.4	18.9
Placebo + Supportive Counseling	74.1	13.2	27.3

Intervention	percentage days of heavy drinking (Median)
Phase 2 Naltrexone for Responders	0
Phase 2 Nalt and Tele for Responders	0
Phase 2 Nalt, MM and CBI for NR	27.7
Phase 2 Placebo, MM and CBI for NR	17.8

Intervention	mean percentage of days (Mean)
Modafinil Plus Naltrexone	34.7
Naltrexone	35.1
Modafinil	33.6
Placebo	33.8

Intervention	number of cocaine negative urine samples (Mean)
ModNal	9.3
Naltrexone and Placebo	7.2
Modafinil and Placebo	10.1
Double Placebo	10.5

Intervention	Participants (Number)
Medisorb Naltrexone 380 mg (VIVITROL)	62
Oral Naltrexone to Medisorb Naltrexone 380 mg (VIVITROL)	11

Intervention	days (Mean)
Naltrexone Plus Gabapentin and CBI	69.9
Naltrexone Plus Placebo and CBI	59.6
Placebo Plus Placebo Plus CBI	57.3

Intervention	Mean % of cocaine-positive urines (Mean)
Modafinil Plus MI, CM, and CBT	31
Levodopa/Carbidopa Plus MI, CM, and CBT	28
Naltrexone HCl Plus MI, CM, and CBT	47
Placebo Plus MI, CM, and CBT	35

Intervention	Participants (Count of Participants)
ON + DNIP, Oral Naltrexone + Depot Placebo Naltrexone Implant	6
DNI + ONP , Naltrexone Implant + Oral Naltrexone Placebo	12
ONP + DNIP, Oral Placebo Naltrexone and Depot Placebo Implant	18

Intervention	composite score (Mean)
ON + DNIP, Oral Naltrexone + Depot Placebo Naltrexone Implant	0.19
DNI + ONP , Naltrexone Implant + Oral Naltrexone Placebo	0.15
ONP + DNIP, Oral Placebo Naltrexone and Depot Placebo Implant	0.18

Intervention	score on a scale (Mean)
ON + DNIP, Oral Naltrexone + Depot Placebo Naltrexone Implant	62.8
DNI + ONP , Naltrexone Implant + Oral Naltrexone Placebo	64.7
ONP + DNIP, Oral Placebo Naltrexone and Depot Placebo Implant	62.5

Intervention	urine tests (Number)
ON + DNIP, Oral Naltrexone + Depot Placebo Naltrexone Implant	.427
DNI + ONP , Naltrexone Implant + Oral Naltrexone Placebo	.636
ONP + DNIP, Oral Placebo Naltrexone and Depot Placebo Implant	.341

Intervention	grams per day (Mean)
ON + DNIP, Oral Naltrexone + Depot Placebo Naltrexone Implant	10.2
DNI + ONP , Naltrexone Implant + Oral Naltrexone Placebo	9.0
ONP + DNIP, Oral Placebo Naltrexone and Depot Placebo Implant	9.6

Intervention	units on a scale (Mean)
ALC and NAL	2.1
Placebo ALC and NAL	1.1
Placebo Pill and ALC	1.8
Placebo Pill and Placebo ALC	1.2

Intervention	units on a scale (Mean)
ALC and NAL	17.9
Placebo ALC and NAL	4.5
Placebo Pill and ALC	14.7
Placebo Pill and Placebo ALC	2.7

Intervention	units on a scale (Mean)
ALC and NAL	11.3
Placebo ALC and NAL	3.9
Placebo Pill and ALC	8.7
Placebo Pill and Placebo ALC	3.2

Intervention	units on a scale (Mean)
ALC and NAL	14.8
Placebo ALC and NAL	13.4
Placebo Pill and ALC	15.9
Placebo Pill and Placebo ALC	15.4

Intervention	Participants (Number)
Naltrexone - MALE	31
Placebo - MALE	24
Naltrexone - FEMALE	30
Placebo - FEMALE	31

Intervention	Pounds (Mean)
Naltrexone - MALE	4.79
Placebo - MALE	5.58
Naltrexone - FEMALE	2.26
Placebo - FEMALE	5.08

Intervention	Participants (Number)
	"Nausea - Mild"	"Nausea - Severe"	"Vomiting - Mild"	"Vomiting - Severe"	"Headache- Mild"	"Headache - Severe"	"Light Headed/Dizzy - Mild"	"Light Headed/Dizzy - Severe"	"Flushed/Warm - Mild"	"Flushed/Warm - Severe"	"Tiredness - Mild"	"Tiredness - Severe"	"Anxiety/Agitation - Mild"	"Anxiety/Agitation - Severe"	"Increased Sexual Desire - Mild"	"Increased Sexual Desire - Severe"	"Insomnia - Mild"	"Insomnia - Severe"	"Constipation - Mild"	"Constipation - Severe"	"Diarrhea - Mild"	"Diarrhea - Severe"	"Joint or Muscle Pain - Mild"	"Joint or Muscle Pain - Severe"
Naltrexone - FEMALE	24	4	3	2	31	0	25	1	24	6	38	10	31	3	9	1	19	5	24	1	5	0	14	2
Naltrexone - MALE	16	4	3	1	28	4	22	5	12	1	42	5	33	3	10	2	13	2	18	1	6	2	21	0
Placebo - FEMALE	13	2	5	0	33	2	17	0	15	6	33	9	32	6	6	0	12	3	14	3	7	1	13	5
Placebo - MALE	5	3	0	0	17	2	16	1	9	1	34	7	35	3	22	6	16	3	20	1	6	0	21	2

Intervention	side effects (Mean)
	Gastrointestinal symptoms	Emotional Symptoms	Neurological Symptoms	Cold Symptoms	Skin Symptoms	Sexual Symptoms	Cardiac Symptoms
Desipramine and Naltrexone	3.052	3.727	4.201	1.891	.591	.737	.389
Desipramine and Placebo	3.653	5.248	4.566	2.253	1.057	.736	.356
Paroxetine and Naltrexone	3.651	4.874	6.212	2.182	1.002	.877	.416
Paroxetine and Placebo	2.688	3.963	5.078	2.393	.859	.932	.474

Intervention	units on a scale (Mean)
	Week 1	Week 13
Desipramine and Naltrexone	18.500	4.296
Desipramine and Placebo	21.458	7.489
Paroxetine and Naltrexone	21.273	10.013
Paroxetine and Placebo	20.700	9.690

naltrexone

Description

Cross-References

Synonyms (110)

Research Excerpts

Toxicity

Pharmacokinetics

Compound-Compound Interactions

Bioavailability

Dosage Studied

Roles (5)

Drug Classes (3)

Pathways (3)

Protein Targets (28)

Potency Measurements

Inhibition Measurements

Activation Measurements

Other Measurements

Biological Processes (146)

Molecular Functions (59)

Ceullar Components (45)

Bioassays (713)

Research

Studies (8,288)

Study Types

Clinical Trials (418)

Trial Overview

Trial Outcomes

Drinking Timeline Follow-back Interview (TFBI)

Penn Alcohol Cravings Scale

Posttraumatic Stress Disorder (PTSD) Symptom Scale - Interview (PSS-I-IV)

Yale-Brown Obsessive Compulsive Scale for Pathological Gambling (PG-YBOCS)

Cigarettes Smoked Per Day.

Point Prevalence Smoking Abstinence at 26 Weeks.

Point Prevalence Smoking Abstinence at 6 Weeks

Weight Gain at 26 Weeks.

Weight Gain at 6 Weeks.

Percentage of Heavy Drinking Days

Count of Responders and Non-responders in Phase 1

Retention in Treatment

Weight Gain

Weight Gain Abstinent Participants

Point Prevalence Abstinence

Smoking Cessation

Percent Days of Heavy Drinking (Measured by Timeline Follow Back Starting at Week Two Through Week 14

Cocaine Use (Measured by Timeline Follow Back and Urine Screen From Week 2-week 14)

Number of Participants Reporting at Least 1 Treatment-emergent Adverse Event (TEAE)

Number of Subjects Who Reported at Least 1 Treatment-emergent Adverse Event (TEAE) While on Study.

Time to Relapse to Drinking

Mean Percentage of Cocaine-positive Urines Over Course of 12 Week Treatment in Subgroup Achieving Abstinence at Baseline

Mean Percentage of Cocaine-positive Urines Over Course of 12 Week Treatment in Subgroup NOT Achieving Abstinence at Baseline

Cocaine Drug Use

Amphetamine Drug Use

Benzodiazepine Drug Use

Composite Score of Psychiatric Problems

Global Assessment Form (GAF)

HIV Risk (Baseline)

Marijuana Drug Use

Number of Subjects Who Dropped Out of Treatment

Positive Opioid Urine Test

Retention Without Relapse to Heroin Addiction (Measured at Month 6)

Use of Alcohol

Profile of Mood States - Vigor

Subjective High From Alcohol Scale

Profile of Mood States - Fatigue Scale

Biphasic Alcohol Effects Scale - Stimulation

Biphasic Alcohol Effects Scale - Sedation

Number of Nicotine Cigarette Choices Taken During the Cigarette Choice Procedure.

7-Day Point Prevalence Smoking Abstinence: 12 Weeks Post Quit-Date

7-Day Point Prevalence Smoking Abstinence: 4 Weeks Post Quit-Date

7-Day Point Prevalence Smoking Abstinence: 26 Weeks Post Quit-Date

7-Day Point Prevalence Smoking Abstinence: 52 Weeks Post Quit-Date

Prolonged Smoking Abstinence: 12 Weeks Post Quit-Date

Prolonged Smoking Abstinence: 4 Weeks Post Quit-Date

Weight Change at End of Treatment (Regardless of Quit Status)

Weight Change at End of Treatment (Smoking Abstinent Only)

Opioid Antagonist Reported Side Effects: 1-Week Post Quit Date

Opioid Antagonist Reported Side Effects: 4-Weeks Post Quit Date

Mean Number of Standard Drinks Per Drinking Day During the Last 4 Weeks of the Trial

% Subjects Abstinent

Intervention	units on a scale (Mean)
	Beginning of Treatment	End of Treatment
Desipramine and Naltrexone	11.195	8.563
Desipramine and Placebo	13.167	8.943
Paroxetine and Naltrexone	13.273	9.328
Paroxetine and Placebo	10.950	8.238

Intervention	Total number of drinks consumed (Mean)
Naltrexone (asn40asn)	3.0
Naltrexone (asp40)	3.8
Placebo (asn40asn )	3.8
Placebo (asp40)	3.1

Intervention	Heart rate (beats/minute) (Mean)
Placebo + Marijuana (0.0%THC)	68.5
Placebo + Marijuana (3.27% THC)	70.7
Naltrexone (12mg) + Marijuana (0.0%THC)	65.8
Naltrexone (12mg) + Marijuana (3.27%THC)	72.1
Naltrexone (25mg) + Marijuana (0.0%THC)	67.3
Naltrexone (25mg) + Marijuana (3.27%THC)	72.7
Naltrexone (50mg) + Marijuana (0.0%THC)	65.6
Naltrexone (50mg) + Marijuana (3.27%THC)	72.2
Naltrexone (100mg) + Marijuana (0.0%THC)	67.7
Naltrexone (100mg) + Marijuana (3.27%THC)	72.4

Intervention	units on a scale (Mean)
Placebo + Marijuana (0.0%THC)	86.2
Placebo + Marijuana (3.27% THC)	86.1
Naltrexone (12mg) + Marijuana (0.0%THC)	86.7
Naltrexone (12mg) + Marijuana (3.27%THC)	84.7
Naltrexone (25mg) + Marijuana (0.0%THC)	83.4
Naltrexone (25mg) + Marijuana (3.27%THC)	83.5
Naltrexone (50mg) + Marijuana (0.0%THC)	83.6
Naltrexone (50mg) + Marijuana (3.27%THC)	82.1
Naltrexone (100mg) + Marijuana (0.0%THC)	82.1
Naltrexone (100mg) + Marijuana (3.27%THC)	83.0

Intervention	units on a scale (Mean)
	"Mean VAS ratings Marijuana Strength"	"Mean VAS ratings High"	"Mean VAS ratings Good Effect"	"Mean VAS ratings Like Drug"
Naltrexone (100mg) + Marijuana (0.0%THC)	10.1	3.9	12.5	11.4
Naltrexone (100mg) + Marijuana (3.27%THC)	34.5	21.3	44.0	44.0
Naltrexone (12mg) + Marijuana (0.0%THC)	6.7	3.7	6.8	7.0
Naltrexone (12mg) + Marijuana (3.27%THC)	34.0	23.0	43.1	44.0
Naltrexone (25mg) + Marijuana (0.0%THC)	8.1	3.0	9.0	9.3
Naltrexone (25mg) + Marijuana (3.27%THC)	31.6	20.4	44.1	34.7
Naltrexone (50mg) + Marijuana (0.0%THC)	9.7	4.0	10.2	10.3
Naltrexone (50mg) + Marijuana (3.27%THC)	36.2	22.2	42.2	38.0
Placebo + Marijuana (0.0%THC)	8.0	4.1	10.0	11.3
Placebo + Marijuana (3.27% THC)	25.0	11.0	38.3	35.0

Intervention	percentage of participants (Number)
	0% Heavy Drinking Days	<= 10% Heavy Drinking Days	<= 20% Heavy Drinking Days	<= 30% Heavy Drinking Days	<= 40% Heavy Drinking Days	<= 50% Heavy Drinking Days	<= 60% Heavy Drinking Days	<= 70% Heavy Drinking Days	<= 80% Heavy Drinking Days	<= 90% Heavy Drinking Days	<= 100% Heavy Drinking Days
Placebo	47.3	59.5	72.3	79.1	83.1	85.1	87.2	89.9	94.6	98.6	100.0
Vivitrol	40.8	59.2	65.8	74.3	80.9	83.6	84.9	90.1	93.4	97.4	100.0

Intervention	percent of days (Mean)
	Percent Days Interlock Fail Pre/on Medication	Percent Days Interlock Fail Post Medication
Participants	-1.29	-0.30

Intervention	Participants (Count of Participants)
	4 Weeks	12 Weeks	24 Weeks
Depot Naltrexone	24	17	16
Oral Naltrexone	20	14	9

Intervention	drinks/week (Mean)
	Drinks/week Baseline	Drinks/week Week 1	Drinks/week Change
Campral (Acamprosate)	44.90	24.37	-20.53
ReVia (Naltrexone)	47.02	25.79	-21.23
Sugar Pill (Placebo)	48.87	21.51	-27.35

Intervention	units on a scale (Mean)
	ACQ-SF Total Screening	ACQ-SF Total Week 1	ACQ-SF Total Change
Campral (Acamprosate)	3.80	3.36	-0.44
ReVia (Naltrexone)	3.81	3.69	-0.12
Sugar Pill (Placebo)	3.99	3.51	-0.48