Naloxone: A specific opiate antagonist that has no agonist activity. It is a competitive antagonist at mu, delta, and kappa opioid receptors. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
naloxone : A synthetic morphinane alkaloid that is morphinone in which the enone double bond has been reduced to a single bond, the hydrogen at position 14 has been replaced by a hydroxy group, and the methyl group attached to the nitrogen has been replaced by an allyl group. A specific opioid antagonist, it is used (commonly as its hydrochloride salt) to reverse the effects of opioids, both following their use of opioids during surgery and in cases of known or suspected opioid overdose. [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 | 5284596 |
CHEMBL ID | 80 |
CHEBI ID | 7459 |
SCHEMBL ID | 34284 |
MeSH ID | M0014441 |
Synonym |
---|
BIDD:GT0110 |
BRD-K67511046-003-03-7 |
gtpl1676 |
gtpl1638 |
[n-allyl-2,3-3h]naloxone |
(1s,5r,13r,17s)-10,17-dihydroxy-4-(prop-2-en-1-yl)-12-oxa-4-azapentacyclo[9.6.1.0^{1,13}.0^{5,17}.0^{7,18}]octadeca-7(18),8,10-trien-14-one |
kloxxado (naloxone hydrochloride nasal spray) |
nyxoid |
[3h]naloxone |
smr000058766 |
MLS000069540 , |
(5alpha)-3,14-dihydroxy-17-prop-2-en-1-yl-4,5-epoxymorphinan-6-one |
normorphinone, n-allyl-7,8-dihydro-14-hydroxy-, (-)- |
nalossone [dcit] |
naloxonum [inn-latin] |
naloxona [inn-spanish] |
n-allyl-4,5alpha-epoxy-3,14-dihydroxy-6-morphinanon |
naloxone [inn:ban] |
einecs 207-365-7 |
brn 1089071 |
nsc 70413 |
morphinan-6-one, 4,5-alpha-epoxy-3,14-dihydroxy-17-(2-propenyl)- |
n-allyl-noroxymorphone |
l-n-allyl-14-hydroxynordihydromorphinone |
l-n-allyl-7,8-dihydro-14-hydroxynormorphinone |
morphinan-6-one,5-epoxy-3,14-dihydroxy-17-(2-propenyl)-, (5.alpha.)- |
l-naloxone |
n-allylnoroxymorphone |
nalone |
narcon |
narcan |
morphinan-6-one,5.alpha.-epoxy-3,14-dihydroxy- |
nsc70413 |
morphinan-6-one,5.alpha.-epoxy-3,14-dihydroxy-17-(2-propenyl)- |
(-)-naloxone |
4ah-8,5-bcd]furan-5(6h)-one, n-allyl-7,7a,8,9-tetrahydro-3,7a-dihydroxy- |
nsc-70413 |
mls000736771 , |
en 1530 base |
BSPBIO_000122 |
PDSP2_001520 |
PRESTWICK2_000111 |
SMP1_000205 |
PRESTWICK3_000111 |
BPBIO1_000136 |
naloxonum |
3,14-dihydroxy-17-(prop-2-en-1-yl)-4,5alpha-epoxymorphinan-6-one |
naloxona |
CHEBI:7459 , |
1-n-allyl-14-hydroxynordihydromorphinone |
morphinan-6-one, 17-allyl-4,5alpha-epoxy-3,14-dihydroxy- (8ci) |
morphinan-6-one, 4,5alpha-epoxy-3,14-dihydroxy-17-(2-propenyl)- |
12-allyl-7,7a,8,9-tetrahydro-3,7a-dihydroxy-4ah-8,9c-iminoethanophenanthro(4,5-bcd)furanone |
(-)-n-allyl-14-hydroxynordihydroxymorphinan-6-one |
hsdb 3279 |
morphinan-6-one, 17-allyl-4,5alpha-epoxy-3,14-dihydroxy- |
(5alpha)-4,5-epoxy-3,14-dihydroxy-17-(2-propenyl)morphinan-6-one |
17-allyl-4,5-alpha-epoxy-3,14-dihydroxymorphinan-6-one |
1-n-allyl-7,8-dihydro-14-hydroxynormorphinone |
17-allyl-4,5alpha-epoxy-3,14-dihydroxymorphinan-6-one |
morphinan-6-one, 4,5-epoxy-3,14-dihydroxy-17-(2-propenyl)-, (5alpha)- (9ci) |
morphinan-6-one, 4,5-epoxy-3,14-dihydroxy-17-(2-propenyl)-, (5alpha)- |
12-allyl-7,7a,8,9-tetrahydro-3,7a-dihydroxy-4ah-8,9c-iminoethanophenanthro[4,5-bcd]furan-5(6h)-one |
465-65-6 |
naloxone |
C07252 |
NLX , |
DB01183 |
17-allyl-3,14-dihydroxy-4,5alpha-epoxymorphinan-6-one |
NCGC00162267-02 |
PRESTWICK1_000111 |
PRESTWICK0_000111 |
SPBIO_002061 |
NCGC00024674-02 |
HMS2090F20 |
dbl naloxone |
CHEMBL80 |
D08249 |
dbl naloxone (tn) |
naloxone (inn) |
(naloxone) 4-allyl-10,17-dihydroxy-(1s,5r,13r,17s)-12-oxa-4-azapentacyclo[9.6.1.01,13.05,17.07,18]octadeca-7(18),8,10-trien-14-one |
bdbm50000788 |
4-allyl-10,17-dihydroxy-(1s,5r,13r,17s)-12-oxa-4-azapentacyclo[9.6.1.01,13.05,17.07,18]octadeca-7(18),8,10-trien-14-one(naxolone) |
4-allyl-10,17-dihydroxy-12-oxa-4-azapentacyclo[9.6.1.01,13.05,17.07,18]octadeca-7(18),8,10-trien-14-one(naloxone)c2h2o4 |
(naloxone)4-allyl-10,17-dihydroxy-(1s,5r,13r,17s)-12-oxa-4-azapentacyclo[9.6.1.01,13.05,17.07,18]octadeca-7(18),8,10-trien-14-one |
4-allyl-10,17-dihydroxy-(1s,5r,13r,17s)-12-oxa-4-azapentacyclo[9.6.1.01,13.05,17.07,18]octadeca-7(18),8,10-trien-14-one |
[17-(2,3-3h-2-propenyl)]-4, 5a -epoxy-3,14-dihydroxymorphinan-6-one |
4-allyl-10,17-dihydroxy-(1s,5r,13r,17s)-12-oxa-4-azapentacyclo[9.6.1.01,13.05,17.07,18]octadeca-7(18),8,10-trien-14-one (naloxone) |
4-allyl-10,17-dihydroxy-(1s,5r,13r,17s)-12-oxa-4-azapentacyclo[9.6.1.01,13.05,17.07,18]octadeca-7(18),8,10-trien-14-one( naloxone) |
(naloxone)4-allyl-10,17-dihydroxy-12-oxa-4-azapentacyclo[9.6.1.01,13.05,17.07,18]octadeca-7(18),8,10-trien-14-one |
4-allyl-10,17-dihydroxy-12-oxa-4-azapentacyclo[9.6.1.01,13.05,17.07,18]octadeca-7(18),8,10-trien-14-one |
NCGC00024674-03 |
36b82amq7n , |
nalossone |
naloxone nasal spray |
unii-36b82amq7n |
dtxsid8023349 , |
dtxcid703349 |
cas-465-65-6 |
tox21_112006 |
AKOS016009988 |
niosh/qd2135000 |
17-allyl-3,14-dihydroxy-4,5-alpha-epoxymorphinan-6-one |
7,8-dihydro-n-allyl-14-hydroxynormorphinone |
ram-301 |
morphinan-6-one, 17-allyl-3,14-dihydroxy-4,5-alpha-epoxy- |
normorphinone, 7,8-dihydro-n-allyl-14-hydroxy- |
QD21350000 , |
naloxone [who-dd] |
naloxone [inn] |
naloxone [usp-rs] |
naloxone [hsdb] |
morphinan-6-one, 4,5-epoxy-3,14-dihydroxy-17-(2-propenyl)- |
naloxone [mi] |
(-)-n-allyl-14-hydroxynordihydromorphinone |
naloxone [vandf] |
naloxone [orange book] |
naloxone [ema epar] |
17-allyl-4,5a-epoxy-3,14-dihydroxymorphinan-6-one |
SCHEMBL34284 |
tox21_112006_1 |
NCGC00274058-01 |
UZHSEJADLWPNLE-GRGSLBFTSA-N |
(4r,4as,7ar,12bs)-4a,9-bis(oxidanyl)-3-prop-2-enyl-2,4,5,6,7a,13-hexahydro-1h-4,12-methanobenzofuro[3,2-e]isoquinoline-7-one;hydrochloride |
bdbm54795 |
(4r,4as,7ar,12bs)-3-allyl-4a,9-dihydroxy-2,4,5,6,7a,13-hexahydro-1h-4,12-methanobenzofuro[3,2-e]isoquinoline-7-one;hydrochloride |
(4r,4as,7ar,12bs)-4a,9-dihydroxy-3-prop-2-enyl-2,4,5,6,7a,13-hexahydro-1h-4,12-methanobenzofuro[3,2-e]isoquinoline-7-one;hydrochloride |
cid_5464092 |
4683B |
Q282902 |
2-(([2-(ethylthio)-3-pyridyl]carbonyl)amino)-4-(methylthio)butanoicacid |
BRD-K67511046-001-02-3 |
(4r,4as,7ar,12bs)-4a,9-dihydroxy-3-prop-2-enyl-2,4,5,6,7a,13-hexahydro-1h-4,12-methanobenzofuro[3,2-e]isoquinolin-7-one |
(5alpha)-4,5-epoxy-3,14-dihydroxy-17-(2-propen-1-yl)morphinan-6-one |
EN300-19748912 |
us11484525, compound naloxone |
bdbm579486 |
naloxone (usp-rs) |
a06ah04 |
naloxona (inn-spanish) |
naloxonum (inn-latin) |
naloxonum (latin) |
naloxoni hydrochloridum |
v03ab15 |
Naloxone is an opioid receptor antagonist that counteracts the effects of an opioid overdose. It is a population-level prevention intervention associated with substantial reductions in overdose mortality and reduction of nonfatal overdose.
Naloxone has a high affinity for the µ-opioid receptor and acts as a competitive antagonist, thus reversing the effects of opioids. The drug has a dose-dependent, significant anorectic effect when administered to normal rats, consistent with an antagonism of central or peripheral enkephalinergic or endorphinergic mechanisms.
Naloxone has been shown to induce LH release in female but not in male rats 10-25 days of age. Nalox one dispensing has substantially increased, in part driven by standing orders. SAIA-NalOXone has strong potential for improving naloxon distribution from syringe service programs.
Naloxone can enhance the antinociceptive/analgesic effects of buprenorphine in humans and rats. Nalox one did not cause changes in ejection fraction or mean pulmonary artery pressure in hypoxic and hypercarbic conditions.
Naloxone pretreatment (82.5 nmol/rat, 30 min before zinc administration) reverted the water intake to the high levels observed in zinc-free dehydrated animals. Treatment induced a marked increase in catecholamine plasma concentrations, metabolism, and cardiovascular stimulation during anesthesia with propofol and methohexital.
Excerpt | Reference | Relevance |
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"Naloxone Treatment in Skåne County - Effect on Drug-related Mortality and Overdose-related Complications, NCT03570099, registered on 26 June 2018." | ( Protocol for a multi-site study of the effects of overdose prevention education with naloxone distribution program in Skåne County, Sweden. Blomé, MA; Dahlman, D; Håkansson, A; Isendahl, P; Troberg, K, 2020) | 2.22 |
"(+)-Naloxone treatment decreased microglia/macrophage activation in the striatum and thalamus, promoted behavioral recovery during the 14-d monitoring period, and reduced neuronal death in the lesioned cortex and ipsilateral thalamus." | ( Post-stroke Intranasal (+)-Naloxone Delivery Reduces Microglial Activation and Improves Behavioral Recovery from Ischemic Injury. Airavaara, M; Albert, K; Anttila, JE; Harvey, BK; Loram, LC; Mätlik, K; Rice, KC; Wang, Y; Watkins, LR; Wires, ES, ) | 0.91 |
"Naloxone pretreatment blocked the suppressive effects of the restraint on NKCC and IL-12 and altered IL-10, IL-6, TNF-α, PRL and ACTH concentrations." | ( Natural killer cell cytotoxicity, cytokine and neuroendocrine responses to opioid receptor blockade during prolonged restraint in pigs. Borman, A; Ciepielewski, ZM; Glac, W; Kamyczek, M; Myślińska, D; Stojek, W, 2013) | 1.11 |
"The naloxone pre-treatment did not alter the antinociception induced by aerobic exercise protocols." | ( Opioid receptors are not involved in the increase of the nociceptive threshold induced by aerobic exercise. Andrade, I; Duarte, I; Galdino, G; Perez, A; Romero, T, 2014) | 0.88 |
"Naloxone treatment decreased the expression of DAT by 8.2 fold in female control offspring but increased it by 4.3 fold in female offspring of JF dams relative to the saline-injected reference groups." | ( Naloxone treatment alters gene expression in the mesolimbic reward system in 'junk food' exposed offspring in a sex-specific manner but does not affect food preferences in adulthood. Gugusheff, JR; Muhlhausler, BS; Ong, ZY, 2014) | 2.57 |
"The naloxone groups were treated with naloxone for 30 minutes before remifentanil treatment." | ( Effects of Remifentanil Preconditioning on Osteoblasts under Hypoxia-Reoxygenation Condition. Baik, SW; Kim, CH; Kim, YD; Kim, YH; Park, BS; Yoon, JU; Yoon, JY, 2015) | 0.9 |
"Naloxone alone treatment did not cause any significant effect on CPP." | ( Dexmedetomidine induces conditioned place preference in rats: Involvement of opioid receptors. Akkan, AG; Barlas, MA; Shahzadi, A; Uskur, T; Uzbay, T, 2016) | 1.16 |
"Naloxone (5 mg/kg) pre-treatment reversed the antinociceptive activities suggesting the involvement of opioid system in the analgesic actions." | ( Synthesis and antinociceptive activities of some pyrazoline derivatives. Can, Ov; Chevallet, P; Kaplancikli, ZA; Ozdemir, A; Turan-Zitouni, G, 2009) | 1.07 |
"Naloxone pretreatment before morphine administration suppressed withdrawal jumping, weight loss, and overexpression of aldolase C." | ( Chronic morphine administration induces over-expression of aldolase C with reduction of CREB phosphorylation in the mouse hippocampus. Pu, XP; Yang, HY, 2009) | 1.07 |
"Naloxone (200 microg) treatment was used to reverse fentanyl effects, but it was associated with hypertension." | ( Naloxone-induced pulmonary edema: a potential cause of postoperative morbidity in laparoscopic donor nephrectomy. Nath, SS; Pandey, C; Rao, B; Tripathi, M, 2009) | 2.52 |
"Naloxone treatment immediately after early life SE could dose-dependently reduce cytokine production, glial activation, and further lower the vulnerability of immature brains to a second hit in adulthood." | ( Protective effects of naloxone in two-hit seizure model. Ge, W; Li, F; Mi, C; Sun, R; Wang, R; Yang, L, 2010) | 2.12 |
"Naloxone treatment may have a beneficial role in lethal doses of amitriptyline ingestion because amitriptyline may affect opioid receptors." | ( Amitriptyline and tianeptine poisoning treated by naloxone. Ari, M; Duru, M; Oktar, S, 2010) | 1.34 |
"In naloxone treated rats visceromotor reflexes to bladder distention were significantly greater in those with an inflamed vs a noninflamed bladder when examined together." | ( Opioid blockade and inflammation reveal estrous cycle effects on visceromotor reflexes evoked by bladder distention. Ball, CL; Ness, TJ; Randich, A, 2010) | 0.87 |
"Naloxone (0.4 mM) pretreated by local perfusion to the NAc, significantly blocked the effects of morphine." | ( Lesions of nucleus accumbens affect morphine-induced release of ascorbic acid and GABA but not of glutamate in rats. Dong, YX; Song, W; Su, GY; Sun, JY; Wang, F; Wang, JY; Wu, CF; Yang, JY, 2011) | 1.09 |
"Naloxone treatment did not affect intake of standard rodent feed in control or JF offspring." | ( A maternal "junk-food" diet reduces sensitivity to the opioid antagonist naloxone in offspring postweaning. Gugusheff, JR; Muhlhausler, BS; Ong, ZY, 2013) | 1.34 |
"Naloxone pretreatment largely abolished rTMS-induced analgesia, as well as rTMS-induced attenuation of BOLD signal response to painful stimuli throughout pain processing regions, including midbrain and medulla." | ( Naloxone-reversible modulation of pain circuitry by left prefrontal rTMS. Borckardt, JJ; Brown, TR; Canterberry, M; George, MS; Hanlon, CA; Li, X; Taylor, JJ, 2013) | 2.55 |
"Naloxone treatment reduced in well-nourished rats the CSD propagation velocity, as compared to saline-injected controls." | ( Early malnutrition attenuates the impairing action of naloxone on spreading depression in young rats. de Albuquerque, Jda M; de Lima, KR; Francisco, Eda S; Guedes, RC; Rocha-de-Melo, AP, 2013) | 1.36 |
"Naloxone pretreatment to nalbuphine produced changes in brain activity possess characteristics of both analgesia and algesia; naloxone selectively blocks activity in areas associated with algesia." | ( Pain facilitation brain regions activated by nalbuphine are revealed by pharmacological fMRI. Becerra, L; Bishop, J; Borsook, D; Gear, R; Levine, J; Pendse, G; Upadhyay, J; Wallin, D, 2013) | 1.11 |
"Naloxone-pretreatment decreased the proportion of M3G-responsive neurones by 10%-25%, implicating a predominantly non-opioidergic mechanism." | ( Morphine-3-glucuronide's neuro-excitatory effects are mediated via indirect activation of N-methyl-D-aspartic acid receptors: mechanistic studies in embryonic cultured hippocampal neurones. Hemstapat, K; Monteith, GR; Smith, D; Smith, MT, 2003) | 1.04 |
"Naloxone treatment in naive rats induced a slight increase in c-Fos immunoreactivity in the central amygdaloid nucleus, the lateral bed nucleus of the stria terminalis and the interstitial nucleus of the posterior limb of the anterior commissure." | ( c-Fos and peptide immunoreactivities in the central extended amygdala of morphine-dependent rats after naloxone-precipitated withdrawal. Freund-Mercier, MJ; Lasbennes, F; Stoeckel, ME; Veinante, P, 2003) | 1.26 |
"Naloxone (alone) treatment of rats had no effect on the levels of CREB and p-CREB protein in the nucleus accumbens." | ( Changes of phosphorylation of cAMP response element binding protein in rat nucleus accumbens after chronic ethanol intake: naloxone reversal. Li, J; Li, YH; Yuan, XR, 2003) | 1.25 |
"In naloxone-treated group, the rats' seizure duration and seizure grade [(5.66+/-2.78) min, (2.97+/-1.18)] significantly decreased (t=5.035, P<0.01; t=3.343, P<0.01) compared with those in FS control group [(21.18+/-4.06) min, (4.54+/-0.78)], although no significant gap was observed on seizure incidence rate(57.7%,84.6% respectively) and seizure latency between them. " | ( [Effect of naloxone on remote seizure susceptibility]. Chang, XZ; Qin, J; Shan, Y; Yang, ZX, 2004) | 1.33 |
"Naloxone pretreatment abolished the effect of morphine, but was enable to block the inhibitory effect of nociceptin." | ( Nociceptin inhibits airway microvascular leakage induced by HCl intra-oesophageal instillation. Advenier, C; Bardou, M; Cui, YY; D'Agostino, B; Faisy, C; Naline, E; Rouget, C, 2004) | 1.04 |
"Naloxone pretreatment (0.006, 0.025 and 0.1 microg/mouse) reversed the effect of pre-test morphine administration." | ( Influence of central administration ATP-dependent K+ channel on morphine state-dependent memory of passive avoidance. Ahmadi, S; Djahanguiri, B; Jafari, MR; Zarrindast, MR, 2004) | 1.04 |
"In naloxone-treated group, the rats' FS duration and FS grade (5.02 +/- 0.63, 2.63 +/- 0.72) were significantly lower (t = 5.508, P < 0.01; t = 8.439, P < 0.01) than those in FS control group (7.70 +/- 2.25 min, 4.52 +/- 0.49), although no significant gap was observed on FS latency between them. " | ( [Neuroprotective effect of naloxone in brain damage caused by repeated febrile seizure]. Chang, XZ; Qin, J; Shan, Y; Yang, ZX, 2004) | 1.24 |
"naloxone-treated rats (NAL 0.8 mg/kg, i.p." | ( Effect of naloxone on aluminum-induced learning and memory impairment in rats. Bachelor, LH; Bachelor, ZY; Dong, HM; Guang-Yu, MA; Shi-Lei, S; Xu, XH, 2005) | 1.45 |
"Naloxone pretreatment affected neither the ventilation nor the development of dyspneic sensation during loaded breathing." | ( Effects of naloxone on respiratory sensation before and after a removal of severe respiratory stress. Ishikawa, T; Isono, S; Nishino, T; Shinozuka, N, 2005) | 1.44 |
"Naloxone pretreatment (5 mg/kg, i.v.) restored ACTH and pPVN CRH mRNA responses after IL-1beta in pregnant rats but reduced the CRH mRNA response in virgins without affecting ACTH." | ( Endogenous opioids and attenuated hypothalamic-pituitary-adrenal axis responses to immune challenge in pregnant rats. Brunton, PJ; Douglas, AJ; Ma, S; Meddle, SL; Ochedalski, T; Russell, JA, 2005) | 1.05 |
"Naloxone pretreatment blocked these effects." | ( Effects of acupuncture at GV01 on experimentally induced colitis in rats: possible involvement of the opioid system. Hahm, DH; Kim, HY; Lee, HJ; Lee, SK; Nam, TC; Pyun, KH; Shim, I, 2005) | 1.05 |
"naloxone in the treatment of suspected opiate overdose patients in the prehospital setting, a prospective, nonrandomized trial of administering i.n." | ( Efficacy of intranasal naloxone as a needleless alternative for treatment of opioid overdose in the prehospital setting. Bailey, J; Barton, ED; Benson, J; Bryan, T; Colwell, CB; Dunn, W; Fosnocht, D; Gravitz, C; Wolfe, T, 2005) | 1.36 |
"In naloxone-pretreated group, insulin administration could significantly reverse the inhibition of SIT produced by naloxone when compared with naloxone per se group, i.e." | ( An inherent acceleratory effect of insulin on small intestinal transit and its pharmacological characterization in normal mice. Dkhar, SA; Naveen, AT; Peddyreddy, MK; Ramaswamy, S; Shewade, DG, 2006) | 0.85 |
"Naloxone pretreatment significantly suppressed the production of tumor necrosis factor-alpha (TNF-alpha), interleukin-6, monocyte chemoattractant protein-1, and superoxide in macrophages after stimulation. " | ( A novel inhibitory effect of naloxone on macrophage activation and atherosclerosis formation in mice. Chen, YH; Hong, JS; Huang, CW; Li, YH; Liu, SL; Shi, GY; Wu, HL, 2006) | 2.07 |
"Naloxone treatment did not modify the 3,4-dihydroxyphenylacetic acid/DA (DOPAC/DA) ratio or serum prolactin concentration in control rats." | ( Dopaminergic mechanisms involved in prolactin release after mifepristone and naloxone treatment during late pregnancy in the rat. Bregonzio, C; Deis, RP; Penissi, A; Soaje, M; Valdez, S, 2006) | 1.28 |
"Naloxone, the standard treatment for heroin overdose, is a safe and effective prescription drug commonly administered by emergency room physicians or first responders acting under standing orders of physicians. " | ( Physicians' knowledge of and willingness to prescribe naloxone to reverse accidental opiate overdose: challenges and opportunities. Beletsky, L; Burris, S; Macalino, GE; Rich, JD; Ruthazer, R; Tan, L, 2007) | 2.03 |
"Naloxone pretreatment in the course of kindling had no effect on seizures development, however it caused an improvement of spatial learning and memory performance in kindled rats." | ( Naloxone improves impairment of spatial performance induced by pentylenetetrazol kindling in rats. Fathi, N; Fathollahi, Y; Ghadami, MR; Omrani, A; Tahmasian, M; Touhidi, A, 2007) | 2.5 |
"Naloxone pretreatment had no effect on the antinociceptive effects of intradermal diclofenac, ketorolac, lysine acetyl salicylate, and sodium salicylate." | ( The local antinociceptive actions of nonsteroidal antiinflammatory drugs in the mouse radiant heat tail-flick test. Deveci, MS; Dogrul, A; Gul, H; Gülmez, SE; Ossipov, MH; Porreca, F; Tulunay, FC, 2007) | 1.06 |
"Naloxone treatment significantly attenuated ethanol intake of rats and antagonized the decrease of CaM kinase IV in the nuclei of NAc neurons." | ( Chronic ethanol intake-induced changes in open-field behavior and calcium/calmodulin-dependent protein kinase IV expression in nucleus accumbens of rats: naloxone reversal. Bian, WL; Cui, SZ; Li, J; Li, YH; Que, LL; Wu, ML; Xie, GQ; Yuan, XR, 2008) | 1.27 |
"Naloxone treatment inhibited the spontaneous fall of adrenal ENK release during the hypotensive phase; the ENK values remained elevated 20- to 35-fold." | ( Release of opioid peptides in canine hemorrhagic hypotension: effects of naloxone. Brückner, UB; Ganten, D; Lang, RE, 1984) | 1.22 |
"Naloxone pretreatment of the cells had no effect on basal nor dopamine-inhibited release of PRL." | ( Does beta-endorphin modulate basal and dopamine-inhibited prolactin release by an action at the anterior pituitary? Cheung, CY, 1984) | 0.99 |
"Naloxone (1 mg/kg) pre-treatment inhibited both heart rate and blood pressure increases." | ( Mechanism of the cardiovascular response to systemic intravenous administration of leucine-enkephalin in the conscious dog. Giles, TD; Sander, GE, ) | 0.85 |
"Naloxone (10 min pretreatment, 0.5 or 1 mg kg-1 s.c.) did not selectively antagonize intestinal action of the morphine since the relief of charcoal transit inhibition was consistently associated with complete loss of analgesia.(ABSTRACT TRUNCATED AT 250 WORDS)" | ( The peripheral narcotic antagonist N-allyl levallorphan-bromide (CM 32191) selectively prevents morphine antipropulsive action and buprenorphine in-vivo binding in the rat intestine. Bianchi, G; Fiocchi, R; Manara, L; Peracchia, F; Petrillo, P; Tavani, A, 1984) | 0.99 |
"6 Naloxone pretreatment (10(-6) M) in the presence of hexamethonium (10(-5)--10(-4) M) enhanced the magnitude of the noncholinergic contracture without affecting responses to exogenous substance P (4 x 10(-11)--4 x 10(-10) M)." | ( Effects of opioids on noncholinergic excitatory responses of the guinea-pig isolated ileum: inhibition of release of enteric substance P. Gintzler, AR; Scalisi, JA, 1982) | 0.82 |
"Naloxone pretreatment antagonized the respiratory depression and death, while the decrease in heart rate was diminished." | ( Cardiovascular and respiratory effects of beta-endorphin in anesthetized and conscious rats. De Jong, W; Sitsen, JM; Van Ree, JM, ) | 0.85 |
"Naloxone pre-treatment failed to modify significantly the latter two responses, while Prl stimulation was inhibited." | ( Inhibition of vasopressin secretion by a met-enkephalin (FK 33-824) in humans. Brownell, J; del Pozo, E; Donatsch, P, 1980) | 0.98 |
"Naloxone pretreatment also obscured the effect of subsequently injected morphine (3 mg/20 kg)." | ( Morphine and naloxone: effects on beta-endorphin immunoreactivity in canine plasma and secretions from rat pituitaries. Carlson, HE; Levin, ER; Meyer, NV; Sharp, B, 1981) | 1.35 |
"Naloxone treatment prior to ECS provides partial protection against the development of tolerance to ECS-induced catalepsy but does not present the tolerance to post-ECS analgesia." | ( Different opioid systems may participate in post-electro-convulsive shock (ECS) analgesia and catalepsy. Frenk, H; Urca, G; Yitzhaky, J, 1981) | 0.98 |
"Naloxone-treated animals also showed less prominent spinal cord abnormalities and significantly improved neurological recovery compared with saline controls." | ( Endorphins in experimental spinal injury: therapeutic effect of naloxone. Faden, AI; Holaday, JW; Jacobs, TP; Mougey, E, 1981) | 1.22 |
"Naloxone pretreatment also antagonized the potentiating effect of morphine on ACTH-induced steroidogenesis in a dose-dependent manner." | ( Naloxone inhibits and morphine potentiates the adrenal steroidogenic response to ACTH. Heybach, JP; Vernikos, J, 1981) | 2.43 |
"Naloxone treatment did not significantly alter the regional pattern of 2DG uptake." | ( Regional glucose metabolism in mouse brain following ACTH peptides and naloxone. Dunn, AJ; Hurd, RW, 1982) | 1.22 |
"Naloxone treatment in hypotensive-hypovolemic, conscious rabbits results in an increase in mean arterial blood pressure (BP) and a decrease in heart rate (HR)." | ( Involvement of both adrenergic and cholinergic receptors in the cardiovascular effects of naloxone during hemorrhagic hypotension in the conscious rabbit. Schadt, JC; York, DH, 1982) | 1.21 |
"Naloxone treatment before testing attenuated bradycardiac orienting responses to tones used as conditioning stimuli." | ( Naloxone induces multiple effects on aversive Pavlovian conditioning in rabbits. Hernández, LL; Powell, DA, 1983) | 2.43 |
"Naloxone pretreatment resulted in a significantly reduced GH increase after the clonidine infusion." | ( Partial blockade by naloxone of clonidine-induced increase in plasma growth hormone in hypertensive patients. Bramnert, M; Hökfelt, B, 1984) | 1.31 |
"Naloxone treatment did not increase the T4 and T3 concentrations; however, serum TSH was elevated in the 15 min sample." | ( Short-term effect of morphine on the thyroid gland in male rats. Endröczi, E; Korányi, L; Kovács, Z; Tal, E, 1984) | 0.99 |
"Naloxone-treated birds showed preening levels similar to those of unhandled and saline-treated birds." | ( Handling, ACTH, ACTH1-24, and naloxone effects on preening behavior in domestic chickens. Scampoli, DL; Williams, NS, 1984) | 1.28 |
"Naloxone treated animals did not show the increased platelet aggregability normally seen in endotoxin shocked dogs." | ( Effect of naloxone on endotoxin-induced pulmonary platelet sequestration. Almqvist, P; Kuenzig, M; Schwartz, SI, 1983) | 1.39 |
"Naloxone pretreatment (4.8 mg, intravenously) partially reversed the blocking effect of morphine on the PP secretion evoked by insulin-induced hypoglycemia (peak: 977 +/- 133 pg/mL, P less than 0.05 vs." | ( Suppressor effect of morphine on the pancreatic polypeptide response to insulin-induced hypoglycemia in man. Correas, I; Marco, J; Zulueta, MA, 1983) | 0.99 |
"Naloxone treatment (0.01, 0.1 and 1.0 mg/kg) produced a dose-dependent decrease in the stress-induced NaCl intake, as did captopril treatment (5, 10 and 50 mg/kg)." | ( Stress, endogenous opioids and salt intake. Bryant, HU; Kuta, CC; Yim, GK; Zabik, JE, 1984) | 0.99 |
"Naloxone pretreatment markedly attenuated the response to high dose FK 33-824." | ( Effects of naloxone and an enkephalin analog on serum prolactin, cortisol, and gonadotropins in the chimpanzee. Blankstein, J; Dent, DW; Faiman, C; Fuller, GB; Gosselin, RE; Hobson, WC; Reyes, FI; Winter, JS, 1983) | 1.38 |
"Naloxone treatment (1) resulted in activation of FBM in association with W, (2) lowered CO2 threshold as compared to that of CO2 tests entered in QS without naloxone, and (3) caused greater FBM responses to CO2 than without naloxone." | ( CO2 and naloxone modify sleep/wake state and activate breathing in the acute fetal lamb preparation. Moss, IR; Scarpelli, EM, 1984) | 1.42 |
"Naloxone-treated animals did not develop high blood pressure or strokes." | ( Naloxone ameliorates the pathophysiologic changes which lead to and attend an acute stroke in stroke-prone/SHR. Wexler, BC, ) | 2.3 |
"Naloxone treatment resulted in dose-related enhancement of motor recovery; greatest functional recovery was observed in rabbits treated with a dose of 2 mg/kg per h." | ( Naloxone in experimental spinal cord ischemia: dose-response studies. Faden, AI; Jacobs, TP; Smith, MT; Zivin, JA, 1984) | 2.43 |
"Naloxone pretreatment (2 or 5 mg/kg, s.c.) reversed the decreasing effect of morphine in the 3rd ventricle (1 microgram/rat) and the increasing effect of morphine in the posterior hypothalamus (1 microgram/side)." | ( Dual action of morphine on cold-stimulated thyrotropin secretion in male rats. Männistö, PT; Mattila, J; Rauhala, P; Tuominen, R, 1984) | 0.99 |
"Naloxone pretreatment attenuated significantly the antinociception developed at 3 mA but failed to affect that produced at 6 mA." | ( Failure to produce a non-opioid foot shock-induced antinociception in rats. Chatterjee, TK; Gebhart, GF, 1984) | 0.99 |
"Naloxone pretreatment (10 mg/kg but not 1 mg/kg) shortened recovery to multiple squeak responses, grid clinging, and locomotion, without affecting recovery of bar pressing, food consumption, or EEG postictal depression." | ( Changes in simple and complex behaviors following kindled seizures in rats: opioid and nonopioid medication. Caldecott-Hazard, S; Camacho, H; Hedlund, J; Liebeskind, JC; Yamagata, N, 1983) | 0.99 |
"Naloxone pretreatment statistically significantly antagonized the cerebral metabolic effect of GHB in 10 of 38 structures examined." | ( Naloxone pretreatment alters the local cerebral metabolic effect of gamma-hydroxybutyrate in rats. Crosby, G; Ito, M; Kaufman, E; Nelson, T; Sokoloff, L, 1983) | 2.43 |
"Naloxone treatment protected against both moderate (20 min aortic occlusion) and severe (25 min aortic occlusion) degrees of ischemic spinal injury, whereas treatment with M154,129 failed to improve recovery in either model." | ( Comparison of naloxone and a delta-selective antagonist in experimental spinal stroke. Faden, AI; Jacobs, TP; Zivin, JA, 1983) | 1.35 |
"Naloxone pretreatment on doses up to 20 mg/kg was not effective in antagonizing PCP-induced behavioral effects." | ( Phencyclidine-induced stereotype in rats: effects of methadone, apomorphine, and naloxone. Kogan, MJ; Mulè, SJ; Verebey, K, 1981) | 1.21 |
"Naloxone treatment significantly improved the cortical somatosensory evoked response and had a beneficial effect on local cerebral blood flow, whereas TRH treatment had no effect on these variables." | ( Treatment of experimental stroke: comparison of naloxone and thyrotropin releasing hormone. Brown, CQ; Faden, AI; Hallenbeck, JM, 1982) | 1.24 |
"naloxone-pretreatment groups) also failed to consistently reverse the clonidine-induced changes in blood pressure, heart rate and sympathetic nerve activity." | ( Failure of naloxone to reduce clonidine-induced changes in blood pressure, heart rate and sympathetic nerve firing in cats. Shropshire, AT; Wendt, RL, 1983) | 1.38 |
"If naloxone pretreatment is effective and posttreatment is not, then it is possible that an opiatelike substance might be released by endotoxin which in turn results in the ultimate release of the lesion-producing substance." | ( Effect of naloxone treatment on the cardiopulmonary response to endotoxin in sheep. Adams, T; Henriksen, N; Jinkins, J; Rice, K; Sziebert, L; Thomson, PD; Traber, DL; Traber, LD, 1983) | 1.18 |
"Naloxone pretreatment (1.0, 3.0 and 10.0 mg/kg i.v.) failed to protect anesthetized pigs from cardiac arrhythmias including ventricular fibrillation (VF) and death following acute occlusion (20 min) or reperfusion of the left anterior descending coronary artery. " | ( Antiarrhythmic evaluation of naloxone against acute coronary occlusion-induced arrhythmias in pigs. Beil, ME; Bergey, JL, 1983) | 2 |
"Naloxone-treated males and sexually receptive females were pair tested for sexual behavior." | ( Endogenous opiate systems and primate reproduction: inability of naloxone to induce sexual activity in rhesus males. Baughman, WL; Glick, BB; Jensen, JN; Phoenix, CH, 1982) | 1.22 |
"Naloxone treatment also prolonged survival time." | ( Naloxone without transfusion prolongs survival and enhances cardiovascular function in hypovolemic shock. Gurll, NJ; Lechner, R; Reynolds, DG; Vargish, T, 1982) | 2.43 |
"The naloxone-treated pups had significantly better scores during the first 15 minutes after birth than the saline-treated pups." | ( Naloxone reverses neonatal depression caused by fetal asphyxia. Chernick, V; Craig, RJ, 1982) | 2.19 |
"The naloxone-treated cats had striking preservation of sensory function and somatosensory evoked potentials at 24 hours after injury." | ( Effect of naloxone on posttraumatic ischemia in experimental spinal contusion. DeCrescito, V; Demopoulos, HB; Flamm, ES; Tomasula, JJ; Young, W, 1981) | 1.15 |
"Naloxone treatment resulted in a rapid increase in mean arterial pressure (MAP) in animals made hypotensive by endotoxin administration." | ( Naloxone treatment of endotoxin shock: stereospecificity of physiologic and pharmacologic effects in the rat. Faden, AI; Holaday, JW, 1980) | 2.43 |
"Naloxone (2 mg/kg) pretreatment abolished this antinocicpetive effect suggesting that an endogenous opiate-like substance was involved." | ( The effect of hypophysectomy on acupuncture analgesia in the mouse. Dewey, WL; Fu, TC; Halenda, SP, 1980) | 0.98 |
"3. Naloxone pretreatment abolished the secondary increase in blood pressure and the tachycardia, but did not blunt the initial pressor response in female Wistar-Kyoto rats." | ( Increased pressor responsiveness to enkephalin in spontaneously hypertensive rats: the role of vasopressin. Crofton, JT; Rockhold, RW; Share, L, 1980) | 0.78 |
"Naloxone treatment, immediately after trauma, attenuated the inactivation of Na(+)-K+/Mg+2 ATPase." | ( Effects of naloxone on sodium- and potassium-activated and magnesium-dependent adenosine-5'-triphosphatase activity and lipid peroxidation and early ultrastructural findings after experimental spinal cord injury. Göçer, AI; Ildan, F; Isbir, T; Karadayi, A; Kaya, M; Oner, A; Polat, S; Tap, O, 1995) | 1.4 |
"Naloxone pretreatment (10 mg/kg s.c.) blocked the effect of U50 alone and in combination with NT, as did the peripheral opioid antagonist, naloxone methiodide (100 mg/kg s.c.)." | ( Interaction between opioid agonists and neurotensin on thermoregulation in the rat. I. Body temperature. Adler, MW; Geller, EB; Handler, CM; Mondgock, DJ; Zhao, SF, 1995) | 1.01 |
"Naloxone pretreatment caused augmented AVP and OT secretion in response to hypertonic saline stimulation and hemorrhage in both the normonatremic and hyponatremic rats; the magnitude of the naloxone augmentations in the hyponatremic rats were sufficient to normalize the OT response to hypertonic saline and both the OT and AVP responses to hemorrhage." | ( Naloxone disinhibits magnocellular responses to osmotic and volemic stimuli in chronically hypoosmolar rats. Dohanics, J; Verbalis, JG, 1995) | 2.46 |
"Naloxone treatment had no effect on GnRH pulse frequency, but significantly increased GnRH pulse size." | ( Endogenous opioid peptides control the amplitude and shape of gonadotropin-releasing hormone pulses in the ewe. Dahl, GE; Evans, NP; Goodman, RL; Karsch, FJ; Parfitt, DB, 1995) | 1.01 |
"Naloxone pretreatment significantly reduced the amphetamine-induced increase in extracellular dopamine in both brain regions and also attenuated the increase in locomotor activity elicited by amphetamine." | ( Naloxone reduces the neurochemical and behavioral effects of amphetamine but not those of cocaine. Holtzman, SG; Justice, JB; Schad, CA, 1995) | 2.46 |
"Naloxone treatment (1 mg/kg per 2 h) was unable to prevent the delay caused by transport (18.0 +/- 1.1 vs 17.5 +/- 1.7 h, n = 8 each), and did not affect the amplitude of the surge (28.4 +/- 5.3 vs 28.1 +/- 2.3 ng/ml, n = 8 each).(ABSTRACT TRUNCATED AT 250 WORDS)" | ( Transport stress delays the oestradiol-induced LH surge by a non-opioidergic mechanism in the early postpartum ewe. Dobson, H; Forhead, AJ; Smart, D; Smith, RF, 1994) | 1.01 |
"Naloxone treatment failed to affect the sexual performance, other than that the post ejaculatory refractory period was increased." | ( Endogenous opioids and sexual motivation and performance during the light phase of the diurnal cycle. van Furth, WR; van Ree, JM, 1994) | 1.01 |
"Naloxone pretreatment significantly augmented the increases in MAP and RSNA induced by icv ET-1." | ( Naloxone augments sympathetic outflow induced by centrally administered endothelin in conscious rabbits. Abe, I; Fujishima, M; Fukuhara, M; Kobayashi, K; Matsumura, K; Tominaga, M; Tsuchihashi, T, 1994) | 2.45 |
"Naloxone treatment increased LH pulse frequency at 4 and 24 weeks of age but not at 12, 18 or 32 weeks of age.(ABSTRACT TRUNCATED AT 250 WORDS)" | ( Opioidergic regulation of gonadotrophin secretion in the early prepubertal bull calf. Currie, WD; Evans, AC; Rawlings, NC, 1993) | 1.01 |
"Naloxone pretreatment (4.0 mg/kg) completely blocked the protective effects of morphine, suggesting the mediation via naloxone-sensitive opiate-receptors; paradoxically, it did not affect the potentiating effects." | ( Immunomodulation by morphine in Plasmodium berghei-infected mice. Dutta, GP; Singh, PP; Singh, S; Srimal, RC, 1994) | 1.01 |
"Naloxone pretreatment significantly decreased the duration of the postseizure akinetic periods in the 1.0- and 10.0-mg/kg groups across all days, suggesting that endogenous opiates are involved in postseizure immobility and that there are interactions between opiate and picrotoxin mechanisms in some seizure-related behaviors." | ( Picrotoxin-induced behavioral tolerance and altered susceptibility to seizures: effects of naloxone. Nores, WL; Pariser, R; Thomas, J, 1993) | 1.23 |
"naloxone (or saline) treatment (4 mg/kg + 2 mg/kg.hr) in the presence or absence of propranolol (1 mg/kg + 1 mg/kg.hr)." | ( Beta-adrenergic-dependent and -independent actions of naloxone on perfusion during endotoxin shock. Dziki, AJ; Law, WR; Lynch, WH; Ramsey, CB, 1993) | 1.26 |
"Naloxone treatment at either 1.1 (Nal-1) or 2.0 (Nal-2) mg/kg BW significantly increased circulating progesterone within 15 min of i.v." | ( Opioids modulate progesterone production in prepubertal Bunaji heifers. Anderson, LL; Gazal, OS, 1995) | 1.01 |
"Naloxone treatment had little effect on VCMs but increased catalepsy scores in both haloperidol and vehicle treated groups." | ( Effects of chronic naloxone administration on vacuous chewing movements and catalepsy in rats treated with long-term haloperidol decanoate. Egan, MF; Ferguson, JN; Hyde, TM, 1995) | 1.34 |
"Naloxone treatment resulted in increased number of 3H-YM-09151-2 binding sites in CTX, HYPO and HIPP." | ( Alteration of D1 and D2 dopaminergic receptor kinetics in specific rat brain regions following repeated administration of opiates. Elwan, MA; Soliman, MR, 1995) | 1.01 |
"Naloxone pretreatment (1 mg kg-1 mL-1 i.v.), however, induced a significant downward shift of the upper limit of the autoregulation, and hypothalamic blood flow started to increase in the 125-145 mmHg arterial pressure range." | ( Endogenous opioid mechanisms in hypothalamic blood flow autoregulation during haemorrhagic hypotension and angiotensin-induced acute hypertension in cats. Dallos, G; Komjáti, K; Nyáry, I; Sándor, P; Tóth, J; Velkei-Harvich, M, 1996) | 1.02 |
"Naloxone treatment significantly reduced the slope of the Patlak plot in receptor-containing regions." | ( Opioid receptor imaging and displacement studies with [6-O-[11C] methyl]buprenorphine in baboon brain. Brodie, J; Dewey, SL; Ferrieri, RA; Fowler, JS; Galynker, I; Gatley, SJ; Holland, MJ; Logan, J; MacGregor, RR; Schlyer, DJ; Simon, E; Wolf, AP, 1996) | 1.02 |
"Naloxone pretreatment produced dose-dependent decreases in heroin self-administration." | ( Smoked heroin self-administration in rhesus monkeys. Carroll, ME; Mattox, AJ, 1996) | 1.02 |
"In naloxone-treated rats, there was a significant decrease in LCMRglu in the locus coeruleus (LC) and an increase in the central nucleus of the amygdala (CAMY), supporting a tonic influence of endogenous opioids on these regions." | ( Naloxone alters the local metabolic rate for glucose in discrete brain regions associated with opiate withdrawal. Kornetsky, C; Kraus, MA; Piper, JM, 1996) | 2.25 |
"Naloxone treatment after application of stressors prevented the elevation of SDLI, whereas naloxone treatment alone did not cause any significant changes." | ( Effects of opioid-type stressors on serum digoxin-like immunoreactivity in rats. Eroglu, L; Uresin, Y; Yildiran, G, 1996) | 1.02 |
"Naloxone treatment showed a significant increase in the frequency of several aggressive actions and the effect was dose dependent." | ( Inhibitory role of opioid peptides in the regulation of aggressive and sexual behaviors in male Japanese quails. Abe, T; Kotegawa, T; Tsutsui, K, 1997) | 1.02 |
"Naloxone pretreatment attenuated serum corticosterone but augmented serum glucose concentrations in ACTH-stimulated broilers." | ( Naloxone attenuates serum corticosterone and augments serum glucose concentrations in broilers stimulated with adrenocorticotropin. Cox, NM; Latour, MA; McDaniel, CD; Peebles, ED; Pond, AL; Thompson, JR, 1997) | 2.46 |
"Naloxone-treated rats (N = 7) receiving sucrose exhibited an analgesia index of 0.20 +/- 0.10 while rats receiving only sucrose (N = 7) had an index of 0.68 +/- 0.11 (t = 0.254, 10 degrees of freedom, P < 0.03)." | ( Sucrose ingestion causes opioid analgesia. Castro-Souza, C; Coimbra, NC; Morato, S; Segato, EN; Segato, FN, 1997) | 1.02 |
"Naloxone treated rats responded at chance levels (53%)." | ( Naloxone impairs spatial performance in rats. Lukaszewska, I, 1997) | 2.46 |
"All naloxone-treated groups exhibited CPA." | ( The effects of naloxone on expression and acquisition of ethanol place conditioning in rats. Bormann, NM; Cunningham, CL, 1997) | 1.13 |
"Naloxone treatment abolished this analgesic effect." | ( Vasoactive intestinal polypeptide induces analgesia and impairs the antinociceptive effect of morphine in mice. Mácsai, M; Szabó, G; Telegdy, G, 1998) | 1.02 |
"Naloxone pretreatment caused specific and selective changes in both the pupillary and cardiovascular responses of CH patients." | ( Combined evaluation of pupillary and cardiovascular responses to cold pressor test in cluster headache patients. Marcheselli, S; Micieli, G; Nappi, G; Osipova, V; Rossi, F; Tassorelli, C, 1998) | 1.02 |
"Naloxone treatment at three days following implantation of pellets containing morphine base increased uptake of tritiated dopamine by the nucleus accumbens but did not alter efflux of tritiated dopamine by the nucleus accumbens or tritiated norepinephrine by the hippocampus. " | ( Presynaptic dopaminergic function in the nucleus accumbens following chronic opiate treatment and precipitated withdrawal. Ghosh, S; Grasing, K, 1999) | 1.75 |
"Naloxone pretreatment enhanced the expression of Fos-IR neurons on the ipsilateral SpVc." | ( Effects of morphine on the distribution of Fos protein in the trigeminal subnucleus caudalis neurons during experimental tooth movement of the rat molar. Aihara, Y; Hanada, K; Maeda, T; Wakisaka, S, 1999) | 1.02 |
"Naloxone pretreatment normalized this sensitized response only at the higher dose (3 mg/kg, i.p.)." | ( Chronic stress sensitizes frontal cortex dopamine release in response to a subsequent novel stressor: reversal by naloxone. Cuadra, G; Lacerra, C; Molina, V; Zurita, A, 1999) | 1.24 |
"In naloxone-treated patients, ST-segment changes and cardiac pain severity during the second inflation were similar to those observed during the first inflation (12+/-6 vs. " | ( Effects of naloxone on myocardial ischemic preconditioning in humans. Chiariello, L; Crea, F; Desideri, G; Ferri, C; Gaspardone, A; Ghini, AS; Gioffré, PA; Tomai, F; Versaci, F, 1999) | 1.31 |
"Naloxone treatment resulted in a strong up-regulation of neostriatal and pallidal mu opioid receptors that was not affected by the concurrent administration of haloperidol." | ( Dopamine-opiate interaction in the regulation of neostriatal and pallidal neuronal activity as assessed by opioid precursor peptides and glutamate decarboxylase messenger RNA expression. Besson, MJ; Mavridis, M, 1999) | 1.02 |
"Naloxone and GnRH treatment both increased (P < 0.05) mean LH concentrations." | ( Correlation between LH response to challenges with GNRH and naloxone during lactation, and LH secretion and follicular development after weaning in the sows. De Rensis, F; Foxcroft, GR, 1999) | 1.27 |
"Naloxone pretreatment (82.5 nmol/rat, 30 min before zinc administration) reverted the water intake to the high levels observed in zinc-free dehydrated animals (7.04 +/- 0.56 ml/100 g body weight)." | ( Zinc and water intake in rats: investigation of adrenergic and opiatergic central mechanisms. Bandeira, IP; Carvalho, FL; Castro, L; De-Castro-e-Silva, E; Ferreira, MG; Fregoneze, JB; Lima, AK; Luz, CP; Macêdo, DF; Maldonado, I; Oliveira, P; Rocha, MA; Souza, F, 1999) | 1.02 |
"Naloxone treatment, in opioid-addicted patients, induced a marked increase in catecholamine plasma concentrations, metabolism, and cardiovascular stimulation during anesthesia with both propofol and methohexital. " | ( Acute detoxification of opioid-addicted patients with naloxone during propofol or methohexital anesthesia: a comparison of withdrawal symptoms, neuroendocrine, metabolic, and cardiovascular patterns. Gastpar, M; Kienbaum, P; Michel, MC; Peters, J; Scherbaum, N; Thürauf, N, 2000) | 2 |
"Naloxone pretreatment overcame the inhibitory effect of morphine and elevated milking-induced cortisol concentrations." | ( Cortisol and ACTH release in dairy cows in response to machine milking after pretreatment with morphine and naloxone. Kraetzl, WD; Schams, D; Tancin, V, 2000) | 1.24 |
"(-)-Naloxone pretreatment suppresses post-ischemic activation and preserves more MAP-2 protein." | ( Cerebral ischemia/reperfusion injury in rat brain: effects of naloxone. Chen, CJ; Chen, WY; Hong, JS; Kuo, JS; Liao, SL, 2001) | 1.03 |
"Naloxone pretreatment did not alter the antinociceptive effect of BV acupoint injection on the abdominal stretch reflex." | ( Visceral antinociception produced by bee venom stimulation of the Zhongwan acupuncture point in mice: role of alpha(2) adrenoceptors. Beitz, AJ; Han, HJ; Kang, MS; Kwon, YB; Lee, JH, 2001) | 1.03 |
"Naloxone pretreatment up-regulated [(3)H]diprenorphine binding and protein expression of the D3.49(164)Q mutant in a time- and dose-dependent manner without affecting its mRNA level." | ( Inverse agonist up-regulates the constitutively active D3.49(164)Q mutant of the rat mu-opioid receptor by stabilizing the structure and blocking constitutive internalization and down-regulation. Chen, C; Huang, P; Li, J; Liu-Chen, LY, 2001) | 1.03 |
"Naloxone pretreatment completely blocked rppOFQ/N(154-181)-induced antinociception in the vlPAG and the amygdala, but not in the LC or RVM." | ( Characterization of rat prepro-orphanin FQ/nociceptin((154-181)): nociceptive processing in supraspinal sites. Abbadie, CA; Allen, RG; Bodnar, RJ; Dustman, J; Jimenez, C; Pasternak, GW; Pellegrino, M; Rossi, GC; Shane, R, 2002) | 1.04 |
"Naloxone pretreatment reduced this inhibition (57.0 % vs 10.3 % for domperidone and induced hyperalgesia by antagonizing the inhibition and enhanced analgesia to the extent of 28.4 % for cisapride)." | ( Opioid mediated anti-nociceptive effect of domperidone and cisapride in mice. Asad, M; Ramaswamy, S; Shashindran, C; Shewade, DG; Topno, I, 2002) | 1.04 |
"Naloxone treatment did not attenuate the exercise-induced H(max)/M(max) percent ratio suppression." | ( Endogenous opioid effects on motoneuron pool excitability: potential analgesic effect of acute exercise. Bulbulian, R, 2002) | 1.04 |
"Naloxone pretreatment (1 mg/kg) partially antagonized the hypothermia and increase in catecholamine synthesis produced by THC." | ( A comparison of some pharmacological actions of morphine and delta9-tetrahydrocannabinol in the mouse. Bloom, AS; Dewey, WL, 1978) | 0.98 |
"Naloxone treatment produced a decrease in locomotor activity and rearing, and an increase in defaecation." | ( Effect of naloxone on the behaviour of rats exposed to a novel environment. Deacon, RM; Rodgers, RJ, 1979) | 1.38 |
"Naloxone treatment rapidly increased mean arterial pressure and pulse pressure in this new shock model." | ( Opiate antagonists: a role in the treatment of hypovolemic shock. Faden, AI; Holaday, JW, 1979) | 0.98 |
"Naloxone pretreatment enhanced freezing only when the animal was given two or three shocks but did not affect freezing when the animal was given only one shock or not shocked at all (Experiments 3, 4, and 5)." | ( Naloxone and shock-elicited freezing in the rat. Bolles, RC; Fanselow, MS, 1979) | 2.42 |
"Naloxone pretreatment (25 mg/kg, i.v.) was also found to block the respiratory depressant effects of CDP in anesthetized cats, but had no effect on the cardiovascular actions of CDP." | ( Effects of picrotoxin, naloxone, and vagotomy on chlordiazepoxide-induced respiratory depression. Billingsley, M; Suria, A; Williams, J, 1979) | 1.29 |
"The naloxone-treated neonates were comparable with the epidural group, although the effects of naloxone were diminishing at 30 minutes." | ( Reversal of narcotic depression in the neonate by nalozone. Evans, JM; Hogg, MI; Rosen, M, 1976) | 0.74 |
"Naloxone (5 mg/kg) pretreatment attenuated by 82% the facilitative effect of heroin on ICSS." | ( Effects of heroin on lever pressing for intracranial self-stimulation, food and water in the rat. Koob, GF; Meyerhoff, JL; Spector, NH, 1975) | 0.98 |
"Naloxone pretreatment had no effect on the PRA response to reduced renal perfusion pressure at any pressure." | ( Effects of an opiate receptor antagonist on renin release in dogs. Cavender, RK; Johnson, MD, 1992) | 1 |
"Naloxone pretreatment (10 mg/kg b.w., ip.) suppressed that increase, Ache activity remaining at the level of non-immobilized, saline treated mice." | ( Effect of naloxone-reversible immobilization stress on the adrenal acetylcholinesterase activity in mice. Konecka, A, ) | 1.26 |
"Naloxone treatment induced an increase of plasma beta-END-LI and cortisol levels in morphine-tolerant animals." | ( Effects of clonidine on pituitary-adrenocortical axis in morphine-tolerant rats and after naloxone-induced withdrawal. Arias, L; Bruger, AJ; Gonzalvez, ML; Martinez, JA; Milanés, MV; Vargas, ML, 1992) | 1.23 |
"Naloxone pretreatment attenuated this decline." | ( Clonidine and yohimbine modulate the effects of naloxone on novelty-induced hypoalgesia. Dawes, P; Rochford, J, 1992) | 1.26 |
"Naloxone treatment (at 27.5 and 18.9 nM) blocked the suppressive effects of CE and lateral amygdaloid stimulation in a dose and time dependent manner." | ( An enkephalinergic mechanism involved in amygdaloid suppression of affective defence behavior elicited from the midbrain periaqueductal gray in the cat. Lu, CL; Shaikh, MB; Siegel, A, 1991) | 1 |
"Naloxone pretreatment partially blocked dexmedetomidine's effect, suggesting a possible endogenous opiate involvement." | ( Alpha 2-adrenoceptors inhibit a nociceptive response in neonatal rat spinal cord. Kendig, JJ; Maze, M; Savola, MK; Woodley, SJ, 1991) | 1 |
"Naloxone pretreatment 30 min prior to hind paw injection partially blocked the initial SPLI increase due to saline or formalin." | ( Time course of the alteration in dorsal horn substance P levels following formalin: blockade by naloxone. Goldstein, BD; McCarson, KE, 1990) | 1.22 |
"Naloxone-treated patients did not show significantly greater recovery." | ( Methylprednisolone or naloxone treatment after acute spinal cord injury: 1-year follow-up data. Results of the second National Acute Spinal Cord Injury Study. Baskin, DS; Bracken, MB; Collins, WF; Eisenberg, HM; Flamm, E; Holford, TR; Leo-Summers, L; Maroon, JC; Marshall, LF; Shepard, MJ, 1992) | 1.32 |
"Naloxone treatment slightly but significantly reduced the level of hypertension attained in the high-salt animals (158 +/- 2 mmHg in naloxone-treated animals vs." | ( Effect of naloxone on hypertension in Dahl salt-sensitive rats. Johnson, MD; Richmond, BK, 1992) | 1.41 |
"Naloxone (10(-5) M) pretreatment of macrophages inhibited only the M-Enk- and 82/205-induced enhanced CSFs elaboration, suggesting an opiate receptors-mediated mechanism of action." | ( Enkephalins-modulation of Plasmodium cynomolgi antigens-induced colony-stimulating factors elaboration by macrophages. Dhawan, BN; Dhawan, VC; Dutta, GP; Haq, W; Mathur, KB; Singh, PP; Singh, S; Srimal, RC, ) | 0.85 |
"Naloxone pretreatment attenuated the increase in the electrochemical signal." | ( Opioid modulation and sensitization of dopamine release elicited by sexually relevant stimuli: a high speed chronoamperometric study in freely behaving rats. Gratton, A; Mitchell, JB, 1991) | 1 |
"With naloxone treatment, dopamine (DA) was significantly increased in the plasma and hypothalamus, but decreased in the cerebral cortex in intact rats; and with castrated rats, there was a tendency to see an increase in plasma DA and significantly increased levels of DA in the thalamus plus mid-brain and hypothalamus." | ( [Effects of ovariectomy on naloxone-modulated hypertension in spontaneously hypertensive rats (SHR)]. Akaike, M; Hirai, M; Kumai, T; Masubuchi, Y; Tanaka, M; Watanabe, M, 1991) | 1.03 |
"Naloxone treatment resulted in greater LH pulse amplitude at 5 and 10 weeks of age (P less than 0.05), lower basal serum concentration of LH at 10 weeks of age (P less than 0.05), greater LH pulse frequency at 25 weeks of age (P less than 0.05), and greater mean serum concentrations of LH, basal LH and LH pulse amplitude at 35 weeks of age (P less than 0.01) than in the controls." | ( Maturational changes in opioidergic control of luteinizing hormone and follicle-stimulating hormone in ram lambs. Churchill, IJ; Currie, WD; Joseph, IB; Rawlings, NC, 1991) | 1 |
"Naloxone treatment did not alter the frequency or magnitude of this relationship, but it did augment the training-induced decrements in evoked neuronal activity at placements that were correlated with bradycardiac response magnitude." | ( Amygdaloid central nucleus neuronal activity accompanying pavlovian cardiac conditioning: effects of naloxone. Gibbs, CM; Hernandez, LL; Powell, DA, 1990) | 1.22 |
"This naloxone treatment disturbed the clear pulsatility of LH secretion observed in the pretreatment control period." | ( Naloxone increases the frequency of the electrical activity of luteinizing hormone-releasing hormone pulse generator in long-term ovariectomized rats. Funabashi, T; Hiruma, H; Kimura, F; Nishihara, M, 1991) | 2.18 |
"Naloxone pretreatment completely blocked the ventilatory depression induced by morphine-6-glucuronide." | ( Antinociceptive and ventilatory effects of the morphine metabolites: morphine-6-glucuronide and morphine-3-glucuronide. Björkman, R; Gong, QL; Hedner, J; Hedner, T; Nordberg, G, 1991) | 1 |
"Naloxone treatment did not increase appreciably carotid chemoreceptor activity or its responses to hypoxia and hypercapnia in either cat group." | ( Endogenous opiates and ventilatory acclimatization to chronic hypoxia in the cat. Lahiri, S; Pokorski, M, 1991) | 1 |
"Naloxone treatment induced an increase in plasma beta-END-LI and cortisol levels in morphine-tolerant animals." | ( Plasma beta-endorphin and cortisol levels in morphine-tolerant rats and in naloxone-induced withdrawal. Antonio Martínez, J; Del Rio Garcia, J; Fuente, T; Milanés, MV; Vargas, ML, 1990) | 1.23 |
"Naloxone pretreatment did not influence airway response to MCh; the mean percent fall in FEV1 was 65.9 +/- 1.3 and 64.7 +/- 1.2% (mean +/- 1 SE) on the placebo day and the naloxone day, respectively." | ( Endogenous opioids modulate the increase in ventilatory output and dyspnea during severe acute bronchoconstriction. Bellofiore, S; Di Maria, GU; Milic-Emili, J; Mistretta, A; Privitera, S; Sapienza, S, 1990) | 1 |
"Naloxone pretreatment exaggerated the pressor response to PE and increased plasma beta-endorphin response to PE infusion but had no effect on baroreflex sensitivity." | ( Comparison of phenylephrine bolus and infusion methods in baroreflex measurements. Liang, CS; Richeson, JF; Sullebarger, JT; Willick, AE; Woolf, PD, 1990) | 1 |
"Naloxone pretreatment (1 mg/kg IP) reversed the effects of beta-casomorphin(1-7) on sleep, a finding which suggests that opiate mu-receptors are involved in mediating the sleep effects of beta-casomorphin." | ( Effect of beta-casomorphin on neonatal sleep in rats. Aalto, J; Hilakivi, I; Hilakivi, LA; Taira, T, ) | 0.85 |
"Naloxone pretreatment did not reverse the effects of hBE on gonadotropin release." | ( The effect of opioid peptides on ovine pituitary gonadotropin secretion in vitro. Matteri, RL; Moberg, GP, ) | 0.85 |
"Naloxone treatment diminished immunoreactive cytoplasmic vasopressin in males more effectively than in females." | ( Sex-specific effects of met-enkephalin treatment on vasopressin immunoreactivity in the rat supraoptic nucleus. Blanco, E; Carretero, J; Riesco, JM; Sànchez, F; Vàzquez, R, ) | 0.85 |
"Naloxone pretreatment was able to antagonize completely the opioid-produced inhibition of capsaicin-evoked SP-LI release." | ( Opioid modulation of capsaicin-evoked release of substance P from rat spinal cord in vivo. Aimone, LD; Yaksh, TL, ) | 0.85 |
"Naloxone pretreatment (50 micrograms/kg) during conditioning prevented the acquisition of heroin-induced CPP, but when given only on the test day, naloxone (50 or 1000 micrograms/kg) did not prevent the expression of heroin CPP." | ( Differential mechanisms in the acquisition and expression of heroin-induced place preference. Hand, TH; Le Moal, M; Stinus, L, 1989) | 1 |
"Naloxone pretreatment inhibited CRH-induced PRL release in a dose-dependent fashion, whereas nalmefene did not, in both normal and ovariectomized monkeys." | ( Naloxone antagonism of corticotropin-releasing hormone stimulation of prolactin secretion in rhesus monkeys. Reid, RL; Vanvugt, DA; Webb, MY, 1989) | 2.44 |
"Naloxone pretreatment (0.3 mg/kg, s.c.) completely attenuated the DYN-induced stimulation of water intake." | ( Dynorphin A (1-13), microinjected into the preoptic area, stimulates water intake in rats. Kobayashi, I; Kobayashi, S; Negishi, M; Shimizu, H; Shimomura, Y, 1989) | 1 |
"Naloxone pretreatment did not alter ketamine's influence on evoked potential amplitudes." | ( Effects of ketamine, naloxone, and physostigmine on flash evoked potentials in rat superior colliculus. Hetzler, BE; Melk, AM, 1989) | 1.32 |
"Naloxone treatment (hourly iv injections of 1 mg/kg BW for 4 h) produced an increase in the frequency of episodic LH secretion at all prepubertal ages, when lambs were highly sensitive to the estradiol negative feedback." | ( Endogenous opioid regulation of pulsatile luteinizing hormone secretion during sexual maturation in the female sheep. Ebling, FJ; Foster, DL; Schwartz, ML, 1989) | 1 |
"Naloxone pretreatment completely antagonized the behavioral stupor and associated EEG slow-wave bursts." | ( Dissociation of naloxone-sensitive and naloxone-insensitive effects of U-50,488H. Young, GA, 1989) | 1.34 |
"Naloxone pretreatment (1 mg/kg, IP) did not antagonize the effect of captopril on food intake indicating that the anorexic action of captopril was not due to alterations in opiate peptide levels." | ( Feeding and drinking behaviour following angiotensin converting enzyme blockade: role of injectant pH. Di Nicolantonio, R; Weisinger, RS, 1988) | 1 |
"Naloxone pretreatment diminished regional blood flow responses to DAGO." | ( [Effect of opioid peptides on regional hemodynamics in waking rats]. Martynova, EA; Medvedev, OS, 1988) | 1 |
"Naloxone-pretreatment also blocked the analeptic and cholinergic activating properties of ACTH1-24." | ( Intraseptal microinjection of adrenocorticotropic hormone1-24 antagonizes pentobarbital-induced narcosis and depression of hippocampal cholinergic activity. Carino, MA; Horita, A, 1988) | 1 |
"Naloxone treatment prevented the development of shock into a progressive stage by several eventual mechanisms: An antagonism of opiate receptors." | ( Hormone changes and beta-endorphin in the pathogenesis of hemorrhagic shock. Machuganska, A; Zaharieva, S, 1985) | 0.99 |
"Naloxone pretreatment and hypophysectomy abolished the caerulein effect, while intracerebroventricular or intra-nucleus accumbens injection of beta-endorphin together with haloperidol administration produced an effect similar to that of caerulein." | ( beta-Endorphin involvement in the antidopaminergic effect of caerulein. Matsubara, K; Matsushita, A, 1986) | 0.99 |
"Naloxone treatment induced a decrease in the beta-endorphin-like immunoreactivity content in the hypothalamus, but had no effect on the beta-endorphin-like immunoreactivity content in the anterior lobe and NIL of the pituitary gland in situ or in the NIL transplant." | ( Neurointermediate lobe transplanted under the kidney capsule modifies the activity of the neurointermediate lobe in situ, but does not respond to opiate treatment. Gianoulakis, C; Gupta, A, 1986) | 0.99 |
"When naloxone-pretreated and control rats were infused with saline (8 ml) the IR-ANF response was the same in the two groups: 257.7 +/- 64 and 247 +/- 52 pg/ml respectively." | ( The morphine effect on plasma ANF. Cantin, M; Garcia, R; Genest, J; Gutkowska, J; Kuchel, O; Racz, K; Thibault, G, 1986) | 0.73 |
"The naloxone-treated young, obese and non-obese SHR (controls) exhibited marked reduction of the weight of their pituitary and adrenal glands, whereas the pituitary and adrenal glands of naloxone-treated mature, obese and non-obese/SHR were greatly increased in weight." | ( Anti-opiate (naloxone) suppression of Cushingoid degenerative changes in obese/SHR. McMurtry, JP; Wexler, BC, 1985) | 1.12 |
"Naloxone treatment had no measurable effect on glucose concentration, turnover, and norepinephrine levels, but stimulated plasma epinephrine, glucagon, and cortisol and inhibited insulin release." | ( Effect of opiate-receptor blockade on normoglycemic and hypoglycemic glucoregulation. Brubaker, PL; Cook, E; el-Tayeb, KM; Lickley, HL; Vranic, M, 1986) | 0.99 |
"Naloxone pretreatment significantly attenuated the antinociceptive effect of cold-restraint stress, suggesting a partial mediation by opioid mechanisms." | ( Methylnalorphinium fails to reverse naloxone-sensitive stress-induced analgesia in mice. Rae, GA; Souza, RL; Takahashi, RN, 1986) | 1.27 |
"Naloxone treatment resulted in significantly impaired delayed response performance when compared to control." | ( The effect of MSH/ACTH 4-10 on delayed response performance and post-test locomotor activity in rats. Miller, LH; Turnbull, BA, ) | 0.85 |
"In naloxone-pretreated arthritic rats, the paradoxical analgesic effect of low doses of naloxone was almost abolished, and the potent analgesic effects of low doses of morphine were also strongly and dose-dependently reduced." | ( Cross-tolerance between analgesic low doses of morphine and naloxone in arthritic rats. Guilbaud, G; Kayser, V, 1987) | 1.03 |
"Naloxone pretreatment, in contrast, induced prehemorrhagic activation of KKS, which was potentiated by subsequent hemorrhage." | ( Effect of intravenous enkephalin administration on kallikrein-kinin system in experimental hemorrhagic shock. Evidence for activation of kallikrein-kinin system by naloxone. Grässler, J; Kühne, H; Scheuch, DW; Slepuschkin, VD; Zoloev, GK, 1988) | 1.19 |
"Naloxone treatment and sampling continued for an additional 8 hr." | ( Effects of progesterone and weaning on LH and FSH responses to naloxone in postpartum beef cows. Cross, JC; Manns, JG; Rutter, LM, 1987) | 1.23 |
"Naloxone treatment improved blood pressure significantly during endotoxin shock, as would be expected with the observed increase in total peripheral vascular resistance and no significant change in cardiac output." | ( Naloxone alters organ perfusion during endotoxin shock in conscious rats. Ferguson, JL; Law, WR, 1988) | 2.44 |
"naloxone treatment: 23.7 +/- 4.2; p = 0.034 by Student's paired t test, n = 6)." | ( Naloxone, ethanol, and the chlorpropamide alcohol flush. Baraniuk, JN; Mabbee, WG; Murray, RB, 1987) | 2.44 |
"Naloxone pretreatment with 2 mg/kg, but not 1 mg/kg s.c., potentiated a hyperglycemic response to i.t." | ( Differential effects of subcutaneous and intrathecal morphine administration on blood glucose in mice: comparison with intracerebroventricular administration. Brase, DA; Dewey, WL; Lux, F, 1988) | 1 |
"Both naloxone-treated and control groups were similarly normotensive at 24 hr postoperation, the MAP being significantly lower than in the sham-operated groups, which regained previously hypertensive levels." | ( Failure of naloxone to influence surgical reversal of two-kidney, one-clip hypertension in the rat. Bing, RF; Edmunds, ME; Russell, GI; Swales, JD; Thurston, H, 1987) | 1.12 |
"The naloxone-treated cats received intrathecal (2 mg in 0.5 ml) as well as systemic (2-mg/kg bolus, 2 mg/kg/hour for 4 hours) doses of naloxone." | ( Effect of naloxone in experimental acute spinal cord injury. Chehrazi, B; Haghighi, SS, 1987) | 1.16 |
"Naloxone (2 mg/kg) treatment caused significant increases in the levels of HVA in hypothalamus and striatum and lithium cotreatment prevented the effect of naloxone." | ( Naloxone and lithium interaction on the levels of homovanillic acid in the rat brain. Eroğlu, L; Genç, E; Hizal, A, ) | 2.3 |
"Naloxone treatment failed to increase serum LH concentrations in these cows." | ( Influence of calf removal on the serum luteinizing hormone response to naloxone in the postpartum beef cow. Barb, CR; Kiser, TE; Thompson, FN; Whisnant, CS, 1986) | 1.23 |
"Naloxone treatment (1 mg/kg; i.m.) given immediately after the delivery of the first fetus reversed the inhibitory effect of relaxin and the interval between successive deliveries was slightly faster than that of controls." | ( Relaxin acts centrally to inhibit oxytocin release during parturition: an effect that is reversed by naloxone. Jones, SA; Summerlee, AJ, 1986) | 1.21 |
"Naloxone treatment of endotoxin shock has been shown to alter many cardiovascular parameters. " | ( Respiratory compensation and acidosis in endotoxin shock: effects of naloxone in conscious rats. Ferguson, JL; Law, WR, 1987) | 1.95 |
"Naloxone treated males were more likely to display behavioral signs of satiety during the first ten minutes of these tests." | ( Opiate antagonists and copulatory behavior of male hamsters. Noble, RG; Wu, FM, 1986) | 0.99 |
"Naloxone treatment failed to alter serum LH concentrations in EF, LF, or OVX gilts and PRL concentrations in OVX gilts.(ABSTRACT TRUNCATED AT 250 WORDS)" | ( Influence of stage of the estrous cycle on endogenous opioid modulation of luteinizing hormone, prolactin, and cortisol secretion in the gilt. Barb, CR; Kraeling, RR; Rampacek, GB; Whisnant, CS, 1986) | 0.99 |
"Naloxone at 1 mg/kg, a treatment providing no therapeutic benefit, has no protective effect on ascorbate." | ( Ascorbic acid: a putative biochemical marker of irreversible neurologic functional loss following spinal cord injury. DeCrescito, V; Demopoulos, HB; Flamm, ES; Pietronigro, DD; Tomasula, JJ, 1985) | 0.99 |
"Naloxone treatment failed to induce LH or PRL release." | ( Opioid peptides in pseudocyesis. Buhi, WC; Devane, GW; Kalra, PS; Vera, MI, 1985) | 0.99 |
"Naloxone treatment significantly shortened the duration of pseudopregnancy but did not prevent it, indicating that only minimal levels of PRL may be necessary to initiate and maintain pseudopregnancy." | ( Endogenous opioid peptides participate in the modulation of prolactin release in response to cervicovaginal stimulation in the female rat. Audsley, AR; Sirinathsinghji, DJ, 1985) | 0.99 |
"Naloxone pretreatment significantly enhanced the plasma adrenaline response to the cold stimulus by 98% (P less than 0.01) with concomitant changes in peak systolic blood pressure (peak increment 31 +/- 6 mmHg) and pulse rate (12.5 +/- 3.5 beats/min) responses (both P less than 0.05)." | ( Enhancement of the sympathoadrenal response to the cold-pressor test by naloxone in man. Al-Damluji, S; Bailey, T; Besser, M; Bouloux, PM; Grossman, A, 1985) | 1.22 |
"Naloxone treatment of mice did not affect the sensitivity of the isolated vas deferens to noradrenaline, carbachol or potassium chloride." | ( Effects of chronic drug treatment on the sensitivity of mouse vas deferens to drugs. McCulloch, CR; Pollock, D, 1985) | 0.99 |
"Pre-treatment with naloxone (1 mg/kg) prevented fentanyl-induced VCC, but naloxone (1 and 2 mg/kg) was unable to reverse VCC when administered after fentanyl." | ( Fentanyl causes naloxone-resistant vocal cord closure: A platform for testing opioid overdose treatments. Janowsky, A; Miner, NB; Schutzer, WE; Torralva, R; Zarnegarnia, Y, 2021) | 1.29 |
"Pretreatment with naloxone, an opioid receptor antagonist, blocked sustained-release buprenorphine analgesic action." | ( Sustained-release buprenorphine induces acute opioid tolerance in the mouse. Fairbanks, CA; Kitto, KF; Larson, CM; Peterson, CD; Wilcox, GL, 2020) | 0.88 |
"Treatment with naloxone (0.5nmol/eye) almost completely negated the protective effects of capsaicin, CGRP, β-endorphin, and substance P in the NMDA-injected rats." | ( Opioid receptor activation is involved in neuroprotection induced by TRPV1 channel activation against excitotoxicity in the rat retina. Ishii, K; Ito, H; Kuroki, T; Mori, A; Nakahara, T; Sagawa, T; Sakamoto, K, 2017) | 0.79 |
"Pretreatment with naloxone blunted the responses to morphine whereas pretreatment with naltrindole or d-penicillamine did not." | ( Co-activation of μ- and δ-opioid receptors elicits tolerance to morphine-induced ventilatory depression via generation of peroxynitrite. Discala, JF; Gruber, RB; Lewis, SJ; May, WJ; McLaughlin, D; Palmer, LA; Young, AP, 2013) | 0.71 |
"treatment with naloxone methiodide potently induced jumping behavior and trembling in morphine-dependent mice." | ( Involvement of supraspinal and peripheral naloxonazine-insensitive opioid receptor sites in the expression of μ-opioid receptor agonist-induced physical dependence. Aoki, S; Inoue, K; Itoh, T; Komiya, S; Mori, T; Shibasaki, M; Suzuki, T; Uzawa, N, 2013) | 0.73 |
"pretreatment with naloxone (5 µg) reversed the decreased acetic acid-induced writhing response." | ( Antinociceptive profiles and mechanisms of orally administered coumarin in mice. Kang, YJ; Kim, CH; Kim, SJ; Kim, SS; Lim, SM; Park, SH; Sim, YB; Suh, HW, 2013) | 0.71 |
"The treatment with naloxone also induced a significant increase in myeloperoxidase levels, osteoclast number and cytokines in periodontal tissues of rats with ligature-induced PD." | ( Endogenous opioids regulate alveolar bone loss in a periodontal disease model. Albergaria, JD; Maltos, KL; Pacheco, CM; Pacheco, DF; Queiroz-Junior, CM; Silva, TA, 2013) | 0.71 |
"Pre-treatment with naloxone significantly increased the gallic acid derivative-induced suppression of novelty-induced grooming." | ( Effect of fractionated extracts and isolated pure compounds of Spondias mombin (L. Anacardiaceae) leaves on novelty-induced rearing and grooming behaviours in mice. Akomolafe, RO; Aladesanmi, JA; Ayoka, AO; Bamitale, SK; Owolabi, RA; Ukponmwan, EO, 2013) | 0.71 |
"Pretreatment with naloxone (1mg/kg) significantly reduced anti-allodynic effect of chronic curcumin in von Frey filament test." | ( Effect of curcumin on diabetic peripheral neuropathic pain: possible involvement of opioid system. Banafshe, HR; Hamidi, GA; Mirhashemi, SM; Mokhtari, R; Noureddini, M; Shoferpour, M, 2014) | 0.73 |
"Pretreatment with naloxone methiodide, a peripherally acting opioid receptor antagonists, also significantly antagonized the antinociceptive effects of BEO and linalool." | ( Effect of plantar subcutaneous administration of bergamot essential oil and linalool on formalin-induced nociceptive behavior in mice. Bagetta, G; Kamio, S; Katsuyama, S; Kishikawa, Y; Komatsu, T; Nakamura, H; Otowa, A; Sakurada, T; Sato, K; Yagi, T, 2015) | 0.74 |
"Pretreatment with naloxone and bicuculline significantly attenuated the reduction of abdominal constrictions produced by all the tested trimethoxy flavones indicating a definite role of opioid and GABAergic mechanisms in the anti-nociceptive effect of trimethoxy flavones." | ( Anti-nociceptive activity of a few structurally related trimethoxy flavones and possible mechanisms involved. Cheriyan, BV; Kadhirvelu, P; Nadipelly, J; Sayeli, V; Shanmugasundaram, J; Subramanian, V, 2016) | 0.76 |
"Pre-treatment with naloxone (1.5 mg/kg, i.p.) did not reverse the antinociceptive activity of the extract at the dose of 100 mg/kg in the first phase of this test." | ( Orofacial antinociceptive effect of the ethanolic extract of Annona vepretorum Mart. (Annonaceae). Almeida, JR; Bonjardim, LR; Lavor, ÉM; Lima-Saraiva, SR; Macedo, LA; Mendes, RL; Oliveira-Junior, RG; Quintans-Júnior, LJ; Silva, JC; Silva, MG; Souza, GR; Souza, MT, ) | 0.45 |
"Pretreatment with naloxone significantly increased the number of capsaicin-induced pERK-LI cells in adult rats but not in aged rats." | ( Attenuation of naloxone-induced Vc pERK hyper-expression following capsaicin stimulation of the face in aged rat. Hasegawa, M; Honda, K; Iwata, K; Kanda, K; Kitagawa, J; Kondo, M; Noma, N; Okamoto, R; Saito, K; Suzuki, I; Tsuboi, Y, 2008) | 1.02 |
"Pre-treatment with naloxone did not modify the antinociceptive effect of Eta, but co-administration with atropine completely prevented it." | ( Antinociceptive activity of Mirabilis jalapa in mice. Ferreira, J; Franciscato, C; Manfron, MP; Pereira, ME; Rossato, MF; Trevisan, G; Walker, CI, 2008) | 0.66 |
"Pretreatment with naloxone 1 mg/kg significantly reduced behavioral seizure scores and the up-regulation of BDNF mRNA expression elicited by i.c.v." | ( Seizure activity involved in the up-regulation of BDNF mRNA expression by activation of central mu opioid receptors. Ko, MC; Zhang, HN, 2009) | 0.68 |
"Pretreatment with naloxone reversed both the functional and structural retinal protection induced by IPC." | ( Opioid receptor-activation: retina protected from ischemic injury. Crosson, CE; Husain, S; Potter, DE, 2009) | 0.68 |
"treatment with naloxone (1 mg/kg) or D-arginine (40 mg/kg)." | ( Mechanisms involved in the antinociception caused by ethanolic extract obtained from the leaves of Melissa officinalis (lemon balm) in mice. Calixto, JB; Chaves, J; Ferreira, VM; Guginski, G; Luiz, AP; Martins, DF; Massaro, M; Mattos, RW; Santos, AR; Silva, MD; Silveira, D, 2009) | 0.69 |
"Pretreatment with naloxone completely prevented the analgesic effects of these drugs in tail-flick and hot plate tests for both juvenile and adult rats." | ( Non-opioid tolerance in juvenile and adult rats. Tsagareli, MG; Tsiklauri, N; Viatchenko-Karpinski, V; Voitenko, N, 2010) | 0.68 |
"Pretreatment with naloxone (5 mg/kg) significantly decreased the latency of discomfort produced by the 100 mg/kg dose of MEZZ in the hot plate test." | ( Antiinflammatory and antinociceptive activities of Zingiber zerumbet methanol extract in experimental model systems. Chear, CT; Israf, DA; Mohamad, AS; Sulaiman, MR; Wong, YY; Zakaria, ZA, 2010) | 0.68 |
"Pretreatment with naloxone significantly increased NO production and iNOS expression in morphine-treated rats after IR (p<0.01 vs morphine dependence+IR)." | ( Nitric oxide and renal protection in morphine-dependent rats. Ajami, M; Babakoohi, S; Ebrahimi, SA; Habibey, R; Hesami, A; Pazoki-Toroudi, H, 2010) | 0.68 |
"Pretreatment with naloxone (0.5 or 2.5 mg/kg) did not block the analgesic effect of CTX." | ( Involvement of cholinergic system in suppression of formalin-induced inflammatory pain by cobratoxin. Feng, YL; Lin, HM; Liu, YL; Qin, ZH; Reid, PF; Shi, GN; Yang, SL, 2011) | 0.69 |
"Pretreatment with naloxone injected intra-DPAG antagonized both the panicolytic effect of chronic fluoxetine as well as that of 5-HT injected intra-DPAG." | ( The panicolytic-like effect of fluoxetine in the elevated T-maze is mediated by serotonin-induced activation of endogenous opioids in the dorsal periaqueductal grey. Audi, EA; Biesdorf, C; Graeff, FG; Roncon, CM; Santana, RG; Zangrossi, H, 2012) | 0.7 |
"Treatment with naloxone (an opioid antagonist) greatly enhanced the oxytocin response to IL-1β in pregnancy, and finasteride did not enhance this effect, indicating that allopregnanolone and the endogenous opioid mechanisms do not act independently." | ( Allopregnanolone and induction of endogenous opioid inhibition of oxytocin responses to immune stress in pregnant rats. Bales, J; Brunton, PJ; Russell, JA, 2012) | 0.72 |
"Pretreatment with naloxone attenuated the sensitivity to selank in BALB/C mice whereas the response to anxiolytic effects of peptide was increased in C57BL/6 mice." | ( [The role of opioid system in peculiarities of anti-anxiety effect of peptide anxiolytic selank]. Andreeva, LA; Kolik, LG; Kozlovskaia, MM; Kozlovskiĭ, II; Nadorova, AV, 2012) | 0.7 |
"Pretreatment with naloxone hydrochloride, an opioid receptor antagonist, or naloxone methiodide, a peripherally acting µ-opioid receptor-preferring antagonist, significantly reversed linalool-induced antiallodynia and antihyperalgesia." | ( Intraplantar injection of linalool reduces paclitaxel-induced acute pain in mice. Katsuyama, S; Kishikawa, Y; Komatsu, T; Kuwahata, H; Nakamura, H; Sakurada, T; Yagi, T, 2012) | 0.7 |
"Pretreatment with naloxone, an opioid receptor antagonist, and β-funaltrexamine, a selective μ-opioid receptor antagonist, reversed the antinociceptive effect of BCP." | ( Involvement of peripheral cannabinoid and opioid receptors in β-caryophyllene-induced antinociception. Bagetta, G; Katsuyama, S; Komatsu, T; Kuwahata, H; Mizoguchi, H; Nagaoka, K; Nakamura, H; Sakurada, S; Sakurada, T, 2013) | 0.71 |
"Treatment with naloxone, L-arginine and glibenclamide reversed the effect of LPEF in glutamate test." | ( Antinociceptive effect of Lecythis pisonis Camb. (Lecythidaceae) in models of acute pain in mice. Almeida, FR; Brandão, MS; Chaves, MH; Ferreira, EL; Lima, DF; Oliveira, JP; Pereira, SS, 2013) | 0.73 |
"Pretreatment with naloxone blocked morphine's effects." | ( Morphine administration selectively facilitates social play in common marmosets. Guard, HJ; Newman, JD; Roberts, RL, 2002) | 0.64 |
"Treatment with naloxone did not exert any effect on immobilization-blocked LH surge but increased basal LH release during immobilization stress." | ( Influence of GnRH agonist and neural antagonists on stress-blockade of LH and prolactin surges induced by 17beta-estradiol in ovariectomized rats. Cheon, MS; Kam, KY; Kang, SS; Kim, K; Park, YB; Ryu, K, 2002) | 0.65 |
"Pretreatment with naloxone significantly attenuated the protective effects of MPC (53.8+/-4, P<0.0002)." | ( Cardioprotection at a distance: mesenteric artery occlusion protects the myocardium via an opioid sensitive mechanism. Gross, GJ; Hsu, AK; Moore, J; Patel, HH, 2002) | 0.64 |
"Treatment with naloxone increases cell proliferation in the dentate gyrus in all groups, although this increase is statistically insignificant." | ( Treadmill running and swimming increase cell proliferation in the hippocampal dentate gyrus of rats. Jang, MH; Kim, CJ; Kim, EH; Kim, H; Kim, KM; Kim, SS; Lee, TH; Lim, BV; Ra, SM; Shin, MC, 2002) | 0.65 |
"Treatment with naloxone [1.5 mg/rat, sc injection], a nonselective opioid receptor antagonist, significantly reversed the inhibitory effects of TIP39 on AVP release." | ( Centrally administered tuberoinfundibular peptide of 39 residues inhibits arginine vasopressin release in conscious rats. Arima, H; Ishizaki, S; Miura, Y; Murase, T; Oiso, Y; Sugimura, Y; Tachikawa, K; Usdin, TB, 2003) | 0.66 |
"The treatment with naloxone was less effective in the homozygous (-/-) mice, because the high dose of naloxone (10 mg/kg) tended to shift the preference." | ( Distinct changes in the behavioural effects of morphine and naloxone in CCK2 receptor-deficient mice. Abramov, U; Bourin, M; Kõks, S; Kurrikoff, K; Luuk, H; Matsui, T; Raud, S; Rünkorg, K; Vasar, E; Veraksits, A, 2003) | 0.88 |
"Pretreatment with naloxone decreased interleukin-1beta serum levels near to those of control group." | ( Involvement of interleukin-1beta in systemic morphine effects on paw oedema in a mouse model of acute inflammation. Ahmadiani, A; Alebouyeh, M; Pourpak, Z, 2004) | 0.65 |
"Pretreatment with naloxone 20 min prior to NMDA injection abolished the inhibition of number of scratches and the duration of scratching produced by the intracisternal injection of NMDA in the late phase." | ( Intracisternal NMDA produces analgesia in the orofacial formalin test of freely moving rats. Ahn, DK; Bae, YC; Choi, HS; Ju, JS; Jung, CY; Kim, SK; Lee, HJ, 2004) | 0.65 |
"Pretreatment with naloxone had no significant effect on infarct size in nonpreconditioned hearts (80+/-6%) and did not inhibit the protective effects of apnea-induced PC (52+/-10% in naloxone+PC group)." | ( Brief apnea induces myocardial ischemic tolerance by an opioid-insensitive mechanism. Blehar, DJ; Darling, CE; Dickson, EW; Hirsch, DJ; Przyklenk, K; Whittaker, P, ) | 0.45 |
"Pretreatment with naloxone did not prevent the morphine effect." | ( Ultra low concentrations of morphine increase neurite outgrowth in cultured rat spinal cord and cerebral cortical neurons. Brailoiu, E; Brailoiu, GC; Chi, M; Dun, NJ; Godbolde, R; Hoard, J, 2004) | 0.65 |
"Pretreatment with naloxone partially reversed the antinociceptive effect of tramadol per se and its combination with naproxen without modifying the per se effect of NSAID." | ( Isobolographic analysis of interaction between cyclooxygenase inhibitors and tramadol in acetic acid-induced writhing in mice. Jain, NK; Kulkarni, SK; Satyanarayana, PS; Singh, A, 2004) | 0.65 |
"Pretreatment with naloxone (5 nmol), but not NOR-AN, blocked cardiovascular responses elicited by EM-1." | ( Cardiovascular responses to microinjection of nociceptin and endomorphin-1 into the nucleus tractus solitarii in conscious rats. Mao, L; Wang, JQ, 2005) | 0.65 |
"Pre-treatment with naloxone methiodide decreased (15%) IL-1beta-induced Fos-immunoreactivity (Fos-IR) in medial parvocellular paraventricular nucleus (mPVN) corticotropin-releasing hormone (CRH) neurons but increased responses in the ventrolateral medulla (VLM) C1 (65%) and nucleus tractus solitarius (NTS) A2 (110%) catecholamine cell groups and area postrema (136%)." | ( Dissection of peripheral and central endogenous opioid modulation of systemic interleukin-1beta responses using c-fos expression in the rat brain. Buller, KM; Hamlin, AS; Osborne, PB, 2005) | 0.65 |
"Pretreatment with naloxone (0.3, 1.0, and 3.0 mg/kg body mass), 10 min before ASH administration, failed to block the extract antinociception." | ( Effect of various antagonists on the Channa striatus fillet extract antinociception in mice. Mat Jais, AM; Somchit, MN; Sulaiman, MR; Zakaria, ZA, 2005) | 0.65 |
"Pre-treatment with naloxone (10 mg/kg), a general opioid receptor antagonist, for 5 min, followed by COAE, was found to completely block its peripheral, but not central, antinociceptive activity." | ( The influences of temperature and naloxone on the antinociceptive activity of Corchorus olitorius L. in mice. Fatimah, CA; Mat Jais, AM; Safarul, M; Somchit, MN; Sulaiman, MR; Valsala, R; Zakaria, ZA, 2005) | 0.93 |
"Pre-treatment with naloxone totally prevented morphine-induced decrease in IOP and miosis." | ( Possible involvement of nitric oxide in morphine-induced miosis and reduction of intraocular pressure in rabbits. Bonfiglio, V; Bucolo, C; Camillieri, G; Drago, F, 2006) | 0.65 |
"Pretreatment with naloxone (1.0 mg/kg, i.p.) prevented serotonin-induced plasma glucose lowering effect in STZ-diabetic rats." | ( Serotonin enhances beta-endorphin secretion to lower plasma glucose in streptozotocin-induced diabetic rats. Chen, WP; Cheng, JT; Chi, TC; Chi, TL; Ho, YJ; Lee, SS; Su, MJ, 2007) | 0.66 |
"Pretreatment with naloxone significantly increased the cortisol response to NS (p<0.01) and to CB (p<0.01), but had no effects on ACTH-induced cortisol release." | ( Beta-adrenergic and opioidergic modulation of cortisol secretion in response to acute stress. Parvizi, N; Phogat, JB, 2007) | 0.66 |
"Pretreatment with naloxone (0.8 mg/kg, ip) can only partially antagonize its antitussive effect." | ( Synthesis and antitussive evaluation of verticinone-cholic acid salt, a novel and potential cough therapeutic agent. Chen, C; Pi, HF; Ruan, HL; Wu, JZ; Xu, FZ; Zhang, P; Zhang, YH, 2007) | 0.66 |
"Treatment with naloxone (0.5 mg/kg-2.0 mg/kg) alone produced marked increases in androgen levels." | ( The role of endogenous opioid peptides in the control of androgen levels in the male nonhuman primate. Almirez, RG; Gilbeau, PM; Holaday, JW; Smith, CG, ) | 0.47 |
"Pretreatment with naloxone (75 micrograms/100 g BW, iv) failed to affect the portal IRS release induced by bombesin (2 micrograms/rat), indicating that the opiate receptor is not likely to be involved in this reaction." | ( Stimulation by bombesin of immunoreactive somatostatin release into rat hypophysial portal blood. Abe, H; Chiba, T; Chihara, K; Fujita, T; Iwasaki, J; Matsukura, S; Minamitani, N, 1981) | 0.59 |
"Pretreatment with naloxone (20 min, 0.5 or 1 mg kg-1 s.c.) lowered buprenorphine binding in intestine and cns." | ( The peripheral narcotic antagonist N-allyl levallorphan-bromide (CM 32191) selectively prevents morphine antipropulsive action and buprenorphine in-vivo binding in the rat intestine. Bianchi, G; Fiocchi, R; Manara, L; Peracchia, F; Petrillo, P; Tavani, A, 1984) | 0.59 |
"Pretreatment with naloxone (1-10 mg kg-1 s.c.) antagonized the corticosterone increase." | ( Elevation of serum corticosterone in rats by bremazocine, a kappa-opioid agonist. Fuller, RW; Leander, JD, 1984) | 0.59 |
"Pretreatment with naloxone (4 mg/kg, 30 min before SP) suppresses the hypothermic effect." | ( [On the role of substance P in thermoregulation of normotensive and spontaneously hypertensive rats (author's transl)]. Bienert, M; Marten, FT; Oehme, P; Richter, R, 1982) | 0.59 |
"Pretreatment with naloxone did not affect the responses of GH, PRL, or cortisol to hypoglycemia or the PRL response to L-dopa." | ( Lack of modulation of pituitary hormone stress response by neural pathways involving opiate receptors. Molitch, ME; Spiler, IJ, 1980) | 0.58 |
"pretreatment with naloxone, an opiate antagonist." | ( Influence of thyrotropin releasing hormone and histidyl-proline diketopiperazine on spontaneous locomotor activity and analgesia induced by delta 9-tetrahydrocannabinol in the mouse. Bhargava, HN; Matwyshyn, GA, 1980) | 0.58 |
"Pretreatment with naloxone, a pure opioid antagonist, abolished the analgesic effect of CRL." | ( Effect of ceruletide on rest pain in patients with arterial insufficiency of the lower extremity. Bagarani, M; Basso, N; Desantis, C; Dintinosante, V; Fiocca, F; Gizzonio, D; Pona, V; Ponzielli, F, 1982) | 0.59 |
"Pretreatment with naloxone prevented the effects of EDS." | ( [Analysis of the effect of increasing electrodermal stimulation on the somatovegetative reactions evoked by stimulation of the ventromedial hypothalamus]. Burchuladze, RA, 1983) | 0.59 |
"Pretreatment with naloxone or beta-funaltrexamine (beta-FNA) antagonized this effect." | ( ICI 154,129, a delta-opioid receptor antagonist raises seizure threshold in rats. Cowan, A; Holaday, JW; Robles, LE; Tortella, FC, 1984) | 0.59 |
"Pretreatment with naloxone (10(-4) M) prevented the increase in water transport due to morphine, a mu-agonist, whereas a higher concentration of naloxone (10(-3) M) was required to inhibit the increase due to D-Ala-methionine-enkephalinamide, a delta-receptor agonist." | ( Role of enkephalins in regulation of basal intestinal water and ion absorption in the rat. Fogel, R; Kaplan, RB, 1984) | 0.59 |
"Rats treated with naloxone throughout both the development of ethanol dependence and during ethanol-withdrawal showed delayed or reduced withdrawal symptomatology compared to rats injected with only saline, naloxone only during the development of dependence and naloxone only during ethanol withdrawal." | ( Effects of naloxone on ethanol dependence in rats. Berman, RF; Goldman, MS; Lee, JA; Olson, KL, 1984) | 0.98 |
"Treatment with naloxone (3 mg/kg bolus and 2 mg/kg/hr infusion for 2.5 hours), a specific opiate antagonist, during septic shock attenuated the hypotension (p less than 0.002) and systemic acidosis (p less than 0.02) without altering cardiac index or total peripheral resistance." | ( Hemodynamic response to naloxone during live Escherichia coli sepsis in splenectomized dogs. Bowen, JC; Rees, M, 1984) | 0.91 |
"Treatment with naloxone administered 30 min before the DER infusion with a bolus dose of 4 mg, followed by a constant infusion of 1 microgram/Kg/min for 150 min, prevented the rise in serum TSH." | ( Dermorphin, a new opioid peptide, stimulates thyrotropin secretion in normal subjects. Bianconi, M; Degli Uberti, E; Emanuele, R; Gnudi, A; Robuschi, G; Roti, E; Rotola, C; Salvadori, S; Tomatis, R; Trasforini, G, 1984) | 0.61 |
"Pretreatment with naloxone 4 mg/kg significantly alleviated the gastric effects of morphine 32 mg/kg." | ( Decreased acid secretion and gastric lesion production by morphine in rats. Dai, S; Ho, MM; Ogle, CW, 1984) | 0.59 |
"Treatment with naloxone or morphine did not significantly affect blood pressure or plasma catecholamine levels." | ( No effect of naloxone or morphine on plasma catecholamines during hemorrhage in rat. Enberg, U; Farnebo, LO, 1984) | 0.98 |
"Pretreatment with naloxone did not affect the analgesia produced by microinjection of pentazocine into NRGC or NRPG, but did antagonize the analgesia produced by injection of pentazocine into PAG." | ( A comparison of the sites at which pentazocine and morphine act to produce analgesia. Azami, J; Gibbs, M; Llewelyn, MB; Roberts, MHT, 1983) | 0.59 |
"Pretreatment with naloxone HCL (2 mg/kg SC, 5 min before immobilization) did not influence SIA in either intact or spinal rats." | ( Immobilization-induced analgesia: possible involvement of a non-opioid circulating substance. Berge, OG; Fasmer, OB; Hole, K; Jørgensen, HA; Tveiten, L, 1984) | 0.59 |
"Pretreatment with naloxone 0.8 mg increased TRH-induced TSH and PRL release in six healthy subjects." | ( Influence of low doses of naloxone on pituitary secretion in man. Barreca, T; Magnani, G; Marabini, A; Rolandi, E; Sannia, A, 1982) | 0.89 |
"Pretreatment with naloxone did not blunt the hypotensive effect of morphine at a dose of 50 micrograms/kg, but enhanced the secretion of vasopressin in response to the morphine stimulus; plasma vasopressin levels were 5-fold greater than those found in animals given morphine but not pretreated with naloxone." | ( Effect of intracarotid administration of morphine and naloxone on plasma vasopressin levels and blood pressure in the dog. Crofton, JT; Rockhold, RW; Share, L; Wang, BC, 1983) | 0.84 |
"Pretreatment with naloxone (3.2 mg x kg-1 i.v." | ( Failure of naloxone to reduce clonidine-induced changes in blood pressure, heart rate and sympathetic nerve firing in cats. Shropshire, AT; Wendt, RL, 1983) | 0.98 |
"Pretreatment with naloxone antagonized the tolerance development to both morphine-induced analgesia and sensitivity changes, indicating a role for opiate receptors in this phenomenon." | ( The development of acute tolerance to analgesia and the sensitivity changes in mouse vas deferens and ileum produced by morphine. Ghosh, MN; Gopalakrishnan, V; Pillai, NP; Ramaswamy, S, 1983) | 0.59 |
"Post-treatment naloxone assays demonstrated the presence of large amounts of naloxone in the patient's blood and urine." | ( Treatment of heroin overdose with endotracheal naloxone. Abercrombie, D; Tandberg, D, 1982) | 0.86 |
"Pretreatment with naloxone at either dose did not attenuate the decrease in FVC, FEV1, or FEF25--75 after cold air in comparison with placebo pretreatment." | ( Naloxone does not affect bronchoconstriction induced by isocapnic hyperpnea of subfreezing air. Balsavich, L; Johnson, TS; von Gal, E; Weinberger, SE; Weiss, ST, 1982) | 2.03 |
"Pretreatment with naloxone (3 mg/kg) antagonized the effects of both enkephalins." | ( Effects of enkephalins on perfusion pressure in isolated hindlimb preparations. Dowling, DA; Moore, RH, 1982) | 0.59 |
"Pretreatment with naloxone (2 mg/kg) antagonized the reinforcing effects of 1.0 microgram morphine as this group showed no significant change in place preference." | ( Reinforcing effects of morphine microinjection into the ventral tegmental area. LePiane, FG; Phillips, AG, 1980) | 0.58 |
"pretreatment with naloxone (10 mg/kg) had no effect on the central SP-induced response." | ( Inhibition by morphine of the cardiovascular and behavioral responses evoked by centrally administered substance P in conscious rats. Badoer, E; Culman, J; Itoi, K; Jost, N; Tschöpe, C; Unger, T, 1994) | 0.61 |
"Pretreatment with naloxone (5 mg/kg i.p.) completely antagonised the disruptive effect of the opiates on working memory." | ( Relationship between morphine and etonitazene-induced working memory impairment and analgesia. Braida, D; Gori, E; Sala, M, 1994) | 0.61 |
"Pretreatment with naloxone (30 micrograms, IC) prior to clonidine administration resulted in a significant attenuation of both the clonidine-induced hypotension and bradycardia." | ( Opioidergic receptors in the arcuate nucleus are not involved in the cardiovascular effects of clonidine. Barber, DA; Tackett, RL, 1994) | 0.61 |
"Pretreatment with naloxone antagonized the effect of medprotine in all assays." | ( Evidence for the involvement of opioidergic systems in medprotine-induced analgesia in the mouse. Amico-Roxas, M; Candido, P; Caruso, A; Cutuli, VM; De Bernardis, E, 1994) | 0.61 |
"Treatment with naloxone or buprenorphine or naloxone + epinephrine resulted in significant improvement in MAP, pH and base excess." | ( Effects of opioid agonists and opioid antagonists in endotoxic shock in rats. Tseng, CS; Tso, HS, 1993) | 0.63 |
"Pretreatment with naloxone inhibited the immediate post-injury decrease of the rostral MNP and some of the increase of MPP latency." | ( Naloxone reduces alterations in evoked potentials and edema in trauma to the rat spinal cord. Nyberg, F; Olsson, Y; Sharma, HS; Stålberg, E; Winkler, T, 1994) | 2.05 |
"Pretreatment with naloxone (Nx) in a dose of 0.1 microgram icv significantly decreased the rise in BP and augmented the increase in HR." | ( Interaction between the central histaminergic and the muscarinic cholinergic systems. Młynarska, MS, 1994) | 0.61 |
"Pretreatment with naloxone (5 micrograms/rat i.c.v.) completely prevented the disappearance of migrating myoelectric complexes induced by the morphine metabolite." | ( Intestinal effect of morphine 6-glucuronide: in vivo and in vitro characterization. Basilico, L; Giagnoni, G; Gori, E; Massi, P; Parolaro, D; Rubino, T, 1994) | 0.61 |
"Pretreatment with naloxone (10 micrograms), which by itself had no effect on micturition, enhanced the facilitatory effects of M3G." | ( Effects of morphine metabolites on micturition in normal, unanaesthetized rats. Andersson, KE; Igawa, Y; Mattiasson, A; Westerling, D, 1993) | 0.61 |
"Pretreatment with naloxone or MK-801 blocked morphine-induced analgesia." | ( Blockade of morphine-induced analgesia and tolerance in mice by MK-801. Hurlbut, DE; Lutfy, K; Weber, E, 1993) | 0.61 |
"Pretreatment with naloxone (1 mg/kg) did not change Fos labeling." | ( Effects of morphine and naloxone on basal and evoked Fos-like immunoreactivity in lumbar spinal cord neurons of arthritic rats. Abbadie, C; Besson, JM, 1993) | 0.92 |
"Treatment with naloxone (10 mg/kg BW, sc) significantly reversed the inhibitory effects of NPFF on AVP release." | ( Centrally administered neuropeptide FF inhibits arginine vasopressin release in conscious rats. Arima, H; Iwasaki, Y; Kondo, K; Murase, T; Oiso, Y, 1996) | 0.63 |
"Pretreatment with naloxone (20 micrograms/mouse) inhibited the enkephalins-induced augmentation of NK cell and macrophage cytotoxic activity." | ( Bidirectional modulation of mouse natural killer cell and macrophage cytotoxic activities by enkephalins. Belowski, D; Kowalski, J; Wielgus, J, ) | 0.45 |
"Treatment with naloxone at either dose antagonised this effect, but naloxone produced no significant hyperalgesia when given alone." | ( Cranial irradiation with Gaalas laser leads to naloxone reversible analgesia in rats. Shephard, RA; Wedlock, PM, 1996) | 0.89 |
"Pretreatment with naloxone suppressed the inhibitory effect of casein, suggesting that stimulation of opioid receptors by beta casomorphins, a product of digestion of casein, might be involved in the motility changes observed." | ( Inhibition of small intestinal motility by casein: a role of beta casomorphins? Charlin, V; Defilippi, C; Gomez, E; Silva, C, ) | 0.45 |
"Pretreatment with naloxone (an unspecific antagonist of opioid receptors) blocked the tumor growth inhibition induced by the treatment with bestatin and thiorphan what could suggest a contribution of endogenous enkephalin in this antitumor effect." | ( Antitumor activity of bestatin and thiorphan in mice. Belowski, D; Herman, ZS; Kowalski, J; Madej, A, 1995) | 0.61 |
"Pretreatment with naloxone, naltrindole or H-Dmt-Tic-Ala-OH (a highly selective delta-opioid receptor antagonist) prevented [Dmt1]deltorphin B antinociception." | ( Opioid receptor selectivity alteration by single residue replacement: synthesis and activity profile of [Dmt1]deltorphin B. Anacardio, R; Attila, M; Bryant, SD; Capasso, A; Guerrini, R; Lazarus, LH; Salvadori, S; Sorrentino, L, 1996) | 0.62 |
"Pretreatment with naloxone attenuated dermorphin-induced effects on core temperature and partially enhanced vasomotor effects of dermorphin." | ( Effect of dermorphin on thermoregulation in rats at selected ambient temperatures. Deigin, VI; Emel'yanova, TG; Kamensky, AA; Usenko, AB; Yarova, EP, 1996) | 0.62 |
"Pretreatment with naloxone (0.01-1.0 mg/kg IM, 10 min presession) and substitution tests with the peripherally acting opioid loperamide (0.1 mg/kg per delivery) were also conducted." | ( Smoked heroin self-administration in rhesus monkeys. Carroll, ME; Mattox, AJ, 1996) | 0.62 |
"Treatment with naloxone resulted in rapid reversal of signs without sequelae." | ( Loperamide poisoning in the dog. Berny, PJ; Buronfosse, F; Cadore, JL; Hugnet, C; Mathet, T; Pineau, X, 1996) | 0.63 |
"Pretreatment with naloxone (12 mg/h) completely blocked the hypertensive and tachycardiac response to U50,488H, but was unable to prevent the loss of variation in heart rate or respiratory depression." | ( Cardiovascular and respiratory actions of U50,488H in the unanaesthetized ovine foetus. Cheng, PY; Soong, Y; Szeto, HH; Taylor, CC; Wu, D; Yee, J, 1996) | 0.62 |
"Pretreatment with naloxone produced only at the highest dose a partial, but significant, antagonism, whereas cyprodime failed to alter the ethanol cue." | ( The influence of opioid antagonists on the discriminative stimulus effects of ethanol. Spanagel, R, 1996) | 0.62 |
"Treatment with naloxone increased SP response in lesioned rats to 41% of control value with no change in smooth muscle reactivity." | ( Effect of chronic sciatic nerve lesion on the neurogenic inflammatory response in intact and acutely injured denervated rat skin. Bassirat, M; Helme, RD; Khalil, Z, 1996) | 0.63 |
"Pretreatment with naloxone abolished this antinociceptive activity both in the hot-plate test and in the first phase of the formalin test without affecting the serum concentration of paracetamol." | ( Naloxone-reversible antinociception by paracetamol in the rat. Ottani, A; Pini, LA; Sandrini, M; Vitale, G, 1997) | 2.06 |
"Pretreatment with naloxone abolished the antinociceptive activity of both ASA and morphine in the hot-plate and formalin tests and prevented the increase in cerebral 5-HT concentration and the reduction in 5-HT2 receptors in cortical membranes induced by ASA." | ( Serotonin and opiate involvement in the antinociceptive effect of acetylsalicylic acid. Pini, LA; Sandrini, M; Vitale, G, 1997) | 0.62 |
"pretreatment with naloxone did not affect the development of tactile allodynia induced by dynorphin A(1-17) or alter sensory threshold when given alone." | ( Single intrathecal injections of dynorphin A or des-Tyr-dynorphins produce long-lasting allodynia in rats: blockade by MK-801 but not naloxone. Lashbrook, JM; Laughlin, T; Malan, TP; Nichols, ML; Ossipov, MH; Porreca, F; Vanderah, TW; Wilcox, GL, 1996) | 0.82 |
"Pretreatment with naloxone hydrochloride enhanced (p < 0.01) SBP, heart rate, noradrenaline, cortisol, and endothelin-1 levels, and reduced (p < 0.01) ANF in low responders in response to MAT, whereas it decreased (p < 0.01) hemodynamic parameters, noradrenaline, and endothelin-1 in high responders." | ( Opioid peptide modulation of circulatory and endocrine response to mental stress in humans. Bernardi, P; Boschi, S; De Iasio, R; Fontana, F; Grossi, G; Pich, EM; Spampinato, S, 1997) | 0.62 |
"Pretreatment with naloxone almost completely blocked both fluid pooling effect and mucosal protective effect of loperamide." | ( Subcutaneous loperamide prevents gastric lesions induced by necrotizing agents in rats. Hatakeyama, Y; Ohtsuka, M; Shimomura, K; Tomoi, M, 1997) | 0.62 |
"Pretreatment with naloxone inhibited the action of morphine, suggesting involvement of classical opioid receptors." | ( Morphine alters the levels of growth hormone receptor mRNA and [125I]growth hormone binding in human IM-9 lymphoblasts via a naloxone-reversible mechanism. Henrohn, D; Le Grevés, P; Nyberg, F, 1997) | 0.83 |
"Pretreatment with naloxone dihydrochloride (5 mg/kg, intraperitoneally) completely inhibited the BE-induced changes in the release of these peptides." | ( Effect of intragastric administration of beta-endorphin on thyrotropin-releasing hormone and somatostatin release into gastric lumen of rats. Kaneko, H; Konagaya, T; Kusugami, K; Mitsuma, T; Nagai, H; Nishio, Y; Yamamoto, H, 1998) | 0.62 |
"Pretreatment with naloxone, a potent opiate receptor antagonist, reversed the effects of morphine, suggesting the involvement of opiate receptors in the regulation of the ganglion cells of the terminal nerve." | ( FMRFamide-like immunoreactivity in the olfactory system responds to morphine treatment in the teleost Clarias batrachus: involvement of opiate receptors. Jain, MR; Khan, FA; Saha, SG; Subhedar, N, 1998) | 0.62 |
"Late treatment with naloxone (4 mg/kg i.v.; 4-37 micrograms/kg V4) accelerated and exaggerated these changes." | ( Correction of hypovolemic hypotension by centrally administered naloxone in conscious rabbits. Blake, DW; Ludbrook, J; Van Leeuwen, AF, 1998) | 0.85 |
"Pretreatment with naloxone (1.0 mg kg-1, i.p.) abolished significantly (P < 0.01) the antinociceptive action of propofol." | ( Effect of propofol on perception of pain in mice: mechanisms of action. Abdel-Rahman, MS; Anwar, MM, 1998) | 0.62 |
"Pretreated rats (naloxone, saline or nor-BNI, Day 1) received an additional acute nor-BNI injection (Day 4) which increased plasma oxytocin concentration in the three groups." | ( Naloxone-induced supersensitivity of oxytocin neurones to opioid antagonists. Carón, RW; Leng, G; Ludwig, M; Russell, JA, 1998) | 2.07 |
"Pretreatment with naloxone (1 mg/kg) failed to modify the effect of stimulation of periaqueductal gray matter on analgesia and corticosterone level." | ( [The role of corticosteroids in analgesic effect caused by stimulation of the periaqueductal gray matter of the midbrain in rats]. Bogdanov, AI; Iarushkina, NI, 1998) | 0.62 |
"pretreatment with naloxone (1 mg/kg i.p.)." | ( The potentiation of analgesic activity of paracetamol plus morphine involves the serotonergic system in rat brain. Ottani, A; Pini, LA; Sandrini, M; Vitale, G, 1999) | 0.63 |
"Pretreatment with naloxone (2.0 mg/kg, i.p.) significantly antagonized sendide (1024 pmol)-induced inhibition of the behavioural responses to neurokinin A, neurokinin B and eledoisin." | ( Opioid activity of sendide, a tachykinin NK1 receptor antagonist. Inoue, M; Kisara, K; Ohba, M; Sakurada, C; Sakurada, S; Sakurada, T; Tan-No, K; Yuhki, M, 1999) | 0.63 |
"Pretreatment with naloxone (0.2 mg/kg) completely eliminated the increase in cardiac electrical stability produced by DALDA." | ( Ligands for opioid and sigma-receptors improve cardiac electrical stability in rat models of post-infarction cardiosclerosis and stress. Maslov, LN; Naryzhnaya, NV; Tam, SW, 1999) | 0.63 |
"Pretreatment with naloxone (4 mg/kg) had no significant effect on the inhibitory effects of either extract in the abdominal constriction test." | ( Influence of temperature, pH and naloxone on the antinociceptive activity of Channa striatus (haruan) extracts in mice. Dambisya, YM; Lee, TL; Mat Jais, A; Sathivulu, V, 1999) | 0.91 |
"Pretreatment with naloxone (5 mg/kg, IP) significantly attenuated the antinociceptive effect induced by the chimeric peptide (90 mg/kg, IP), indicating involvement of an opioidergic mechanism." | ( Chimeric peptide of Met-enkephalin and FMRFa induces antinociception and attenuates development of tolerance to morphine antinociception. Bhardwaj, DK; Gupta, S; Gupta, YK; Pasha, S, 1999) | 0.63 |
"Treatment with naloxone completely abolished all these modifications." | ( Role of gonadal hormones in formalin-induced pain responses of male rats: modulation by estradiol and naloxone administration. Aloisi, AM; Ceccarelli, I, 2000) | 0.86 |
"Pretreatment with naloxone greatly enhanced the response in the sex-steroid treated rats, and was less effective in the controls." | ( Sex-steroid induction of endogenous opioid inhibition on oxytocin secretory responses to stress. Brunton, P; Douglas, AJ; Johnstone, H; Russell, JA, 2000) | 0.63 |
"Pretreatment with naloxone attenuated the effect of morphine, whereas nor-binaltorphimine, a selective kappa-opioid receptor antagonist, abolished the effect of U-50,488H on Fos induction." | ( Activation of c-fos expression in hypothalamic nuclei by mu- and kappa-receptor agonists: correlation with catecholaminergic activity in the hypothalamic paraventricular nucleus. Castells, MT; Laorden, ML; Martínez, MD; Martínez, PJ; Milanés, MV, 2000) | 0.63 |
"Pretreatment with naloxone in the baro-denervated animals abolished these changes." | ( Suppressive effects of remifentanil on hemodynamics in baro-denervated rabbits. Aono, H; Goto, H; Kindscher, JD; Shinohara, K; Unruh, GK, 2000) | 0.63 |
"Treatment with naloxone before ischemia-reperfusion had no effect on animals compared with the I/R group." | ( Role of endogenous opioid peptides in protection of ischemic preconditioning in rat small intestine. Dun, Y; Hao, YB; Wu, YX; Yang, SP; Zhang, Y, 2001) | 0.65 |
"Pretreatment with naloxone abolished paracetamol antinociceptive activity both in hot-plate and in the first phase, but not in the second phase of the formalin test, while MR 2266 pretreatment was able to antagonise paracetamol effect either in the hot-plate test or in both phases of the formalin test." | ( The effect of paracetamol on nociception and dynorphin A levels in the rat brain. Candeletti, S; Capobianco, A; Morelli, G; Pini, LA; Romualdi, P; Sandrini, M; Vitale, G, 2001) | 0.63 |
"Pretreatment with naloxone alone did not induce emesis in its own right nor did it modify emesis induced by a single challenge to a motion stimulus." | ( Opioid receptor involvement in the adaptation to motion sickness in Suncus murinus. Javid, FA; Naylor, RJ, 2001) | 0.63 |
"Treatment with naloxone [10 mg/kg, intraperitoneal (i.p.)], atropine (5 mg/kg, i.p.), or ketanserin (10 mg/kg, i.p.) at either 1200 or 1400 h prevented the afternoon decrease of TIDA neuronal activity and the prolactin (PRL) surge." | ( Prostaglandins may participate in opioidergic and cholinergic control of the diurnal changes of tuberoinfundibular dopaminergic neuronal activity and serum prolactin level in ovariectomized, estrogen-treated rats. Chu, YC; Pan, JT; Tsou, MY, 2001) | 0.65 |
"Treatment with naloxone benzoylhydrazone in morphine-dependent wild-type mice caused a significant increase in cyclic AMP levels in the thalamus while it had no effect in the nociceptin receptor knockout mice." | ( Morphine tolerance and dependence in the nociceptin receptor knockout mice. Mamiya, T; Nabeshima, T; Nagai, T; Noda, Y; Ren, X; Takeshima, H; Ukai, M, 2001) | 0.65 |
"Pretreatment with naloxone, an opioid receptor antagonist (1.0 and 4.0 mg/kg, s.c.), failed to reverse the morphine-evoked behavioral response, suggesting that the morphine effect is not mediated through the opioid receptors in the spinal cord." | ( Intrathecal high-dose morphine induces spinally-mediated behavioral responses through NMDA receptors. Moriyama, T; Okuda, K; Sakurada, C; Sakurada, S; Sakurada, T; Sugiyama, A; Tan-No, K; Watanabe, C, 2002) | 0.64 |
"Pretreatment with naloxone (5 mg/kg sc) was able to block both endomorphin-1 and endomorphin-2 effects on lordosis." | ( Activation of mu-opioid receptors inhibits lordosis behavior in estrogen and progesterone-primed female rats. Acosta-Martinez, M; Etgen, AM, 2002) | 0.64 |
"Pretreatment with naloxone before HS attenuated the protective effects in a dose-dependent fashion, with significant attenuation of protection occurring at 15 mg/kg naloxone versus heat shock (42 +/- 6 vs." | ( Attenuation of heat shock-induced cardioprotection by treatment with the opiate receptor antagonist naloxone. Gross, GJ; Hsu, A; Patel, HH, 2002) | 0.85 |
"Pretreatment with naloxone increased the heart rate response in animals that were long-term tether housed (n=12)." | ( Opioid activity in behavioral and heart rate responses of tethered pigs to acute stress. Janssens, CJ; Loijens, LW; Schouten, WG; Wiegant, VM, 2002) | 0.64 |
"Pretreatment with naloxone (5 mg/kg IP), a specific narcotic antagonist, abolished tail erection produced by low electrical current." | ( Naloxone antagonism of electrical stimulation induced tail erection in mice. Chai, CY; Kao, LC; Lee, HK; Wayner, MJ, 1979) | 2.03 |
"Pretreatment with naloxone hydrochloride (5 mg/kg IP) effectively blocked the opiate-induced hypothermia in the restrained animal, but a total dose of 10 mg/kg was necessary to completely block the hyperthermic response in the free-moving rat." | ( Restraint alters the effects of morphine and heroin on core temperature in the rat. Martin, GE; Pryzbylik, AT; Spector, NH, 1977) | 0.58 |
"Pretreatment with naloxone, a narcotic antagonist, significantly antagonized the effects of Substance P on self-stimulation." | ( Effect of substance P on medial forebrain bundle self-stimulation in rats following intracerebral administration. Goldstein, JM; Malick, JB, 1977) | 0.58 |
"Pretreatment with naloxone eliminated analgesia but not seizures induced by SRIF." | ( Opiate-like naloxone-reversible actions of somatostatin given intracerebrally. Friesen, H; Havlicek, V; LaBella, FS; Leybin, L; Rezek, M, 1978) | 0.96 |
"Pretreatment with naloxone (60 mg/kg i.p.) produced a 200 percent increase of the dose of d-propoxyphene or heroin needed to produce a seizure." | ( Antagonism of the convulsant effects of heroin, d-propoxyphene, meperidine, normeperidine and thebaine by naloxone in mice. Gilbert, PE; Martin, WR, 1975) | 0.79 |
"Pretreatment with naloxone (1 mg/kg, sc) inhibited the morphine (7.5 micrograms) hyperlocomotion elicited from all three pallidal areas." | ( Pallidal substrate of morphine-induced locomotion. Anagnostakis, Y; Krikos, Y; Spyraki, C, 1992) | 0.61 |
"Treatment with naloxone of morphine-exposed mice resulted in the typical jumping behavior indicative of opiate withdrawal." | ( Modifications of striatal D2 dopaminergic postsynaptic sensitivity during development of morphine tolerance-dependence in mice. Cebeira, M; Fernández-Ruiz, JJ; Hernández, ML; Navarro, M; Ramos, JA; Rodriguez de Fonseca, F, 1992) | 0.62 |
"Treatment with naloxone (1 mg/kg i.v.) had no effect on CA.OC in the LC." | ( In vivo catechol activity in the rat locus coeruleus following different nociceptive stimuli and naloxone. Hong, M; Jhamandas, K; Loomis, CW; Milne, B, 1992) | 0.84 |
"Pretreatment with naloxone (0.5 mg kg-1) partially antagonized the inhibitory action of loperamide on the nerve-mediated detrusor contraction." | ( In vivo motor effects of loperamide on the rat urinary bladder. Berggren, A; Rubenson, A; Sillén, U, 1992) | 0.61 |
"Pretreatment with naloxone, an opioid antagonist, resulted in a reversible effect on the behavioural reduction of NK-2 and NK-3 receptor agonists produced by spantide." | ( Naloxone-reversible effect of spantide on the spinally mediated behavioural response induced by neurokinin-2 and -3 receptor agonists. Katsumata, K; Kisara, K; Manome, Y; Sakurada, S; Sakurada, T; Tan-No, K; Uchiumi, H, 1992) | 2.05 |
"Pretreatment with naloxone (5 or 10 mg/kg i.v.) reduced the initial rate of decline in firing rate and the duration of inhibition but did not prevent a single dose of 40 mg/kg of (+/-)-HA-966 from totally inhibiting DA cell impulse flow." | ( (+-)-1-hydroxy-3-aminopyrrolidone-2 (HA-966) inhibits the activity of substantia nigra dopamine neurons through a non-N-methyl-D-aspartate receptor-mediated mechanism. Lehmann, H; Shepard, PD, 1992) | 0.61 |
"Pretreatment with naloxone resulted in cocaine-induced seizures of 0%, 50%, and 60% (p less than or equal to 0.05 at the 75 mg/kg dose)." | ( The effect of morphine and naloxone on cocaine toxicity. Albertson, TE; Derlet, RW; Tharratt, RS; Tseng, CC, 1992) | 0.9 |
"pretreatment with naloxone (10 nmol), whereas an i.c." | ( Inhibitory interactions between alpha 2-adrenergic and opoid but not NPY mechanisms controlling the CRF-ACTH axis in the rat. Assenmacher, I; Barbanel, G; Gaillet, S; Malaval, F; Pelletier, G; Szafarczyk, A, 1991) | 0.6 |
"pretreatment of naloxone reduced the compound 48/80-induced water intake but had no effects on other variables." | ( Participation of opioid peptide (beta-endorphin) and norepinephrine in the control of compound 48/80-induced hypovolemic thirst in the rats. Izumi, H, 1991) | 0.62 |
"Pretreatment with naloxone (10 mg/kg) significantly attenuated the inhibitory effect of GABA (100 micrograms) on AVP release." | ( Possible involvement of endogenous opioid peptides in the inhibition of arginine vasopressin release by gamma-aminobutyric acid in conscious rats. Kondo, K; Oiso, Y; Otake, K, 1991) | 0.6 |
"Pretreatment with naloxone (1 and 3 mg/kg, IP) prior to daily fighting failed to antagonize defeat-induced copulatory disorder." | ( Ethopharmacology of copulatory disorder induced by chronic social conflict in male mice. Kimura, N; Yoshimura, H, 1991) | 0.6 |
"Pretreatment with naloxone antagonized the activity of morphiceptin but prevented only the stimulating effect of DTLET in normotensive rats." | ( Normotensive Wistar rats differ from spontaneously hypertensive and renal hypertensive rats in their cardiovascular responses to opioid agonists. Członkowski, A; Widy-Tyszkiewicz, E, 1991) | 0.6 |
"Pretreatment with naloxone (10 mg/kg, SC, 30 min prior to testing), which did not affect the responsiveness of nonstressed mice to the hot plate or to the convulsant treatments, attenuated the development of analgesia following CRS, but not SS, and further prolonged the latency to onset of PTZ-induced convulsions in both stressed groups." | ( Effects of cold-restraint and swim stress on convulsions induced by pentylenetetrazol and electroshock: influence of naloxone pretreatment. De Lima, TC; Rae, GA, 1991) | 0.81 |
"Treatment with naloxone (1 mg/kg) had no effect on rCBF, calculated cerebral vascular resistance, or cerebral oxygen consumption of normotensive or hypotensive piglets." | ( Opioids and the prostanoid system in the control of cerebral blood flow in hypotensive piglets. Armstead, WM; Busija, DW; Leffler, CW; Mirro, R, 1991) | 0.62 |
"Post-treatment with naloxone dose-dependently reversed the analgesic effects of both E-2078 and morphine, but E-2078-induced analgesia was relatively resistant to naloxone antagonism." | ( Analgesia produced by E-2078, a systemically active dynorphin analog, in mice. Furuya, Y; Kaneko, T; Nakazawa, T; Tachibana, S; Yamatsu, K; Yoshino, H, 1990) | 0.59 |
"Pretreatment with naloxone caused a reduction in plasma BEIR increase following Hypnorm, ether and urethane; and in the analgesia following Hypnorm and urethane." | ( Effect of anaesthetics on the release of beta-endorphin-immunoreactivity in rat plasma. Barna, I; de Jong, W; Ramirez-Gonzalez, MD; Wiegant, VM, 1991) | 0.6 |
"Treatment with naloxone enhanced the evoked release of oxytocin significantly without effect on vasopressin secretion." | ( Kappa-opioid receptor agonists differentially affect the release of neurohypophysial hormones. Christensen, JD; Fjalland, B, 1990) | 0.62 |
"Pretreatment with naloxone did not modify the AVP and OT responses to hypoglycemia in normal weight subjects, whereas it significantly enhanced both hormonal responses in obese subjects." | ( Increase by naloxone of arginine vasopressin and oxytocin responses to insulin-induced hypoglycemia in obese men. Bianconi, L; Capretti, L; Castelli, A; Cavazzini, U; Chiodera, P; Coiro, V; Marcato, A; Speroni, G; Volpi, R, 1990) | 0.98 |
"Pretreatment with naloxone can also produce supersensitivity to morphine." | ( Naloxone-induced analgesia and morphine supersensitivity effects are contingent upon prior exposure to analgesic testing. Cappell, H; Knoke, DM; Le, AD; Poulos, CX, 1990) | 2.05 |
"Pretreatment with naloxone completely eliminated this analgesia." | ( Prolonged analgesia by enkephalinase inhibition in rats with spinal cord adrenal medullary transplants. Sagen, J; Wang, H, 1990) | 0.6 |
"Pretreatment with naloxone induced a significant activation of KKS, which was potentiated by subsequent hemorrhage." | ( [Effect of enkephalins and naloxone on the activity of the kallikrein-kinin system in experimental hemorrhagic shock]. Grässler, J; Kühne, H; Slepuschkin, VD; Steinke, M; Zoloev, GK, 1990) | 0.9 |
"Pretreatment with naloxone (5 mg/kg, i.p.) abolished the antinociceptive effects of [D-Trp7,9,Leu11]SP, implying that opiate receptors in the spinal cord mediate at least in part the antinociceptive effects." | ( Behavioural and antinociceptive effects of intrathecally injected substance P analogues in mice. Folkers, K; Post, C, 1985) | 0.59 |
"Pretreatment with naloxone did not prevent any of the neurochemical responses to ICV CRF, but naloxone alone increased DOPAC:DA in medial profrontal cortex, and decreased MHPG:NE in nucleus accumbens in CRF-injected mice." | ( Corticotropin-releasing factor administration elicits a stress-like activation of cerebral catecholaminergic systems. Berridge, CW; Dunn, AJ, 1987) | 0.6 |
"Pretreatment with naloxone diminished the rises in plasma beta-endorphin, epinephrine, and norepinephrine without affecting the responses of plasma glucagon and cortisol." | ( Effects of naloxone on glucose homeostasis during insulin-induced hypoglycemia. Abumrad, NN; Hourani, H; Lacy, DB; Nash, JA; Radosevich, PM; Rizk, N; Williams, PE, 1989) | 0.99 |
"Pretreatment with naloxone (2.0 mg/kg s.c.) did not reduce the rise in plasma levels of ACTH or corticosterone produced by PCP." | ( Naloxone does not antagonize PCP-induced stimulation of the pituitary-adrenal axis in the rat. George, R; Pechnick, RN; Poland, RE, 1989) | 2.04 |
"Pretreatment with naloxone (0.5 mg/kg) also significantly prolonged AVP secretion induced by intracerebroventricular injection of angiotensin-II (100 ng)." | ( Effects of naloxone on vasopressin secretion in conscious rats: evidence for inhibitory role of endogenous opioid peptides in vasopressin secretion. Arai, H; Hosoda, K; Itoh, H; Mukoyama, M; Nakao, K; Saito, Y; Shiono, S; Shirakami, G; Sugawara, A; Yamada, T, 1989) | 0.99 |
"Pretreatment with naloxone (2 mg/kg iv) 5 min before the administration of motilin (400-500 micrograms/kg iv) did not block the initiation of MMCs by motilin." | ( Opioid receptors and the initiation of migrating myoelectric complexes in dogs. Condon, RE; Szurszewski, JH; Telford, GL, 1989) | 0.6 |
"Pretreatment with naloxone blocked the pressor response of only a subsequent injection with 20 nmoles/kg but not 60 nmoles/kg of dynorphin A or NE (8.0 nmoles/kg)." | ( Opiate and alpha receptor antagonists block the pressor responses of conscious rats given intravenous dynorphin. Gregor, L; Saunders, WS; Thornhill, JA, ) | 0.45 |
"3. Treatment with naloxone (intravenous, 0.04-0.4 mg kg-1; intracisternal, 0.2-2 micrograms kg-1) did not affect either phase of the haemodynamic response to simulated haemorrhage." | ( Intracisternal naloxone and cardiac nerve blockade prevent vasodilatation during simulated haemorrhage in awake rabbits. Evans, RG; Ludbrook, J; Potocnik, SJ, 1989) | 0.95 |
"Pretreatment with naloxone modified the response of the hypothalamus-pituitary-adrenal system to oxytocin, producing partial blockade." | ( [Effect of oxytocin and naloxone on the plasma levels of corticosterone in the rat]. Montilla, P; Muñoz, JL; Muñoz, MC; Ríos, JE, 1989) | 0.91 |
"In untreated women naloxone infusion significantly reduced body core temperature." | ( Regulation of body temperature in postmenopausal women: interactions between bromocriptine and the endogenous opioid system. Cagnacci, A; Fioretti, P; Gambacciani, M; Melis, GB; Paoletti, AM; Soldani, R, 1989) | 0.6 |
"Pretreatment with naloxone (100 micrograms/kg i.a.) 10 min prior to pindolol administration prevented the hypotensive response." | ( Catecholaminergic and opioidergic mechanisms involved in the hypotensive response of pindolol. Jones, LF; Tackett, RL, 1989) | 0.6 |
"Pretreatment with naloxone (0.1 mg/kg, i.v.) 15 min prior to the administration of atenolol completely prevented the hypotensive response in SHR and decreased the maximum hypotensive response by approximately 50% in WKY rats." | ( Naloxone pretreatment blocks the hypotensive effects of atenolol in SHR and WKY rats. Jones, LF; Laskey, RE; Tackett, RL, 1989) | 2.04 |
"Pretreatment with naloxone 15 min prior to the administration of BHT 933 completely abolished the hypotensive response and significantly inhibited the bradycardia." | ( Naloxone inhibits the centrally-mediated hypotensive actions of BHT-933 (azepexole). Laskey, R; Tackett, RL, 1987) | 2.04 |
"Pretreatment with naloxone (0.5 mg/kg) effectively blocked this depressor effect and reduction in renal nerve activity.(ABSTRACT TRUNCATED AT 250 WORDS)" | ( Opiate receptor-mediated decrease in renal nerve activity during hypotensive hemorrhage in conscious rabbits. Hosomi, H; Morita, H; Motochigawa, H; Nishida, Y; Uemura, N; Vatner, SF, 1988) | 0.6 |
"Pretreatment with naloxone failed to affect any of these responses." | ( Endogenous opioid modulation of pancreatic hormone secretion: studies in dogs. Levin, ER; Levin, S; Mills, S; Yamada, T, 1986) | 0.59 |
"Pre-treatment with naloxone at the higher dosage resulted in an enhanced (P less than 0.05) GH response to clonidine and guanfacine, respectively, whereas the lower dosage of naloxone was without effect." | ( Naloxone enhances the increase in plasma growth hormone induced by alpha 2-adrenergic stimulation in healthy males. Bramnert, M; Hökfelt, B, 1987) | 2.03 |
"Treatment with naloxone did not exert any significant effect on LH release in androgenized females and in deandrogenized males of any age." | ( Neonatal organization of the brain opioid systems controlling prolactin and luteinizing hormone secretion. Dondi, D; Limonta, P; Maggi, R; Martini, L; Piva, F, 1989) | 0.62 |
"Pretreatment with naloxone (0.04, 0.2, 1.0 mg/kg SC) attenuated the rewarding effect of beta-endorphin (2.5 micrograms) at all doses tested." | ( Rewarding properties of beta-endorphin as measured by conditioned place preference. Amalric, M; Bloom, FE; Cline, EJ; Koob, GF; Martinez, JL, 1987) | 0.6 |
"Pretreatment with naloxone (20 micrograms/kg IV) did not alter the anticonvulsant effect of morphine (250 micrograms/kg IV)." | ( Inhibition of penicillin-induced EEG discharges by low doses of morphine or naloxone in the rabbit. Evidence for a possible non-opioid receptor-mediated mechanism at the sensorimotor cortex. Massotti, M; Spillantini, MG, 1986) | 0.82 |
"Pretreatment with naloxone attenuated both arrhythmias and augmentation of cAMP levels to a similar extent." | ( Naloxone attenuates augmentation of cAMP levels and arrhythmias following myocardial ischaemia and reperfusion in the isolated perfused rat heart. Lee, AY; Wong, TM, 1986) | 2.04 |
"Pretreatment with naloxone antagonized the analgesic effect of central type BZ-receptor agonists." | ( Naloxone-sensitive and GABAA receptor mediated analgesic response of benzodiazepines in mice. Kulkarni, SK; Kunchandy, J, 1987) | 2.04 |
"Pretreatment with naloxone 10 min before beta EP injection abolished not only the PRL response to beta EP but also the conjugated effect of beta EP and TRH." | ( Opioid modulation of thyrotropin releasing hormone induced prolactin secretion. Buydens, P; Finné, E; Golstein, J; Vanhaelst, L; Velkeniers, B, 1987) | 0.6 |
"Pretreatment with naloxone reversed the increase in NSA and also unmasked N2O reduction in NR." | ( Comparison of nitrous oxide, morphine and diazepam effects in the mouse staircase test. Emmanouil, DE; Quock, RM; Wojcechowskyj, JA, 1987) | 0.6 |
"Pretreatment with naloxone failed to antagonize dextrorphan-induced blockade of THE." | ( Anticonvulsant effects of dextrorphan in rats: possible involvement in dextromethorphan-induced seizure protection. Ferkany, JW; Pontecorvo, MJ; Tortella, FC, 1988) | 0.6 |
"Pretreatment with naloxone (10 mg/kg) attenuated the pressor response to AII (0.3 or 1 microgram/min) by 25-50% but did not alter similar pressor responses to phenylephrine." | ( Attenuation by naloxone of the pressor effects of angiotensin II in conscious cynomolgus monkeys. Kirby, DA; Spealman, RD, 1988) | 0.95 |
"Pretreatment with naloxone on the stimulatory behavioral effect of licking, produced a significant inhibitory effect." | ( A functional separation of behavioral stereotypy based on naloxone-reversible effects of seryl enkephalinamide: comparison with morphine. Blaha, CD; Broderick, PA; Lane, RF, 1987) | 0.84 |
"Pretreatment with naloxone, an antagonist of opioids at their receptors, did not reduce the vasopressin levels (47.7 +/- 9 pg/ml)." | ( Nicotine-induced release of vasopressin in the conscious rat: role of opioid peptides and hemodynamic effects. Aubert, JF; Brunner, HR; Burnier, M; Nussberger, J; Waeber, B, 1987) | 0.6 |
"Pretreatment with naloxone (10 mg/kg s.c.) produced a significant decrease in %MPE and an increase in variance of response after exposures to 80% nitrous oxide in a double blind study." | ( Nitrous oxide analgesia: partial antagonism by naloxone and total reversal after periaqueductal gray lesions in the rat. Joseph, S; Knigge, K; Zuniga, J, 1987) | 0.85 |
"Treatment with naloxone of single-housed C and Pb2 was without effect, except for Pb2 treated undefeated mice: here, naloxone abolished the analgesic effect of lead treatment." | ( Two types of chronic lead treatment in C57BL/6 mice: interaction with behavioural determinants of pain. Paterson, AT; Vickers, C, 1986) | 0.61 |
"Treatment with naloxone was associated with a cessation in the fall in the mean arterial pressure and the contractility." | ( The effect of naloxone on the hemodynamics of the newborn piglet with septic shock. Bickers, RG; Hansen, NB; Menke, JA; Miller, RR; Nowicki, PT; Zwick, DL, 1986) | 0.97 |
"Pre-treatment with naloxone (0.1-1.0 mg/kg) before determination of cumulative dose-effect curves for morphine caused the morphine generalization curves to be shifted, in a parallel manner, rightward." | ( Quantitative analysis of naloxone antagonism of the discriminative stimulus properties of morphine in the pigeon. McMillan, DE; Wessinger, WD, 1986) | 0.89 |
"Pretreatment with naloxone (4 mg i.v." | ( Morphine-induced TSH release in normal and hypothyroid subjects. Devilla, L; Giusti, M; Lotti, G; Morgano, A; Musso, NR; Pende, A, 1985) | 0.59 |
"Pretreatment with naloxone (0.5, 2 and 8 mg/kg), an opioid antagonist, administered subcutaneously antagonized the antinociceptive effect of cyclo (His-Pro)." | ( The antinociceptive effects of histidyl-proline diketopiperazine and thyrotropin-releasing hormone in the mouse. Kawamura, S; Kisara, K; Sakurada, S; Sakurada, T; Sasaki, Y; Suzuki, K, 1985) | 0.59 |
"Treatment with naloxone caused significant decreases in the metabolic and electrocardiographic changes induced by endotoxin." | ( Decrease by naloxone of some electrocardiographic and biochemical changes following endotoxin induced shock in rats. Ageel, AM; Parmar, NS; Tariq, M, 1986) | 0.99 |
"Pretreatment with naloxone(1 mg/kg s.c.) significantly inhibited the analgesic effects of KTP and D-KTP at the PAG and LSS but not at the NRPG." | ( Sites of analgesic actions of kyotorphin and D-kyotorphin in the central nervous system of rats. Iwama, T; Satoh, M; Takagi, H; Wada, T, 1985) | 0.59 |
"Treatment with naloxone improves cardiovascular function and survival in a variety of shock models, and numerous sites and mechanisms for its action have been proposed. " | ( Intracoronary naloxone in hemorrhagic shock: dose-dependent stereospecific effects. Gurll, NJ; Lechner, RB; Reynolds, DG, 1985) | 0.98 |
Naloxone is an intrinsically safe drug, and may be administered in large doses with minimal clinical effect in non-opioid-dependent patients.
The addition of raltegravir to stabilized patients receiving buprenorphine/naloxone does not significantly affect the pharmacokinetic or pharmacodynamic parameters. Such pharmacokinetics behavior appeared to be related to the contractive effect of morphine on the bile duct.
Naloxone combined with acyclovir in the treatment of children viral encephalitis and the impacts on inflammatory factors IL-1 and IL-6. The most efficient strategies (ie, those conferring the greatest health benefit for a particular budget) were naloxones combined with PrEP and linkage to addiction treatment.
Excerpt | Reference | Relevance |
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" Recently, a method of using acupuncture and electrical stimulation (AES) in combination with naloxone for fast detoxification was reported." | ( Fast detoxification of heroin addicts by acupuncture and electrical stimulation (AES) in combination with naloxone. Wen, HL, ) | 0.56 |
"8 mg/70 kg) alone and in combination with naloxone (0." | ( Buprenorphine alone and in combination with naloxone in non-dependent humans. Bigelow, GE; Farre, M; Liebson, IA; Preston, KL; Weinhold, LL, 1992) | 0.81 |
"Lignocaine was tested either alone or in combination with a low dose of morphine by intrathecal administration on the C- and A-beta evoked responses of nociceptive neurones in the dorsal horn of the halothane-anaesthetized rat." | ( Spinal local anaesthetic actions on afferent evoked responses and wind-up of nociceptive neurones in the rat spinal cord: combination with morphine produces marked potentiation of antinociception. Chapman, V; Dickenson, AH; Fraser, HM, 1992) | 0.28 |
"A series of agents were tested for their ability to interact with the analgetic actions of either d-amphetamine (d-AMP) or l-amphetamine (l-AMP), or morphine in rats using the hot plate procedure." | ( Differential analgetic actions of amphetamine enantiomers in the mouse: a drug-drug interaction study. Maickel, RP; Spratto, GR; Tocco, DR, 1985) | 0.27 |
" Additionally, d-amphetamine or naloxone was administered with Gbl to test hypotheses of Gbl's neurochemical mechanisms of action." | ( Gamma-butyrolactone's discriminability and effect on low rates of lever pressing by rats: alone and in combination with D-amphetamine and naloxone. Cleary, J; McIntire, KD; Weinfurter, S, 1988) | 0.76 |
"The behavioral effects of phencyclidine (PCP) and ketamine administered alone and in combination with naloxone, atropine, methyl atropine, chlorpromazine and d-amphetamine were studied in squirrel monkeys trained to press a response lever under a fixed-ratio 30 schedule maintained by the termination of a stimulus associated with electric shock presentation." | ( Behavioral effects of phencyclidine and ketamine alone and in combination with other drugs. Byrd, LD; Howell, LL; Standish, LJ, 1987) | 0.49 |
" Studies revealed that tripelennamine (Tp) alone produced antinociception (ANTI) in mice and also caused potentiation when combined with morphine (M) or nalbuphene (NB)." | ( The effect of tripelennamine alone and in combination with opiates to produce antinociception in mice. Hanig, JP; Hui, FW; Sun, CJ; Tocus, EC, 1983) | 0.27 |
" A post-embedding immunogold cytochemical technique for Leu-enk, CHH and the CHH neurohormone related moult inhibiting hormone (MIH) was combined with a scintillator intensified autoradiographic method to demonstrate binding of the opioid antagonist [3H] naloxone." | ( Autoradiographic localization of opioid binding sites combined with immunogold detection of Leu-enkephalin, crustacean hyperglycaemic hormone and moult inhibiting hormone at the electron microscopic level in the sinus gland of the shore crab, Carcinus mae Hanke, J; Jaros, PP; Willig, A, 1993) | 0.47 |
" In contrast, SR 141716 in combination with naloxone had a significantly supra-additive anorectic action." | ( Effects of the cannabinoid receptor antagonist SR 141716, alone and in combination with dexfenfluramine or naloxone, on food intake in rats. Mukherjee, M; Robertson, K; Rowland, NE, 2001) | 0.79 |
") administration of D-serine, a selective agonist for the glycine site of the NMDA receptors, alone or in combination with morphine using the tail-flick test." | ( Activation of supraspinal NMDA receptors by both D-serine alone or in combination with morphine leads to the potentiation of antinociception in tail-flick test of rats. Akahori, K; Hashimoto, A; Ito, K; Jin, XL; Kobayashi, H; Maeda, M; Matsuda, M; Oka, T; Suzuki, T; Takahashi, S; Yoshikawa, M, 2007) | 0.34 |
"This randomized, double-blind, placebo- and active-controlled, parallel-group study was designed to demonstrate the superiority of oxycodone in combination with naloxone in a prolonged release (PR) formulation over placebo with respect to analgesic efficacy." | ( Analgesic efficacy and safety of oxycodone in combination with naloxone as prolonged release tablets in patients with moderate to severe chronic pain. Fleischer, W; Grothe, B; Hermanns, K; Hopp, M; Leyendecker, P; Meissner, W; Reimer, K; Ruckes, C; Szombati, I; Vondrackova, D; Weber, S, 2008) | 0.78 |
"To investigate if naloxone combined with epinephrine can increase the resuscitation rate in cardiac arrest rat models induced by asphyxia." | ( Small-dose naloxone combined with epinephrine improves the resuscitation of cardiopulmonary arrest. Gao, L; Meng, L; Wang, Y, 2008) | 1.07 |
"Twenty-four rats were allocated into SA group (treated with 1 mL of saline, n = 8), EP group (treated with epinephrine 5 microg/100g, n = 8), and NA group (treated with epinephrine 5 microg/100g in combination with naloxone100 microg/100g, n = 8)." | ( Small-dose naloxone combined with epinephrine improves the resuscitation of cardiopulmonary arrest. Gao, L; Meng, L; Wang, Y, 2008) | 0.92 |
"Naloxone combined with epinephrine was tested in a cardiac arrest rat model in which asphyxia was induced to determine if this drug combination could increase the resuscitation rate (survival) and decrease the cerebral damage." | ( Naloxone combined with epinephrine decreases cerebral injury in cardiopulmonary resuscitation. Gao, L; Meng, L; Wang, Y, 2010) | 3.25 |
"Twenty-four male Wistar rats were randomly assigned to one of three groups: the group treated with 1 mL saline (SA group; n = 8), the group treated with only epinephrine 5 microg/100 g (EP group; n = 8), or the group treated with epinephrine 5 microg/100 g combined with naloxone 1 mg/kg (NA group; n = 8)." | ( Naloxone combined with epinephrine decreases cerebral injury in cardiopulmonary resuscitation. Gao, L; Meng, L; Wang, Y, 2010) | 1.98 |
"Naloxone combined with epinephrine significantly increased the resuscitation rate in a rat model." | ( Naloxone combined with epinephrine decreases cerebral injury in cardiopulmonary resuscitation. Gao, L; Meng, L; Wang, Y, 2010) | 3.25 |
" BALB/c mice were divided into three groups: the Vac group received the HKLM vaccine alone; the NLX-Vac group received the HKLM vaccine in combination with the adjuvant NLX; and the control group received phosphate buffered saline (PBS)." | ( Evaluation of the adjuvant activity of naloxone, an opioid receptor antagonist, in combination with heat-killed Listeria monocytogenes vaccine. Ghasemnejad, H; Hassan, ZM; Jazani, NH; Karimzad, M; Mazloomi, E; Roshan-Milani, S; Shahabi, S; Sohrabpour, M, 2010) | 0.63 |
"To observe the effects of remifentanil combined with naloxone on human sperm motility in vitro and to investigate its possible mechanism." | ( [Effects of remifentanil combined with naloxone on human sperm motility]. Hu, YP; Li, Q; Wang, XH; Wang, YJ; Wang, ZP; Xu, B, 2011) | 0.89 |
" The STR was mimicked in mice treated with BD 1047 (a putative σ(1) receptor antagonist), but not SM-21, a putative σ(2) receptor antagonist, in combination with METH." | ( Straub tail reaction in mice treated with σ(1) receptor antagonist in combination with methamphetamine. Hall, FS; Kitanaka, J; Kitanaka, N; Nishiyama, N; Takemura, M; Tanaka, K; Uhl, GR, 2012) | 0.38 |
"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 |
"A hollow fiber liquid phase microextraction (HF-LPME) combined with ultra-high performance liquid chromatography-tandem mass spectrometry (UHPLC-MS/MS) method was developed for the extraction and determination of naloxone (NLX), buprenorphine (BP) and its major metabolite norbuprenorphine (NBP) in human plasma." | ( Hollow fiber liquid-phase microextraction combined with ultra-high performance liquid chromatography-tandem mass spectrometry for the simultaneous determination of naloxone, buprenorphine and norbuprenorphine in human plasma. Du, Z; Qu, S; Sun, W, 2014) | 0.78 |
"To investigate the effects of intrathecal morphine and fentanyl combined with low-dose naloxone on the expression of motilin and its receptor in a rat model of postoperative pain." | ( Effects of intrathecal opioids combined with low-dose naloxone on motilin and its receptor in a rat model of postoperative pain. Cao, JL; Gao, B; Liu, H; Zhang, Y; Zhao, J; Zheng, B, 2014) | 0.87 |
"Respiratory depression has been attributed to buprenorphine (BUP) misuse or combination with benzodiazepines." | ( Respiratory effects of buprenorphine/naloxone alone and in combination with diazepam in naive and tolerant rats. Chevillard, L; Cohier, C; Mégarbane, B; Risède, P; Roussel, O, 2014) | 0.68 |
" We evaluated the efficacy and the safety of a prolonged release oral formulation of oxycodone hydrochloride combined with naloxone hydrochloride dehydrate, in a fixed ratio of 2:1 (OXN PR)." | ( Efficacy and safety profile of prolonged release oxycodone in combination with naloxone (OXN PR) in Parkinson's disease patients with chronic pain. Dauri, M; Madeo, G; Natoli, S; Pierantozzi, M; Pisani, A; Schirinzi, T; Stefani, A, 2015) | 0.85 |
" The primary outcome was reporting frequency of the MedDRA System Organ Class (SOC) 'Cardiac Disorders' for naloxone alone and in fixed-dose combination with opioids." | ( Cardiovascular disorders associated with naloxone monotherapy and in fixed-dose combination with opioids: Data from international safety surveillance. Haigney, MC; Kao, D; Krantz, MJ; Mehler, PS; Sandhu, A, 2016) | 0.91 |
" Drug-drug interaction screening tools built into electronic health records and other services identify the interaction as risk of opioid withdrawal rather than hypersensitivity." | ( Potential drug interaction with opioid agonist in the setting of chronic low-dose opioid antagonist use. Diaz, CJ; Goode, PA; Leonard, JB; Nair, V; Penoyar, JB, 2017) | 0.46 |
" Subjects received methadone (arm 1) or buprenorphine-naloxone (arm 2) once daily (QD) per their existing individual prescriptions alone (days 1 to 9) and then in combination with glecaprevir at 300 mg QD and pibrentasvir at 120 mg QD (days 10 to 16) each morning." | ( No Clinically Relevant Drug-Drug Interactions between Methadone or Buprenorphine-Naloxone and Antiviral Combination Glecaprevir and Pibrentasvir. Asatryan, A; Geoffroy, P; Kort, J; Kosloski, MP; Liu, W; Zhao, W, 2017) | 0.93 |
" The most efficient strategies (ie, those conferring the greatest health benefit for a particular budget) were naloxone distribution combined with linkage to addiction treatment (cost saving), and naloxone distribution combined with PrEP and linkage to addiction treatment (ICER $95 337 per QALY) at a willingness-to-pay threshold of $100 000." | ( Effects of naloxone distribution alone or in combination with addiction treatment with or without pre-exposure prophylaxis for HIV prevention in people who inject drugs: a cost-effectiveness modelling study. Braithwaite, RS; Buchelli, M; Fiellin, DA; Rodriguez-Santana, R; Uyei, J, 2017) | 1.06 |
"Naloxone distribution through syringe service programmes is cost-effective compared with syringe distribution alone, but when combined with linkage to addiction treatment is cost saving compared with no additional services." | ( Effects of naloxone distribution alone or in combination with addiction treatment with or without pre-exposure prophylaxis for HIV prevention in people who inject drugs: a cost-effectiveness modelling study. Braithwaite, RS; Buchelli, M; Fiellin, DA; Rodriguez-Santana, R; Uyei, J, 2017) | 2.29 |
"BACKGROUND The aim of this research was to investigate the treatment effect of naloxone combined with hemodialysis on acute severe alcoholism." | ( Clinical Therapeutic Effect of Naloxone Combined with Hemodialysis on Acute Severe Alcoholism. Li, M; Li, Z; Liu, J; Liu, S; Shan, T; Wang, G; Zhang, Y, 2018) | 0.99 |
" The applications of XNJ combined with NX for ICH show some advantages compared with NX applied individually." | ( Role of Xingnaojing combined with naloxone in treating intracerebral haemorrhage: A systematic review and meta-analysis of randomized controlled trials. Hei, SY; Li, HY; Liang, WX; Ma, YZ; Wang, Q; Wang, XC; Wen, ZH; Xu, TT; Xu, YM; Zhang, SJ, 2018) | 0.76 |
"The effectiveness and safety of XNJ combined with NX for ICH cannot be determined due to the low quality of literature, publication bias and heterogeneity." | ( Role of Xingnaojing combined with naloxone in treating intracerebral haemorrhage: A systematic review and meta-analysis of randomized controlled trials. Hei, SY; Li, HY; Liang, WX; Ma, YZ; Wang, Q; Wang, XC; Wen, ZH; Xu, TT; Xu, YM; Zhang, SJ, 2018) | 0.76 |
"We aimed to evaluate immune-stimulatory effects of naloxone (NLX), an opioid receptor antagonist, in combination with alum in mice vaccinated with excretory-secretory antigens (E/S) of Fasciola hepatica." | ( A Survey on the Adjuvant Role of Naloxone Alone or Combined with Alum in Vaccination Against Fasciolosis in BALB/c Mice. Azizi, H; Bagheri, A; Bazi, A; Elikaee, S; Khamesipour, A; Khatami, M; Mirzaeei, H; Mirzapour, A; Yaghoobi, H, 2019) | 1.05 |
"To study the effect of epidural infusion of morphine combined with small-dose naloxone on gastrointestinal interstitial cells of Cajal (ICC) in rabbits." | ( Effects of epidural infusion of morphine combined with small-dose naloxone on gastrointestinal interstitial cells of Cajal in rabbits. Li, YH; Luo, H; Yang, H, 2019) | 0.98 |
"Epidural infusions of morphine combined with small-dose naloxone effectively inhibit the gastrointestinal motility of rabbits via the reduction of ICC in the proximal colon of the gastrointestinal tract of rabbits." | ( Effects of epidural infusion of morphine combined with small-dose naloxone on gastrointestinal interstitial cells of Cajal in rabbits. Li, YH; Luo, H; Yang, H, 2019) | 1 |
" The present research was conducted to observe the clinical efficacy of puerarin combined with naloxone in the treatment of traumatic cerebral infarction (TCI)." | ( Clinical efficacy and CT perfusion of puerarin combined with naloxone in the treatment of traumatic cerebral infarction. Houfa, N; Lubo, L; Sulin, N; Zhimei, D, 2020) | 1.02 |
"To analyze the clinical efficacy of naloxone combined with acyclovir in the treatment of children viral encephalitis and the impacts on inflammatory factors IL-1 and IL-6." | ( Observation of the efficacy of naloxone combined with acyclovir in the treatment of children viral encephalitis and its impacts on IL-1 and IL-6. Li, XY; Liu, CX; Niu, L; Yang, G; Yu, M; Zhao, XZ, 2020) | 1.12 |
" They were divided into control group (45 cases treated with acyclovir) and observation group (51 cases treated with acyclovir combined with naloxone)." | ( Observation of the efficacy of naloxone combined with acyclovir in the treatment of children viral encephalitis and its impacts on IL-1 and IL-6. Li, XY; Liu, CX; Niu, L; Yang, G; Yu, M; Zhao, XZ, 2020) | 1.05 |
"In the treatment of children, viral encephalitis has naloxone combined with ganciclovir had a more significant effect on the decrease of levels of serum IL-1 and IL-6; naloxone combined with acyclovir in the treatment of children viral encephalitis had better effects, lower adverse reactions and lower prevalence of sequelae compared with sole medication, which is worth clinical promotion." | ( Observation of the efficacy of naloxone combined with acyclovir in the treatment of children viral encephalitis and its impacts on IL-1 and IL-6. Li, XY; Liu, CX; Niu, L; Yang, G; Yu, M; Zhao, XZ, 2020) | 1.09 |
"The aim of this study was to systematically evaluate the efficacy and prognosis of acyclovir combined with naloxone in the treatment of patients with viral encephalitis (VE)." | ( Acyclovir Combined with Naloxone in the Treatment of Viral Encephalitis: A Meta-Analysis. Wang, W; Zhang, Q; Zhao, Q, 2022) | 1.24 |
" The treatment group was treated with acyclovir combined with naloxone, and the control group was treated with acyclovir alone." | ( Acyclovir Combined with Naloxone in the Treatment of Viral Encephalitis: A Meta-Analysis. Wang, W; Zhang, Q; Zhao, Q, 2022) | 1.27 |
The mean absolute bioavailability of naloxone from the orally administered PR tablets was very low, ranging from 0.5% to 10%. The low oral bioavailability makes the precipitation of the acute opioid withdrawal symptoms unlikely following oral oxycodone/nalox one exposure.
Excerpt | Reference | Relevance |
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" The similarity of this behavior to that seen after systemic administration to experimental animals of exogenous neuroleptics suggests that a disturbance in the bioavailability of this neuropeptide to receptor sites in brain-perhaps due to lack of enzymatic cleavage from the circulating parent hormone, beta-lipotropin--may be an etiological factor in those psychopathological states for which the exogenous neuroleptics exert an ameliorative influence." | ( The C-fragment of beta-lipotropin: an endogenous neuroleptic or antipsychotogen? Jacquet, YF; Marks, N, 1976) | 0.26 |
" 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 |
" First-pass glucuronidation limits systemic bioavailability of oral naloxone." | ( Treatment of opioid-induced constipation with oral naloxone: a pilot study. Culpepper-Morgan, JA; Foley, K; Houde, RW; Inturrisi, CE; Kreek, MJ; Marsh, F; Portenoy, RK, 1992) | 0.77 |
" Ocular bioavailability of morphine is higher than after non-parenteral routes." | ( Systemic morphine pharmacokinetics after ocular administration. Bardin, C; Callaert, S; Chast, F; Chaumeil, JC; Sauvageon-Martre, H, 1991) | 0.28 |
" These preclinical data support its use as an antipsychotic agent and show that it is well absorbed following oral administration with an apparent elimination half-life of approximately 24 h, supporting a once-daily dose regimen." | ( Bromperidol, a new butyrophenone neuroleptic: a review. Dubinsky, B; Janssen, PA; McGuire, JL; McKenzie, BE; Niemegeers, CJ; Weintraub, HS, 1982) | 0.26 |
" Although naloxone is poorly absorbed after oral administration, there was a positive response during oral as well as intravenous treatment, suggesting that the primary effect of naloxone is at specific opiate receptor sites in the myenteric plexus and other neural and endocrine cells of the intestinal wall." | ( Naloxone, a specific opioid antagonist, reverses chronic idiopathic constipation. Fishman, J; Hahn, EF; Kreek, MJ; Schaefer, RA, 1983) | 2.11 |
" 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 |
" We conclude (a) that therapeutic doses of codeine increase net intestinal absorption (and thereby reduce stool volume) by increasing the contact time of luminal fluid with mucosal cells, not by increasing the rate of absorption by the mucosal cells; and (b) that endogenous opiates do not regulate intestinal absorption in humans." | ( Studies of the mechanism of the antidiarrheal effect of codeine. Davis, GR; Fordtran, JS; Morawski, SG; Santa Ana, CA; Schiller, LR, 1982) | 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) | 0.5 |
"22 GHz with a peak specific absorption rate of 420 W/kg and corresponding incident power density of 15 mW/cm2 for 15 min or sham-exposed." | ( Electromagnetic millimeter waves increase the duration of anaesthesia caused by ketamine and chloral hydrate in mice. Rojavin, MA; Ziskin, MC, 1997) | 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) | 0.83 |
" Enteral administration of naloxone blocks opioid action at the intestinal receptor level but has low systemic bioavailability due to marked hepatic first-pass metabolism." | ( Oral naloxone reverses opioid-associated constipation. Hartmann, M; Kath, R; Meissner, W; Reinhart, K; Schmidt, U, 2000) | 1.12 |
"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 |
" Buprenorphine and naloxone bioavailability was approximately 40 and 10%, respectively." | ( Buprenorphine and naloxone co-administration in opiate-dependent patients stabilized on sublingual buprenorphine. Harris, DS; Jones, RT; Lin, E; Mendelson, J; Upton, RA; Welm, S, 2000) | 0.97 |
"Due to low central nervous system (CNS) bioavailability of delta-opioid peptides, little is known about the effect of systemic administration of delta-opioid receptor ligands." | ( Spinal delta-opioid receptors mediate suppression of systemic SNC80 on excitability of the flexor reflex in normal and inflamed rat. Cao, CQ; Dray, A; Hong, Y; Perkins, M, 2001) | 0.31 |
" Initiation of oral administration of an orally bioavailable opiate antagonist may precipitate a florid opioid-withdrawal-like reaction in patients with pruritus complicating cholestasis." | ( Opiate antagonist therapy for the pruritus of cholestasis: the avoidance of opioid withdrawal-like reactions. Bergasa, NV; Jones, EA; Neuberger, J, 2002) | 0.31 |
" The addition of naloxone does not affect the efficacy of buprenorphine for two reasons: (1) naloxone is poorly absorbed sublingually relative to buprenorphine and (2) the half-life for buprenorphine is much longer than for naloxone (32 vs." | ( Pharmacokinetics of the combination tablet of buprenorphine and naloxone. Chiang, CN; Hawks, RL, 2003) | 0.9 |
" Naloxone did not change the bioavailability or effects of the buprenorphine 16 mg tablet." | ( Pharmacokinetics and subjective effects of sublingual buprenorphine, alone or in combination with naloxone: lack of dose proportionality. Harris, DS; Jones, RT; Lin, ET; Mendelson, JE; Upton, RA, 2004) | 1.45 |
" Buprenorphine has significant sublingual bioavailability and a long half-life, making administration on a less than daily basis possible." | ( Buprenorphine-containing treatments: place in the management of opioid addiction. Robinson, SE, 2006) | 0.33 |
" 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 |
" Naloxone, an opiate antagonist, is very poorly absorbed with sublingual administration, but if it is injected intravenously, it will antagonise the effects of buprenorphine." | ( Buprenorphine + naloxone: new combination. Opiate dependence: no proof of reduced risk of self-administered injection. , 2007) | 1.6 |
" Relative bioavailability of intramuscular and intranasal naloxone was 36% and 4%, respectively." | ( Population pharmacokinetics of intravenous, intramuscular, and intranasal naloxone in human volunteers. Dowling, J; Graudins, A; Isbister, GK; Kirkpatrick, CM; Naidoo, D, 2008) | 0.82 |
" Treatments were considered bioequivalent if the 90% CIs for relative bioavailability calculations fell within a predetermined range of 80% to 125%." | ( Single- and multiple-dose pharmacokinetic evaluation of oxycodone and naloxone in an opioid agonist/antagonist prolonged-release combination in healthy adult volunteers. Bailey, P; Grothe, B; Hopp, M; Leyendecker, P; Mundin, G; Reimer, K; Smith, K; Uhl, R, 2008) | 0.58 |
" These findings suggest that the coadministration of oxycodone PR and naloxone PR in an FDC would not significantly affect the bioavailability of either of its constituents in these subjects." | ( Single- and multiple-dose pharmacokinetic evaluation of oxycodone and naloxone in an opioid agonist/antagonist prolonged-release combination in healthy adult volunteers. Bailey, P; Grothe, B; Hopp, M; Leyendecker, P; Mundin, G; Reimer, K; Smith, K; Uhl, R, 2008) | 0.81 |
"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) | 0.83 |
" Oxycodone displays high bioavailability after oral administration and may be better than morphine in patients with renal impairment due to the decreased production of active metabolites." | ( Role of oxycodone and oxycodone/naloxone in cancer pain management. Leppert, W, ) | 0.41 |
"2 mg naloxone for bioavailability assessment)." | ( The pharmacodynamic and pharmacokinetic profile of intranasal crushed buprenorphine and buprenorphine/naloxone tablets in opioid abusers. Lofwall, MR; Middleton, LS; Moody, DE; Nuzzo, PA; Walsh, SL, 2011) | 1.1 |
" Buprenorphine bioavailability was 38-44% and T(max) was 35-40 minutes after all intranasal doses." | ( The pharmacodynamic and pharmacokinetic profile of intranasal crushed buprenorphine and buprenorphine/naloxone tablets in opioid abusers. Lofwall, MR; Middleton, LS; Moody, DE; Nuzzo, PA; Walsh, SL, 2011) | 0.58 |
" Greater bioavailability and faster onset of pharmacodynamic effects compared to sublingual administration suggests a motivation for intranasal misuse in non-dependent opioid abusers." | ( The pharmacodynamic and pharmacokinetic profile of intranasal crushed buprenorphine and buprenorphine/naloxone tablets in opioid abusers. Lofwall, MR; Middleton, LS; Moody, DE; Nuzzo, PA; Walsh, SL, 2011) | 0.58 |
" To determine in vivo transdermal absorption rate of naloxone, the iontophoretic patch system was applied to the dorsal skin of conscious rat with a constant current supply for 24h." | ( In vitro and in vivo transdermal iontophoretic delivery of naloxone, an opioid antagonist. Ito, M; Kanamura, K; Kato, Y; Kinoshita, M; Kominami, K; Mafune, S; Sutoh, C; Takasuga, S; Yamamoto, R; Yamauchi, M; Yoshida, Y, 2012) | 0.87 |
"To determine the absolute bioavailability of naloxone from oral doses ranging from 5 mg to 120 mg." | ( Low absolute bioavailability of oral naloxone in healthy subjects. Bailey, P; Bell, D; Bond, S; Hopp, M; Mundin, G; Smith, K; Woodward, J, 2012) | 0.91 |
"The mean oral absolute bioavailability of naloxone in this study was ≤ 2% at doses ranging from 5 mg to 120 mg." | ( Low absolute bioavailability of oral naloxone in healthy subjects. Bailey, P; Bell, D; Bond, S; Hopp, M; Mundin, G; Smith, K; Woodward, J, 2012) | 0.92 |
"The rate of absorption of oxycodone from OXN PR tablets correlated well with the in vitro release rates, demonstrating that a Level A IVIVC with internal predictability has been successfully developed for OXN PR tablets." | ( Validated in vitro/in vivo correlation of prolonged-release oxycodone/naloxone with differing dissolution rates in relation to gastrointestinal transit times. Hahn, U; Heun, G; Krämer, M; Leuner, C; Mundin, GE; Mysicka, J; Smith, KJ, 2012) | 0.61 |
"The combined decrease in Ago2 and increases in Nurr1 and Pitx3 might represent some of the mechanisms that served to protect against accumbal TH regulation observed in morphine withdrawn rats, which may be critical for DA bioavailability to influence behaviour." | ( Morphine administration modulates expression of Argonaute 2 and dopamine-related transcription factors involved in midbrain dopaminergic neurons function. García-Pérez, D; Laorden, ML; Milanés, MV; Núñez, C; Sáez-Belmonte, F, 2013) | 0.39 |
" The new fluorinated inhibitor showed higher analgesic activity and bioavailability compared to thiorphan and C20 when administered by both intravenous and intrathecal injections." | ( NESS002ie: a new fluorinated thiol endopeptidase inhibitor with antinociceptive activity in an animal model of persistent pain. Lazzari, P; Olimpieri, F; Pinna, GA; Reali, R; Tambaro, S; Volonterio, A; Zanda, M, 2013) | 0.39 |
" The aim of this formulation is to counteract opioid-induced constipation through the local antagonist effect of naloxone in the gut wall, while maintaining analgesia due to the low bioavailability of oral naloxone." | ( Oxycodone/Naloxone prolonged-release: a review of its use in the management of chronic pain while counteracting opioid-induced constipation. Burness, CB; Keating, GM, 2014) | 1.02 |
" The low oral bioavailability (< 2%) of naloxone makes the precipitation of the acute opioid withdrawal symptoms unlikely following oral oxycodone/naloxone exposure." | ( Oxycodone/naloxone preparation can cause acute withdrawal symptoms when misused parenterally or taken orally. Graudins, A; Greene, SL; Koutsogiannis, Z; Macleod, D; Robinson, J; Wong, A, 2015) | 1.09 |
" The only published study of pharmacokinetics and bioavailability finds that nasal naloxone has poor bioavailability." | ( Clinical provision of improvised nasal naloxone without experimental testing and without regulatory approval: imaginative shortcut or dangerous bypass of essential safety procedures? Day, E; McDonald, R; Strang, J; Tas, B, 2016) | 0.93 |
" Evidence of adequate bioavailability and acceptable pharmacokinetic curves are vital preliminary steps, especially when effective approved formulations exist." | ( Clinical provision of improvised nasal naloxone without experimental testing and without regulatory approval: imaginative shortcut or dangerous bypass of essential safety procedures? Day, E; McDonald, R; Strang, J; Tas, B, 2016) | 0.7 |
" In this study we examined the effects of ([d-Ala(2)]-Endomorphin 2, TAPP), a synthetic opioid μ-receptor agonist, on blood pressure (MABP), tissue NO bioavailability and renal hemodynamics and excretion." | ( An endomorphine analog ([d-Ala(2)]-Endomorphin 2, TAPP) lowers blood pressure and enhances tissue nitric oxide in anesthetized rats. Kompanowska-Jezierska, E; Kuczeriszka, M; Lipkowski, AW; Sadowski, J, 2016) | 0.43 |
"Exploratory analysis identified intranasal bioavailability as associated positively with dose and negatively with volume." | ( International patent applications for non-injectable naloxone for opioid overdose reversal: Exploratory search and retrieve analysis of the PatentScope database. Dale, O; Danielsson Glende, Ø; McDonald, R; Strang, J, 2018) | 0.73 |
"We find consistent direction of development of intranasal sprays to high-concentration, low-volume formulations with bioavailability in the 20-60% range." | ( International patent applications for non-injectable naloxone for opioid overdose reversal: Exploratory search and retrieve analysis of the PatentScope database. Dale, O; Danielsson Glende, Ø; McDonald, R; Strang, J, 2018) | 0.73 |
" On the basis of plasma concentrations of compound 1 and SN38 (14), the oral bioavailability of compound 3a and 15 in beagle dogs was found to be 97." | ( Oral Delivery of Propofol with Methoxymethylphosphonic Acid as the Delivery Vehicle. Chu, H; Gao, Q; Gong, A; Huang, Q; Huang, X; Lei, B; Li, P; Li, Y; Liao, P; Liu, J; Lu, Y; Luo, X; Ni, J; Qian, G; Qin, L; Qiu, G; Tang, P; Wei, Y; Yan, P; Yu, Y; Zhang, C; Zhang, X; Zheng, S; Zhou, Y; Zhu, G, 2017) | 0.46 |
" We compared the bioavailability and pharmaceutical properties of BNX-RDT with conventional buprenorphine/naloxone sublingual tablets (BNX)." | ( Pharmacokinetic and pharmaceutical properties of a novel buprenorphine/naloxone sublingual tablet for opioid substitution therapy versus conventional buprenorphine/naloxone sublingual tablet in healthy volunteers. Jönsson, M; Mundin, G; Sumner, M, 2018) | 0.93 |
" These include pre-filled syringes and auto-injectors and, crucially, new concentrated nasal sprays (four formulations recently approved in different countries) with speed of onset comparable to intramuscular naloxone and relative bioavailability of approximately 40-50%." | ( Take-Home Naloxone for the Emergency Interim Management of Opioid Overdose: The Public Health Application of an Emergency Medicine. Campbell, G; Dale, O; Degenhardt, L; McDonald, R; Nielsen, S; Ritter, A; Strang, J, 2019) | 1.1 |
"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 |
" The study aimed to investigate the bioavailability and absorption pattern for a new naloxone nasal spray." | ( Naloxone nasal spray - bioavailability and absorption pattern in a phase 1 study. Dale, O; Nilsen, T; Skarra, S; Skulberg, AK; Tylleskar, I, 2019) | 2.18 |
" We examined the bioavailability of an investigational 5 mg intramuscular naloxone in a prefilled syringe (PFS) compared to 2 mg intramuscular naloxone in an autoinjector (AI) at the current approved dose in a crossover design which included 14 healthy subjects." | ( An open-label, randomized, single-dose, two-period, two-treatment crossover bioavailability study comparing 5 mg/0.5 mL of intramuscular naloxone hydrochloride to 2 mg/0.4 mL intramuscular naloxone hydrochloride autoinjector in healthy subjects. Carleton, F; Carlo, DJ; Lollo, CP; Moss, RB, ) | 0.56 |
" Additionally, because of the very low oral bioavailability of naloxone, an oral formulation is not currently available." | ( Novel Oral Nanoparticle Formulation of Sustained Release Naloxone with Mild Withdrawal Symptoms in Mice. Arora, M; Eitan, S; Kumar, MNVR; Madison, CA, 2020) | 1.04 |
" This study investigates the bioavailability and the opioid-like activity of this peptide after its oral administration." | ( Implication of Opioid Receptors in the Antihypertensive Effect of a Novel Chicken Foot-Derived Peptide. Aragonès, G; Arola-Arnal, A; Bravo, FI; Iglesias-Carres, L; Mas-Capdevila, A; Muguerza, B, 2020) | 0.56 |
" Approved formulations of nasal naloxone with bioavailability of approximately 50% have only undergone trials in healthy volunteers, while off-label nasal sprays with low bioavailability have been studied in patients." | ( NTNU intranasal naloxone trial (NINA-1) study protocol for a double-blind, double-dummy, non-inferiority randomised controlled trial comparing intranasal 1.4 mg to intramuscular 0.8 mg naloxone for prehospital use. Braarud, AC; Dale, J; Dale, O; Heyerdahl, F; Mellesmo, S; Skulberg, AK; Tylleskär, I; Valberg, M, 2020) | 1.19 |
" However, in patients with hepatic impairment, porto-systemic shunting can increase systemic bioavailability of naloxone, potentially compromising the analgesic efficacy of oral naloxone-oxycodone combinations." | ( Oxycodone/naloxone prolonged-release tablets in patients with moderate-to-severe, chronic cancer pain: Challenges in the context of hepatic impairment. Aggarwal, G; Ahmedzai, S; Douglas, C; Green, M; Le, BH; Nicoll, A, 2022) | 1.33 |
"Remifentanil has been shown to increase the bioavailability of nasally administered naloxone." | ( The pharmacokinetic interaction between nasally administered naloxone and the opioid remifentanil in human volunteers. Dale, O; Skarra, S; Skulberg, AK; Tylleskar, I, 2021) | 1.09 |
"Remifentanil increases the bioavailability of naloxone after nasal administration by reducing the pre-systemic metabolism of the swallowed part of the nasal dose." | ( The pharmacokinetic interaction between nasally administered naloxone and the opioid remifentanil in human volunteers. Dale, O; Skarra, S; Skulberg, AK; Tylleskar, I, 2021) | 1.12 |
" Because naloxone has relatively low sublingual bioavailability compared with buprenorphine, adverse effects are generally considered mild and rare." | ( The Naloxone Component of Buprenorphine/Naloxone: Discouraging Misuse, but at What Cost? Blazes, C; Gregg, J; Hartley, J; Lawrence, D; Risser, A, ) | 1.11 |
"Due to the poor oral bioavailability of buprenorphine, an oral formulation has not been thought possible." | ( A novel long-acting formulation of oral buprenorphine/naloxone produces prolonged decreases in fentanyl self-administration by rhesus monkeys. Comer, SD; Foltin, RW; Nagaraj, N; Scranton, RE; Sykes, KA; Zale, S, 2022) | 0.97 |
Fentanyl is responsible for the majority of non-fatal opioid overdoses. We compared the concentration of fentanyl in blood to naloxone dosing in the presence and absence of a concurrent sedative-hypnotic exposure.
Excerpt | Relevance | Reference |
---|---|---|
" Dose-response curves for locomotor activity were also determined with morphine and methadone administered intraventricularly." | ( Interactions between narcotic analgesics and benzodiazepine derivatives on behavior in the mouse. Davis, DC; Holtzman, SG; Shannon, HE, 1976) | 0.26 |
" Dose-response data revealed essentially the same ED50's for naloxone in both tests." | ( Antagonism by naloxone of morphine-induced single-dose dependence and antinociception in mice. Smits, SE, 1976) | 0.86 |
" Dose-response curves were determined for chlorpromazine (0." | ( Failure of naloxone to modify the effects of chlorpromazine and d-amphetamine on avoidance behavior in the squirrel monkey. Holtzman, SG, 1979) | 0.65 |
" A simple dose-response relationship was not observed, with the most potent effects exerted by the 1 mg/kg dose." | ( Effect of naloxone on the behaviour of rats exposed to a novel environment. Deacon, RM; Rodgers, RJ, 1979) | 0.66 |
"1 Dose-response curves for normorphine in the absence and presence of naloxone have been obtained from myenteric plexus-longitudinal muscle strip preparations from normal and morphine pretreated guinea-pigs." | ( Opiate binding and effect in ileum preparations from normal and morphine pretreated guinea-pigs. Cox, BM; Padhya, R, 1977) | 0.49 |
" Two populations of units were observed in the latter group: two-thirds of cells showed a dose-response curve similar to that of the non-pretreated group whereas the remaining one-third were unaffected either by morphine or naloxone." | ( The depressive effects of morphine on the C fibre response of dorsal horn neurones in the spinal rat pretreated or not by pCPA. Besson, JM; Guilbaud, G; Le Bars, D; Menetrey, D; Rivot, JP, 1979) | 0.44 |
" The three diarrheal agents, administered intraperitoneally, showed dose-dependent and parallel dose-response curves with the following order of decreasing potency: PGF2 alpha, methacholine and 5-HTP." | ( Naloxone reversal of drug-induced diarrhea in mice. Bertermann, RE; Dajani, EZ; Roge, EA; Schweingruber, FL; Woods, EM, 1979) | 1.7 |
" Naloxone (5-500 microgram/kg) uniformly produced a dose dependent, parallel shift of the morphine dose-response curves to right." | ( A dose ratio comparison of the interaction between morphine and cyclazocine with naloxone in rhesus monkeys on the shock titration task. Rudy, TA; Yaksh, TL, 1977) | 1.39 |
"Twenty opioids have been subdivided into four classes by using flurothyl-induced seizures in rats to measure dose-response relationships, stereospecificity, naloxone sensitivity, and tolerance-cross-tolerance." | ( Classification of opioids on the basis of change in seizure threshold in rats. Adler, MW; Cowan, A; Geller, EB, 1979) | 0.46 |
" dose-response relationships induced by repeated opioid administration." | ( Quantitative assessment of tolerance to and dependence on morphine in mice. Coper, H; Fernandes, M; Kluwe, S, 1977) | 0.26 |
") dosing produced only a slight cross-tolerance to the rate-decreasing effects of anileridine and alphaprodine." | ( Comparing the effects of anileridine, alphaprodine and fentanyl on schedule-controlled responding by pigeons. Leander, JD, 1978) | 0.26 |
" In the rats, naloxone administered systemically in doses of 10--100 microgram/kg produced a parallel shift in the dose-response curves of both nociceptive measures suggesting a competitive antagonism." | ( Antinociceptive effects of intrathecally administered human beta-endorphin in the rat and cat. Henry, JL; Yaksh, TL, 1978) | 0.62 |
" Naloxone caused a parallel shift to the right of the dose-response curve for morphine." | ( Inhibition by morphine of prostaglandin-stimulated fluid secretion in rat jejunum. Coupar, IM, 1978) | 1.17 |
"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) | 0.48 |
" The drug was found to be effective and safe for a wide range of ungulates and pachyderms and Burchell's zebra (Equus burchelli) did not react to expected dosage levels." | ( Immobilisation of free-ranging wild animals using a new drug. De Vos, V, 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 |
" Subjects in the Medium Naloxone group demonstrated an apparent avoidance of the lever, suggesting that the morphine infusions were aversive at this dosage level of naloxone." | ( Morphine-based secondary reinforcement: effects of different doses of naloxone. Carnathan, G; Cochin, J; Marcus, R; Meyer, RE, 1976) | 0.8 |
" Cumulative dose-response curves for morphine and for morphine after naloxone yielded the value pA2=6." | ( Miosis and fluctuation in the rabbit pupil: effects of morphine and naloxone. Adler, MW; Kester, RA; Kramer, MS; Murray, RB; Roy, JW; Tallarida, RJ, 1977) | 0.73 |
"A biphasic dose-response pattern is generated by the isoquinoline, 3-carboxysalsolinol, in analgesia tests conducted in mice." | ( Analgesic effects of 3-carboxysalsolinol alone and in combination with morphine. Blum, K; Hirst, M; Marshall, A, 1977) | 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 |
" The analgesia dose-response curves for the surrogate pairs, nalodeine-nalorphine and codeine-morphine, were parallel but had significantly different slopes." | ( A comparative study of the analgesic and respiratory effects of N-allylnorcodeine (nalodeine), nalorphine, codeine and morphine. Elliott, HW; Rundlett Beyer, J, 1976) | 0.26 |
" Dose-response curves were determined for the effects of morphine (0." | ( Comparison of the effects of morphine, pentazocine, cyclazocine and amphetamine on intracranial self-stimulation in the rat. Holtzman, SG, 1976) | 0.26 |
" Possibly, morphine has a diphasic dose-response curve with respect to cardiovascular function and, by inference, on brain noradrenergic mechanisms." | ( Effects of morphine on central catecholamine turnover, blood pressure and heart rate in the rat. Gomes, C; Svensson, TH; Trolin, G, 1976) | 0.26 |
" Strength of the conditioned reinforcer, measured in terms of responding on a lever for the stimulus plus infusion of saline solution, was proportional to the unit dosage of morphine employed in pairings of buzzer and drug." | ( Role of conditioned reinforcers in the initiation, maintenance and extinction of drug-seeking behavior. Davis, WM; Smith, SG, ) | 0.13 |
" The shift of the morphine dose-response curve to the right is expressed in terms of dose ratios, which were calculated from the ED50 values for morphine obtained 9 days before, and 1, 8, 15, 22 and 29 days after implantation of the polymer." | ( Preparation and evaluation of a sustained naloxone delivery system in rats. Fishman, J; Foldes, FF; Hahn, EF; Norton, BI; Ronai, A, 1975) | 0.52 |
" 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 |
" It was found that 10 mg of naloxone was sufficient to antagonize wide dosage ranges of etorphine hydrochloride or fentanyl, used in combination with a variety of tranquilizers." | ( An appraisal of naloxone hydrochloride as a narcotic antagonist in the capture and release of wild herbivores. Smuts, GL, 1975) | 0.89 |
" 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 |
" The discriminable ED50 values for both pentazocine and morphine were estimated from dose-response curves and when given in combination (pentazocine ED50 + morphine ED50), more drug-related responding occurred than occurred after either drug (ED50) alone." | ( Stimulus properties of the narcotic antagonist pentazocine: similarity to morphine and antagonism by naloxone. Appel, JB; Greenberg, I; Kuhn, DM, 1976) | 0.47 |
"In a community-based abstinence program, 108 chronic heroin abusers, paroled from Maryland correctional institutions, were administered the narcotic antagonist, naloxone, in escalating 500 mg dosages to a daily maximum dosage of 2,000 mg when either urine analysis indicated narcotic drug use or unexcused absences led to the suspicion of narcotic intake." | ( Contingent naloxone treatment of the narcotic addict: a pilot study. Hanlon, T; Kurland, AA; McCabe, L, 1976) | 0.84 |
" The degree of aversion was related to the maintenance dosage of morphine." | ( Conditioned flavor aversions for assessing precipitated morphine abstinence in rats. Pilcher, CW; Stolerman, IP, 1976) | 0.26 |
" 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 |
" Although both were effective, the dose-response curves were different for NAL and MENK." | ( Naloxone is an inappropriate antagonist of met-enkephalin-modulated superoxide anion release. Haberstok, H; Marotti, T, 1992) | 1.73 |
" Cumulative dose-response curves to D-amphetamine were constructed in separate groups on day 6 or day 8 (0." | ( Effects of naloxone infusion upon spontaneous and amphetamine-induced activity. Holtzman, SG; Jones, DN, 1992) | 0.67 |
" It was confirmed that naloxone and amiphenazole in the dosage range studied do not influence spontaneous respiration in healthy adults." | ( [Development of continuous monitoring of spontaneous respiration in the postoperative phase. 2. Cutaneous oxygen and carbon dioxide partial pressures following i.v. bolus application of fentanyl, buprenorphine, naloxone and amiphenazole in healthy adult s Huttarsch, H; Lehmann, KA; Schroeder, B; Zech, D, 1992) | 0.78 |
" The opioid antagonist naloxone and the alpha-2 adrenergic antagonist idazoxan were given as intrathecal pretreatments at doses chosen to shift the dose-response curves of their corresponding agonist (given alone) 4- to 10-fold to the right; this always resulted in a smaller, but significant (2- to 4-fold) shift in the dose-response curve of the other agonist given alone." | ( Spinal interactions between opioid and noradrenergic agonists in mice: multiplicativity involves delta and alpha-2 receptors. Hylden, JK; Kitto, K; Lei, S; Roerig, SC; Wilcox, GL, 1992) | 0.59 |
" A daily 8-mg SL dosage was sufficient to maintain individuals without producing reports of withdrawal symptoms." | ( Development of buprenorphine for the treatment of opioid dependence. Fudala, PJ; Johnson, RE, 1992) | 0.28 |
" There were no differences between naloxone dosage groups for any measured variables." | ( Release of luteinizing hormone after administration of naloxone in pre- and peripuberal heifers. Bertrand, JK; Byerley, DJ; Kiser, TE; Kraeling, RR, 1992) | 0.81 |
" The dosage used was a 10 mg dose plus 7 mg/hr (total = 94 mg)." | ( Effect of 12-hour infusion of naloxone on mood and cognition in normal male volunteers. Besser, GM; Grossman, A; Martín del Campo, AF; McMurray, RG, 1992) | 0.57 |
" Dose-response curves were obtained either non-cumulatively with morphine alone or cumulatively with morphine alone and in combination with different concentrations of naloxone." | ( Naloxone counteracts the fast development of tolerance to morphine in guinea-pig ileum. Hustveit, O; Oye, I; Setekleiv, J, 1992) | 1.92 |
" Considered together, the site-localization, pharmacologic blocking, and dose-response data support the hypothesis that specific regions of the mPRF can contribute to the long-recognized ability of morphine to inhibit REM sleep and alter respiratory control." | ( Sleep disruption and increased apneas after pontine microinjection of morphine. Baghdoyan, HA; Keifer, JC; Lydic, R, 1992) | 0.28 |
" The mid-points of the dose-response curves for (1)-naloxone and (d)-naloxone were 10 micrograms/kg and 100 micrograms/kg, respectively." | ( Significance of an opiate mechanism in the adjustment of cerebrocortical oxygen consumption and blood flow during hypercapnic stress. Dora, E; Hines, K; Kunos, G; McLaughlin, AC, 1992) | 0.53 |
" Twenty micrograms naloxone caused a similar increase, but 10 micrograms caused only a slight increase that peaked at 30 minutes, suggesting a dose-response of naloxone effect." | ( Increases in cerebral blood flow in rat hippocampus after medial septal injection of naloxone. Endo, Y; Kimura, F; Nishimura, J, 1992) | 0.84 |
"4 mg/ml for morphine and methadone, respectively, were achieved using an ascending dosage schedule." | ( Morphine and methadone dependence in the rat: withdrawal and brain met-enkephalin levels. Olley, JE; Pierce, TL; Tiong, GK, 1992) | 0.28 |
" Morphine dose-response curves at different temperatures (30, 37 or 40 degrees C) from right atria of the rat were obtained." | ( Temperature-dependent effects of morphine on the isolated right atrium. Laorden, ML; Ruiz, F; Valcarcel, MI, 1992) | 0.28 |
" The dose-response relationship was U-shaped." | ( Buprenorphine and gastrointestinal transit in rats: effect of naloxone on the biphasic dose-response curve. Cowan, A, 1992) | 0.52 |
"min/ml and with dosing intervals less than 3 hours." | ( Treatment of opioid-induced constipation with oral naloxone: a pilot study. Culpepper-Morgan, JA; Foley, K; Houde, RW; Inturrisi, CE; Kreek, MJ; Marsh, F; Portenoy, RK, 1992) | 0.54 |
" Opiates display similar dose-response relationships for Na(+)-Ca2+ exchange and its partial reaction, the Ca(2+)-Ca2+ exchange." | ( The effect of opiate agonists and antagonists on Na(+)-Ca2+ exchange in cardiac sarcolemma vesicles. Khananshvili, D; Sarne, Y, 1992) | 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 |
" The present study was designed to examine in rats the temporal and dosage parameters of naloxone-induced potentiation of morphine analgesia and the effect of continuous infusion of naloxone on the analgesic potency of other mu agonists." | ( Increased analgesic potency of mu agonists after continuous naloxone infusion in rats. Holtzman, SG; Paronis, CA, 1991) | 0.75 |
"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 |
" Insulin had no significant influence on the carbachol contractile dose-response curve nor did it affect the cholinergically mediated 'on-contraction' at onset of the electrical stimulus." | ( Modulatory effect of insulin on rat small intestinal motility and peptide release in vitro. Allescher, HD; Classen, M; Schusdziarra, V; Willis, S, 1991) | 0.28 |
" Naloxone antagonized this action of NP and shifted the SPF dose-response curve 4-fold to the left." | ( Opioid and neurokinin activities of substance P fragments and their analogs. Lei, SZ; Lipkowski, AW; Wilcox, GL, 1991) | 1.19 |
" injection of either 37 nmol/kg SP, equimolar dosed SPC or corresponding diluent vehicle." | ( Naloxone blocks conditioned place preference induced by substance P and [pGlu6]-SP(6-11). Gerhardt, P; Hasenöhrl, RU; Huston, JP, 1991) | 1.72 |
" To extend that study, we report herein the results of a dose-response and antagonist challenge experiment." | ( Effects of heroin and naloxone on cerebral blood flow in the conscious rat. Fuller, SA; Stein, EA, 1991) | 0.6 |
" 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 |
" Sprague-Dawley rats were assigned randomly to 10 groups (n = 10) relating to two factors: intensity of injury and dosage of naloxone." | ( Naloxone and experimental spinal cord injury: effect of varying dose and intensity of injury. Black, P; Finkelstein, SD; Gillespie, JA; Markowitz, RS, 1991) | 1.93 |
" Dose-response curves for IT morphine were obtained in the presence of fixed doses (0." | ( Interaction of intrathecal morphine and ST-91 on antinociception in the rat: dose-response analysis, antagonism and clearance. Monasky, MS; Stevens, CW; Yaksh, TL; Zinsmeister, AR, 1990) | 0.28 |
" Naloxone at a dosage of 2 mg/h was infused intravenously for 4 hours, and serum was obtained every 15 minutes for 6 hours." | ( Induction of hypothalamic opioid activity with transdermal estradiol administration in postmenopausal women. D'Amico, JF; Greendale, GA; Judd, HL; Lu, JK, 1991) | 1.19 |
" The dose-response curve for minute ventilation was steeper for morphine-6-glucuronide than for morphine." | ( Antinociceptive and ventilatory effects of the morphine metabolites: morphine-6-glucuronide and morphine-3-glucuronide. Björkman, R; Gong, QL; Hedner, J; Hedner, T; Nordberg, G, 1991) | 0.28 |
" When buprenorphine was administered in the fourth day of morphine addiction, the results demonstrate that the administration of the partial agonist opioid produce a bell-shaped dose-response curve." | ( Buprenorphine: bell-shaped dose-response curve for its antagonist effects. Leza, JC; Lizasoain, I; Lorenzo, P, 1991) | 0.28 |
" ACH dose-response curves for dexamethasone (DM)- and corticosterone (B)-treated but not deoxycorticosterone (DOC)-treated BSM were significantly shifted to the right; this provides evidence that glucocorticoid treatment reduced the sensitivity of BSM to ACH." | ( Effect of acetylcholine and morphine on bronchial smooth muscle contraction and its modulation by steroid hormones. Kadir, BA; Khalid, BA; Morat, PB; Nabishah, BM, 1990) | 0.28 |
" A final study evaluated the dose-response relationship of clonidine-induced erectile dysfunction." | ( Clonidine suppresses copulatory behavior and erectile reflexes in male rats: lack of effect of naloxone pretreatment. Clark, JT; Smith, ER, 1990) | 0.5 |
"A study of the dose-response effects of naloxone and methylprednisolone after rat ventral spinal cord injury is presented." | ( Dose-dependent effects of naloxone and methylprednisolone in the ventral compression model of spinal cord injury. Beal, JA; Benzel, EC; Hoffpauir, GM; Kesterson, L; Lancon, JA; Thomas, MM, 1990) | 0.85 |
" However, a dose-response relationship was not observed." | ( Participation of opiate pathways in the lateral hypothalamic area in the control of renal electrolyte and water excretion. Perez, SE; Silva-Netto, CR; Silveira, JE, 1990) | 0.28 |
" For the DSP4-pretreated mice that received naloxone before training on both days, the dose-response characteristics for retention scores were similar to those of vehicle-pretreated mice; 1 mg/kg naloxone was the facilitatory dose." | ( Interaction between catecholaminergic and opioid systems in an active avoidance task. Bennett, MC; Hock, FJ, 1990) | 0.54 |
" An inactive dose of intrathecally-administered midazolam (20 micrograms) produced a leftward shift in the dose-response curve for intrathecally administered morphine, in the thermal antinociceptive tests." | ( Interaction of midazolam and morphine in the spinal cord of the rat. Sabbe, MB; Stevens, CW; Yaksh, TL; Yanez, A, 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, ) | 0.41 |
"05) by GnRH compared to control, but the dose-response to GnRH was absent." | ( Opioid modulation of LH secretion by pig pituitary cells in vitro. Barb, CR; Barrett, JB; Kraeling, RR; Rampacek, GB; Wright, JT, 1990) | 0.28 |
"The effect of the dosage and timing of administration of naloxone after spinal cord injury in rats via the ventral compression technique is presented." | ( Effect of dosage and timing of administration of naloxone on outcome in the rat ventral compression model of spinal cord injury. Bairnsfather, S; Benzel, EC; Kesterson, L; Lancon, JA, 1990) | 0.78 |
" To establish the safety and efficacy of an anesthetic regimen using intravenous meperidine and diazepam, all endoscopic procedures performed at one teaching institution in a 4-month period were retrospectively analyzed with regard to: (1) type and dosage of sedation/anesthesia, (2) endoscopic procedure involved, (3) effect of any underlying disease state, (4) side effects, (5) endoscopic complications, and (6) overall patient acceptance." | ( Evaluation of safe, effective intravenous sedation for utilization in endoscopic procedures. Andrus, CH; Dean, PA; Ponsky, JL, 1990) | 0.28 |
" Because the dosage and timing of these agents are considered critical factors in their efficacy, we investigated both dosage and timing of naloxone." | ( Naloxone in septic shock. Hackshaw, KV; Parker, GA; Roberts, JW, 1990) | 1.92 |
" 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 |
" gamma E (beta-LPH-(61-77)), beta-endorphin-(1-17)), and DT gamma E (beta-LPH-(62-77), beta-endorphin-(2-17)) were without effect in the dosage used." | ( The effect of gamma-type endorphins on alpha-MSH release in the rat. Andringa-Bakker, EA; de Rotte, AA; de Wied, D; van de Buuse, M; van Wimersma Greidanus, TB, 1985) | 0.27 |
" Mathematic analysis of the dose-response (wheal) relationship suggested that two different effects were involved." | ( Morphine-induced skin wheals: a possible model for the study of histamine release. Erill, S; Saucedo, R, 1985) | 0.27 |
" The study was done in three phases: a training phase in which training drugs were identified to subjects by letter code before the session, a test of acquisition phase in which the subject's ability to identify the training drug by letter code was tested and a generalization phase in which dose-response curves for the two active training drugs were tested." | ( Three-choice drug discrimination in opioid-dependent humans: hydromorphone, naloxone and saline. Bickel, W; Bigelow, GE; Liebson, IA; Preston, KL, 1987) | 0.5 |
" Dose-response curves at 1 hr revealed similar potencies of oxymorphone and the derivatives, with the exception of OxyPNPH which was significantly less potent." | ( Irreversible opiate agonists and antagonists. IV. Analgesic actions of 14-hydroxydihydromorphinone hydrazones. Bodnar, RJ; Burks, TF; Clark, JE; Hahn, EF; Pasternak, GW; Williams, CL, 1988) | 0.27 |
" Physiologic measures and subject- and observer-rated behavioral responses were measured before dosing and for 120 min after drug administration." | ( Buprenorphine and naloxone alone and in combination in opioid-dependent humans. Bigelow, GE; Liebson, IA; Preston, KL, 1988) | 0.61 |
" Physiologic measures and subject- and observer-rated behavioral responses were measured before dosing and for 2 hr after drug administration." | ( Butorphanol-precipitated withdrawal in opioid-dependent human volunteers. Bigelow, GE; Liebson, IA; Preston, KL, 1988) | 0.27 |
" A U-shaped dose-response relation was observed." | ( Beta-endorphin and related peptides suppress phorbol myristate acetate-induced respiratory burst in human polymorphonuclear leukocytes. de Wied, D; Diamant, M; Henricks, PA; Nijkamp, FP, 1989) | 0.28 |
" Medroxyprogesterone acetate was given orally to the 6 study subjects over a 10-day period in an incremental dosage to mimic the luteal phase." | ( Opioidergic regulation of LH pulsatility in women with polycystic ovary syndrome. Berga, SL; Yen, SS, 1989) | 0.28 |
" Antinociception was determined by observing the response to a clamp applied to the tail (Haffner test) in mice and by the tail-flick test in rats; log dose-response curves for antinociception were generated for morphine, clonidine, and each drug combination." | ( Antinociceptive interactions between alpha 2-adrenergic and opiate agonists at the spinal level in rodents. Ossipov, MH; Spaulding, TC; Suarez, LJ, 1989) | 0.28 |
" The latter inhibited GRF-stimulated GH release by shifting the dose-response curve to the right." | ( The synergistic effects of His-D-Trp-Ala-Trp-D-Phe-Lys-NH2 on growth hormone (GH)-releasing factor-stimulated GH release and intracellular adenosine 3',5'-monophosphate accumulation in rat primary pituitary cell culture. Barreto, A; Chan, WW; Cheng, K; Convey, EM; Smith, RG, 1989) | 0.28 |
"In a small clinical trial, a new therapeutic approach was studied, whether naloxone, in high dosage over a prolonged period of time, will attenuate withdrawal symptoms in acute opiate detoxification." | ( Continuous naloxone administration suppresses opiate withdrawal symptoms in human opiate addicts during detoxification treatment. Lenz, K; Loimer, N; Presslich, O; Schmid, RW, 1989) | 0.9 |
" A dosage of 100 mg/kg (-) naloxone, which blocked the opioid receptor for 12-16 hr/day, did not alter body weight in comparison to control levels." | ( Naloxone modulates body and organ growth of rats: dependency on the duration of opioid receptor blockade and stereospecificity. McLaughlin, PJ; Zagon, IS, 1989) | 2.02 |
" Naloxonazine shifted the supraspinal DAGO dose-response curve 4-fold to the right without changing the curve for spinal DAGO." | ( Different mu receptor subtypes mediate spinal and supraspinal analgesia in mice. Bodnar, RJ; Gistrak, MA; Pasternak, GW; Paul, D, 1989) | 0.28 |
" The slopes of the dose-response lines were parallel, but the delta compound was about 250 times less potent than DAMGO." | ( Sympathoadrenal, cardiovascular and blood gas responses to highly selective mu and delta opioid peptides. Kiritsy-Roy, JA; Marson, L; Van Loon, GR, 1989) | 0.28 |
" The dose-response curves are U-shaped, with no detectable effect at low or high concentrations." | ( Phagocytosis in Tetrahymena thermophila: naloxone-reversible inhibition by opiates. De Jesus, S; Renaud, FL, 1989) | 0.54 |
"Pregnant Long-Evans hooded rats were dosed subcutaneously with 1 or 5 mg/kg/day naloxone hydrochloride, or an equal volume of vehicle, from gestational Day 4 (GD4) through GD19." | ( Behavioral and neuroanatomical sequelae of prenatal naloxone administration in the rat. Allen, KS; Royall, GD; Shepanek, NA; Smith, RF; Tyer, ZE, ) | 0.61 |
" We investigated whether naloxone possessed gastric cytoprotective properties, generating a dose-response curve existed for both intragastric (IG) and intravenous (IV) administration." | ( Naloxone exerts a dose-dependent gastric cytoprotective effect. Adair, CG; Ephgrave, KS; Kleiman, RL, 1989) | 2.02 |
" In contrast, the reference NSAIDS (piroxicam, indomethacin, naproxen and ibuprofen) exhibited similar dose-response relationships for the analgesic, anti-inflammatory and gastric irritant effects." | ( Pemedolac: a novel and long-acting non-narcotic analgesic. Chau, TT; Weichman, BM, 1989) | 0.28 |
" Dose-response curves describing the relationship between the duration of balloon inflation and the percentage of animals with a persistent neurologic deficit were constructed and compared for differences by use of a group t test." | ( The effect of fentanyl anesthesia and intrathecal naloxone on neurologic outcome following spinal cord injury in the rat. Brauer, FS; Cole, DJ; Drummond, JC; Hertzog, RE; Shapiro, HM, 1989) | 0.53 |
" All animals reduced their food intake in response to the dietary adulteration, with evidence of a dose-response effect, but this response did not differ as a function of litter size." | ( Effects of early rearing experience on feeding behavior in B6D2F2 mice. Gardner, D; McCutcheon, D; Pelkman, C; Wainwright, PE; Young, C, 1989) | 0.28 |
" The dose-response curves of the preferential mu- ligands morphine and [D-Ala2, MePhe4, Gly-ol5] enkephalin (DAGO) were shifted by naloxone at low doses but not by ICI 174,864." | ( The role of mu- and delta- opioid receptors on the intestinal propulsion in rats. La Regina, A; Petrillo, P; Sbacchi, M; Tavani, A, 1986) | 0.48 |
" After 1 week of treatment and after pump removal, dose-response curves for the induction of antinociception by morphine against noxious heat, pressure and electrical stimulation were shifted to the left across the entire time course of action: this supersensitivity subsided over a period of 1 week postremoval." | ( Antagonist-induced opioid receptor up-regulation. I. Characterization of supersensitivity to selective mu and kappa agonists. Herz, A; Millan, MJ; Morris, BJ, 1988) | 0.27 |
" Slightly conflicting results have been obtained, depending on the dosage of naloxone used." | ( Endorphins: what are they? How are they measured? What is their role in exercise? Grossman, A; Sutton, JR, 1985) | 0.5 |
" The dose-response curves for CCK8 were shifted in parallel to the right by 10(-6) to 10(-5) M of the three benzodiazepines, although the maximum response to CCK8 was depressed by higher concentrations." | ( Cholecystokinin antagonism by benzodiazepines in the contractile response of the isolated guinea-pig gallbladder. Kubota, K; Matsuda, I; Sugaya, K; Sunagane, N; Uruno, T, 1985) | 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) | 0.56 |
" The mu receptor agonists produce a biphasic (primary and secondary slope) dose-response curve (DRC) whereas kappa agonist and mixed agonist/antagonist analgesics produce single-slope DRCs." | ( Antinociceptive profiles of mu and kappa opioid agonists in a rat tooth pulp stimulation procedure. Cook, L; Steinfels, GF, 1986) | 0.27 |
" The dose-response curves were monotonic and the slopes were log-linear." | ( Epidural injections of bupivacaine, morphine, fentanyl, lofentanil, and DADL in chronically implanted rats: a pharmacologic and pathologic study. Durant, PA; Yaksh, TL, 1986) | 0.27 |
" The slopes of the monotonic dose-response curves for the five opioids did not differ significantly." | ( Studies of the pharmacology and pathology of intrathecally administered 4-anilinopiperidine analogues and morphine in the rat and cat. Durant, PA; Noueihed, RY; Yaksh, TL, 1986) | 0.27 |
" (+/-)-Propranolol caused rightward shifts, usually parallel, of the dose-response curves for (-)-isoprenaline." | ( The antinociceptive action of some beta-adrenoceptor agonists in mice. Bentley, GA; Starr, J, 1986) | 0.27 |
" Dose-response curves for the relatively specific ligands for the mu-, kappa-, and sigma-receptors were determined using morphine (mu-receptors), dynorphin-(1-13) (kappa-receptors), and N-allylnormetazocine (sigma-receptors)." | ( Sites of action of mu-, kappa- and sigma-opiate receptor agonists at the feline ileocecal sphincter. Cohen, S; Ouyang, A; Vos, P, 1988) | 0.27 |
" Naloxonazine (10 mg/kg) shifted the morphine hyperphagia dose-response curve to the right." | ( Differential sensitivity of opioid-induced feeding to naloxone and naloxonazine. Arjune, D; Bodnar, RJ; Hahn, EF; Mann, PE; Pasternak, GW; Romero, MT, 1988) | 0.52 |
" The purpose of this study was to examine further this phenomenon in humans by characterizing the antagonist dose-response function." | ( Acute opioid physical dependence in postaddict humans: naloxone dose effects after brief morphine exposure. Bigelow, GE; Heishman, SJ; Liebson, IA; Stitzer, ML, 1989) | 0.52 |
") shifted the dose-response curves to morphine to the right in a parallel manner." | ( Antinociceptive effects of azepexole (BHT 933) in mice. Bansinath, M; Puig, MM; Turndorf, H; Vargas, ML, 1989) | 0.28 |
" The slope of the dose-response curve was steeper after pre-exposure." | ( Behavioral effects of morphine and phencyclidine in rats: the influence of repeated testing before and after single treatment. Leys, A; Van Ree, JM, 1985) | 0.27 |
" one hour before ethanol), caused increases of up to 23-fold in the hepatic acetaldehyde level, without influencing the cytosolic NAD+:NADH ratio in ethanol dosed rats, while significantly reducing the ethanol elimination rate by up to 44%, compared with controls." | ( The roles of the hepatocellular redox state and the hepatic acetaldehyde concentration in determining the ethanol elimination rate in fasted rats. Chakraborty, J; Ryle, PR; Thomson, AD, 1985) | 0.27 |
" These effects were dose related, with the pyloric dose-response profile being essentially linear." | ( Dose-related effects of synthetic human beta-endorphin and naloxone on fed gastrointestinal motility. Camilleri, M; Kao, PC; Li, CH; Malagelada, JR; Stanghellini, V; Zinsmeister, AR, 1986) | 0.51 |
" Complete dose-response data for morphine, heroin, etorphine, d- and l-ethylketazocine, d- and l-pentazocine, and d- and l-N-allylnormetazocine revealed a predominant response of hyperthermia." | ( Body temperature effects of opioids in rats: intracerebroventricular administration. Adler, MW; Geller, EB; Rowan, CH, 1986) | 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 |
" Full dose-response curves show a 4-fold shift to the right (P less than ." | ( Separation of opioid analgesia from respiratory depression: evidence for different receptor mechanisms. Ling, GS; Lockhart, SH; Pasternak, GW; Spiegel, K, 1985) | 0.27 |
" Antagonism by competition at same opioid receptor subtypes is suggested from parallel shifts of the dose-response curve of etorphine or beta h-EP in the presence of increasing doses of beta h-EP-(1-28)." | ( Inhibition of analgesia by C-terminal deletion analogs of human beta-endorphin. Li, CH; Nicolas, P, 1985) | 0.27 |
" Naltrexone, naloxone, nalorphine, and morphine (in this order of decreasing potency) bind to the lambda site in vivo in intact rat brain over dosage ranges that are commonly employed in pharmacological studies." | ( Characterization of a labile naloxone binding site (lambda site) in rat brain. Grevel, J; Sadée, W; Yu, V, 1985) | 0.93 |
" Antagonism by competition at the same site(s) is suggested from parallel shifts of the dose-response curves of etorphine or beta-endorphin in the presence of beta-endorphin-(1-27)." | ( Beta-endorphin-(1-27) is a naturally occurring antagonist to etorphine-induced analgesia. Li, CH; Nicolas, P, 1985) | 0.27 |
" But a number of kappa agonists, including bremazocine, tifluadom, ethylketocyclazocine, ketocyclazocine, U-50,488 and Win 42,610 all depressed contractions, producing parallel dose-response curves." | ( Profile of activity of kappa receptor agonists in the rabbit vas deferens. Hayes, A; Kelly, A, 1985) | 0.27 |
" The dose-response curves for the biological response were suggestive of positive cooperativity and systematically occurred at lower ligand concentrations than those for the binding of [3H] [D-Ala2, D-Leu5]enkephalin (DADLE), which were instead shallow and suggestive of a site heterogeneity or of a cooperative phenomenon." | ( Multiple states of opioid receptors may modulate adenylate cyclase in intact neuroblastoma X glioma hybrid cells. Costa, T; Gramsch, C; Herz, A; Wüster, M, 1985) | 0.27 |
" In these experiments, dose-response curves were recorded." | ( New models for the evaluation of opioid effects in the guinea-pig ileum. Donnerer, J; Lembeck, F, 1985) | 0.27 |
" Cannabinol (CBN) showed the same activity but required a dosage of approximately eight times that of THC to produce an equivalent effect." | ( The quasi-morphine withdrawal syndrome: effect of cannabinol, cannabidiol and tetrahydrocannabinol. Chesher, GB; Jackson, DM, 1985) | 0.27 |
" There were significant falls in systolic blood pressure during captopril dosing alone, but there was no fall in blood pressure during combination therapy." | ( Effect of naloxone on the actions of captopril. Ajayi, AA; Campbell, BC; Reid, JL; Rubin, PC, 1985) | 0.67 |
" Experiment 1 established a dose-response function for inhibition of intake by naloxone (NAL) in short (60 min) 2-bottle tests." | ( Opiate blockade inhibits saccharin intake and blocks normal preference acquisition. Lynch, WC, 1986) | 0.5 |
" In post-test locomotor activity determination, an apparent dose-response existed for MSH/ACTH 4-10 with the two highest doses (190 and 285 micrograms/kg) resulting in significantly increased locomotor activity." | ( The effect of MSH/ACTH 4-10 on delayed response performance and post-test locomotor activity in rats. Miller, LH; Turnbull, BA, ) | 0.13 |
" Naloxonazine also shifted full morphine dose-response curves to the right." | ( Antagonism of morphine analgesia by intracerebroventricular naloxonazine. Bodnar, RJ; Pasternak, GW; Portzline, T; Simone, DA, 1986) | 0.27 |
"The dose-response relationship of neonatal (days 1-7) administration of beta-endorphin (BE) and corticotropin-releasing factor (CRF) on body weight, eye opening, response to thermal pain, and concentrations of plasma and adrenal corticosterone were measured in developing rat pups." | ( Neonatal peptides affect developing rats: beta-endorphin alters nociception and opiate receptors, corticotropin-releasing factor alters corticosterone. Kastin, AJ; Zadina, JE, 1986) | 0.27 |
"1 micrograms/kg, ip) exerted effects opposite to those elicited by naloxone, that is, shifted the dose-response curve of clenbuterol to the right." | ( Opioid peptidergic systems modulate the activity of beta-adrenergic mechanisms during memory consolidation processes. Baratti, CM; Introini-Collison, IB, 1986) | 0.51 |
" pairs of time-response curves, pairs of dose-response lines were constructed at various times; these lines showed decreasing displacement with time, indicative of the disappearance of naloxone." | ( Estimation of the affinity of naloxone at supraspinal and spinal opioid receptors in vivo: studies with receptor selective agonists. Heyman, JS; Koslo, RJ; Mosberg, HI; Porreca, F; Tallarida, RJ, 1986) | 0.75 |
" The slope of the analgesic dose-response curve for the highly specific delta agonist, cyclic [D-Penicillamine2, D-Penicillamine5]enkephalin (DPDPE), was significantly different (flatter) from those of mu agonists or DADLE." | ( Continuous intrathecal opioid analgesia: tolerance and cross-tolerance of mu and delta spinal opioid receptors. Chang, KJ; Leslie, JB; Russell, RD; Su, YF; Watkins, WD, 1987) | 0.27 |
" The accumulation of O2- in response to the potent chemotactic peptide formyl-methionine-leucine-phenylalanine was studied and a distinctly different dose-response profile with a peak response at 10(-8) M was observed." | ( Beta-endorphin stimulates human polymorphonuclear leukocyte superoxide production via a stereoselective opiate receptor. Gekker, G; Keane, WF; Peterson, PK; Sharp, BM; Tsukayama, DT, 1987) | 0.27 |
" This effect was time-dependent and dose-dependent, and the usual naloxone dose-response function could be recaptured 1 week after the pretreatment effect was obtained." | ( Effects of acute morphine pretreatment on the rate-decreasing and antagonist activity of naloxone. Young, AM, 1986) | 0.73 |
" The slope of this sigmoid dose-response curve varied with the inspirate; it increased as the concentration of CO2 was higher." | ( Respiratory effects of morphine in awake unrestrained rats. Colpaert, FC; van den Hoogen, RH, 1986) | 0.27 |
", the morphine dose-response curve was shifted to the right." | ( Potentiation of disruptive effects of dextromethorphan by naloxone on fixed-interval performance in rats. Taşkin, T, 1986) | 0.52 |
"The efficacy of two dosage regimens of intravenous naloxone were compared to avoid nonrespiratory side effects and respiratory depression and yet to preserve analgesia (maximum tolerance to periostial pressure over the tibia) after administration of 200 micrograms epidural fentanyl." | ( Effect of naloxone infusion on analgesia and respiratory depression after epidural fentanyl. Benhamou, D; Carli, P; Ecoffey, Cl; Gross, JB; Gueneron, JP, 1988) | 0.93 |
" An ischemia control group received NS, whereas experimental groups were given Nx, SOD, APL, or DEF with the same previous dosage schedule." | ( Experimental pharmacologic cerebroprotection. Donovan, DL; Fink, JA; Pigott, JP; Sharp, WV, 1988) | 0.27 |
" Similarly, chronic dosing with acetorphan after withdrawal produced no significant effect on body weight." | ( Amelioration of naloxone-precipitated opioid withdrawal symptoms by peripheral administration of the enkephalinase inhibitor acetorphan. Livingston, SJ; Rooney, KF; Sewell, RD; Smith, HJ, 1988) | 0.62 |
" Dose-response curves for diprenorphine and naloxone were determined prior to and following chronic administration of 10." | ( Diprenorphine and naloxone in squirrel monkeys with enhanced sensitivity to opioid antagonists. Dykstra, LA; Oliveto, AH, 1988) | 0.87 |
" Therefore, insofar as this dosage of naloxone may be used to examine the functional role of opioid-mediated mechanisms, our findings are not tenable with the hypothesis that endogenous opioids play a role in maintenance of thermal homeostasis during exercise." | ( Effect of opioid antagonism on esophageal temperature during exercise. Gordon, NF; Schwellnus, MP, 1988) | 0.55 |
" Under this dosing schedule, the behavior-suppressing effects of buprenorphine returned to base-line levels within 4 days." | ( Effects of buprenorphine, methadone and naloxone on acquisition of behavioral chains. Cleary, J; Ho, B; Nader, M; Thompson, T, 1988) | 0.54 |
" The severity and the duration of this intoxication are not explained solely by the high dosage of Tramadol." | ( [Acute poisoning with a narcotic (Tramadol) in an infant of five weeks]. Beutler, A; Bianchetti, MG; Ferrier, PE, 1988) | 0.27 |
" Morphine altered dose-response curves for exogenous PGE2, evoking a parallel surmountable shift to the right, but did not affect the inotropic action of added PGF2 alpha." | ( Morphine diminishes the constancy of spontaneous uterine contractions, antagonizes the positive inotropic effects of prostaglandin E2, but not of prostaglandin F2 alpha and inhibits prostaglandin E and F outputs from the uterus of ovariectomized rats. Chaud, MA; Faletti, A; Gimeno, AL; Gimeno, MA, 1988) | 0.27 |
" After establishing a dose-response relationship, we chose a control dose that produced intermediate hypertensive responses." | ( Hemodynamic responses of chronically instrumented piglets to bolus injections of group B streptococci. Barefield, E; Godoy, G; Gray, BM; Graybar, G; Lyrene, RK; Philips, JB; Sams, JE, 1988) | 0.27 |
" Dose-response curves revealed that adult animals were more than 10-fold less sensitive to NMDA than their younger counterparts." | ( Characterization and possible opioid modulation of N-methyl-D-aspartic acid induced increases in serum luteinizing hormone levels in the developing male rat. Bell, RD; Cicero, TJ; Meyer, ER, 1988) | 0.27 |
" The results of this study confirm previous reports of acute physical dependence in man and extend those findings by demonstrating a morphine dose-response function." | ( Acute physical dependence in man: effects of naloxone after brief morphine exposure. Bickel, WK; Bigelow, GE; Liebson, IA; Stitzer, ML, 1988) | 0.53 |
"25-50 micrograms) in ICR mice, which showed a bell-shaped hyperglycemic dose-response relationship and a brief explosive motor behavior at the higher doses (25-50 micrograms)." | ( Differential effects of subcutaneous and intrathecal morphine administration on blood glucose in mice: comparison with intracerebroventricular administration. Brase, DA; Dewey, WL; Lux, F, 1988) | 0.27 |
" Yohimbine, but not naloxone, antagonized the antinociceptive effects of clonidine, whereas both yohimbine and naloxone altered the dose-response function for the effects of clonidine on blood pressure." | ( Intrathecal morphine and clonidine: antinociceptive tolerance and cross-tolerance and effects on blood pressure. Gebhart, GF; Solomon, RE, 1988) | 0.6 |
" In light of these conflicting reports, we have conducted a systematic dose-response analysis of the effects of morphine on FBM in 27 fetal lambs." | ( Dual action of morphine on fetal breathing movements. Amione, J; Clare, S; Dwyer, G; Szeto, HH; Umans, JG; Zhu, YS, 1988) | 0.27 |
" Naloxone at a dosage of 1 mg/kg disinhibited release of LH and abruptly increased serum concentrations of LH in a variety of experimental models." | ( Effects of exogenous estradiol-17 beta and progesterone on naloxone-reversible inhibition of the release of luteinizing hormone in ewes. Malven, PV; Trout, WE, 1987) | 1.43 |
" The dose-response relationship was quadratic, with the greatest reduction in food intake occurring at the 10 mg/kg body weight dose." | ( Naloxone attenuates food but not water intake in Japanese quail. Denbow, DM; McCormack, JF, 1987) | 1.72 |
" In contrast to the above, either morphine or [Met5]enkephalin in subthreshold dosage administrated together with the peptidase inhibitors displayed antinociceptive activity in the two groups of tests." | ( Dissociated effects of inhibitors of enkephalin-metabolising peptidases or naloxone on various nociceptive responses. Aveaux, D; Ben Natan, L; Chaillet, P; Costentin, J; Schwartz, JC; Vlaiculescu, A, 1986) | 0.5 |
" Pharmacokinetic data for drugs administered endotracheally are lacking; therefore, dosage recommendations are empirical." | ( Endotracheal drug therapy in cardiopulmonary resuscitation. Raehl, CL, 1986) | 0.27 |
" Biological, static or dynamic dosage of opioid activity in peripheral liquids, trying to correlate those measures either with a syndrome, or with a clinical trait." | ( [Endorphins. Physiological and pharmacological aspects, and research in psychiatry]. Leboyer, M, ) | 0.13 |
" The acetylcholine dose-response curves for steroid pretreated ileum but not duodenum were significantly shifted to the right; evidence that pretreated ileum required higher dose of acetylcholine than normal to cause 50% maximal contraction." | ( The effect of corticosteroid pretreatment in vivo on the contraction of guinea-pig ileum and duodenum. Alias, AK; Idid, SZ; Khalid, BA; Merican, Z; Morat, P, 1987) | 0.27 |
" To better define the interactions between gamma irradiation and these opiate-mediated phenomena, dose-response studies were undertaken of the effect of irradiation on morphine-induced antinociception, and on the naloxone-precipitated withdrawal syndrome of morphine-dependent rats." | ( Irradiation exposure modulates central opioid functions. Dafny, N; Dougherty, PM, 1987) | 0.46 |
" The slope of the dose-response curves was similar in both strains of rat, but the average response to the same concentrations of clonidine was less in the SHR." | ( Modification of clonidine-induced pressor responses in morphine-dependent and hypophysectomised rats. Conway, EL, 1986) | 0.27 |
" Dose-response and time-course experiments were carried out using both static incubation of paired hemipituitary glands and perifusion of whole glands." | ( Effects of two enkephalin analogues, morphine sulphate, dopamine and naloxone on prolactin secretion from rat anterior pituitary glands in vitro. Bentley, AM; Wallis, M, 1986) | 0.51 |
" After bleeding so that arterial pressure fell to 40 mmHg, the dose-response relationship for naloxone had two components." | ( Factors influencing the effects of intravenous naloxone on arterial pressure and heart rate after haemorrhage in conscious rabbits. Ludbrook, J; Potocnik, SJ; Rutter, PC, 1986) | 0.75 |
" At t = 120 minutes, IV fluid administration was begun (all dogs) and continued for 1 hour (lactated Ringer's solution at a dosage of 70 ml/kg/hr)." | ( Effects of naloxone in treating hemorrhagic shock in dogs with maintained baroreceptor responsiveness. Gross, DR; Wagner-Mann, CC, 1986) | 0.66 |
"The role of the increased hepatocellular redox-state [( NADH]/[NAD+] ratio) as a mechanism underlying hepatic triglyceride deposition after acute ethanol dosing has been investigated in the rat." | ( The role of the hepatocellular redox state in the hepatic triglyceride accumulation following acute ethanol administration. Chakraborty, J; Ryle, PR; Thomson, AD, 1986) | 0.27 |
" ED50 values were derived from the dose-response lines." | ( Intrathecal injection of codeine, buprenorphine, tilidine, tramadol and nefopam depresses the tail-flick response in rats. Bernatzky, G; Jurna, I, 1986) | 0.27 |
" Morphine analgesic effect during subchronic dosage (50 mg/kg a day) was gradually decreased." | ( Stimulation-produced analgesia under repeated morphine treatment in rats. Morozova, AS; Zvartau, EE, 1986) | 0.27 |
" Dose-response curves for the convulsive effect of pentylenetetrazol obtained at the peak of the withdrawal signs shifted greatly to the left in alcohol withdrawn animals but less in barbital withdrawn animals." | ( Differentiation of alcohol and barbital physical dependence. Kaneda, H; Kaneto, H; Kawatani, S, 1986) | 0.27 |
" Accordingly, opiate receptors sensitive to naloxone in a moderate dosage seem not to be involved in the cardiovascular response and the increase in plasma catecholamines, PRA and plasma aldosterone induced by exercise." | ( Lack of effect of naloxone in a moderate dosage on the exercise-induced increase in blood pressure, heart rate, plasma catecholamines, plasma renin activity and plasma aldosterone in healthy males. Bramnert, M; Hökfelt, B, 1985) | 0.86 |
" Most importantly, however, we showed that the GPT-LHRH produced equivalent, parallel shifts to the right in the dose-response curves for LHRH and naloxone, indicative of competitive inhibition." | ( Luteinizing hormone releasing hormone mediates naloxone's effects on serum luteinizing hormone levels in normal and morphine-sensitized male rats. Cicero, TJ; Meyer, ER; Miller, BT; Schmoeker, PF, 1985) | 0.73 |
"The dose-response of serum prolactin (PRL) values to different doses of naloxone (NAL) in rats is bellshaped." | ( Effect of different doses of naloxone on serum levels of prolactin and gonadotropins in young male volunteers. Knuth, UA; Nieschlag, E, 1985) | 0.79 |
" Schedule-controlled responding was disrupted when morphine maintenance was abruptly discontinued but not when the maintenance dosage was gradually reduced to zero." | ( Behavioral effects of naloxone and nalorphine preceding and following morphine maintenance in the rhesus monkey. Bergman, J; Schuster, CR, 1985) | 0.58 |
" The degree of drug tolerance was assessed by determining cumulative dose-response functions for morphine before, during and after chronic administration." | ( Modification of morphine tolerance by behavioral variables. Sannerud, CA; Young, AM, 1986) | 0.27 |
" Due to naloxone's short half life and a long duration of action of most opioids, repeated naloxone dosing often is required to prevent the recurrence of respiratory depression." | ( A dosing nomogram for continuous infusion intravenous naloxone. Errick, JK; Goldfrank, L; Lo, MW; Weisman, RS, 1986) | 0.95 |
" The N-methyl-quaternary analog of naloxone (methylnaloxone, which presumably entails selective action at opiate receptors outside the CNS) was also effective, indicating peripheral effects at the dosage level used (0." | ( Colonic motor responses in the pony: relevance of colonic stimulation by opiate antagonists. Bardon, T; Roger, T; Ruckebusch, Y, 1985) | 0.55 |
" Naloxonazine, a relatively selective mu 1 blocker, at certain dosage (50 micrograms per rabbit, icv), could abolish the analgesia but not the respiratory inhibition produced by MET." | ( The analgesic and respiratory depressant actions of metorphamide in mice and rabbits. Chang, JK; He, XP; Lu, WX; Niu, SF; Weber, E; Xu, SF; Xu, WM; Zhang, AZ; Zhou, KR, 1985) | 0.27 |
" at a dosage 1000 times lower than that of morphine on a molar basis." | ( Comparative study on the electrophysiological responses at thalamic level to different analgesic peptides. Biella, G; Braga, PC; Fraschini, F; Guidobono, F; Pecile, A; Tiengo, M, 1985) | 0.27 |
" But to objectify the mode of action, or to measure dose-response functions, to evaluate the optimal therapeutic dosage, or to compare the relative efficacy of the drug tested with known substances--all these investigations can best be performed in a sample of healthy, informed, intelligent and cooperative volunteers, as homogenous as possible." | ( Modern techniques to measure pain in healthy man. Bromm, B, 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 |
" After animals had achieved the required performance criterion, dose-response and phase-generalization tests were conducted in each group." | ( A drug discrimination analysis of ethanol-induced behavioral excitation and sedation: the role of endogenous opiate pathways. Altshuler, HL; Shippenberg, TS, ) | 0.13 |
" Naloxone, in the dosage used (40 micrograms/kg body wt as a bolus, followed by 10 micrograms/kg body wt X h) had no independent effects on motility or flow, but did blunt the stimulatory effects of morphine and atropine on migrating motor complexes." | ( Effects of morphine and atropine on motility and transit in the human ileum. Borody, TJ; Haddad, A; Phillips, SF; Quigley, EM; Tucker, RL; Wienbeck, M; Zinsmeister, AR, 1985) | 1.18 |
" Under conditions of high stress, rats first showed diminished, and then enhanced, hyperthermic responding across repeated morphine dosing (5 or 35 mg/kg)." | ( Influence of stress on morphine-induced hyperthermia: relevance to drug conditioning and tolerance development. Baker, TB; Tiffany, ST; Zelman, DC, 1985) | 0.27 |
"Tolerance to the behavioral effects of selected opiate compounds (cyclazocine, ketocyclazocine, naloxone and the stereoisomers of N-allylnormetazocine) and phencyclidine was evaluated using cumulative dosing procedures in rhesus monkeys responding under a fixed-ratio (FR) schedule of food presentation." | ( Behavioral effects of selected opiates and phencyclidine in the nondependent and cyclazocine-dependent rhesus monkey. Bergman, J; Hassoun, J; Schuster, CR, 1985) | 0.49 |
" Due to the rather high dosage necessary (1-2 mg/ml), well-known side-effects of these opiates must also be taken into consideration." | ( [Local anesthetic effects of morphine and naloxone]. Gilly, H; Kramer, R; Zahorovsky, I, 1985) | 0.53 |
" The daily dosage was limited to 400 mg." | ( Clinical investigation on the development of dependence during oral therapy with tramadol. Barth, H; Flohé, L; Giertz, H; Richter, W, 1985) | 0.27 |
" Addition of naloxone to propranolol shifted the dose-response curve of propranolol to the left significantly, indicating an additive effect of the two drugs in their antiarrhythmic activity." | ( Cardiac antiarrhythmic evaluation of naloxone with or without propranolol using a modified chloroform-hypoxia screening test in the rat. Lee, AY; Wong, TM, ) | 0.77 |
" 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 |
" In general, opioid mechanisms sensitive to the present dosage of naloxone do not appear to mediate bacteremia-induced changes in hormonal or clinical parameters." | ( Bacteremia-induced changes in pituitary hormone release and effect of naloxone. Leshin, LS; Malven, PV, 1984) | 0.74 |
" Dose-response experiments indicated that cyclo (leu-Gly) was much more potent than MIF in these tests." | ( Development of narcotic tolerance and physical dependence: effects of Pro-Leu-Gly-NH2 and cyclo (Leu-Gly). Bhargava, HN; Ritzmann, RF; Walter, R, 1980) | 0.26 |
" 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 |
"5 mum produced a 1000 fold shift in the opiate dose-response curve but the anaesthetic responses showed only slight sensitivity to antagonism by naloxone." | ( Opiate-like analgesic activity in general anaesthetics. Lawrence, D; Livingston, A, 1981) | 0.46 |
" Similar dose-response curves in an apparent sine-wave pattern were noted with both MIF-1 and naloxone when comparisons were made both at 20 minutes after administration of morphine and over the entire 150 minutes of the experiment." | ( Similar antagonism of morphine analgesia by MIF-1 and naloxone in Carassius auratus. Ehrensing, RH; Kastin, AJ; Michell, GF, 1982) | 0.73 |
" A reliable dose-response and time-response relations were observed for both groups of analgesics." | ( A new method for the rapid measurement of analgesic activity in rabbits. Ayhan, IH; Melli, M; Türker, RK, 1983) | 0.27 |
"3 alpha-Adrenoceptors appear to be involved in the reaction, since noradrenaline showed stereospecificity, and the alpha-adrenoceptor antagonists phentolamine and piperoxan both shifted the dose-response curves of the alpha-adrenoceptor agonist drugs to the right, usually parallel to the control curves." | ( Studies on the antinociceptive action of alpha-agonist drugs and their interactions with opioid mechanisms. Bentley, GA; Newton, SH; Starr, J, 1983) | 0.27 |
" Naloxone caused a parallel displacement to the right of the antisecretory dose-response line to morphine." | ( Characterization of the opiate receptor population mediating inhibition of VIP-induced secretion from the small intestine of the rat. Coupar, IM, 1983) | 1.18 |
" Thus, the dose-response curve shows an U-shaped form." | ( The impairment of retention induced by beta-endorphin in mice may be mediated by a reduction of central cholinergic activity. Baratti, CM; Introini, IB, 1984) | 0.27 |
" Although the group X dosage interaction was not significant, an internally consistent tendency effect of naloxone among the different treatment groups was observed." | ( The effect of ovariectomy, estradiol and progesterone on opioid modulation of feeding. Gosnell, BA; Grace, M; Kneip, J; Levine, AS; Morley, JE, 1984) | 0.48 |
" More than 45% of ventromedial hypothalamic units reacted in a dose-response fashion to local application of morphine." | ( Microiontophoretic application of morphine and naloxone to neurons in hypothalamus of rat. Dafny, N; Prieto-Gomez, B; Reyes-Vazquez, C, 1984) | 0.52 |
" Similar intracerebral dose-response curves were obtained by the structurally related undecapeptides, physalaemin and eledoisin, but not by several unrelated peptides (TRH, neurotensin, bradykinin, somatostatin), prostaglandins E2 and F2a, dibutyryl cyclic AMP or dibutyrylcyclic GMP." | ( Intracerebral substance P in mice: behavioral effects and narcotic agents. Rackham, A; Share, NN, 1981) | 0.26 |
" Morphine in the dosage used did not influence the intradental sensory nerve conductivity." | ( Morphine inhibits substance P release from peripheral sensory nerve endings. Brodin, E; Gazelius, B; Olgart, L; Panopoulos, P, 1983) | 0.27 |
"4 Naloxone dose-dependently shifted the dose-response curve of met-enkephalin to the right." | ( Effects of endorphins on different parts of the gastrointestinal tract of rat and guinea-pig in vitro. Nijkamp, FP; Van Ree, JM, 1980) | 0.98 |
" Analysis of the effect of naloxone on GABA dose-response curves indicates that naloxone acts as a competitive antagonist at the neuronal GABA receptors." | ( Naloxone antagonism of GABA-evoked membrane polarizations in cultured mouse spinal cord neurons. Barker, JL; Gruol, DL; Smith, TG, 1980) | 2 |
" As dosage was increased, the hyperthermias diminished and in some cats hypothermia developed." | ( Thermoregulatory effects of (D-ala2)-methionine-enkephalinamide in the cat. Evidence for multiple naloxone-sensitive opioid receptors. Clark, WG; Ponder, SW, ) | 0.35 |
" Morphine's direct effect on activity is believed to have a biphasic dose-response curve; therefore, the relation of dose to conditioning was also studied." | ( Conditioned increases in locomotor activity produced with morphine as an unconditioned stimulus, and the relation of conditioning to acute morphine effect and tolerance. Kalant, H; Mucha, RF; Volkovskis, C, 1981) | 0.26 |
" The parallelism of the dose-response curves of opiates in the presence and absence of naloxone indicated competitive reversible antagonism." | ( Opiate receptors in the rabbit iris. Dal Bello, A; Drago, F; Gorgone, G; Moro, F; Panissidi, G; Scapagnini, U; Spina, F, 1980) | 0.48 |
" 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 |
" Thus, inhibition of opiate receptors and endorphins by naloxone in an otherwise clinically effective dosage does not influence the adrenocortical, hyperglycemic, or hemodynamic responses to surgical stress." | ( Cortisol, glucose, and hemodynamic responses to surgery after naloxone administration. Blichert-Toft, M; Engquist, A; Hicquet, J; Saurbrey, N, 1981) | 0.75 |
" Dose-response determinations were made for responses to phencyclidine, to a racemic mixture of N-allylnormetazocine, and to the pure levo and dextro isomers of N-allylnormetazocine." | ( Stereoisomers of N-allylnormetazocine: phencyclidine-like behavioral effects in squirrel monkeys and rats. Balster, RL; Brady, KT; May, EL, 1982) | 0.26 |
" Dose-response curves for serotonin before morphine application and in the presence of morphine show a noncompetitive mechanism of morphine-serotonin interaction." | ( [Naloxone-dependent morphine-induced depression of the snail response to serotonin]. Bezrukova, LV; Solntseva, EI, 1981) | 1.17 |
" It is found that the graft of f tau vs log [D] exhibits features similar to the in vivo dose-response curves for the drugs." | ( Drug affinities for the agonist and antagonist states of the opioid receptor. Barsuhn, C; Cheney, BV; Lahti, RA, 1982) | 0.26 |
" Ethylketazocine produced a biphasic dose-response curve." | ( Characterization of the opiate receptor in the guinea-pig ileal mucosa. Kachur, JF; Miller, RJ, 1982) | 0.26 |
" Unilateral injection resulted in a U-shaped dose-response relationship with a fall in mean arterial pressure and heart rate occurring at low doses (less than 10 ng)." | ( Cardiovascular effects of beta-endorphin after microinjection into the nucleus tractus solitarii of the anaesthetised rat. De Jong, W; Petty, MA, 1982) | 0.26 |
" After reliable discriminative control of lever choice was established, dose-response determinations for generalization to the training dose of PCP were made with several doses of PCP, a racemic mixture of cyclazocine and the pure (+)- and (-)-isomers of cyclazocine." | ( Discriminative stimulus properties of stereoisomers of cyclazocine in phencyclidine-trained squirrel monkeys. Balster, RL; Brady, KT, 1982) | 0.26 |
" In a further series of tests, a 50 mg/kg dose of naloxazone 20 hr prior to the assessment of morphine or metkephamid analgesia in the mouse hot plate test substantially shifted the dose-response curve for morphine to the right, while leaving the dose-response curve for metkephamid unchanged." | ( Cross-tolerance studies distinguish morphine- and metkephamid-induced analgesia. Frederickson, RC; Hynes, MD, ) | 0.13 |
" Dose-response curves were plotted with naloxone against the changes produced by each agonist, and the effect of a number of anticonvulsant drugs on agonist-induced seizures was ascertained." | ( The epileptogenic spectrum of opiate agonists. Bearden, LJ; Snead, OC, 1982) | 0.53 |
"The relationship between opiate binding density and morphine-induced catalepsy was estimated via dose-response analysis of the brain sites in which naloxone microinjections reversed the catalepsy induced by intraperitoneal morphine." | ( Reversal of morphine-induced catalepsy by naloxone microinjections into brain regions with high opiate receptor binding: a preliminary report. Bozarth, M; Levitt, RA; Wilcox, RE, 1983) | 0.73 |
" It increased the IC50 values and slopes of their dose-response curve for enkephalins and their analogs, and shifted to the right the curves for FK33824, levorphanol and normorphine." | ( Functional opiate receptor in mouse vas deferens: evidence for a complex interaction. Garzón, J; Lee, NM; Sánchez-Blázquez, P, 1983) | 0.27 |
" PCP pretreatment caused a shift to the right in the dose-response curve to acetylcholine (ACh) that was not parallel with the control dose-response curve." | ( Effects of phencyclidine and its derivatives on enteric neurones. Gintzler, AR; Zukin, RS; Zukin, SR, 1982) | 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 |
" A parallel shift in the dose-response curve of beta h-endorphin in the presence of beta h-endorphin-(1-27) suggests competition at the same site." | ( beta-endorphin-(1-27) is an antagonist of beta-endorphin analgesia. Hammonds, RG; Li, CH; Nicolas, P, 1984) | 0.27 |
" The application of naloxone alone in naive and morphine-dependent rats demonstrated that the PF units responded in a characteristic dose-response manner to incremental naloxone administration." | ( Microiontophoretically applied morphine and naloxone on single cell activity in the parafasciculus nucleus of naive and morphine-dependent rats. Dafny, N; Reyes-Vazquez, C, 1984) | 0.85 |
" An increase in the naloxone dosage (up to 1 mg/kg) was necessary to demonstrate the naloxone antagonistic effect (8-fold increase in the morphine ED50 value) when morphine was given with halothane." | ( Effect of morphine on the heart rate response to noxious stimulation: interaction with halothane and naloxone. Kerr, RC; Kissin, I; Smith, RL, 1984) | 0.81 |
" A parallel shift of the dose-response curve for analgesia to the right was observed when either beta h-EP or [ Trp27 ] -beta h-EP was coinjected with various doses of [Gln8, Gly31 ]-beta h-EP-Gly-Gly-NH2, [Arg9,19,24,28,29]-beta h-EP, or [ Cys11 ,26, Phe27 , Gly31 ]-beta h-EP." | ( beta-Endorphin-induced analgesia is inhibited by synthetic analogs of beta-endorphin. Hammonds, RG; Li, CH; Nicolas, P, 1984) | 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 |
" There was no evidence that beta-endorphins released during shock were responsible for the hemodynamic changes, blood flow changes, plasma enzyme changes, or energy deficits, because naloxone, at this dosage level, did not prevent these endotoxin-induced changes." | ( Effects of naloxone on endotoxin-induced changes in ponies. Bottoms, GD; Fessler, JF; Moore, AB; Roesel, OF, 1983) | 0.85 |
" Experiment 1 examined the effects of naloxone dosage and interstimulation interval (ISI) on kindled seizures." | ( The effects of naloxone and interstimulation interval on post-ictal depression in kindled seizures. Freeman, FG; Jarvis, MF, 1983) | 0.89 |
" In conscious man essentially similar results were found following intravenous dosing with a stable met-enkephalin analogue (DAMME, FK33824) or naloxone with decreases and increases respectively in the sensitivity of baroreflex responses to sodium nitroprusside." | ( Opioid peptides and central control of blood pressure. Petty, MA; Reid, JL; Rubin, PC, 1984) | 0.47 |
", delayed nociceptive reaction on a 55 degrees C hot-plate with a dose-response curve not readily fitting a single straight line; this effect was antagonized by high doses of naloxone." | ( Bremazocine induces antinociception, but prevents opioid-induced constipation and catatonia in rats and precipitates withdrawal in morphine-dependent rats. Gambino, MC; Petrillo, P; Tavani, A, 1984) | 0.46 |
"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 |
" This randomized double-blind study describes the effect of various dosing regimens of naloxone and MPSS upon hemodynamics and plasma catecholamines in patients with septic shock (n = 57)." | ( Naloxone and methylprednisolone sodium succinate enhance sympathomedullary discharge in patients with septic shock. Hughes, GS, 1984) | 1.93 |
" Dose-response studies indicated a 4-fold reduction in opiate responsiveness in the 10 days preceding the first ovulation." | ( Opiatergic control of gonadotropin secretion during puberty in the rat: a neurochemical basis for the hypothalamic 'gonadostat'? Bhanot, R; Wilkinson, M, 1983) | 0.27 |
" Comprehensive dose-response curves for naloxone anorexia (15 doses) and CTA (nine doses) are presented." | ( Suppression of feeding by naloxone in rat: a dose-response comparison of anorexia and conditioned taste aversion suggesting a specific anorexic effect. Leshem, M, 1984) | 0.84 |
" Dose-response curves for subcutaneous (SC) morphine (0." | ( Reinforcing properties of morphine and naloxone revealed by conditioned place preferences: a procedural examination. Iversen, SD; Mucha, RF, 1984) | 0.54 |
" When retested 24 h later, all groups that had previously received naloxone exhibited greatly reduced activity and rearing, with no evidence of a dose-response relationship." | ( Naloxone administration following brief exposure to novelty reduces activity and rearing in mice upon 24-h retest: a conditioned aversion? Precious, JI; Richards, C; Rodgers, RJ, 1984) | 1.95 |
" Footshock intensity thresholds for eliciting locomotion were determined and dose-response curves for EKC and MS analgesia were obtained." | ( Analgesic effects of ethylketocyclazocine and morphine in rat and toad. Aleman, DO; Carr, KD; Holland, MJ; Simon, EJ, 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 |
"A dose-response study of the effect of naloxone on schedule-induced drinking confirmed that this type of drinking is resistant to the opiate antagonist at doses which depressed drinking induced by water-deprivation, hypertonic saline and salbutamol." | ( The effect of naloxone on schedule-induced and other drinking. Singer, G; Wallace, M; Willis, G, 1984) | 0.9 |
" Simultaneous application of Hi and 10 micrograms of diphenhydramine, pyrilamine or promethazine, apparently causing no analgesic effect from a single administration, caused a parallel shift of the dose-response curve of Hi to the right." | ( Analgesic effect of histamine induced by intracerebral injection into mice. Chung, YH; Kamei, C; Miyake, H; Tasaka, K, 1984) | 0.27 |
" In most experimental situations, indications for bell-shaped dose-response curves of DSIP were found." | ( Some pharmacological effects of delta-sleep-inducing peptide (DSIP). Aeppli, L; Haefely, W; Polc, P; Scherschlicht, R, 1984) | 0.27 |
" Naloxone clearly antagonizes the release of prolactin induced by 5-hydroxytryptophan administered alone at a dosage of 50 mg/Kg/b." | ( Effects of naloxone on the secretion of prolactin and corticosterone induced by 5-hydroxytryptophan and a serotonergic agonist, mCPP. Cerrito, F; Preziosi, P; Vacca, M, 1983) | 1.57 |
" Similar treatment of castrated males (wethers) with this dosage of naloxone failed to increase plasma LH." | ( Effects of naloxone and electroacupuncture treatment on plasma concentrations of LH in sheep. Bossut, DF; Diekman, MA; Malven, PV, 1984) | 0.89 |
"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 |
" Required dosage of pentobarbital, arousal and walk times (measured from injection of antagonists), respiratory rate, and heart rate were measured." | ( Comparison of five preanesthetic medicaments in pentobarbital-anesthetized dogs: antagonism by 4-aminopyridine, yohimbine, and naloxone. Booth, NH; Clark, JD; Hatch, RC; Kitzman, JV, 1983) | 0.47 |
" Naloxone dose-response curves revealed that the naloxone ED50 was reduced by either morphine pretreatment regimen, but was much more pronounced in pellet-implanted animals [181." | ( Morphine-induced supersensitivity to the effects of naloxone on luteinizing hormone secretion in the male rat. Cicero, TJ; Meyer, ER; Owens, DP; Schmoeker, PF, 1983) | 1.43 |
", dose-response curves were shifted to the right) but failed to block the effects of diprenorphine." | ( Effects of naloxone, diprenorphine, buprenorphine and etorphine on unpunished and punished food-reinforced responding in the squirrel monkey. DeRossett, SE; Holtzman, SG, 1984) | 0.66 |
" The dose-response curve was an inverted U in this range of dose." | ( Possible interaction between central cholinergic muscarinic and opioid peptidergic systems during memory consolidation in mice. Baratti, CM; Huygens, P; Introini, IB, 1984) | 0.27 |
") administered in combination with naloxone and picrotoxin shifted dose-response curves for both naloxone and picrotoxin to the right." | ( Comparison of the effects of naloxone and picrotoxin on schedule-controlled responding in the pigeon: possible GABA-antagonistic effects of naloxone. Carter, RB; Leander, JD, 1984) | 0.84 |
" 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) | 0.82 |
" Rats were trained to press a lever on a variable interval (1 min) schedule of food presentation and dose-response curves were determined for morphine (0." | ( Schedule-controlled behavior in the morphine-dependent and post-dependent rat. Brady, LS; Holtzman, SG, 1980) | 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 |
"0 mg/kg) shifted the clonidine dose-response curves to the right, suggesting competitive antagonism." | ( An analysis of the effects of systemically administered clonidine on the food and water intake of rats. Sanger, DJ, 1983) | 0.27 |
" Ketocyclazocine dose-response functions were determined for each monkey under their original training conditions and then the conditions were reversed and dose-response functions were re-determined under the new conditions." | ( Effects of ketocyclazocine alone and in combination with naloxone on schedule-controlled responding in squirrel monkeys. Dykstra, LA; Milar, KS, 1983) | 0.51 |
" 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) | 0.88 |
" The ability of enkephalin to relax caerulein-induced contractions and the manner in which the caerulein dose-response curve was shifted in the presence of enkephalin strongly suggest that enkephalin and caerulein are functional antagonists in this system." | ( Interaction of enkephalin and caerulein on guinea pig small intestine. Lingle, PF; Yau, WM; Youther, ML, 1983) | 0.27 |
" This work was performed in order to evaluate the dose-response relationship, time course, and naloxone reversibility of fentanyl suppression of neurons that are involved with the transmission of information about pain." | ( Dose-response suppression of noxiously evoked activity of WDR neurons by spinally administered fentanyl. Collins, JG; Kitahata, LM; Matsumoto, M; Suzukawa, M; Yuge, O, 1983) | 0.48 |
" Nevertheless, the antinociceptive action of vasopressin does not appear to be secondary to its pressor activity, since phenylephrine failed to induce an antinociceptive effect at a dosage that mimicked the pressor response to vasopressin." | ( Vasopressin-induced antinociception: an investigation into its physiological and hormonal basis. Berntson, GG; Berson, BS; Kirk, WT; Torello, MW; Zipf, W, 1983) | 0.27 |
" Group II drugs, upon reaching a threshold value, cause first a dose-dependent increase in water intake to a maximum; additional dosage increments produce a dose-dependent decrease." | ( A simple animal test system to predict the likelihood of a drug causing human physical dependence. Maickel, RP; Zabik, JE, 1980) | 0.26 |
" In a second experiment, rats were injected for ten days with the same dosage of naloxone." | ( Behavioral alterations produced by chronic naloxone injections. Baker, MJ; Hood, JL; Layng, MP; Malin, DH; Swank, P, 1982) | 0.75 |
"Insulin and glucagon release from monolayer pancreatic islet cell cultures were inhibited in a dose-response fashion by various enkephalins." | ( Disparate effects of enkephalin and morphine upon insulin and glucagon secretion by islet cell cultures. Ensinck, JW; Fujimoto, WY; Kanter, RA, 1980) | 0.26 |
" This diminished LH-response to a second naloxone injection satisfied the two pharmacological criteria for the establishment of tolerance: a parallel shift to the right in the dose-response curve; and a reduced response to naloxone at the same brain concentration of the antagonist in "tolerant" vs." | ( Development of acute tolerance to the effects of naloxone on the hypothalamic-pituitary-luteinizing hormone axis in the male rat. Cicero, TJ; Owens, DP, 1981) | 0.78 |
" These data would suggest that, at least in respect to the effects of narcotics on water intake, naloxone is a partial agonist of the nalorphine type, but the slopes of naloxone and of morphine dose-response regression lines are not in keeping with this hypothesis." | ( Dual effect of naloxone on drinking behaviour of rats. Cantalamessa, F; de Caro, G; Massi, M; Micossi, LG, 1982) | 0.83 |
" 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 |
" In either type of experiment the dose-response lines of naloxone against caerulein were very shallow as compared with those against morphine." | ( Caerulein and morphine: an attempt to differentiate their antinociceptive effects. Zetler, G, 1982) | 0.51 |
" Since the log dose-response curves were displaced to the right in quasi-parallel fashion, and Lineweaver-Burk plots of the data showed an intersection very close to the origin of the horizontal axis, the antagonism between naloxone and the three peptides appears to be competitive." | ( Retrograde amnesia caused by Met-, Leu- and des-Try-Met-enkephalin in the rat and its reversal by naloxone. Dias, RD; Izquierdo, I, 1981) | 0.66 |
" 2 The dose-response curves to naloxone obtained in tissues individually exposed to different opiates showed that their relative potency in increasing sensitivity to naloxone was as follows: levorphan greater than morphine greater than Met-enkephalin greater than nalorphine greater than pentazocine." | ( Pharmacological characterization of opiate physical dependence in the isolated ileum of the guinea-pig. Luján, M; Rodríguez, R, 1981) | 0.55 |
"3 Pretreatment of the mice with naloxone caused a dose-dependent shift to the right of the dose-response curve to morphine." | ( Evidence for an action of morphine and the enkephalins on sensory nerve endings in the mouse peritoneum. Bentley, GA; Newton, SH; Starr, J, 1981) | 0.55 |
" In the same dosage naloxone did not induce detrusor reflex in 2 patients with areflexic bladder caused by complete suprasacral spinal lesions." | ( Enhancement of detrusor reflex activity by naloxone in patients with chronic neurogenic bladder dysfunction. Preliminary report. Chary, KS; Das, N; Rao, MS; Sharma, PL; Vaidyanathan, S, 1981) | 0.85 |
" The dose-response curves for dopamine before morphine application and in its presence indicate a noncompetitive mechanism of interaction between morphine and dopamine." | ( [Naloxone-dependent morphine reduction of excitatory responses of mollusk neurons to dopamine]. Bezrukova, LV; Solntseva, EI, 1981) | 1.17 |
"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 |
" The dose-response curves of the naloxone group were shifted to the right of those for the saline group." | ( Time course of antagonism of morphine antinociception by intracerebroventricularly administered naloxone in the rat. Cowan, A; Porreca, F; Tallarida, RJ, 1981) | 0.76 |
" The heptapeptide Leu5-enkephalin-Arg6-Phe7 and the Met5-analogue, both in the amidized form, displayed dose-response relationship with a sensitivity of about 10 nmol." | ( Enkephalin-related peptides: direct action on the octopus heart. Frösch, D; Kiehling, C; Martin, R; Schiebe, M; Voigt, KH, 1981) | 0.26 |
" The manufacturer's present recommended dosage may not be sufficient to reverse the effects of large narcotic ingestions." | ( Naloxone: underdosage after narcotic poisoning. Conner, CS; Moore, RA; Peterson, RG; Rumack, BH, 1980) | 1.7 |
" Naloxone reduced drinking at all dosage levels used (0." | ( Naloxone depresses osmoregulatory drinking in rats. Czech, DA; Stein, EA, 1980) | 2.61 |
" naloxone produced a dose-dependent rightward shifting of the morphine dose-response lines, the shift produced by the 10-micrograms dose being sufficient to abolish the analgetic action of morphine doses as large as 75 mg/kg." | ( Sites of antinociceptive action of systemically injected morphine: involvement of supraspinal loci as revealed by intracerebroventricular injection of naloxone. Rudy, TA; Yeung, JC, 1980) | 1.37 |
" administration of 5 mg/kg morphine, a mu-opioid agonist, or U50488H (U50), a kappa 1-opioid agonist, for 5 days in male CD-1 mice results in a 2-3-fold shift to the right of the respective analgesic (tail flick) dose-response curves, indicating the development of tolerance." | ( The NMDA receptor antagonists, LY274614 and MK-801, and the nitric oxide synthase inhibitor, NG-nitro-L-arginine, attenuate analgesic tolerance to the mu-opioid morphine but not to kappa opioids. Elliott, K; Inturrisi, CE; Kolesnikov, YA; Minami, N; Pasternak, GW, 1994) | 0.29 |
" Naloxone also caused a rightward shift of the dose-response curve for dynorphin A, suggesting a competitive antagonism mechanism." | ( Identification of dynorphins as endogenous ligands for an opioid receptor-like orphan receptor. Yu, L; Zhang, S, 1995) | 1.2 |
" By contrast, morphine treatment during hibernation resulted in significantly reduced abstinence compared with that observed after treatment during the NH state, with no significant morphine dose-response or duration-response trends evident." | ( Quantitative and qualitative aspects of the hibernation-related reduction of morphine physical dependence in the ground squirrel (Citellus lateralis). Beaver, TA; Beckman, AL; Lewis, FC; Newman, JR, 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 |
"Pregnant Long-Evans hooded rats were dosed with 1, 5, or 10 mg/kg per day naloxone from gestational day 7 (GD7) through GD20." | ( Behavioral and developmental changes associated with prenatal opiate receptor blockade. Anderson, LA; Medici, CN; Shepanek, NA; Smith, RF, 1995) | 0.52 |
" The dose-response curves of [Lys7]dermorphin antinociception were shifted to the right by the pretreatment with naloxone (0." | ( Production of antinociception by peripheral administration of [Lys7]dermorphin, a naturally occurring peptide with high affinity for mu-opioid receptors. Lattanzi, R; Melchiorri, P; Negri, L, 1995) | 0.5 |
" We have further investigated the non-opioid nature of this activity by comparing the efficacies of dyn A(1-13) and (2-17) under different experimental protocols with a variety of dosing regimens." | ( Dynorphin A modulates acute and chronic opioid effects. He, L; Hooke, LP; Lee, NM, 1995) | 0.29 |
" The effect depended on the timing of naloxone addition to the cultures and on its concentration, with a bell-shaped dose-response curve." | ( Naloxone interferes with granulocytopoiesis in long-term cultures of mouse bone marrow; buffering by the stromal layer. Boranić, M; Kardum, I; Krizanac-Bengez, L; Testa, NG, 1994) | 2 |
"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 |
" Twenty-seven-, 20- and 15-day-old rats all developed tolerance as indicated by a rightward shift of the dose-response curve after chronic morphine." | ( The ontogeny of mu opiate tolerance and dependence in the rat: antinociceptive and biochemical studies. Kuhn, CM; Little, PJ; Windh, RT, 1995) | 0.29 |
" The combination of an opioid with DMED might reduce the dosage requirements for each drug and thereby allow the same anesthetic depth to be achieved with lesser degrees of their individual side effects." | ( Anesthetic and hemodynamic interactions of dexmedetomidine and fentanyl in dogs. Hug, CC; Salmenperä, MT; Szlam, F, 1994) | 0.29 |
"This work studies the antinociceptive effect of a sustained (7 day) release dosage form of vapreotide, a peptidic analogue of somatostatin, in rats submitted to a nociceptive mechanical stimulus (paw pressure)." | ( Seven-day antinociceptive effect of a sustained release vapreotide formulation. Betoin, F; Duchene-Marullaz, P; Eschalier, A; Lavarenne, J, 1994) | 0.29 |
" After repeated dosing (12-15 days), moguisteine did not induce tolerance in either guinea-pigs or dogs." | ( Moguisteine: a novel peripheral non-narcotic antitussive drug. Borghi, A; Ceserani, R; Dalla Rosa, C; Gallico, L; Tognella, S, 1994) | 0.29 |
" In the PAG/DR, the HA dose-response curve had an inverted U-shape, showing that HA can induce both antinociceptive (0." | ( Histamine-induced modulation of nociceptive responses. Hough, LB; Mischler, SA; Nalwalk, JW; Thoburn, KK, 1994) | 0.29 |
"All urine drug screens using the enzyme-multiplied immunoassay technique were negative for opiates at both dosage levels." | ( Does naloxone cause a positive urine opiate screen? Mikkelsen, SL; Norton, J; Storrow, AB; Wians, FH, 1994) | 0.8 |
" No sooner than 3 days after implantation, naloxone dose-response functions were determined with several behavioral paradigms and ratings of a variety of somatic withdrawal signs." | ( Relative sensitivity to naloxone of multiple indices of opiate withdrawal: a quantitative dose-response analysis. Gold, LH; Koob, GF; Markou, A; Schulteis, G; Stinus, L, 1994) | 0.86 |
"3 mg/kg) which shifted the dose-response curve to the right." | ( An investigation into the discriminative stimulus and reinforcing properties of the CCKB-receptor antagonist, L-365,260 in rats. Bentley, G; Bourson, A; Hargreaves, R; Iversen, S; Jackson, A; Rycroft, W; Tattersall, D; Tricklebank, M, 1994) | 0.29 |
" Naloxone shifted to the right the dose-response curves for each opioid peptide significantly enhancing the ED50 values." | ( Modulation of non-adrenergic non-cholinergic inhibitory transmission in rat duodenum: role of opiates and 5-hydroxytryptamine. Adamo, EB; Di Giovanni, G; Marini, R; Mulè, F; Postorino, A; Serio, R, 1993) | 1.2 |
" The different temporospatial pattern of immediate early gene expression in neurons of the spinal cord dorsal horn following noxious stimulation suggest that variable transcription complexes may interact with DNA regulatory sequences and could thus activate alternative secondary response genes, even under protection of a high dosage of morphine applied before noxious stimulation." | ( Application of morphine prior to noxious stimulation differentially modulates expression of Fos, Jun and Krox-24 proteins in rat spinal cord neurons. Bravo, R; Herdegen, T; Schadrack, J; Tölle, TR; Zieglgänsberger, W; Zimmermann, M, 1994) | 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 |
"Recommendations for the dosage of naloxone to reverse opiate depression in neonates were revised by the American Academy of Pediatrics in 1989." | ( [Administration of naloxone to newborn infants at obstetric departments in Norway]. Fagerli, I; Hansen, TW, 1994) | 0.9 |
" A randomized, placebo-controlled study comparing the time-action, dose-response and potency of the respiratory effects of M6G to morphine was done using a nonanesthetized neonatal guinea pig model and a noninvasive computerized plethysmograph technique." | ( Morphine-6-beta-D-glucuronide respiratory pharmacodynamics in the neonatal guinea pig. Murphey, LJ; Olsen, GD, 1994) | 0.29 |
"4 mg), indicating a very narrow dose-response range." | ( (+)Naloxone potentiates the inotropic effect of epinephrine in the isolated dog heart. Barron, BA; Caffrey, JL; Gaugl, JF; Gu, H, 1993) | 0.91 |
" Dose-response curve for naloxone inhibition of intake was shifted leftward in obese compared with lean sheep." | ( Feeding behavior and its responsiveness to naloxone differ in lean and obese sheep. Alavi, FK; Mauromoustakis, A; McCann, JP; Sangiah, S, 1993) | 0.85 |
" Both devazepide and L-365,260 showed a bell-shaped dose-response curve." | ( Increased release of immunoreactive cholecystokinin octapeptide by morphine and potentiation of mu-opioid analgesia by CCKB receptor antagonist L-365,260 in rat spinal cord. Han, JS; Sun, YH; Zhang, ZW; Zhou, Y, 1993) | 0.29 |
"Naloxone, which increases endogenous corticotropin-releasing hormone (CRH) release by blocking an inhibitory opioidergic tone on the hypothalamic-pituitary-adrenal (HPA) axis, was administered in a dose-response protocol to seven healthy volunteers and 13 patients with treated posttraumatic stress disorder (PTSD)." | ( Hypersensitivity of the hypothalamic-pituitary-adrenal axis to naloxone in post-traumatic stress disorder. Grice, JE; Hockings, GI; Jackson, RV; Jensen, GR; Walters, MM; Ward, WK, ) | 1.81 |
" Aspirin did not influence the cortisol responses to synthetic ACTH administration given according to a dose-response protocol." | ( Aspirin increases the human hypothalamic-pituitary-adrenal axis response to naloxone stimulation. Crosbie, GV; Grice, JE; Hockings, GI; Jackson, AJ; Jackson, RV; Walters, MM, 1993) | 0.52 |
" Dose-response curves for precipitated abstinence evaluated as changes in mean arterial pressure and heart rate show a gradual increase in maximum followed by a progressive shift to the left as dependence progresses." | ( Acute opioid dependence in the cardiovascular system of the spinal rat. Cruz, SL; Villarreal, JE, 1993) | 0.29 |
" Unilateral intratesticular injection of 10 micrograms naloxone led to a dose-dependent increase in the hCG-responsiveness without altering the slope of the hCG dose-response curve." | ( Local regulation of testicular immunoreactive-arginine vasopressin and steroidogenesis by naloxone. Allevard, AM; Bedin, M; Fillion, C; Gharib, C; Huges, JN; Pointis, G; Tahri-Joutei, A, 1993) | 0.75 |
" We report age-related changes in the drug dosage needed to improve 1 week retention in the P/8 but not R/1 line." | ( Age-related changes in the pharmacological improvement of retention in senescence accelerated mouse (SAM). Flood, JF; La Reginna, M; Morley, JE, ) | 0.13 |
" Morphine dependence was induced by multiple injections of the drug on an incremental staircase dosage regimen for 6 days." | ( Noninvasive subthreshold auricular electrical stimulation reduces the severity of precipitated and abrupt opiate withdrawal. Dafny, N; Dougherty, PM, 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) | 0.76 |
" The fentanyl dose-response curve was unchanged by opioid receptor blockade with 10(-6)M naloxone and by alpha and beta adrenoceptor blockade produced by 10(-6)M prazosin and 10(-6)M propranolol." | ( Direct effects of fentanyl on canine coronary artery rings. Bridges, MT; Grover, TE; Introna, RP; Pruett, JK; Yodlowski, EH, 1995) | 0.51 |
" The idazoxan dose-response curve for this suppression of fentanyl antinociception assessed with tail flick latency was the same as that for suppression of xylazine." | ( Antinociceptive actions of intrathecal xylazine: interactions with spinal cord opioid pathways. Davies, A; Gent, JP; Goodchild, CS; Guo, Z, 1996) | 0.29 |
"To assess effects of stimulus intensity, dose-response curves in rats for radiant heat-evoked withdrawal of the hind paw was assessed after the intrathecal (i." | ( Differential right shifts in the dose-response curve for intrathecal morphine and sufentanil as a function of stimulus intensity. Dirig, DM; Yaksh, TL, 1995) | 0.29 |
" The dosage based on experimental studies." | ( [Clinical investigations of an i.m. combination anesthesia with fentanylclimazolam/xylazine and postoperative i.v. antagonism with naloxone/sarmazenil/yohimbine in guinea pigs]. Brill, T; Erhardt, W; Henke, J; Lendl, C; Matis, U; Otto, K; Roberts, U, 1996) | 0.5 |
" Each morphine dosing level was maintained for 2 weeks, with test drugs administered during the second week of maintenance of each morphine dose." | ( Buprenorphine, morphine and naloxone effects during ascending morphine maintenance in humans. Bigelow, GE; Preston, KL; Schuh, KJ; Stitzer, ML; Walsh, SL, 1996) | 0.59 |
"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 |
" The dose-response relationship showed a U-shaped curve; the smallest dose had a minor inhibitory effect and the highest dose had no further effect on the PRL rise." | ( Modulating effect of the nootropic drug, piracetam on stress- and subsequent morphine-induced prolactin secretion in male rats. Bollengier, F; Engelborghs, S; Finné, E; Matton, A; Vanhaeist, L, 1996) | 0.29 |
" Treatment included naloxone (12 patients), admission to the pediatric intensive care unit (8), ventilation (5), and reduction in dosage (1)." | ( Opiate-induced respiratory depression in pediatric patients. Choonara, IA; Cousins, A; Gill, AM; Nunn, AJ, 1996) | 0.62 |
"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) | 0.56 |
" 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 |
" 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 |
" Repetitive dosing (1/4 of the greatest dose every 30 min) was as effective as a single bolus dose for both drugs." | ( Attenuation of c-Fos expression in the rat lumbosacral spinal cord by morphine or tramadol following noxious colorectal distention. Gebhart, GF; Stitt, S; Traub, RJ, 1995) | 0.29 |
" We also examined tolerance on these analgesic systems by using a daily morphine injection paradigm which shifts the dose-response curve for systemic morphine approximately 2-fold after 5 days." | ( Peripheral morphine analgesia: synergy with central sites and a target of morphine tolerance. Jain, S; Kolesnikov, YA; Pasternak, GW; Wilson, R, 1996) | 0.29 |
" In contrast, the single dosing of all agents failed to show antinociceptive effect." | ( Antinociceptive effects of angiotensin-converting enzyme inhibitors and an angiotensin II receptor antagonist in mice. Miyazaki, M; Okunishi, H; Song, K; Takai, S; Tanaka, T, 1996) | 0.29 |
" Finally dose-response curves were found highly reproducible across transfection experiments, opening the possibility for a direct comparison of distinct recombinant receptor preparations." | ( [35S]GTP gamma S binding: a tool to evaluate functional activity of a cloned opioid receptor transiently expressed in COS cells. Befort, K; Kieffer, BL; Tabbara, L, 1996) | 0.29 |
" Three scoring systems to quantify dose-response relationships for withdrawal are described: (1) using the mean number of withdrawal behaviors per animal within each treatment group; (2) using the sum of the percentage of animals within a treatment group displaying each of the withdrawal behaviors; and (3) a modification of these, to further isolate the naloxone-induced component of the withdrawal score, that is, subtraction of data obtained from saline-challenged animals from those of naloxone-challenged rats." | ( The induction and quantitation of methadone dependence in the rat. Hope, W; Pierce, TL; Raper, C, 1996) | 0.46 |
" Dose-response curves were obtained for each drug individually; for morphine:clonidine at 1:3, 1:1, and 1:0." | ( Interaction of morphine and clonidine on gastrointestinal transit in mice. Pol, O; Puig, MM; Warner, W, 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 |
" Buprenorphine, when injected systemically, revealed a potent analgesic effect by tailflick assay, with a biphasic dose-response curve, which was reversed by naloxone." | ( Pharmacological characterization of buprenorphine, a mixed agonist-antagonist with kappa 3 analgesia. Peter, Y; Pick, CG; Schreiber, S; Weizman, R, 1997) | 0.49 |
" No dose-response relationships could be elicited with U-50488H or ICI-204448, and their antitransit effects were analogous in SS- and CO-treated animals." | ( Peripheral effects of opioids in a model of intestinal inflammation in mice. Pol, O; Puig, MM; Sanchez, B, 1996) | 0.29 |
" Further, we examined whether an ovulation-blocking dosage of pentobarbital sodium (PB) would affect the NAL-induced Fos expression." | ( Fos expression by naloxone in LHRH neurons of the mediobasal hypothalamus and effects of pentobarbital sodium in the proestrous rat. Funabashi, T; Jinnai, K; Kimura, F, 1997) | 0.63 |
" Pairing Delt II (5 microg) with low (100-200 mg/kg) 2DG doses significantly enhanced intake, producing a leftward (3-fold) shift in 2DG's hyperphagic dose-response curve." | ( Delta and kappa opioid receptor subtypes and ingestion: antagonist and glucoprivic effects. Bodnar, RJ; Ruegg, H; Yu, WZ, 1997) | 0.3 |
" Dosage with naloxone (1 and 10 mg/kg) had no effect on the level of analgesia or corticosteroid concentrations." | ( Stress-induced analgesia. The role of hormones produced by the hypophyseal-adrenocortical system. Bogdanov, AI; Filaretov, AA; Yarushkina, NI, ) | 0.5 |
" In addition, NLX produced a rightward shift in the inverted U-shaped dose-response curve for cocaine reward during self-administration, indicating a decrease in sensitivity for the reinforcing effects of cocaine." | ( Naloxone inhibits the reinforcing and motivational aspects of cocaine addiction in mice. Gerrits, MA; Kuzmin, AV; van Ree, JM; Zvartau, EE, 1997) | 1.74 |
" 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 |
" The lack of subjective symptoms and physiological signs of opioid withdrawal during 72 h of acute dose omission supports the feasibility of less-than-daily dosing at buprenorphine doses of 8 mg/day in patients who have demonstrated an ability to remain drug-free for an extended period." | ( Controlled opioid withdrawal evaluation during 72 h dose omission in buprenorphine-maintained patients. Bigelow, GE; Eissenberg, T; Johnson, RE; Liebson, IA; Stitzer, ML; Strain, EC; Walsh, SL, 1997) | 0.3 |
"055 nmol from the dose-response curve." | ( Central regulation of urine production by a selective mu-opioid agonist, [D-Ala2, N-Me-Phe4, Gly5-ol]-enkephalin, in rats. Matsuda, T; Mori, M; Tsushima, H, 1997) | 0.3 |
" Groups IV and V consisted of a dose-response effect of QNL on ischemic PC in which QNL (0." | ( Ischemic preconditioning is mediated by a peripheral opioid receptor mechanism in the intact rat heart. Gross, GJ; Hsu, AK; Schultz, JJ, 1997) | 0.3 |
" Naloxone (1 microM) or norbinaltorphimine (10 nM) shifted the dose-response curve of (-)-U50,488H to the right by 100-fold." | ( Activation of the cloned human kappa opioid receptor by agonists enhances [35S]GTPgammaS binding to membranes: determination of potencies and efficacies of ligands. Chen, C; Li, JG; Liu-Chen, LY; Luo, LY; Zhu, J, 1997) | 1.21 |
" Dose-response curves to (+)-WIN 55212 and CP 55940 were shifted to the right, with no reduction of maximal response, by pretreatment with SR141716A (31." | ( Inhibition by cannabinoid receptor agonists of acetylcholine release from the guinea-pig myenteric plexus. Coutts, AA; Pertwee, RG, 1997) | 0.3 |
" Prolonged exposure to agonists induced desensitization of the receptor as estimated by a reduction in the maximal stimulation of GTP[gamma-35S] binding by DAMGO and rightward shifts in the dose-response curves." | ( Down-regulation of mu-opioid receptor by full but not partial agonists is independent of G protein coupling. Medzihradsky, F; Yabaluri, N, 1997) | 0.3 |
" Cumulative dose-response analysis in the tail-flick test revealed an ED50 value for intrathecal (spinal) l-methadone of 15." | ( d-Methadone is antinociceptive in the rat formalin test. Elliott, KJ; Inturrisi, CE; Shimoyama, M; Shimoyama, N, 1997) | 0.3 |
" This dosing regimen can be prepared with 400 microg naloxone in 1,000 ml crystalloid given in 24 h to a patient weighing 70 kg." | ( Opioid-sparing effects of a low-dose infusion of naloxone in patient-administered morphine sulfate. Fortney, J; Gan, TJ; Ginsberg, B; Glass, PS; Jhaveri, R; Perno, R, 1997) | 0.8 |
"Case 1: A 72-year-old 84-kg white man with cancer of the bladder and bone metastases had intense back and leg pain that was treated with intrathecal morphine for 6 months at an increasing dosage up to 10 mg twice daily." | ( Respiratory depression following administration of intrathecal bupivacaine to an opioid-dependent patient. Barjhoux, CE; Danel, VC; Lemoigne, AH; Mallaret, MP; Piquet, CY; Vincent, FH, 1998) | 0.3 |
"5 nmol/h) of the agonist for 5 days, the OFQ dose-response curves for its antinociceptive effect in the tail-flick and paw-pressure tests were significantly shifted to the right." | ( Antinociceptive and morphine modulatory actions of spinal orphanin FQ. Henderson, G; Jhamandas, KH; Sutak, M, 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 |
" The enhanced brain permeability with the subsequent decrease in peripheral dosage of these opioid peptides did not result in lowering constipation." | ( Glycodermorphins: opioid peptides with potent and prolonged analgesic activity and enhanced blood-brain barrier penetration. Lattanzi, R; Negri, L; Rocchi, R; Scolaro, B; Tabacco, F, 1998) | 0.3 |
" Whereas cycling mares responded to all dosages of NAL, AN mares responded only to the higher dosages for FSH, and LH failed to increase at any dosage employed." | ( Gonadotropin response to naloxone in the mare: effect of time of year and reproductive status. Davison, LA; Fitzgerald, BP; McManus, CJ, 1998) | 0.6 |
" 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) | 0.71 |
" A rightward shift of the dose-response curve was observed in rats made tolerant to systemic morphine with subcutaneous morphine pellets." | ( Characterization of the antihyperalgesic action of a novel peripheral mu-opioid receptor agonist--loperamide. Nozaki-Taguchi, N; Yaksh, TL, 1999) | 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) | 0.55 |
"Each patient received an IV bolus of naloxone at a dosage of 125 microg/kg." | ( Influence of body mass on the hypothalamic-pituitary-adrenal-axis response to naloxone in patients with polycystic ovary syndrome. Barini, A; Caruso, A; Cento, R; Ciampelli, M; de Marinis, L; Fulghesu, AM; Guido, M; Lanzone, A; Pavone, V, 1999) | 0.8 |
" Pretreatment with a non-opioid receptor-selective dose (2 mg/kg) of NLXM produced a rightward shift in the dose-response function of EMD 61,753." | ( Effects of kappa opioids in the inflamed rat colon. Gebhart, GF; Sengupta, JN; Snider, A; Su, X, 1999) | 0.3 |
" The dose-response curves for oxymorphone and hydromorphone were shifted 5- and 12." | ( Enhancement mu opioid antinociception by oral delta9-tetrahydrocannabinol: dose-response analysis and receptor identification. Cichewicz, DL; Martin, ZL; Smith, FL; Welch, SP, 1999) | 0.3 |
" Comparisons of physiological and subjective measures collected in agonist exposure sessions indicate that LAAM is not less potent than methadone under acute dosing conditions." | ( Relative potency of levo-alpha-acetylmethadol and methadone in humans under acute dosing conditions. Bigelow, GE; Buchhalter, AR; Eissenberg, T; Stitzer, ML; Walsh, SL, 1999) | 0.3 |
" In contrast, there were no sex differences in morphine's hotplate or tail withdrawal effects under repeated (1-week interval) dosing conditions." | ( Sex differences in development of morphine tolerance and dependence in the rat. Bartok, RE; Craft, RM; King, SJ; Stratmann, JA; Walpole, TI, 1999) | 0.3 |
" A dose-response relationship was identified for lordosis in experimental animals receiving icv injection of beta-EP." | ( Facilitatory and inhibitory effects of beta-endorphin on lordosis in female rats: relation to time of administration. Kubo, K; Sasaki, T; Torii, M, 1999) | 0.3 |
" Morphine dosage must therefore be carefully controlled in patients with renal failure." | ( [Morphine poisoning in chronic kidney failure. Morphine-6-glucuronide as a pharmacologically active morphine metabolite]. Caduff, B; Dubs, A; Wiedemeier, P, 1999) | 0.3 |
" There was no dose-response relationship for bromfenac." | ( Comparison of tilidine/naloxone, tramadol and bromfenac in experimental pain: a double-blind randomized crossover study in healthy human volunteers. Högger, P; Rohdewald, P, 1999) | 0.61 |
" Furthermore, morphine-induced analgesia in a hot-plate test showed a leftward shift in the morphine dose-response curve after naloxone treatment." | ( Effects of continuous opioid receptor blockade on alcohol intake and up-regulation of opioid receptor subtype signalling in a genetic model of high alcohol drinking. Hyytiä, P; Ingman, K; Korpi, ER; Laitinen, JT; Soini, SL, 1999) | 0.51 |
"1-235 nmol site(-1)) injected intradermally into the rostral back elicited scratching of the injected site, with bell-shaped dose-response relationship." | ( Itch-associated response induced by intradermal serotonin through 5-HT2 receptors in mice. Kuraishi, Y; Nagasawa, T; Satoh, M; Yamaguchi, T, 1999) | 0.3 |
" These data replicate earlier findings describing the acceptability of alternate-day buprenorphine treatment using multiples of the daily maintenance dose and extend these findings by establishing the clinical efficacy of daily and alternate-day dosing regimens with the combination buprenorphine naloxone tablet." | ( Efficacy of daily and alternate-day dosing regimens with the combination buprenorphine-naloxone tablet. Amass, L; Kamien, JB; Mikulich, SK, 2000) | 0.71 |
" Together with the fact that this dosage of PB blocks the surge of LH secretion in rats in proestrus, the concept of the existence of separate neuronal mechanisms responsible for the surge and pulsatile secretion of LH are supported." | ( Pentobarbital stimulates the activity of the GnRH pulse generator interacting with opioid neurons in rats in proestrus. Funabashi, T; Jinnai, K; Kimura, F; Sano, A; Shinohara, K, 2000) | 0.31 |
"We observed chest wall rigidity in 8 patients after low dosage of fentanyl (3-5 microg/kg body weight)." | ( Fentanyl-induced chest wall rigidity and laryngospasm in preterm and term infants. Bartmann, P; Fahnenstich, H; Kau, N; Steffan, J, 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 |
" 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 |
" Dosing was double-blind and double-dummy." | ( Effects of buprenorphine versus buprenorphine/naloxone tablets in non-dependent opioid abusers. Bigelow, GE; Stoller, K; Strain, EC; Walsh, SL, 2000) | 0.57 |
"We examined two methods of generating a dose-response curve to the opioid receptor antagonist naloxone." | ( Plasma adrenocorticotropin responses to opioid blockade with naloxone: generating a dose-response curve in a single session. Ali, M; Mangold, D; McCaul, ME; Wand, GS, 2000) | 0.77 |
") 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 |
" In the presence of morphine the ACh dose-response curve was shifted to the right in a parallel fashion, suggesting a competitive interaction." | ( Morphine inhibits an alpha9-acetylcholine nicotinic receptor-mediated response by a mechanism which does not involve opioid receptors. Elgoyhen, AB; Guth, PS; Holt, JC; Lioudyno, MI; Verbitsky, M, 2000) | 0.31 |
" Therefore, activity at opioid receptors appears to influence the expression of TS, and the difference in response to naloxone in TS subjects may be based on a dose-response effect." | ( Patterns of response to acute naloxone infusion in Tourette's syndrome. Chappell, PB; Leckman, JF; Scahill, LD; van Wattum, PJ; Zelterman, D, 2000) | 0.8 |
" When combined with naloxone in a sublingual tablet, buprenorphine has been shown to be effective 1) in retaining patients in treatment, 2) in reducing opioid use and craving, and 3) when dosed less-than-daily." | ( Buprenorphine and naloxone for heroin dependence. Johnson, RE; McCagh, JC, 2000) | 0.96 |
"A sublingual tablet formulation of buprenorphine combining 8 mg of buprenorphine with 2 mg of naloxone is being targeted for use in settings where less than daily dosing strategies and/or prescription-based dispensing will likely be employed." | ( Thrice-weekly supervised dosing with the combination buprenorphine-naloxone tablet is preferred to daily supervised dosing by opioid-dependent humans. Amass, L; Kamien, JB; Mikulich, SK, 2001) | 0.77 |
" With increasing stimulus intensity, the dose-response curves showed a progressive shift to the right, but this shift was only slight with the highest intensity stimuli." | ( Effects of intravenous and intrathecal sufentanil on a C-fibre reflex elicited by a wide range of stimulus intensities in the rat. Adam, F; Chauvin, M; Guirimand, F, 2001) | 0.31 |
" Because of the equivalence of different dose strengths of Valoron N tablets, patients are able to exchange low dosed Valoron N retard tablets for higher-dosed ones (50 mg, 100 mg and 200 mg tilidine/tablet), if necessary." | ( Pharmacokinetics of nortilidine and naloxone after administration of tilidine/naloxone solution or tilidine/naloxone sustained release tablets. Brennscheidt, U; Seiler, KU; Thomann, P, 2000) | 0.58 |
" 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 |
" This dose-response analysis suggests that the increase in the severity of autonomic manifestations of MW is associated with a gradual activation of major structures of the autonomic nervous system." | ( Sensitivity to naloxone of the behavioral signs of morphine withdrawal and c-Fos expression in the rat CNS: a quantitative dose-response analysis. Besson, JM; Gestreau, C; Le Guen, S, 2001) | 0.66 |
" The time course and dose-response studies demonstrated that mu receptor phosphorylation was a rapid event, exhibited a positive dose-dependent response, and was similar to that observed in the cloned mu receptor in CHO cells." | ( Agonist-induced mu opioid receptor phosphorylation and functional desensitization in rat thalamus. Deng, HB; Guang, W; Wang, H; Wang, JB; Yu, Y, 2001) | 0.31 |
" Relative to morphine-naive control mice, significant rightward shifts in the morphine dose-response curve, resulting in increased morphine ED(50) values (approximately two to three-fold), was observed for all genotypes following three days of repeated systemic morphine injections." | ( Morphine tolerance and dependence in nociceptin/orphanin FQ transgenic knock-out mice. Chen, ZP; Hopkins, E; Kest, B; Mogil, JS; Palmese, CA; Pintar, JE, 2001) | 0.31 |
" Test sessions were twice per week; dosing was double-blind." | ( Effects of buprenorphine/naloxone in opioid-dependent humans. Bigelow, GE; Stoller, KB; Strain, EC; Walsh, SL, 2001) | 0.61 |
") and three others received multiple infusions, with the maximal dosage being 10 mg, and the effect of naloxone on symptom severity was determined." | ( Effect of naloxone therapy on depersonalization: a pilot study. Hamper, N; Kushnir, ON; Morozova, MG; Nuller, YL, 2001) | 0.93 |
" The association of calcium and Nx at low dosage is a safe method to treat milk fever in cows and reduces muscular complications." | ( Effects of naloxone on calcium turnover in cows affected by milk fever. Dell'Aquila, ME; Minoia, P; Sciorsci, RL, 2001) | 0.7 |
"Morphine pretreatment 1 h prior to assessment of the cocaine dose-response function significantly enhanced the discriminative stimulus effects of cocaine." | ( Temporal factors affecting cocaine-opioid interactions: a cocaine drug discrimination study in rats. Green-Jordan, K; Kantak, KM; Warren, L, 2001) | 0.31 |
" The infrequent use of resuscitation medications has impeded rigorous investigations to determine the most effective agents and/or dosing regimens." | ( Medications during resuscitation -- what is the evidence? Niermeyer, S; Perlman, J; Wyckoff, MH, 2001) | 0.31 |
" Both sexes displayed a positive dose-response relationship between acute morphine and naloxone doses and jumping frequency." | ( Assessment of acute and chronic morphine dependence in male and female mice. Adler, M; Hopkins, E; Juni, A; Kest, B; Palmese, CA, 2001) | 0.53 |
" The need for clear guidelines regarding the drug's appropriate parenteral dosing and administration is essential." | ( Seizures with intravenous codeine phosphate. Al Mohaimeed, SA; Zolezzi, M, 2001) | 0.31 |
" We used the tail-flick test to construct dose-response curves before and 4 days after chronic morphine (75-mg pellets, subcutaneously (s." | ( Reduced development of tolerance to the analgesic effects of morphine and clonidine in PKC gamma mutant mice. Basbaum, AI; Gilbert, H; Malmberg, AB; Zeitz, KP, 2001) | 0.31 |
") potentiated the cataleptic response of morphine as shown by a rightward shift in the morphine-log dose-response curve." | ( Role of nitric oxide in catalepsy and hyperthermia in morphine-dependent rats. Abou Zeit-Har, MS; Afify, EA; Daabees, TT; Gabra, BH, 2001) | 0.31 |
" Increasing clinical experience will more fully elucidate indications for, and optimal dosing of, naloxone in valproic acid toxic states." | ( Use of naloxone in valproic acid overdose: case report and review. Francis, EH; Roberge, RJ, 2002) | 0.99 |
"To test the opioid blockade efficacy of sublingual buprenorphine/naloxone versus buprenorphine alone and determine whether: (1) the blockade efficacy of buprenorphine/naloxone varies between the time of expected maximal and minimal effects of naloxone, (2) the blockade efficacy of buprenorphine/naloxone and buprenorphine varies as a function of maintenance dose level, and (3) there are adaptive changes over time associated with repeated daily dosing of buprenorphine/naloxone and buprenorphine." | ( Blockade of hydromorphone effects by buprenorphine/naloxone and buprenorphine. Bigelow, GE; Strain, EC; Walsh, SL, 2002) | 0.8 |
" Changes over time associated with repeated daily dosing of buprenorphine/naloxone and buprenorphine were minimal." | ( Blockade of hydromorphone effects by buprenorphine/naloxone and buprenorphine. Bigelow, GE; Strain, EC; Walsh, SL, 2002) | 0.8 |
" The failure of naloxone to completely antagonize the effect of the higher concentration of EM-1 or EM-2 could be due to insufficient dosage or might indicate the involvement of non-opiate receptor mechanisms." | ( Effect of endomorphin on somatostatin secretion in the isolated perfused rat stomach. Allescher, HD; Lippl, F; Schusdziarra, V, ) | 0.48 |
" 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 |
" Naloxone was administered as an intravenous bolus, followed by continuous infusion according to an intravenous dosing nomogram." | ( Influence of naloxone on gastric emptying of solid meals, myoelectrical gastric activity and blood hormone levels in young healthy volunteers. Brenneisen, R; Gaia, C; Lourens, ST; Lüscher, D; Netzer, P; Noelpp, U; Reber, PU; Scheurer, U; Varga, L; Wildi, S, 2002) | 1.59 |
"We report the use of a sensitive non-tomographic positron detecting system to measure the dose-response curve of naloxone in human brain." | ( Naloxone displacement at opioid receptor sites measured in vivo in the human brain. Malizia, AL; Melichar, JK; Nutt, DJ, 2003) | 1.97 |
" After the morphinistic models of white rats and mice were made by ever increasing doses of morphine each time, the animals were divided into large dosage QJY group, small dosage QJY group, sustained morphine group and control group." | ( [Experimental study on the effect of abstinence with herbal preparation qingjunyin]. Lan, S; Lu, H; Shi, C; Wang, G; Zhan, C, 1998) | 0.3 |
"To evaluate the efficacy and safety of moderate dosage naloxone in acute moderate and severe traumatic brain injury." | ( [Randomized double-blind clinical trial of moderate dosage naloxone in acute moderate and severe traumatic brain injury]. Chen, B; Liu, YS, 2002) | 0.81 |
"Early application of moderate dosage naloxone in acute traumatic brain injury may significantly reduce the mortality rate and improve the recovery of nerve function." | ( [Randomized double-blind clinical trial of moderate dosage naloxone in acute moderate and severe traumatic brain injury]. Chen, B; Liu, YS, 2002) | 0.83 |
"Male, Long-Evans rats were habituated to an open-field, locomotor activity chamber, and the effects of cocaine and various opioids were tested under a cumulative dosing procedure." | ( Interactions between opioids and cocaine on locomotor activity in rats: influence of an opioid's relative efficacy at the mu receptor. Bryant, PA; Craig, CK; Ferguson, ME; French, AM; Gordon, KA; Gray, JD; McClean, JM; Smith, MA; Tetirick, JC, 2003) | 0.32 |
" Morphine exhibited a bell-shaped dose-response curve in Lewis rats, these animals being more sensitive than F344 at 1 and 5 mg/kg but less sensitive at 10 mg/kg." | ( The contribution of alpha2-adrenoceptor and opioid receptor mechanisms to antinociception differs in Lewis and Fischer 344 rats. Alguacil, LF; Herradón, G; Morales, L; Pérez-García, C, 2003) | 0.32 |
" A relatively flat dose-response relationship was observed, which did not increase monotonically with morphine dose." | ( A new progressive ratio schedule for support of morphine self-administration in opiate dependent rats. Delich, J; Glowa, J; Grasing, K; He, S; Li, N; Parrish, C, 2003) | 0.32 |
"For biotherapeutic agents, there is a lack of information on dose-response relationships and mechanism of action." | ( Dose-response relationship and mechanism of action of Saccharomyces boulardii in castor oil-induced diarrhea in rats. Gillardin, JM; Girard, P; Lorette, I; Pansart, Y, 2003) | 0.32 |
"), which produced a significant shift to the right of the morphine dose-response curve." | ( Role of Na(+), K(+)-ATPase in morphine-induced antinociception. Agil, A; Baeyens, JM; Del Pozo, E; Horvath, G; Masocha, W; Ocana, M; Szikszay, M, 2003) | 0.32 |
" Rats were then anesthetized, and the electromyographic response in the rectus abdominis muscle to UCD was recorded in the absence and presence of cumulative dosing with intrathecal morphine." | ( Intrathecal morphine reduces the visceromotor response to acute uterine cervical distension in an estrogen-independent manner. Eisenach, JC; Shin, SW, 2003) | 0.32 |
") from saline on a fixed-ratio schedule (FR 10), and ethanol dose-response tests were conducted once rats had acquired ethanol-saline discrimination." | ( Micro1-opioid antagonist naloxonazine alters ethanol discrimination and consumption. Holloway, F; Mhatre, M, 2003) | 0.32 |
" Drug tests were then begun and produced a significant dose-response threshold increase across animals, without reinstating the latency to escape nucleus reticularis gigantocellularis stimulation." | ( Effects of naloxone on rewarding and aversive brain sites. Bielajew, C; Diotte, M; Milairessis, E, 2003) | 0.71 |
" Dose-response curves (s." | ( Interaction between metamizol and tramadol in a model of acute visceral pain in rats. Planas, E; Pol, O; Poveda, R; Puig, MM; Romero, A; Sánchez, S, 2003) | 0.32 |
" On the 7th day, morphine dose-response studies were determined using the tail flick." | ( Chronic opioid antagonist treatment dose-dependently regulates mu-opioid receptors and trafficking proteins in vivo. Patel, CN; Patel, K; Purohit, V; Rajashekara, V; Yoburn, BC, 2003) | 0.32 |
" The lowest dosage of NTX significantly reduced SIB in subjects with baseline levels of beta-E higher than after SIB." | ( beta-Endorphin and ACTH are dissociated after self-injury in adults with developmental disabilities. Chicz-DeMet, A; Lenjavi, M; Marion, S; Sandman, CA; Touchette, P, 2003) | 0.32 |
"In this article we described a 15-year-old female who was admitted to the Clinic of Toxicology because of suicidal, oral intoxication with morphine sulphate in the total dosage of 360 mg." | ( [Non-invasive positive pressure respiration in acute respiratory failure caused by suicidal oral intoxication with morphine sulphate]. Anand, JS; Chodorowski, Z; Wujtewicz, M, 2003) | 0.32 |
" Microinfusions of naloxone alone in similar dosage completely blocked the predatory attack response as indicated by an increase in the threshold current strength for somatomotor as well as affective display components." | ( Enkephalinergic involvement in substantia nigra in the modulation of hypothalamically-induced predatory attack behavior. Bhatia, SC; Nayar, U; Saha, SN, 2003) | 0.65 |
" 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 |
" Naloxone 2 mg by gastric tube every 8 hours for 8 days was started; the dosage then was increased to 4 mg every 8 hours." | ( Enteral administration of naloxone for treatment of opioid-associated intragastric feeding intolerance. Bloom, K; Liebl, MG; Mixides, G, 2004) | 1.53 |
" Separate groups of animals at each interval between morphine and naloxone received cumulative naloxone dosing after all morphine pretreatments (NAL ALL DAYS) or after just the first and last morphine pretreatment (NAL FIRST/LAST)." | ( Conditioning processes contribute to severity of naloxone-precipitated withdrawal from acute opioid dependence. Liu, J; Morse, AC; Schulteis, G, 2004) | 0.81 |
" However, the few studies that have investigated the performance effects of buprenorphine in opioid-abusing volunteers examined effects of single acute doses rather than effects of repeated dosing and included a very limited range of measures." | ( A dose-effect study of repeated administration of buprenorphine/naloxone on performance in opioid-dependent volunteers. Correia, CJ; Mintzer, MZ; Strain, EC, 2004) | 0.56 |
" Furthermore, the differences between intermittent and continuous dosing protocols were evaluated." | ( Opioid agonist and antagonist treatment differentially regulates immunoreactive mu-opioid receptors and dynamin-2 in vivo. Patel, K; Purohit, V; Yoburn, BC; Zhang, Q, 2004) | 0.32 |
" However, using access to unsupervised dosing to promote abstinence from heroin probably limits the potential benefits of unsupervised administration to a very small proportion of patients." | ( A pilot study of buprenorphine-naloxone combination tablet (Suboxone) in treatment of opioid dependence. Bell, J; Byron, G; Gibson, A; Morris, A, 2004) | 0.61 |
" Pre-exposure to ICI174864 also induced a shift to the left in dose-response curves for bremazocine and TIPP." | ( Reciprocal regulation of agonist and inverse agonist signaling efficacy upon short-term treatment of the human delta-opioid receptor with an inverse agonist. Azzi, M; Bouvier, M; deLéan, A; Piñeyro, G; Schiller, PW, 2005) | 0.33 |
" The effects of individual and fixed-ratio combinations of locally (subcutaneous) and systemically (intraperitoneal) dosed tramadol were evaluated using the formalin test in rats." | ( Evidence of self-synergism in the antinociceptive effect of tramadol in rats. Aguirre-Bañuelos, P; Arellano-Guerrero, A; de Pozos-Guillén, AJ; Hoyo-Vadillo, C; Pérez-Urizar, J, 2004) | 0.32 |
" Morphine and R-PIA were administered to obtain the dose-response curve and the 50% effective dose (ED(50))." | ( Morphine can enhance the antiallodynic effect of intrathecal R-PIA in rats with nerve ligation injury. Cho, SK; Han, SM; Hwang, GS; Hwang, JH, 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) | 0.77 |
" In conclusion, from the above results one may suggest that, in determination of the dose-response of at least some drugs, the study of the effects of doses much lower than two orders of magnitude of the minimum effective dose are warranted." | ( Effects of ultra-low doses of morphine, naloxone and ethanol on morphine state-dependent memory of passive avoidance in mice. Djahanguiri, B; Tayebi Meybodi, K; Vakili Zarch, A; Zarrindast, MR, 2005) | 0.6 |
" However, the dose-response curve against dermorphine inhibition of the response to CCK-8 was bell-shaped and the highest SR concentration also significantly decreased the mu-withdrawal response." | ( Involvement of the cannabinoid CB1 receptor in the opioid inhibition of the response to cholecystokinin and acute withdrawal response. Amico, MC; Morrone, LA; Palmery, M; Romanelli, L; Tucci, P; Valeri, P, 2005) | 0.33 |
" Three groups of rats were compared in an experimental procedure of rapid withdrawal induction by an antagonist under anaesthesia using sub-anaesthetic dosage of midazolam, ketamine or saline." | ( Effects of anaesthetic agents in interference of naloxone-induced opiate-withdrawal are dose-dependent in opiate-dependent rats. Antoniali, V; Campanella, S; Clement, B; Dan, B; Hanak, C; Pelc, I; Streel, E; Vanderlinden, P; Verbanck, P, 2005) | 0.58 |
" Maintenance dosing was individualized to treat chronic pain." | ( Sublingual buprenorphine is effective in the treatment of chronic pain syndrome. Barkin, RL; Malinoff, HL; Wilson, G, ) | 0.13 |
" Consistent with its long duration of action, alvimopan has a slow dissociation rate from the micro opioid receptor compared to other shorter acting antagonists and may be more potent if administered prior to dosing with exogenous opioids." | ( [(3)H]Alvimopan binding to the micro opioid receptor: comparative binding kinetics of opioid antagonists. Cassel, JA; Daubert, JD; DeHaven, RN, 2005) | 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 |
" Mice were then given morphine in a 4-day escalating morphine administration paradigm followed by reassessment of the morphine dose-response relationship." | ( Chronic pain and genetic background interact and influence opioid analgesia, tolerance, and physical dependence. Clark, DJ; Guo, T; Kingery, WS; Liang, DY; Liao, G; Peltz, G, 2006) | 0.33 |
" Moreover, dose-response curves of the agonists showed that mu and CB1 receptors mediating inhibition of [3H]glutamate release display a non-additive interaction, whereas these receptors synergistically interact regarding their inhibitory control of [3H]GABA release." | ( Interactions between CB1 cannabinoid and mu opioid receptors mediating inhibition of neurotransmitter release in rat nucleus accumbens core. De Vries, TJ; Hogenboom, F; Schoffelmeer, AN; Wardeh, G, 2006) | 0.33 |
" At a dosage of 20 or 40 mg/kg, PF preconditioning 48 h before MCAO followed by 24-h reperfusion significantly reduced the mortality and infarct volume and reversed the neurological deficits caused by ischemia." | ( Involvement of multitargets in paeoniflorin-induced preconditioning. Cai, X; Chen, DM; Xiao, L; Zeng, R; Zhu, XZ, 2006) | 0.33 |
"Buprenorphine has a long duration of action that allows less than daily dosing for opioid dependence, but pharmacologic characterization of buprenorphine's duration of effects over multiple days is incomplete." | ( Effects associated with double-blind omission of buprenorphine/naloxone over a 98-h period. Bigelow, GE; Correia, CJ; Strain, EC; Walsh, SL, 2006) | 0.57 |
" In the abdominal constriction test, LXM-10 had a significant dose-response effect, and the maximal inhibition ratio was 79." | ( Antinociceptive effects of the novel spirocyclopiperazinium salt compound LXM-10 in mice. Li, CL; Li, RT; Sun, Q; Ye, J; Yue, CQ, 2007) | 0.34 |
" It consisted of a 24-day uniform double-blind induction phase followed by single-blind flexible dosing based on structured clinical criteria, for a total of 6 months." | ( A stepped care strategy using buprenorphine and methadone versus conventional methadone maintenance in heroin dependence: a randomized controlled trial. Grönbladh, L; Heilig, M; Kakko, J; Nilsson, LH; Rawlings, B; Rück, C; Svanborg, KD; von Wachenfeldt, J, 2007) | 0.34 |
"5mg) may be an effective mechanism for safely dosing this medication in persons with higher levels of physical dependence." | ( Sublingual buprenorphine/naloxone precipitated withdrawal in subjects maintained on 100mg of daily methadone. Bigelow, GE; Rosado, J; Strain, EC; Walsh, SL, 2007) | 0.64 |
" The mean intended fees for buprenorphine - naloxone according to different dosing and takeaway regimens ranged from $19." | ( The impact of community pharmacy dispensing fees on the introduction of buprenorphine - naloxone in Australia. Lea, T; Ritter, A; Winstock, AR, 2007) | 0.82 |
"To compare the effectiveness and cost-effectiveness of unobserved versus observed dosing of patients seeking treatment of heroin dependence." | ( A randomized trial of effectiveness and cost-effectiveness of observed versus unobserved administration of buprenorphine-naloxone for heroin dependence. Batey, R; Bell, J; Dunlop, A; Mutch, C; Rea, F; Ryan, A; Shanahan, M; Winstock, A, 2007) | 0.55 |
"Participants were allocated randomly to observed or unobserved dosing for 3 months." | ( A randomized trial of effectiveness and cost-effectiveness of observed versus unobserved administration of buprenorphine-naloxone for heroin dependence. Batey, R; Bell, J; Dunlop, A; Mutch, C; Rea, F; Ryan, A; Shanahan, M; Winstock, A, 2007) | 0.55 |
"Retention and heroin use was not significantly different between observed and unobserved dosing groups." | ( A randomized trial of effectiveness and cost-effectiveness of observed versus unobserved administration of buprenorphine-naloxone for heroin dependence. Batey, R; Bell, J; Dunlop, A; Mutch, C; Rea, F; Ryan, A; Shanahan, M; Winstock, A, 2007) | 0.55 |
" Endomorphin-1, endomorphin-2 and deltorphin I at the dosage of 1, 10, 100 nmol/embryo could stimulate angiogenesis dose-dependently, respectively." | ( Endogenous opioid peptides, endomorphin-1 and -2 and deltorphin I, stimulate angiogenesis in the CAM assay. Cui, SG; Dai, X; Liu, Q; Song, HJ; Wang, R; Wang, T, 2008) | 0.35 |
" Dose-response and time course curves were done." | ( Role of nociceptin/orphanin FQ and the pseudopeptide [Phe1Psi(CH2NH)Gly2]-nociceptin(1-13)-NH2 and their interaction with classic opioids in the modulation of thermonociception in the land snail Helix aspersa. Cruz, SL; León-Olea, M; Miller-Pérez, C; Pellicer, F; Rodríguez-Manzo, G; Sánchez-Islas, E, 2008) | 0.35 |
"Morphine and buprenorphine had parallel dose-response curves in blocking FPS, with buprenorphine 40 times more potent than morphine." | ( Anxiolytic-like effects of morphine and buprenorphine in the rat model of fear-potentiated startle: tolerance, cross-tolerance, and blockade by naloxone. Davis, M; Glover, EM, 2008) | 0.55 |
"The registration of combination buprenorphine/naloxone, a formulation designed to reduce risk of diversion, has led some Australian jurisdictional authorities to allow treatment without direct observation of dosing for stable, opioid-dependent patients." | ( Optimising the benefits of unobserved dose administration for stable opioid maintenance patients: follow-up of a randomised trial. Batey, R; Bell, JR; Mutch, C; Rea, F; Ryan, A, 2008) | 0.6 |
" There was a non-significant trend for people initiated with observed dosing to be better retained during the allocation phase; at 6 months, 13 subjects (22%) from the original unobserved group, and 22 (34%) from the observed group, were retained in treatment (chi2=2." | ( Optimising the benefits of unobserved dose administration for stable opioid maintenance patients: follow-up of a randomised trial. Batey, R; Bell, JR; Mutch, C; Rea, F; Ryan, A, 2008) | 0.35 |
" If access to unobserved dosing is to be restricted to stable patients, it appears preferable to initiate dosing with observation and allow unobserved doses for people who successfully stabilize, than to initiate with unobserved doses and transfer unstable patients to observation." | ( Optimising the benefits of unobserved dose administration for stable opioid maintenance patients: follow-up of a randomised trial. Batey, R; Bell, JR; Mutch, C; Rea, F; Ryan, A, 2008) | 0.35 |
" Thus, like given systemically, (+)-morphine given into the posterior nucleus accumbens shell also induces a U-shaped dose-response curve for attenuating the (-)-morphine-produced conditioned place preference." | ( (+)-Morphine attenuates the (-)-morphine-produced conditioned place preference and the mu-opioid receptor-mediated dopamine increase in the posterior nucleus accumbens of the rat. Hong, JS; Hung, KC; Schwasinger, ET; Terashvili, M; Tseng, LF; Wu, HE, 2008) | 0.35 |
" After implementation of standard order sets for patients receiving PCA, 57% of patients' pain was documented as being controlled, and the orders for 93% of patients were in compliance with the recommended dosage interval of > or =10 minutes." | ( Implementation of standard order sets for patient-controlled analgesia. Ghafoor, VL; Phelps, P; Weber, LM, 2008) | 0.35 |
" Opioids are often reduced in dosage or even discontinued as a result of impaired bowel function, leading to insufficient pain treatment." | ( Analgesic efficacy and safety of oxycodone in combination with naloxone as prolonged release tablets in patients with moderate to severe chronic pain. Fleischer, W; Grothe, B; Hermanns, K; Hopp, M; Leyendecker, P; Meissner, W; Reimer, K; Ruckes, C; Szombati, I; Vondrackova, D; Weber, S, 2008) | 0.59 |
" National guidelines recommend directly observed initial dosing followed by multiple in-clinic visits during the induction week." | ( Home buprenorphine/naloxone induction in primary care. DiRocco, D; Gourevitch, MN; Grossman, E; Lee, JD, 2009) | 0.68 |
" Patients initiated dosing off-site at a later time." | ( Home buprenorphine/naloxone induction in primary care. DiRocco, D; Gourevitch, MN; Grossman, E; Lee, JD, 2009) | 0.68 |
"Non-blinded dosing with Suboxone during the 1-month stabilization phase included 3 weeks of flexible dosing as determined appropriate by the study physicians." | ( Buprenorphine tapering schedule and illicit opioid use. Annon, J; Bilangi, R; Boverman, J; Domier, C; Doraimani, G; Hasson, A; Hillhouse, M; Hunter, J; Jenkins, J; Ling, W; Saxon, A; Selzer, J; Thomas, C, 2009) | 0.35 |
" Development of opioid withdrawal symptoms was the primary outcome, however the only symptom that was significantly associated with BPN/NLX dosage was the report of "stomach pains" (p = ." | ( Lack of reduction in buprenorphine injection after introduction of co-formulated buprenorphine/naloxone to the Malaysian market. Altice, FL; Bruce, RD; Govindasamy, S; Kamarulzaman, A; Sylla, L, 2009) | 0.57 |
" These effects were not associated with alterations in ethanol pharmacokinetic properties or with shifts in the biphasic ethanol dose-response curve." | ( Ethanol-induced social facilitation in adolescent rats: role of endogenous activity at mu opioid receptors. Spear, LP; Varlinskaya, EI, 2009) | 0.35 |
") enhanced the ascending (3 mgxkg(-1)) and descending (30 mgxkg(-1)) portions of buprenorphine's dose-response curve, but only spinal, not supraspinal, nociceptin (10 nmolxL(-1)) enhanced buprenorphine anti-nociception." | ( Identification of an additional supraspinal component to the analgesic mechanism of action of buprenorphine. Ding, Z; Raffa, RB, 2009) | 0.35 |
" In the second experiment, using the same dosing regimen, sampling continued 3 h after morphine or saline in AV411- or vehicle-treated rats." | ( The glial activation inhibitor AV411 reduces morphine-induced nucleus accumbens dopamine release. Bland, ST; Hutchinson, MR; Johnson, KW; Maier, SF; Watkins, LR, 2009) | 0.35 |
" No dosage modification of BUP/NLX is required when co-administered with TPV/r." | ( Pharmacokinetic interactions between buprenorphine/naloxone and tipranavir/ritonavir in HIV-negative subjects chronically receiving buprenorphine/naloxone. Altice, FL; Andrews, L; Bruce, RD; Conner, C; Fang, WB; Friedland, GH; Lin, SN; Moody, DE; Piliero, PJ; Sabo, JP; Wruck, JM, 2009) | 0.6 |
"The present investigation examines baseline patient characteristics to predict dosing of buprenorphine-naloxone, a promising treatment for opioid addiction in youths." | ( Predictors of buprenorphine-naloxone dosing in a 12-week treatment trial for opioid-dependent youth: secondary analyses from a NIDA Clinical Trials Network study. Chakrabarti, A; Griffin, ML; Subramaniam, G; Weiss, RD; Woody, GE, 2010) | 0.87 |
" Outpatients aged 15-21 were randomized to a 12-week buprenorphine-naloxone dosing condition (including 4 weeks of taper)." | ( Predictors of buprenorphine-naloxone dosing in a 12-week treatment trial for opioid-dependent youth: secondary analyses from a NIDA Clinical Trials Network study. Chakrabarti, A; Griffin, ML; Subramaniam, G; Weiss, RD; Woody, GE, 2010) | 0.89 |
" During the dosing period, there were no significant differences in opioid use, as measured by urinalysis, by level of pain." | ( Predictors of buprenorphine-naloxone dosing in a 12-week treatment trial for opioid-dependent youth: secondary analyses from a NIDA Clinical Trials Network study. Chakrabarti, A; Griffin, ML; Subramaniam, G; Weiss, RD; Woody, GE, 2010) | 0.65 |
" This can be achieved by converting the regular dosage into the equivalent in diazepam and then reducing this dosage by a maximum of 25% a week." | ( [Guideline 'Medicinal care for drug addicts in penal institutions']. Arends, MT; de Haan, HA; Klazinga, NS; van Everdingen, JJ; Westra, M, 2009) | 0.35 |
" Intrathecal opioid dosing is limited, however, by opioid-related side effects, most importantly respiratory depression." | ( Postoperative analgesia after radical prostatectomy with high-dose intrathecal morphine and intravenous naloxone: a retrospective review. Andrykowski, M; Rebel, A; Sloan, P, ) | 0.35 |
" A total of 77 patients were included and were switched from buprenorphine to sublingual tables of buprenorphine/naloxone; the buprenorphine dosage was titrated to achieve good control of withdrawal symptoms." | ( Safety and efficacy of buprenorphine/naloxone in opioid-dependent patients: an Italian observational study. Biondi, L; Calabria, R; Fiore, A; Magnelli, F; Peluso, E; Rota, AG; Vonella, D, 2010) | 0.84 |
" Treatment was self-administered by the patients every 2 weeks and the mean buprenorphine dosage at 1 year was 8 mg/day." | ( Clinical experience with fortnightly buprenorphine/naloxone versus buprenorphine in Italy: preliminary observational data in an office-based setting. Amato, P, 2010) | 0.61 |
" Dose-response curves of tapentadol (intravenous) were determined in combination with vehicle or a fixed dose (intraperitoneal) of the mu-opioid receptor antagonist naloxone (1mg/kg), the alpha2-adrenoceptor antagonist yohimbine (2." | ( Differential contribution of opioid and noradrenergic mechanisms of tapentadol in rat models of nociceptive and neuropathic pain. Christoph, T; Jahnel, U; Schröder, W; Tzschentke, TM; Vry, JD, 2010) | 0.56 |
" Buprenorphine/naloxone and LPV/r can be safely coadministered without need for dosage modification." | ( Pharmacokinetic interactions between buprenorphine/naloxone and once-daily lopinavir/ritonavir. Altice, FL; Andrews, L; Bruce, RD; Fang, WB; Friedland, GH; Lin, SN; Ma, Q; Moody, DE; Morse, GD, 2010) | 0.97 |
" The aim of this review is to outline the pharmacodynamic and pharmacokinetic properties, drug interactions, dosing rules, adverse effects, equianalgesic dose ratio with other opioids and clinical studies of oxycodone in patients with cancer pain." | ( Role of oxycodone and oxycodone/naloxone in cancer pain management. Leppert, W, ) | 0.41 |
" Subsequent studies show that the efficacy of buprenorphine sublingual tablet (Subutex®) or buprenorphine/naloxone sublingual tablet (Suboxone®) is equivalent to that of methadone when sufficient buprenorphine doses, rapid induction, and flexible dosing are used." | ( Buprenorphine-based regimens and methadone for the medical management of opioid dependence: selecting the appropriate drug for treatment. Gerra, G; Maremmani, I, ) | 0.34 |
" Lethal dose to cause 50 % death (LD50) was calculated from a dose-response curve (100-5000 mg/kg body wt." | ( Chemical composition, acute toxicity, and antinociceptive activity of the essential oil of a plant breeding cultivar of basil (Ocimum basilicum L.). Alves, PB; Antoniolli, AR; Blank, AF; de Araujo, BS; Estevam, Cdos S; Lira, AF; Marchioro, M; Onofre, AS; Venâncio, AM, 2011) | 0.37 |
"The effectiveness of intrathecal opioids (ITOs) for postoperative analgesia has been limited by reduced opioid dosing because of opioid-related side effects, most importantly respiratory depression." | ( Retrospective analysis of high-dose intrathecal morphine for analgesia after pelvic surgery. Andrykowski, M; Rebel, A; Sloan, P, ) | 0.13 |
"After 3 weeks of flexible dosing, 516 participants were categorized by dose provided in the final dosing week (9." | ( Participant characteristics and buprenorphine dose. Canamar, CP; Doraimani, G; Hasson, A; Hillhouse, M; Ling, W; Thomas, C, 2011) | 0.37 |
" These groups also differed in opioid use during the four dosing weeks, with the lowest use in the 8 mg group and highest use in the 24 mg group (p < ." | ( Participant characteristics and buprenorphine dose. Canamar, CP; Doraimani, G; Hasson, A; Hillhouse, M; Ling, W; Thomas, C, 2011) | 0.37 |
"The purpose of this study was to examine the effects of a clinically relevant opioid on the production of augmented breaths (ABs) in unanesthetized animals breathing normal room air, using a dosage which does not depress breathing." | ( The "other" respiratory effect of opioids: suppression of spontaneous augmented ("sigh") breaths. Azubike, E; Bell, HJ; Haouzi, P, 2011) | 0.37 |
"Clients from two opioid treatment programs, one implementing ICM and one implementing the TBCM, were recruited to undertake a self-complete survey examining satisfaction with case-management during dosing hours over 7 months." | ( Individual versus team-based case-management for clients of opioid treatment services: an initial evaluation of what clients prefer. Curry, K; Day, CA; Demirkol, A; Haber, PS; Hines, S; Lintzeris, N; Tynan, M, 2012) | 0.38 |
"Buprenorphine/naloxone has recently been introduced in Australia and is available for unsupervised dosing within Queensland." | ( Use and misuse of opioid replacement therapies: a Queensland study. Kemp, R; Smirnov, A, 2012) | 0.74 |
"The dosing of opioid receptor agonist medications adequately and on an individual basis is crucial in the pharmacotherapy of opioid dependence." | ( Evaluation of buprenorphine dosage adequacy in opioid receptor agonist substitution therapy for heroin dependence: first use of the BUprenorphine-naloxone Dosage Adequacy eVAluation (BUDAVA) questionnaire. Amato, P; Armenante, C; Auriemma, F; Biancolillo, V; Cassese, F; D'Amore, A; Del Tufo, S; Lauro, G; Oliva, P; Pizzirusso, A; Romano, F; Ruoppolo, C, 2012) | 0.58 |
" Dosage adequacy was assessed with the BUDAVA questionnaire." | ( Evaluation of buprenorphine dosage adequacy in opioid receptor agonist substitution therapy for heroin dependence: first use of the BUprenorphine-naloxone Dosage Adequacy eVAluation (BUDAVA) questionnaire. Amato, P; Armenante, C; Auriemma, F; Biancolillo, V; Cassese, F; D'Amore, A; Del Tufo, S; Lauro, G; Oliva, P; Pizzirusso, A; Romano, F; Ruoppolo, C, 2012) | 0.58 |
"The buprenorphine-naloxone dosage was found to be inadequate in 61 of the 196 patients." | ( Evaluation of buprenorphine dosage adequacy in opioid receptor agonist substitution therapy for heroin dependence: first use of the BUprenorphine-naloxone Dosage Adequacy eVAluation (BUDAVA) questionnaire. Amato, P; Armenante, C; Auriemma, F; Biancolillo, V; Cassese, F; D'Amore, A; Del Tufo, S; Lauro, G; Oliva, P; Pizzirusso, A; Romano, F; Ruoppolo, C, 2012) | 0.91 |
" Pharmacokinetic profiles of buprenorphine, norbuprenorphine, and naloxone were measured over the 24-hour dosing interval on day -1 (buprenorphine/naloxone alone, reference) and day 7 of telaprevir coadministration (test)." | ( Effect of telaprevir on the pharmacokinetics of buprenorphine in volunteers on stable buprenorphine/naloxone maintenance therapy. Garg, V; Luo, X; Smith, F; Trevejo, J; van Heeswijk, RP, 2012) | 0.83 |
" 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) | 0.69 |
" 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 |
"Currently published information on buprenorphine-naloxone withdrawal recommends a gradually decreasing dosage over weeks to months." | ( Course and treatment of buprenorphine/naloxone withdrawal: an analysis of case reports. McCance-Katz, EF; Westermeyer, J, ) | 0.66 |
" In the present study, a digoxin dose-response curve was conducted to observe the effects on naloxone-precipitated withdrawal and locomotor activity in mice." | ( A comparison of the effects of digoxin, ouabain and milrinone on naloxone-precipitated withdrawal syndrome in mice. Bai, YL; Chen, YY; Chu, QJ; Li, J; Li, WJ; Zhang, Q, 2012) | 0.84 |
" In the present study, unanesthetized rats were studied to: (1) determine the involvement of naloxone-sensitive receptor pathways, and (2) establish the dose-response relationship of this side effect." | ( Augmented breaths ('sighs') are suppressed by morphine in a dose-dependent fashion via naloxone-sensitive pathways in adult rats. Bell, HJ; Pankuch, G, 2013) | 0.83 |
"Male Spragne-Dawley rats were randomly divided into Saline + Saline group, Saline + sodium hydrosulfide (NaHS) group, Saline + Heroin group, NaHS + Heroin group according to the principle of increasing heroin dosage day by day, with the establishment of heroin-naloxone-induced withdrawal symptoms determined at day 10." | ( Exogenous sodium hydrosulfide can attenuate naloxone-precipitated withdrawal syndromes and affect cAMP signaling pathway in heroin-dependent rat's nucleus accumbens. Cheng, TT; Jiang, LH; Liang, QY; Wang, J; Wei, XL, 2012) | 0.82 |
" This study compared the two formulations on subjective dose effects and equivalence, trough plasma levels, adverse events, patient satisfaction, supervised dosing time, and impact upon treatment outcomes (substance use, psychosocial function)." | ( A randomised controlled trial of sublingual buprenorphine-naloxone film versus tablets in the management of opioid dependence. Ali, R; Degenhardt, L; Dunlop, AJ; Holland, RM; Hurley, M; Larance, B; Leung, SY; Lintzeris, N; Muhleisen, P; Rivas, GR; White, N, 2013) | 0.63 |
" In study II, we performed a dose-response test in these six phenothiazine antipsychotics (0." | ( Phenothiazine-type antipsychotics may attenuate naloxone-precipitated withdrawal jumping in morphine-dependent mice. Chen, JY; Chen, KT; Chu, CC; Liu, KS; Sung, KC; Wang, JJ; Wu, SZ, 2012) | 0.63 |
" Forty-six pharmacies (85%) were willing to dispense buprenorphine-naloxone to more clients; however, 43 pharmacies (80%) perceived that supervision of buprenorphine-naloxone dosing is not a suitable task for pharmacists in Finland." | ( First insights into community pharmacy based buprenorphine-naloxone dispensing in Finland. Bell, JS; Ilomäki, J; Laitinen, K; Tacke, U; Turunen, JH; Uosukainen, H, 2013) | 0.87 |
" Our results demonstrate, for the first time, that LEDT induced a dose-response analgesic effect in the model of PI in mice." | ( Light-emitting diode therapy induces analgesia in a mouse model of postoperative pain through activation of peripheral opioid receptors and the L-arginine/nitric oxide pathway. Cidral-Filho, FJ; Martins, DF; Mazzardo-Martins, L; Santos, AR, 2014) | 0.4 |
" Digital 12-lead ECGs were recorded at baseline and at 10 time points over 24 hours after dosing in each treatment period." | ( Evaluation of the effect of Naloxegol on cardiac repolarization: a randomized, placebo- and positive-controlled crossover thorough QT/QTc study in healthy volunteers. Carlson, G; Gottfridsson, C; Lappalainen, J; Sostek, M, 2013) | 0.39 |
" Similar findings were observed using QTcB; the upper limits of the 2-sided 90% CI were <10 msec at all time points after dosing with naloxegol 25 or 150 mg." | ( Evaluation of the effect of Naloxegol on cardiac repolarization: a randomized, placebo- and positive-controlled crossover thorough QT/QTc study in healthy volunteers. Carlson, G; Gottfridsson, C; Lappalainen, J; Sostek, M, 2013) | 0.39 |
" At the longest trial duration, a bell-shaped dose-response curve was obtained with buprenorphine, which was shifted significantly to the right with naloxone combination." | ( Rewarding or aversive effects of buprenorphine/naloxone combination (Suboxone) depend on conditioning trial duration. Canestrelli, C; Marie, N; Noble, F, 2014) | 0.86 |
" The specific dosage of 100 nM produced additional marked reduction in activity for planaria exposed to either morphine or naloxone while only 1 pM of morphine produced this effect." | ( Comparisons of responses by planarian to micromolar to attomolar dosages of morphine or naloxone and/or weak pulsed magnetic fields: revealing receptor subtype affinities and non-specific effects. Murugan, NJ; Persinger, MA, 2014) | 0.83 |
" Administration of pioglitazone also prevented morphine-induced 50 % effective dose (ED50) shift to the right in the dose-response curve and increased the global analgesic effect of morphine." | ( Pioglitazone prevents morphine antinociception tolerance and withdrawal symptoms in rats. Azarfardian, A; Charkhpour, M; Ghasami, S; Ghavimi, H; Hassanzadeh, K; Maleki-Dizaji, N; Zolali, E, 2014) | 0.4 |
" BUP produces dose- and time-related alterations of μOR availability but some clinicians express concern about whether doses higher than those needed to prevent opioid withdrawal symptoms are warranted, and policymakers consider limiting reimbursement for certain BUP dosing regimens." | ( Buprenorphine maintenance and mu-opioid receptor availability in the treatment of opioid use disorder: implications for clinical use and policy. Comer, SD; Fiellin, DA; Greenwald, MK, 2014) | 0.4 |
" Dosing strategies that take into account both the treatment of the opioid-related effects as well as the negative effects reversal will have on the patient are offered." | ( Use of naloxone for reversal of life-threatening opioid toxicity in cancer-related pain. Faley, B; Gonzalez, R; Howlett, C; Yerram, P, 2016) | 0.89 |
" Adequate dosing levels are important to control cravings, prevent withdrawal syndrome, and maintain patients in treatment." | ( Analysis of buprenorphine/naloxone dosing impact on treatment duration, resource use and costs in the treatment of opioid-dependent adults: a retrospective study of US public and private health care claims. Kharitonova, E; Khemiri, A; Ruby, J; Toumi, M; Zah, V, 2014) | 0.7 |
" The threshold for differentiating the dosing groups was set at 15 and 15." | ( Analysis of buprenorphine/naloxone dosing impact on treatment duration, resource use and costs in the treatment of opioid-dependent adults: a retrospective study of US public and private health care claims. Kharitonova, E; Khemiri, A; Ruby, J; Toumi, M; Zah, V, 2014) | 0.7 |
" There is wide variation between states regarding EMS naloxone dosing protocol and route of administration." | ( Emergency medical services naloxone access: a national systematic legal review. Dailey, MW; Davis, CS; Niehaus, VR; Southwell, JK; Walley, AY, 2014) | 0.95 |
" Repeated morphine injections alone led to a significant rightward shift in the morphine dose-response curve compared with that with A-317491." | ( Blockade and reversal of spinal morphine tolerance by P2X3 receptor antagonist. Jiang, W; Ma, X; Xu, H; Xu, T, 2015) | 0.42 |
"001; n = 373), using a final average daily dosage of 252." | ( [Tapentadol prolonged release improves analgesia, functional impairment and quality of life in patients with chronic pain who have previously received oxycodone/naloxone]. Kern, KU; Krings, D; Waldmann-Rex, S, 2014) | 0.6 |
"Repeat dosing of ALO-02 for up to 12 months is safe and well tolerated in a CNCP population of both opioid-experienced and opioid-naïve patients." | ( A multicenter, 12-month, open-label, single-arm safety study of oxycodone-hydrochloride/naltrexone-hydrochloride extended-release capsules (ALO-02) in patients with moderate-to-severe chronic noncancer pain. Arora, S; Clemmer, R; Goli, V; Hudson, JD; Meisner, P; Michael, D; Pixton, GC; Setnik, B; Sommerville, KW, ) | 0.13 |
" Patient-, provider-, and systems-based factors that might have contributed to the events included chronic health conditions that could predispose an individual to an opioid-related adverse event, failure to adjust opioid dosing in the elderly and for hepatic or renal impairment, multiple doses and routes of administration of opioids, coadministration of opioids with other sedating medications, and systems-based problems with patient handoffs and pharmacy oversight." | ( Preventing iatrogenic overdose: a review of in-emergency department opioid-related adverse drug events and medication errors. Babu, KM; Beaudoin, FL; Janicki, A; McKaig, DM; Merchant, RC, 2015) | 0.42 |
" A total of 1251 participants were randomly assigned to either (1) a 1-year intervention consisting of 2 opportunities for a 15-day detoxification with buprenorphine/naloxone (BUP/NX) combined with up to 21 sessions of behavioral drug and risk counseling [short-term medication-assisted treatment (ST-MAT)] or (2) thrice-weekly dosing for 48 weeks with BUP/NX and up to 21 counseling sessions [long-term medication-assisted treatment (LT-MAT)] followed by dose tapering." | ( Expanding substance use treatment options for HIV prevention with buprenorphine-naloxone: HIV Prevention Trials Network 058. Aramrattana, A; Beauchamp, G; Burns, DN; Celentano, DD; Chawarski, M; Chen, RY; Donnell, D; Dye, BJ; Fu, L; Jackson, JB; Lucas, GM; Ma, J; Metzger, DS; Richardson, P; Rose, SM; Ruan, Y; Shao, Y; Shin, K; Sugarman, J; Wei, L, 2015) | 0.84 |
" Clinically fentanyl dosage adjustments may become necessary when ketoconazole or other strong CYP3A inhibitors are given simultaneously." | ( Pharmacokinetic interaction of intravenous fentanyl with ketoconazole. Haefeli, WE; König, SK; Mahlke, NS; Mikus, G; Skopp, G; Ziesenitz, VC, 2015) | 0.42 |
" Thus, varying the dosage regimen of morphine can reduce the severity of morphine-induced dependency and neurodegeneration." | ( The effect of various morphine weaning regimens on the sequelae of opioid tolerance involving physical dependency, anxiety and hippocampus cell neurodegeneration in rats. Asadighaleni, M; Fatima, S; Karimian, SM; Motaghinejad, M; Motaghinejad, O; Shabab, B, 2015) | 0.42 |
" This study examined (i) how initiations and transfers were implemented, (ii) the profile and predictors of adverse effects as self-reported by BNX film clients, and (iii) dosing issues." | ( The introduction of buprenorphine-naloxone film in opioid substitution therapy in Australia: Uptake and issues arising from changing buprenorphine formulations. Ali, R; Degenhardt, L; Dietze, P; Jenkinson, R; Larance, B; Lintzeris, N; White, N, 2015) | 0.7 |
" The administration of simvastatin also prevented the morphine-induced shift to the right of the 50% effective dose (ED50) in the dose-response curve." | ( Simvastatin prevents morphine antinociceptive tolerance and withdrawal symptoms in rats. Ghasemi, F; Hassanzadeh, K; Izadpanah, E; Moloudi, MR; Moradi, A; Rahimmi, A, 2015) | 0.42 |
"To analyse drug users' views and experiences of naloxone during emergency resuscitation after illicit opiate overdose to identify (i) any evidence of harm caused by excessive naloxone dosing ('over-antagonism'); and (ii) implications for the medical administration of naloxone within contemporary emergency settings." | ( Naloxone--does over-antagonism matter? Evidence of iatrogenic harm after emergency treatment of heroin/opioid overdose. Neale, J; Strang, J, 2015) | 2.12 |
" Participants believed that hospital staff should administer naloxone selectively and cautiously, and prescribe counter-naloxone medication if dosing precipitated withdrawals." | ( Naloxone--does over-antagonism matter? Evidence of iatrogenic harm after emergency treatment of heroin/opioid overdose. Neale, J; Strang, J, 2015) | 2.1 |
" Subsequently, the dosing regimen was increased to 3 mg/kg twice a day over 10 days, although further marked tolerance did not develop." | ( Effects of Acute and Repeated Administration of Oxycodone and Naloxone-Precipitated Withdrawal on Intracranial Self-Stimulation in Rats. Beardsley, PM; Walentiny, DM; Wiebelhaus, JM, 2016) | 0.67 |
" Opioids were not dosed in an equipotent manner." | ( The Changing Use of Intravenous Opioids in an Emergency Department. Albertson, TE; Chenoweth, JA; Clarke, SO; Gutierrez, R; Roche, BM; Sutter, ME; Wintemute, GJ, 2015) | 0.42 |
" The JCAHO program likely was at least indirectly responsible for this change in relative dosing of the opioids." | ( The Changing Use of Intravenous Opioids in an Emergency Department. Albertson, TE; Chenoweth, JA; Clarke, SO; Gutierrez, R; Roche, BM; Sutter, ME; Wintemute, GJ, 2015) | 0.42 |
"Treating animals repeatedly with intermittent and increasing morphine doses has been suggested to allow some withdrawal during each dosing interval, which causes repeated stress." | ( Spontaneous withdrawal in intermittent morphine administration in rats and mice: effect of clonidine coadministration and sex-related differences. Allahverdiyev, O; Enginar, N; Nurten, A; Sehirli, I; Türkmen, AZ, 2015) | 0.42 |
"Male and female rats and mice were administered with increasing doses of morphine twice daily at different dosing intervals." | ( Spontaneous withdrawal in intermittent morphine administration in rats and mice: effect of clonidine coadministration and sex-related differences. Allahverdiyev, O; Enginar, N; Nurten, A; Sehirli, I; Türkmen, AZ, 2015) | 0.42 |
"Male rats and male and female rats displayed manifestations of morphine withdrawal at the end of 14-h and 24-h dosing intervals, respectively." | ( Spontaneous withdrawal in intermittent morphine administration in rats and mice: effect of clonidine coadministration and sex-related differences. Allahverdiyev, O; Enginar, N; Nurten, A; Sehirli, I; Türkmen, AZ, 2015) | 0.42 |
" As speed of drug liberation is the critical performance attribute for a solid dosage form designed to deliver drug in an emergency, a novel imaging based in vitro disintegration assay for buccal tablets was developed." | ( Amorphous Formulation and in Vitro Performance Testing of Instantly Disintegrating Buccal Tablets for the Emergency Delivery of Naloxone. Ahmed, S; Allen, E; Alqurshi, A; Buanz, A; Cameron, P; Forbes, B; Holt, C; Kumar, Z; McDonald, R; Rickard, JA; Royall, PG; Sandhu, V; Stansfield, R; Strang, J; Taylor, D, 2016) | 0.64 |
" When dosing recommendations were different for opioid-tolerant patients these were also recorded." | ( The Evolution of Recommended Naloxone Dosing for Opioid Overdose by Medical Specialty. Connors, NJ; Nelson, LS, 2016) | 0.73 |
" When patients are discontinuing opioid therapy, the dosage should be decreased slowly, especially in those who have intolerable withdrawal." | ( Weighing the Risks and Benefits of Chronic Opioid Therapy. Humphreys, K; Lembke, A; Newmark, J, 2016) | 0.43 |
" These patients required higher dosing and prolonged infusions of naloxone." | ( Fatal Fentanyl: One Pill Can Kill. Adams, AJ; Albertson, TE; Black, HB; Chenoweth, JA; Colby, DK; Davis, MT; Ford, JB; Gerona, RR; Owen, KP; Roche, BM; Sutter, ME, 2017) | 0.69 |
" Stable subjects were dosed intravenously on 5 consecutive days." | ( Abuse deterrence testing: A dose ratio escalation study examining naloxone coadministered with intravenous hydromorphone in non-treatment-seeking, opioid-dependent drug users. Chakaraborty, B; Geoffroy, P; Levy-Cooperman, N; Michalko, KJ; Reiz, JL; Schoedel, KA; Thompson, D, ) | 0.37 |
" 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, ) | 0.34 |
"The aims of the present study are first, to replicate our previous findings in a larger-sized study; second, to examine if high sensitizers (subjects presenting with large SHA after a thermal injury) develop a higher degree of hypersensitivity after naloxone challenge than low sensitizers (subjects presenting with restricted SHA after a thermal injury); and third to examine a dose-response relationship between 3 stable naloxone concentrations controlled by target-controlled infusion, and the unmasking of latent sensitization." | ( Effects of target-controlled infusion of high-dose naloxone on pain and hyperalgesia in a human thermal injury model: a study protocol: A randomized, double-blind, placebo-controlled, crossover trial with an enriched design. Jensen, EK; Springborg, AD; Taylor, BK; Werner, MU, 2016) | 0.87 |
" Based on the findings of the case reviews and results of the opioid knowledge assessments, a series of interventions to address noted deficiencies was implemented over the ensuing months, including enhanced monitoring for sedation, improved clinical decision support in the electronic medical record (EMR), and various adjustments to dosing for high-risk patients." | ( Implementation of solutions to reduce opioid-induced oversedation and respiratory depression. Ley, C; Meisenberg, B; Ness, J; Rao, S; Rhule, J, 2017) | 0.46 |
" This study aimed to determine: 1) if patients who received a 2-mg dose of nasal naloxone administered by BLS required repeat dosing while in the emergency department (ED), and 2) the disposition of these patients." | ( Use of Intranasal Naloxone by Basic Life Support Providers. Dyer, KS; Langlois, BK; Mitchell, PM; Temin, ES; Weiner, SG, ) | 0.69 |
"8 articles met the inclusion criteria: intramuscular, intranasal, intravenous, and subcutaneous dosage forms of naloxone were analyzed to compare their time to administration, time to efficacy, financial impact, administrator safety, and administrator preference." | ( Naloxone Administration for Opioid Overdose Reversal in the Prehospital Setting: Implications for Pharmacists. Bastianelli, KMS; Palombi, L; Weaver, L, 2018) | 2.13 |
" Intranasal naloxone appears to be the optimal dosage form when considering cost, effectiveness, and administrator safety." | ( Naloxone Administration for Opioid Overdose Reversal in the Prehospital Setting: Implications for Pharmacists. Bastianelli, KMS; Palombi, L; Weaver, L, 2018) | 2.3 |
" Additional endpoints assessed at every visit were the impact of pain on quality of life (QoL), breakthrough cancer pain (BTCP) episodes, opioid dosage escalation index, bowel dysfunction, safety, and other side effects." | ( High dosage of a fixed combination oxycodone/naloxone prolonged release: efficacy and tolerability in patients with chronic cancer pain. Amato, F; Ceniti, S; Consoletti, L; Magaldi, D; Mameli, S; Marcassa, C; Notaro, P; Palmieri, V; Pisanu, GM; Vellucci, R, 2017) | 0.71 |
" Daily dosage of OXN-PR slightly increased (T0: 81." | ( High dosage of a fixed combination oxycodone/naloxone prolonged release: efficacy and tolerability in patients with chronic cancer pain. Amato, F; Ceniti, S; Consoletti, L; Magaldi, D; Mameli, S; Marcassa, C; Notaro, P; Palmieri, V; Pisanu, GM; Vellucci, R, 2017) | 0.71 |
" The increase in MNA provides support for a dosage review." | ( Multiple Naloxone Administrations Among Emergency Medical Service Providers is Increasing. Crabaugh, C; Dailey, MW; Faul, M; Kinsman, JM; Lurie, P; Sasser, SM, ) | 0.55 |
"When injectable hydromorphone and diacetylmorphine are individually dosed and monitored, their opioid-related side effects, including potential fatal overdoses, are safely mitigated and treated by health care providers." | ( Safety profile of injectable hydromorphone and diacetylmorphine for long-term severe opioid use disorder. Anis, AH; Brissette, S; Guh, D; Harrison, S; Janmohamed, A; Jutha, S; Krausz, M; MacDonald, S; Marchand, K; Marsh, DC; Oviedo-Joekes, E; Schechter, MT; Zhang, DZ, 2017) | 0.46 |
" This study aimed to determine the frequency of repeat naloxone dosing in suspected narcotic overdose (OD) patients and identify patient characteristics." | ( Incidence of Naloxone Redosing in the Age of the New Opioid Epidemic. Ariyaprakai, N; Bauter, R; Dudley, LS; Harris, MI; Hill, RD; Klebacher, R; Koneru, S; Merlin, MA; Robbins, V; Shanes, A; Tagore, A; Wasserman, E, ) | 0.75 |
"To synthesize evidence on 1) the effects of naloxone route of administration and dosing for suspected opioid overdose in out-of-hospital settings on mortality, reversal of overdose, and harms, and 2) the need for transport to a health care facility after reversal of overdose with naloxone." | ( Management of Suspected Opioid Overdose With Naloxone in Out-of-Hospital Settings: A Systematic Review. Chou, R; Coffin, PO; Davis-O'Reilly, C; Daya, M; Griffin, JC; Grusing, S; Korthuis, PT; McCarty, D, 2017) | 0.98 |
" Vaccination shifted the dose-response curves to the right, representing protection, for each of these endpoints." | ( Safety and efficacy of an oxycodone vaccine: Addressing some of the unique considerations posed by opioid abuse. Baruffaldi, F; Carroll, FI; Comer, SD; Langston, TL; Laudenbach, M; Navarro, HA; Pentel, PR; Peterson, SJ; Pravetoni, M; Raleigh, MD; Runyon, SP; Winston, S, 2017) | 0.46 |
" Four weeks after inducing diabetes, tapentadol dose-response curves were obtained from animals pre-treated with RX821002 or naloxone (alpha2-adrenoceptors and opioid receptors antagonists, respectively)." | ( Opioid and noradrenergic contributions of tapentadol to the inhibition of locus coeruleus neurons in the streptozotocin rat model of polyneuropathic pain. Berrocoso, E; Borges, GDS; Mico, JA; Torres-Sanchez, S, 2018) | 0.69 |
"This quick guide provides you with naloxone dosing information and steps you'll want to take once the crisis has passed." | ( The naloxone option. Abaid, B; Khaleel, MS; Lippman, M; Lippman, S; Naik, S; Prabhu, A, 2018) | 1.32 |
" Most participants with a naloxone kit stated that their frequency and dosage of opiate use did not change after access to naloxone (n = 17 [63%]), and a few used opiates more often (n = 1 [4%]) or less often (n = 9 [33%])." | ( Naloxone Use Among Emergency Department Patients with Opioid Overdose. Ballester, M; Cook, A; Mann, D; Marco, CA; Perkins, O; Rasp, J; Trautman, W, 2018) | 2.22 |
" Participants who had access to a naloxone kit stated that their frequency and dosage of opioid use did not change." | ( Naloxone Use Among Emergency Department Patients with Opioid Overdose. Ballester, M; Cook, A; Mann, D; Marco, CA; Perkins, O; Rasp, J; Trautman, W, 2018) | 2.2 |
"Haemodialysis performed 6-10 h after dosing removed ∼10% of the administered dose of oxycodone predominantly as unconjugated oxycodone and noroxycodone or conjugated oxymorphone and noroxymorphone." | ( Pharmacokinetics of oxycodone/naloxone and its metabolites in patients with end-stage renal disease during and between haemodialysis sessions. Amico, P; Dickenmann, M; Duthaler, U; Hammann, F; Haschke, M; Jehle, AW; Kalbermatter, S; Krähenbühl, S; Lenherr, C; Leuppi-Taegtmeyer, A; Liechti, ME; Meyer Zu Schwabedissen, HE; Schmid, Y, 2019) | 0.8 |
" This sucrose analgesia was completely prevented by systemic dosing of the endocannabinoid CB1 receptor antagonist rimonabant." | ( Hedonic drinking engages a supraspinal inhibition of thermal nociception in adult rats. Davies, AJ; Kim, D; Lee, JY; Oh, SB; Park, J; Pickering, AE; Vang, H, 2019) | 0.51 |
" Dose-response effects of an ethanol crude extract were investigated in the writhing and formalin tests in mice and rats, respectively." | ( Identification of some bioactive metabolites and inhibitory receptors in the antinociceptive activity of Tagetes lucida Cav. Díaz-Reval, MI; González-Trujano, ME; Gutiérrez-Valentino, C; Hernández-Arámburo, MY; Pellicer, F, 2019) | 0.51 |
" Naloxone is an effective antidote to opioid toxicity, yet its optimal dosing in the context of fentanyl and ultra-potent opioid overdoses remains unknown." | ( Naloxone interventions in opioid overdoses: a systematic review protocol. Brasher, PMA; Buxton, JA; Curran, J; Doyle-Waters, MM; Godwin, J; Hau, JP; Hohl, CM; Moe, J; Purssell, R; Shaw, LV, 2019) | 2.87 |
" If we find sufficient variation in dose, we will fit a random effects one-stage model to estimate a dose-response relationship." | ( Naloxone interventions in opioid overdoses: a systematic review protocol. Brasher, PMA; Buxton, JA; Curran, J; Doyle-Waters, MM; Godwin, J; Hau, JP; Hohl, CM; Moe, J; Purssell, R; Shaw, LV, 2019) | 1.96 |
" We will disseminate study results widely to update overdose treatment guidelines and naloxone dosing in Take Home Naloxone programs." | ( Naloxone interventions in opioid overdoses: a systematic review protocol. Brasher, PMA; Buxton, JA; Curran, J; Doyle-Waters, MM; Godwin, J; Hau, JP; Hohl, CM; Moe, J; Purssell, R; Shaw, LV, 2019) | 2.18 |
"Naloxone is an established antidote for the treatment of heroin poisoning; however, dosing regimens vary widely, with a current trend towards small titrated intravenous dosing." | ( One single large intramuscular dose of naloxone is effective and safe in suspected heroin poisoning. Brier, AJ; Harris, K; Isoardi, KZ; Page, CB; Parker, L; Samantray, S, 2020) | 2.27 |
" Further evaluation of naloxone stocking and dosing protocols is needed." | ( Naloxone Dosing After Opioid Overdose in the Era of Illicitly Manufactured Fentanyl. Atti, S; Carpenter, J; Moran, TP; Morgan, B; Murray, BP; Yancey, A, 2020) | 2.31 |
" Excessive naloxone dosing in these circumstances, however, may lead to naloxone-precipitated opioid withdrawal in individuals with opioid dependence." | ( Treatment of acute naloxone-precipitated opioid withdrawal with buprenorphine. Aks, SE; Chhabra, N, 2020) | 1.28 |
" Buprenorphine is also a potent analgesic with high opioid-receptor affinity and binding coefficient; when buprenorphine is administered simultaneously with a μ-opioid receptor full agonist ("full agonist opioid" [FAO]), the combination can yield unexpected outcomes depending on dosing and timing." | ( Perioperative Buprenorphine Continuous Maintenance and Administration Simultaneous With Full Opioid Agonist: Patient Priority at the Interface Between Medical Disciplines. Acampora, GA; Nisavic, M; Zhang, Y, 2020) | 0.56 |
" High-quality comparative naloxone dosing studies assessing effectiveness and safety are needed." | ( Naloxone dosing in the era of ultra-potent opioid overdoses: a systematic review. Brasher, PMA; Buxton, JA; Curran, J; Doyle-Waters, MM; Godwin, J; Hau, JP; Hohl, CM; Moe, J; O'Sullivan, F; Purssell, E; Purssell, R, 2020) | 2.3 |
" Further studies are warranted to explore the optimal dosing strategy for buprenorphine to consistently maintain reversal of respiratory depression but not precipitate withdrawal." | ( Buprenorphine to reverse respiratory depression from methadone overdose in opioid-dependent patients: a prospective randomized trial. Buckley, NA; Hassanian-Moghaddam, H; Zamani, N, 2020) | 0.56 |
" hospitalizations and arrests) and average naloxone dosage per victim." | ( A descriptive study of racial and ethnic differences of drug overdoses and naloxone administration in Pennsylvania. Angulski, K; Barboza, GE, 2020) | 1.05 |
" In this study, rates of opioid withdrawal symptoms (OW) and reversal of opioid toxicity in patients treated with two naloxone dosing regimens were evaluated." | ( Comparison of rates of opioid withdrawal symptoms and reversal of opioid toxicity in patients treated with two naloxone dosing regimens: a retrospective cohort study. Balshaw, R; Brubacher, JR; Buxton, J; Cochrane, CK; Crabtree, A; DeWitt, C; Erdelyi, S; Godwin, J; Ho, V; Jiang, A; Kestler, A; Moe, J; Ng, B; Purssell, R; Risi, A; Rowe, A; Scheuermeyer, F, 2021) | 1.04 |
" According to the Canadian National clinical practice guideline on the management of opioid use disorders, given the superior safety profile of buprenorphine/naloxone and its potential for flexible take-home dosing in comparison to other opioid agonist medication it is strongly recommended to initiate opioid agonist treatment with buprenorphine/naloxone as the preferred first-line treatment when possible." | ( Rapid Micro-induction of Buprenorphine/Naloxone for Opioid Use Disorder in a Critically ill Intubated Patient: A Case Report. Griesdale, D; Hamata, B; Hann, J; Rezazadeh-Azar, P, 2020) | 1.02 |
"This review-with tables summarizing opioid options, dosing considerations, and recommendations for tapering-will help you provide rigorous Tx for noncancer pain while ensuring patient safety." | ( Tips and tools for safe opioid prescribing. Aschenbrenner, H; Berg, JM; Linn, BS; Mahvan, T; Oung, AB; Smith, BEY, ) | 0.13 |
" We measured duration and efficacy of 1 mg/kg buprenorphine after 1 mg/kg sustained-release buprenorphine, and also quantified a dose-response curve of buprenorphine (0." | ( Sustained-release buprenorphine induces acute opioid tolerance in the mouse. Fairbanks, CA; Kitto, KF; Larson, CM; Peterson, CD; Wilcox, GL, 2020) | 0.56 |
" We investigated the route of administration and dosage of naloxone, clinical and demographic variables relating to initial naloxone dose and use of multiple naloxone doses and one-week mortality." | ( Prehospital naloxone administration - what influences choice of dose and route of administration? Bjørnsen, LP; Braarud, AC; Dale, O; Gjersing, L; Heyerdahl, F; Skulberg, AK; Tylleskar, I, 2020) | 1.18 |
" Advice given tends to be based on dosage algorithms used by medical personnel." | ( A qualitative study of repeat naloxone administrations during opioid overdose intervention by people who use opioids in New York City. Brandt, L; Brown, C; Campbell, ANC; Castillo, F; Comer, SD; Jones, JD; Neale, J; Parkin, S; Strang, J, 2021) | 0.91 |
" In the postimplementation group, common reasons for identifying a patient as at high risk for an overdose or adverse event were a prescription for a pain medication at a daily dosage greater than or equal to 50 morphine milligram equivalents (50% of patients), concomitant opioid and benzodiazepine use (19%), history of substance use disorder (11%), and medication-assisted treatment (9%)." | ( Dispensing a Naloxone Kit at Hospital Discharge: A Retrospective QI Project. Acquisto, NM; Pasho, M; Patel, N; Thapa, K; Train, MK, 2020) | 0.93 |
" Naloxone has been showing relative safety, leading to trivial adverdse effects which are mostly due to acute withdrawal effects, but when used in patients with known long-term addiction, it usually requires additional dosing or rapid infusion to achieve detoxification effects in a timely manner or to sustain the effects after they fade away." | ( Naloxone-Induced Acute Pulmonary Edema is Dose-Dependent: A Case Series. Al-Azzawi, M; Al-Taei, M; Alsaoudi, G; Alshami, A; Costanzo, E; Douedi, S, 2021) | 2.97 |
" The portability, dosage form, and effects of naloxone are important considerations for women who use opioids." | ( "They're not doing enough.": women's experiences with opioids and naloxone in Toronto. Hamilton-Wright, S; Laliberte, N; Macleod, ER; Matheson, FI; Tajbakhsh, I; Wiese, JL, 2021) | 1.12 |
" Naloxone effectively reverses opioid overdoses on a physiological level; however, there are outstanding questions on community THN program effectiveness (adverse events, dosing requirements, dose-response between routes of administration) and implementation (accessibility, availability, and affordability)." | ( Take-home naloxone programs for suspected opioid overdose in community settings: a scoping umbrella review. Ali, F; Buxton, JA; Dhillon, D; Elton-Marshall, T; Ferguson, M; Leece, P; Moustaqim-Barrette, A; Ng, J; Rittenbach, K; Sundvick, K, 2021) | 1.93 |
" The most common subject themes were: naloxone effectiveness, safety, provision feasibility/acceptability of naloxone distribution, dosing and routes of administration, overdose response after naloxone administration, cost-effectiveness, naloxone training and education, and recommendations for policy, practice and gaps in knowledge." | ( Take-home naloxone programs for suspected opioid overdose in community settings: a scoping umbrella review. Ali, F; Buxton, JA; Dhillon, D; Elton-Marshall, T; Ferguson, M; Leece, P; Moustaqim-Barrette, A; Ng, J; Rittenbach, K; Sundvick, K, 2021) | 1.29 |
" We identified the following themes: (1) provider credentials: state licensure for OBBT providers and continuing medical education requirements; (2) new patients: objective symptoms patients must have before receiving OBBT and exceptions for special populations; (3) educating patients: general informed consent requirements, and specific information to provide; (4) counseling: minimum counselor credentials, minimum counseling frequency, counseling alternatives; (5) patient monitoring: required prescription drug monitoring checks, frequency of drug screening, and responses to lost/stolen medications; (6) enhanced clinician monitoring: evidence-based treatment protocols, minimum clinician-patient contact frequency, health assessment requirements, and individualized treatment planning; and (7) patient safety: reconciling prescriptions, dosage limitations, naloxone coprescribing, tapering, and office closures." | ( Toward a Typology of Office-based Buprenorphine Treatment Laws: Themes From a Review of State Laws. Andraka-Christou, B; Bouskill, K; Golan, M; Gordon, AJ; Randall-Kosich, O; Smart, R; Stein, BD; Totaram, R, ) | 0.28 |
" In a locale where fentanyl is responsible for the majority of non-fatal opioid overdoses, we compared the concentration of fentanyl in blood to naloxone dosing in the presence and absence of a concurrent sedative-hypnotic exposure." | ( Sentanyl: a comparison of blood fentanyl concentrations and naloxone dosing after non-fatal overdose. Babu, KM; Chapman, BP; Devin-Holcombe, K; Fogarty, MF; Krotulski, AJ; Logan, BK; Marks, SJ; Merchant, RC; Ontiveros, ST; Trieu, H, 2022) | 1.16 |
" Among the sedative-hypnotic exposed, fentanyl concentrations were lower, but naloxone dosing was similar to those without a concomitant exposure." | ( Sentanyl: a comparison of blood fentanyl concentrations and naloxone dosing after non-fatal overdose. Babu, KM; Chapman, BP; Devin-Holcombe, K; Fogarty, MF; Krotulski, AJ; Logan, BK; Marks, SJ; Merchant, RC; Ontiveros, ST; Trieu, H, 2022) | 1.19 |
"Dynamic, adaptive pharmacologic treatment for opioid use disorder (OUD) has been previously recommended over static dosing to prevent relapse, and is aligned with personalized medicine." | ( Association between dynamic dose increases of buprenorphine for treatment of opioid use disorder and risk of relapse. Díaz, I; Fishman, M; Nunes, EV; Rotrosen, J; Rudolph, KE; Shulman, M, 2022) | 0.72 |
" counterfactual) intervention in which their BUP-NX dosage would be increased following their own subject-specific opioid use during the first 12 weeks of treatment versus a hypothetical intervention in which dose would remain constant." | ( Association between dynamic dose increases of buprenorphine for treatment of opioid use disorder and risk of relapse. Díaz, I; Fishman, M; Nunes, EV; Rotrosen, J; Rudolph, KE; Shulman, M, 2022) | 0.72 |
" The secondary aim was to identify if comorbidities, sex, co-prescribed medications, or dosing site and observation were associated with BPN detection." | ( Buprenorphine not detected on urine drug screening in supervised treatment. Athavale, A; Jamshidi, N; Murnion, B, 2021) | 0.62 |
"Data extracted included UDS results, age, sex, indication for BPN, frequency of observed doses, dose of BPN, dosing site, comorbid medical conditions, and medications." | ( Buprenorphine not detected on urine drug screening in supervised treatment. Athavale, A; Jamshidi, N; Murnion, B, 2021) | 0.62 |
" No significant association between median dose, dosing site, and observed dosing and BPN detection was identified." | ( Buprenorphine not detected on urine drug screening in supervised treatment. Athavale, A; Jamshidi, N; Murnion, B, 2021) | 0.62 |
"7 individuals were co-dispensed naloxone for every 1000 receiving an opioid dosage ≥90 MME/day with a past overdose compared to 17." | ( Naloxone dispensing among the commercially insured population in the United States from 2015 to 2018. Dunphy, C; Guy, GP; Jones, CM; Zhang, K, 2021) | 2.35 |
" During the transition, she experienced some withdrawal in the setting of swallowed buprenorphine/naloxone tablets, which were intended to be dosed sublingually." | ( Transition from Oxycodone to Buprenorphine/Naloxone in a Hospitalized Patient with Sickle Cell Disease: A Case Report. DeFries, T; Leyde, S; Pratt, L; Suen, L, 2022) | 1.2 |
" Prior research has assessed the effectiveness of naloxone in the hospital setting; however, it is challenging to assess naloxone dosing regimens in the community/first-responder setting, including reversal of respiratory depression effects of fentanyl and its derivatives (fentanyls)." | ( Development of a Translational Model to Assess the Impact of Opioid Overdose and Naloxone Dosing on Respiratory Depression and Cardiac Arrest. Ahmadi, SF; Bloom, S; Chaturbedi, A; Dahan, A; Eshleman, A; Florian, J; Han, X; Janowsky, A; Li, Z; Mann, J; Olofsen, E; Samieegohar, M; Strauss, DG; Swanson, T; Wolfrum, K; Zirkle, J, 2022) | 1.2 |
" Paramedics and AEMTs have the greatest authority to select the dosage and route of administration." | ( Legal review of state emergency medical services policies and protocols for naloxone administration. Davis, CS; Haffajee, RL; Smart, R, 2022) | 0.95 |
" Complete fentanyl dose-response functions were determined during each session." | ( A novel long-acting formulation of oral buprenorphine/naloxone produces prolonged decreases in fentanyl self-administration by rhesus monkeys. Comer, SD; Foltin, RW; Nagaraj, N; Scranton, RE; Sykes, KA; Zale, S, 2022) | 0.97 |
"We analyzed data from a multicentric, pragmatic, 24-week open-label randomized controlled trial conducted in participants with POUD (N = 272) who were randomly assigned to BUP/NX model of care with flexible take-home dosing (n = 138) or the standard model of care with closely supervised methadone (n = 134)." | ( Buprenorphine/naloxone and methadone effectiveness for reducing craving in individuals with prescription opioid use disorder: Exploratory results from an open-label, pragmatic randomized controlled trial. Bastien, G; Brissette, S; Bruneau, J; Eugenia Socias, M; Foll, BL; Jutras-Aswad, D; Ledjiar, O; Lim, R; Marsan, S; McAnulty, C; Talbot, A, 2022) | 1.08 |
"Compared to the standard methadone model of care, flexible take-home dosing of BUP/NX was associated with lower craving in individuals with POUD." | ( Buprenorphine/naloxone and methadone effectiveness for reducing craving in individuals with prescription opioid use disorder: Exploratory results from an open-label, pragmatic randomized controlled trial. Bastien, G; Brissette, S; Bruneau, J; Eugenia Socias, M; Foll, BL; Jutras-Aswad, D; Ledjiar, O; Lim, R; Marsan, S; McAnulty, C; Talbot, A, 2022) | 1.08 |
" Female D2 and B6 mice failed to show significant antinociceptive effects in alcohol dose-response studies." | ( Thermal antinociceptive responses to alcohol in DBA/2J and C57BL/6J inbred male and female mouse strains. Caillaud, M; Carper, M; Damaj, MI; Miles, MF; Poklis, J; White, A, 2023) | 0.91 |
"Once a baseline incidence is known, predictors for serious ORADEs in surgical inpatients are useful in guiding medical-surgical nurses' opioid safety practices, with more frequent focused respiratory assessments before opioid dosing and closer monitoring when opioids are prescribed postoperatively, especially in higher-risk surgical inpatients." | ( Incidence of and predictors for serious opioid-related adverse drug events. Atem, FD; Denke, L; Khazzam, M, 2022) | 0.72 |
" Specific areas lacking trial or systematic review evidence include: (1) methods to optimize psychological and psychosocial comorbidities relevant to acute pain management around delivery; (2) alternative nonopioid and nonpharmacologic analgesia methods; (3) whether or not to use opioids for severe breakthrough pain and how best to prescribe and monitor its use after discharge; (4) monitoring for respiratory depression and sedation with coadministration of other analgesics; (5) optimal neuraxial analgesia dosing and adjuncts; and (6) benefits of abdominal wall blocks after cesarean delivery." | ( A Systematic Scoping Review of Peridelivery Pain Management for Pregnant People With Opioid Use Disorder: From the Society for Obstetric Anesthesia and Perinatology and Society for Maternal Fetal Medicine. Bateman, BT; Carvalho, B; Chyan, A; George, RB; Klem, ML; Krans, EE; Landau, R; Lim, G; Osmundson, SS; Soens, M; Terplan, M; Wanaselja, A, 2022) | 0.72 |
"We performed an interrupted time series analysis looking at naloxone prescriptions and daily opioid dosing in morphine milligram equivalents (MMEs), before and after initiation of the EHR advisory." | ( Electronic Advisories Increase Naloxone Prescribing Across Health Care Settings. Carpenter, J; Heiman, E; Lanh, S; Moran, TP; Steck, A, 2023) | 1.44 |
"Patients were classified as opioid-tolerant based on opioid dosing history ≥60 morphine milligram equivalents/day for ≥7 consecutive days prior to naloxone administration." | ( Comparing the safety and efficacy of intravenous naloxone administration in opioid-naive and opioid-tolerant hospitalized oncology patients. Buga, S; Lee, S; Pon, D; Tatla, V, ) | 0.59 |
" Use of opioid dosing history to identify potentially opioid-dependent patients should be considered prior to naloxone administration to guide dosing and reduce the risk for precipitating OWSs." | ( Comparing the safety and efficacy of intravenous naloxone administration in opioid-naive and opioid-tolerant hospitalized oncology patients. Buga, S; Lee, S; Pon, D; Tatla, V, ) | 0.6 |
"The majority of pharmacies stocked the most commonly prescribed 8/2 mg dosage strength of buprenorphine/naloxone films and tablets (69." | ( Demographic and socioeconomic correlates to buprenorphine access in pharmacies. Conrad, TA; Crawford, ND; Kan, M; Kee, C; Mataczynski, MJ; Peralta, AM; Sitar, SI; Welsh, JW; Yarbrough, CR; Young, HN, ) | 0.35 |
" 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) | 1.12 |
" While low dosing is thought to be a factor limiting naloxone's efficacy, the timing between fentanyl exposure and initiation of naloxone treatment may be another important factor." | ( The pattern of brain oxygen response induced by intravenous fentanyl limits the time window of therapeutic efficacy of naloxone. Curay, CM; Irwin, MR; Kiyatkin, EA, 2023) | 1.37 |
" Variation exists in the recommended agent and dosing strategies." | ( Evaluation of Nonintubated Analgesia Practices in Critical Care Transport. Bondurant, M; Esteves, AM; Gilchrist, HE; Markwood, JM; Roginski, MA, ) | 0.13 |
" Mianserin and mirtazapine (separately) induced dose-dependent antinociception, each one yielding a biphasic dose-response curve, and they were antagonized by naloxone." | ( Treatment-Resistant Depression (TRD): Is the Opioid System Involved? Keidan, L; Pick, CG; Schreiber, S, 2023) | 1.11 |
"Experts recommend using the lowest effective dose of naloxone to balance the reversal of opioid-induced respiratory depression and avoid precipitated opioid withdrawal, however, there is no established dosing standards within the emergency department (ED)." | ( Systematic Review of Naloxone Dosing and Adverse Events in the Emergency Department. McManus, K; Nelson, LS; Parris, MA; Ramdin, C; Yugar, B, 2023) | 1.48 |
"The aim of this review was to determine current naloxone dosing practice in the ED and their association with adverse events." | ( Systematic Review of Naloxone Dosing and Adverse Events in the Emergency Department. McManus, K; Nelson, LS; Parris, MA; Ramdin, C; Yugar, B, 2023) | 1.48 |
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. |
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 alkaloid | An isoquinoline alkaloid based on a morphinan skeleton and its substituted derivatives. |
tertiary alcohol | A tertiary alcohol is a compound in which a hydroxy group, -OH, is attached to a saturated carbon atom which has three other carbon atoms attached to it. |
[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 |
---|---|---|
Naloxone Action Pathway | 31 | 11 |
Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
RAR-related orphan receptor gamma | Mus musculus (house mouse) | Potency | 21.1317 | 0.0060 | 38.0041 | 19,952.5996 | AID1159521 |
pregnane X nuclear receptor | Homo sapiens (human) | Potency | 12.5893 | 0.0054 | 28.0263 | 1,258.9301 | AID1346985 |
estrogen nuclear receptor alpha | Homo sapiens (human) | Potency | 33.4915 | 0.0002 | 29.3054 | 16,493.5996 | AID743080 |
cytochrome P450 2D6 | Homo sapiens (human) | Potency | 21.8761 | 0.0010 | 8.3798 | 61.1304 | AID1645840 |
[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) |
---|---|---|---|---|---|---|---|
ATP-binding cassette sub-family C member 3 | Homo sapiens (human) | IC50 (µMol) | 133.0000 | 0.6315 | 4.4531 | 9.3000 | AID1473740 |
Multidrug resistance-associated protein 4 | Homo sapiens (human) | IC50 (µMol) | 133.0000 | 0.2000 | 5.6774 | 10.0000 | AID1473741 |
Bile salt export pump | Homo sapiens (human) | IC50 (µMol) | 272.3333 | 0.1100 | 7.1903 | 10.0000 | AID1443980; AID1449628; AID1473738 |
Muscarinic acetylcholine receptor M1 | Rattus norvegicus (Norway rat) | Ki | 0.0011 | 0.0001 | 0.5797 | 10.0000 | AID141512 |
Muscarinic acetylcholine receptor M3 | Rattus norvegicus (Norway rat) | Ki | 0.0011 | 0.0001 | 1.4833 | 9.1400 | AID141512 |
Muscarinic acetylcholine receptor M4 | Rattus norvegicus (Norway rat) | Ki | 0.0011 | 0.0001 | 0.6868 | 8.2600 | AID141512 |
Muscarinic acetylcholine receptor M5 | Rattus norvegicus (Norway rat) | Ki | 0.0011 | 0.0001 | 0.6661 | 8.2600 | AID141512 |
Cytochrome P450 2D6 | Homo sapiens (human) | IC50 (µMol) | 2.0000 | 0.0000 | 2.0151 | 10.0000 | AID625249 |
Muscarinic acetylcholine receptor M2 | Rattus norvegicus (Norway rat) | Ki | 0.0011 | 0.0001 | 0.5890 | 8.2600 | AID141512 |
Cytochrome P450 2C9 | Homo sapiens (human) | IC50 (µMol) | 50.0000 | 0.0000 | 2.8005 | 10.0000 | AID1210069 |
D(3) dopamine receptor | Rattus norvegicus (Norway rat) | Ki | 20.0000 | 0.0001 | 0.2567 | 5.8000 | AID65625 |
Adenosine receptor A1 | Homo sapiens (human) | Ki | 50.0000 | 0.0002 | 0.9316 | 10.0000 | AID437483 |
Delta-type opioid receptor | Mus musculus (house mouse) | IC50 (µMol) | 125.0323 | 0.0001 | 0.7298 | 10.0000 | AID148624; AID150253 |
Delta-type opioid receptor | Mus musculus (house mouse) | Ki | 0.0370 | 0.0000 | 0.5393 | 9.4000 | AID149069 |
Delta-type opioid receptor | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.0219 | 0.0003 | 0.3887 | 7.0000 | AID149041; AID149626; AID150392; AID226060 |
Delta-type opioid receptor | Rattus norvegicus (Norway rat) | Ki | 0.0527 | 0.0000 | 0.6068 | 9.2330 | AID1587571; AID1901075 |
Kappa-type opioid receptor | Mus musculus (house mouse) | IC50 (µMol) | 500.0000 | 0.0013 | 1.5380 | 10.0000 | AID150253 |
Mu-type opioid receptor | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.0019 | 0.0001 | 0.8874 | 10.0000 | AID149041; AID150392; AID226060 |
Mu-type opioid receptor | Rattus norvegicus (Norway rat) | Ki | 0.0018 | 0.0000 | 0.3845 | 8.6000 | AID1186504; AID141762; AID151759; AID151900 |
Kappa-type opioid receptor | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.0019 | 0.0005 | 0.3698 | 7.0000 | AID149041; AID150392; AID226060 |
Mu-type opioid receptor | Homo sapiens (human) | IC50 (µMol) | 0.0397 | 0.0001 | 0.8133 | 10.0000 | AID1055367; AID1146100; AID1458130; AID148624; AID150821; AID152239; AID1823682; AID1854007; AID255309; AID274396; AID274417; AID286314; AID325959; AID625163 |
Mu-type opioid receptor | Homo sapiens (human) | Ki | 0.0242 | 0.0000 | 0.4197 | 10.0000 | AID1167044; AID1185657; AID1268024; AID1268040; AID150975; AID150990; AID1604691; AID1633367; AID1655378; AID1669023; AID1777977; AID274390; AID274411; AID286302; AID325957; AID338153; AID410718; AID437485; AID443797; AID596551; AID600431; AID603169; AID603170; AID603171; AID625163 |
Delta-type opioid receptor | Homo sapiens (human) | IC50 (µMol) | 0.1896 | 0.0002 | 0.7521 | 8.0140 | AID1146100; AID148078; AID148624; AID149626; AID1604701; AID1633374; AID1669028; AID226060; AID255309; AID286239; AID286936; AID311996; AID378465; AID625161 |
Delta-type opioid receptor | Homo sapiens (human) | Ki | 0.1315 | 0.0000 | 0.5978 | 9.9300 | AID1167045; AID1185659; AID1230327; AID148250; AID148251; AID149069; AID150030; AID1604692; AID1633368; AID1655377; AID1669024; AID1777978; AID274392; AID274413; AID286304; AID325962; AID338154; AID410719; AID443798; AID596638; AID600432; AID625161 |
Kappa-type opioid receptor | Cavia porcellus (domestic guinea pig) | IC50 (µMol) | 0.0500 | 0.0003 | 0.7123 | 7.0700 | AID147958 |
Kappa-type opioid receptor | Cavia porcellus (domestic guinea pig) | Ki | 0.0435 | 0.0000 | 0.2018 | 6.4240 | AID149425; AID149546; AID1901076; AID223587; AID223596 |
Kappa-type opioid receptor | Homo sapiens (human) | IC50 (µMol) | 0.0795 | 0.0000 | 1.2011 | 10.0000 | AID1146100; AID147854; AID147859; AID148624; AID1714339; AID255309; AID286310; AID625162 |
Kappa-type opioid receptor | Homo sapiens (human) | Ki | 0.0321 | 0.0000 | 0.3624 | 10.0000 | AID1167046; AID148006; AID148018; AID148019; AID148251; AID1777979; AID274391; AID274412; AID286303; AID325960; AID410720; AID443796; AID481097; AID596552; AID600433; AID625162 |
Mu-type opioid receptor | Mus musculus (house mouse) | IC50 (µMol) | 250.0077 | 0.0008 | 1.6992 | 10.0000 | AID150253; AID1528330 |
Cytochrome P450 2J2 | Homo sapiens (human) | IC50 (µMol) | 50.0000 | 0.0120 | 2.5312 | 9.4700 | AID1210069 |
Mu-type opioid receptor | Cavia porcellus (domestic guinea pig) | IC50 (µMol) | 0.0089 | 0.0002 | 0.6603 | 10.0000 | AID148992 |
Mu-type opioid receptor | Cavia porcellus (domestic guinea pig) | Ki | 0.0017 | 0.0000 | 0.2786 | 9.0000 | AID141512; AID1901077 |
Sigma non-opioid intracellular receptor 1 | Cavia porcellus (domestic guinea pig) | Ki | 0.1030 | 0.0000 | 0.3385 | 10.0000 | AID1185659 |
Beta-2 adrenergic receptor | Cavia porcellus (domestic guinea pig) | IC50 (µMol) | 0.0055 | 0.0004 | 0.1680 | 0.9772 | AID1146100 |
Canalicular multispecific organic anion transporter 1 | Homo sapiens (human) | IC50 (µMol) | 133.0000 | 2.4100 | 6.3433 | 10.0000 | AID1473739 |
Sigma non-opioid intracellular receptor 1 | Homo sapiens (human) | Ki | 100.0000 | 0.0000 | 0.4901 | 10.0000 | AID204005 |
Sigma non-opioid intracellular receptor 1 | Rattus norvegicus (Norway rat) | Ki | 0.0030 | 0.0003 | 0.2671 | 5.0700 | AID443796 |
[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) | 0.0015 | 0.0005 | 0.0015 | 0.0030 | AID1133438 |
Delta-type opioid receptor | Mus musculus (house mouse) | Kd | 0.0002 | 0.0002 | 0.0887 | 0.5000 | AID277679 |
Delta-type opioid receptor | Rattus norvegicus (Norway rat) | EC50 (µMol) | 0.0015 | 0.0005 | 0.3649 | 6.9000 | AID1133438 |
Delta-type opioid receptor | Rattus norvegicus (Norway rat) | Kd | 0.1200 | 0.0021 | 2.5985 | 10.0000 | AID149052; AID149533 |
Mu-type opioid receptor | Rattus norvegicus (Norway rat) | EC50 (µMol) | 0.0015 | 0.0000 | 0.0647 | 0.9320 | AID1133438 |
Mu-type opioid receptor | Rattus norvegicus (Norway rat) | Kd | 0.0784 | 0.0002 | 1.2965 | 10.0000 | AID149052; AID151464; AID151585; AID152211 |
Kappa-type opioid receptor | Rattus norvegicus (Norway rat) | EC50 (µMol) | 0.0015 | 0.0004 | 0.0039 | 0.0180 | AID1133438 |
Kappa-type opioid receptor | Rattus norvegicus (Norway rat) | Kd | 0.0935 | 0.0000 | 1.8069 | 10.0000 | AID148456; AID148459; AID149052 |
Mu-type opioid receptor | Homo sapiens (human) | Kd | 0.0005 | 0.0001 | 0.1825 | 0.8300 | AID148456; AID277679; AID314189 |
Delta-type opioid receptor | Homo sapiens (human) | Kd | 0.0010 | 0.0004 | 0.5147 | 1.9800 | AID148456 |
Kappa-type opioid receptor | Cavia porcellus (domestic guinea pig) | Kd | 0.0180 | 0.0021 | 1.4444 | 4.8940 | AID149533 |
Kappa-type opioid receptor | Homo sapiens (human) | EC50 (µMol) | 0.0083 | 0.0000 | 0.2244 | 8.9900 | AID149989; AID286308 |
Kappa-type opioid receptor | Homo sapiens (human) | Kd | 0.0010 | 0.0000 | 0.0670 | 0.8300 | AID148456 |
Mu-type opioid receptor | Cavia porcellus (domestic guinea pig) | Kd | 0.0002 | 0.0000 | 0.7209 | 2.1420 | AID277679 |
[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) |
---|---|---|---|---|---|---|---|
Delta-type opioid receptor | Mus musculus (house mouse) | Ke | 0.0248 | 0.0001 | 0.1472 | 6.1080 | AID148813; AID148928 |
Kappa-type opioid receptor | Mus musculus (house mouse) | Ke | 0.0159 | 0.0000 | 0.3225 | 1.5510 | AID148313 |
Mu-type opioid receptor | Homo sapiens (human) | Ke | 0.0023 | 0.0000 | 0.2488 | 3.0700 | AID1197355; AID296738; AID413920; AID443809; AID577293; AID607797; AID612052; AID647797; AID749673 |
Delta-type opioid receptor | Homo sapiens (human) | Ke | 0.0350 | 0.0001 | 0.6979 | 9.0700 | AID443812 |
Kappa-type opioid receptor | Homo sapiens (human) | Ke | 0.0105 | 0.0000 | 0.3540 | 5.8100 | AID443806; AID612053 |
Mu-type opioid receptor | Mus musculus (house mouse) | Ke | 0.0014 | 0.0002 | 0.0233 | 0.0554 | AID151146 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
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. |
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. |
AID1346411 | Rat kappa receptor (Opioid receptors) | 1993 | Proceedings of the National Academy of Sciences of the United States of America, Nov-01, Volume: 90, Issue:21 | Cloning and pharmacological characterization of a rat kappa opioid receptor. |
AID1346329 | Human kappa receptor (Opioid receptors) | 1997 | The Journal of pharmacology and experimental therapeutics, Aug, Volume: 282, Issue:2 | Activation of the cloned human kappa opioid receptor by agonists enhances [35S]GTPgammaS binding to membranes: determination of potencies and efficacies of ligands. |
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. |
AID1346411 | Rat kappa receptor (Opioid receptors) | 1993 | The Biochemical journal, Nov-01, Volume: 295 ( Pt 3) | Molecular cloning and expression of a rat kappa opioid receptor. |
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. |
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. |
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. |
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. |
AID1346411 | Rat kappa receptor (Opioid receptors) | 1993 | The Biochemical journal, Nov-01, Volume: 295 ( Pt 3) | Molecular cloning of a rat kappa opioid receptor reveals sequence similarities to the mu and delta opioid receptors. |
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. |
AID1346373 | Mouse delta 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 | Life sciences, , Volume: 56, Issue:9 | Cloning of a human kappa opioid receptor from the brain. |
AID1346330 | Mouse mu receptor (Opioid receptors) | 1994 | Molecular pharmacology, Feb, Volume: 45, Issue:2 | Pharmacological characterization of the cloned kappa-, delta-, and mu-opioid receptors. |
AID357096 | Down-regulation of CCR5 mRNA expression in C57BL/6J mouse | 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. |
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. |
AID1714339 | Antagonist activity at human KOR expressed in CHO cell membranes assessed as reduction in U50,488 induced response incubated for 1 hr by liquid scintillation counting based [35S]GTP-gamma-S assay | 2016 | Journal of medicinal chemistry, 11-23, Volume: 59, Issue:22 | Structure-Activity Relationships of [des-Arg |
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. |
AID443802 | Displacement of [3H](+)-pentazocine from sigma1 receptor in rat brain homogenate | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3 | Synthesis and opioid activity of enantiomeric N-substituted 2,3,4,4a,5,6,7,7a-octahydro-1H-benzofuro[3,2-e]isoquinolines. |
AID1211235 | Drug metabolism in human kidney microsomes assessed as UGT1A8/2B7-mediated unbound intrinsic glucuronidation clearance at 1 uM after 30 to 60 mins by LC-MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4 | Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin. |
AID277679 | Antagonist activity against mu opioid receptor assessed as effect on endomorphin-2-induced calcium response in CHO cells by aequorin luminescence based calcium assay | 2007 | Journal of medicinal chemistry, Feb-08, Volume: 50, Issue:3 | Synthesis and characterization of potent and selective mu-opioid receptor antagonists, [Dmt(1), D-2-Nal(4)]endomorphin-1 (Antanal-1) and [Dmt(1), D-2-Nal(4)]endomorphin-2 (Antanal-2). |
AID148456 | Compound was evaluated for Opioid receptor kappa 1 affinity against the receptor site model site 4(kappa) | 1986 | Journal of medicinal chemistry, Apr, Volume: 29, Issue:4 | N-substituent modulation of opiate agonist/antagonist activity in resolved 3-methyl-3-(m-hydroxyphenyl)piperidines. |
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. |
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. |
AID1255660 | Agonist activity at kappa opioid receptor in human HEK293 cells after 30 mins by [35S]GTPgammaS binding assay | 2015 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22 | Conformationally restricted κ-opioid receptor agonists: Synthesis and pharmacological evaluation of diastereoisomeric and enantiomeric decahydroquinoxalines. |
AID147891 | Ratio of antagonistic activity against mu receptors in guinea pig ileum in presence and absence of mu agonist DAGO | 1995 | Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20 | Novel deltorphin heptapeptide analogs with potent delta agonist, delta antagonist, or mixed mu antagonist/delta agonist properties. |
AID1669023 | Displacement of [3H]-diprenorphine from human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by competition radioligand binding assay | |||
AID196927 | The compound was evaluated for the morphine-like behavioral effects. '--' indicates decrease in the locomotor activity. | 1985 | Journal of medicinal chemistry, Dec, Volume: 28, Issue:12 | Factors affecting binding of trans-N-[2-(methylamino)cyclohexyl]benzamides at the primary morphine receptor. |
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. |
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. |
AID327869 | Inhibition of morphine-stimulated human mu opioid receptor expressed in HEK293a cells co-expressing YFP-labelled alphai1 and CFP-labelled beta1gamma2 Gi subunits assessed as decrease in fluorescence resonance energy transfer signal at 10 uM | 2007 | The Journal of biological chemistry, Sep-14, Volume: 282, Issue:37 | Live cell monitoring of mu-opioid receptor-mediated G-protein activation reveals strong biological activity of close morphine biosynthetic precursors. |
AID1358121 | Displacement of [3H]diprenorphine from human MOR expressed in African green monkey COS1 cell membranes at 1 uM incubated for 1 hr by scintillation counting method | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Synthesis of 7β-hydroxy-8-ketone opioid derivatives with antagonist activity at mu- and delta-opioid receptors. |
AID147892 | Ratio of antagonistic activity against mu receptors in guinea pig ileum in presence and absence of mu agonist dermorphin | 1995 | Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20 | Novel deltorphin heptapeptide analogs with potent delta agonist, delta antagonist, or mixed mu antagonist/delta agonist properties. |
AID450517 | Induction of ERK phosphorylation in rat primary astrocyte at 10 uM after 10 mins | 2009 | Bioorganic & medicinal chemistry, Aug-15, Volume: 17, Issue:16 | Synthesis and characterizations of novel quinoline derivatives having mixed ligand activities at the kappa and mu receptors: Potential therapeutic efficacy against morphine dependence. |
AID1146572 | Antiwrithing activity in sc dosed mouse assessed as prevention of phenyl-p-benzoquinone-induced abdominal constriction response | 1978 | Journal of medicinal chemistry, Dec, Volume: 21, Issue:12 | (2-exo-3-endo)-2-Aryltropane-3-carboxylic esters, a new class of narcotic antagonists. |
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). |
AID151145 | Antagonistic activity (Ke) against nor-morphine and Opioid receptor mu 1 of mouse vas deferens assay | 1990 | Journal of medicinal chemistry, Apr, Volume: 33, Issue:4 | Synthesis and biological evaluation of 14-alkoxymorphinans. 3. Extensive study on cyprodime-related compounds. |
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. |
AID148314 | Binding potency of ethylketocyclazocine to Opioid receptor kappa 1 in mouse vas deferens | 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. |
AID1473738 | Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to 20 mins by membrane vesicle transport assay | 2013 | Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1 | A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. |
AID108550 | Tested for reduction in the analgesic response to morphine after subcutaneous administration of 1.25 mg/kg in abdominal stretching assay | 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. |
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). |
AID357090 | Binding affinity to CCR5 in C57BL/6J mouse brain membrane | 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. |
AID1211279 | Renal clearance in human | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4 | Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin. |
AID1211245 | Unbound intrinsic glucuronidation clearance in human liver microsomes at 1 uM after 30 to 60 mins by LC-MS/MS analysis in presence of UDP-glucuronosyltransferase | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4 | Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin. |
AID487869 | Displacement of [3H]U69593 from kappa opioid receptor in guinea pig cerebellum by beta plate scintillation counting | 2010 | Journal of natural products, Jun-25, Volume: 73, Issue:6 | A bastadin with potent and selective delta-opioid receptor binding affinity from the Australian sponge Ianthella flabelliformis. |
AID21849 | In vitro clearance in dog in 1000000 cells | 1999 | Journal of medicinal chemistry, Dec-16, Volume: 42, Issue:25 | Combining in vitro and in vivo pharmacokinetic data for prediction of hepatic drug clearance in humans by artificial neural networks and multivariate statistical techniques. |
AID1901077 | Displacement of [3H]-DAMGO from MOR in guinea pig brain membranes measured by competitive radioligand receptor binding assay | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Synthesis of 8-aminomorphans with high KOR affinity. |
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AID624607 | Specific activity of expressed human recombinant UGT1A3 | 2000 | Annual review of pharmacology and toxicology, , Volume: 40 | Human UDP-glucuronosyltransferases: metabolism, expression, and disease. |
AID26304 | Partition coefficient (logD6.5) | 2000 | Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13 | QSAR model for drug human oral bioavailability. |
AID180011 | The effective dose was measured by using rat tail flick assay after the compound administered intraperitoneally. | 1980 | Journal of medicinal chemistry, Feb, Volume: 23, Issue:2 | Analgesic narcotic antagonists. 2. 8-Alkymorphinan-6-ones. |
AID622104 | Antinociceptive activity in sc dosed mouse assessed as inhibition of acetic acid-induced writhing administered 15 mins before acetic acid challenge measured after 10 mins relative to control | 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). |
AID1167046 | Displacement of [3H]U-69593 from human KOR expressed in HEK293 cells after 60 mins by scintillation counting analysis | 2014 | Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21 | Nonpeptide small molecule agonist and antagonist original leads for neuropeptide FF1 and FF2 receptors. |
AID132847 | Opioid agonistic activity was measured in mouse vas deferens; infinite | 1981 | Journal of medicinal chemistry, Feb, Volume: 24, Issue:2 | Some 14 beta-substituted analogues of N-(cyclopropylmethyl)normorphine. |
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. |
AID128020 | Inhibition of acetic acid induced mouse writhing assay following s.c. administration; Inactive. | 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. |
AID1221961 | Apparent permeability from basolateral to apical side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of P-gp inhibitor LY335979 | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2 | Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model. |
AID148903 | Tested for irreversible inhibition of [3H]- Naltrexone binding with in the presence of NaCl (washed) | 1984 | Journal of medicinal chemistry, Dec, Volume: 27, Issue:12 | Diastereomeric 6-desoxy-6-spiro-alpha-methylene-gamma-butyrolactone derivatives of naltrexone and oxymorphone. Selective irreversible inhibition of naltrexone binding in an opioid receptor preparation by a conformationally restricted michael acceptor liga |
AID114391 | Tested for analgesic activity using writhing test in mice at 20 mg/kg upon subcutaneous administration; Inactive | 1980 | Journal of medicinal chemistry, Jun, Volume: 23, Issue:6 | 14-(Arylhydroxyamino)codeinones and derivatives as analgetics and antagonists. |
AID29811 | Oral bioavailability in human | 2000 | Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13 | QSAR model for drug human oral bioavailability. |
AID1211282 | Fraction metabolized glucuronidation in human liver microsomes in presence of UDP-glucuronosyltransferase | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4 | Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin. |
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. |
AID496820 | Antimicrobial activity against Trypanosoma brucei | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
AID1230327 | Displacement of [3H]DPDPE from delta opioid receptor (unknown origin) transfected into HEK293 cells by microplate scintillation counting | 2015 | Journal of natural products, Jun-26, Volume: 78, Issue:6 | Flavonoids from Perovskia atriplicifolia and Their in Vitro Displacement of the Respective Radioligands for Human Opioid and Cannabinoid Receptors. |
AID745765 | Displacement of [3H]-enkephalin from human delta opioid receptor transfected in CHOK1 cells at 10 uM after 60 mins relative to control | 2013 | Journal of natural products, 05-24, Volume: 76, Issue:5 | Neocosmospora sp.-derived resorcylic acid lactones with in vitro binding affinity for human opioid and cannabinoid receptors. |
AID450624 | Agonist activity at FLAG-tagged delta opioid receptor expressed in HEK293 cells assessed as receptor down regulation at 10 uM by Bradford assay relative to control | 2009 | Bioorganic & medicinal chemistry, Sep-01, Volume: 17, Issue:17 | Novel delta opioid receptor agonists exhibit differential stimulation of signaling pathways. |
AID235331 | Selectivity ratio of mu opioid receptor to delta opioid receptor | 1988 | Journal of medicinal chemistry, Feb, Volume: 31, Issue:2 | Application of the message-address concept in the design of highly potent and selective non-peptide delta opioid receptor antagonists. |
AID624657 | Inhibition of morphine glucuronidation by human UGT enzymes from liver microsomes | 2005 | Pharmacology & therapeutics, Apr, Volume: 106, Issue:1 | UDP-glucuronosyltransferases and clinical drug-drug interactions. |
AID295932 | Displacement of [3H]DAMGO from mu opioid receptor in guinea pig brain membrane | 2007 | European journal of medicinal chemistry, Oct, Volume: 42, Issue:10 | Synthesis of bridged piperazines with sigma receptor affinity. |
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. |
AID1221965 | Transporter substrate index of efflux ratio in human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of P-gp inhibitor LY335979 | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2 | Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model. |
AID151147 | Binding potency of normorphine to Opioid receptor mu 1 in the mouse vas deferens | 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. |
AID8002 | Observed volume of distribution | 2004 | Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5 | Prediction of human volume of distribution values for neutral and basic drugs. 2. Extended data set and leave-class-out statistics. |
AID314199 | Antinociceptive activity in mouse assessed as jumping latency at 5 ug, icv in presence of endomorphin-2 by hot plate test | 2008 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 18, Issue:4 | Novel highly potent mu-opioid receptor antagonist based on endomorphin-2 structure. |
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. |
AID1211219 | Ratio of unbound intrinsic glucuronidation clearance in human liver microsomes in presence of 2% bovine serum albumin to unbound intrinsic glucuronidation clearance in human liver microsomes in absence of bovine serum albumin | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4 | Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin. |
AID148628 | Percent recovery of specific binding of 0.5 nM [3H]bremazocine binding from opioid receptor at 1000 nM dose of the compound | 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. |
AID1528336 | Inhibition of opioid-withdrawal symptom in morphine-pelleted Swiss Webster mouse assessed as reduction in escape jumps at 1 mg/kg, sc observed after 20 mins | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24 | Application of Bivalent Bioisostere Concept on Design and Discovery of Potent Opioid Receptor Modulators. |
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AID647797 | Antagonist activity at human mu receptor expressed in CHO cells membrane assessed as inhibition of DAMGO-induced [35S]GTPgammaS binding after 3 hrs by liquid scintillation counting | 2012 | European journal of medicinal chemistry, Apr, Volume: 50 | Probes for narcotic receptor mediated phenomena. 44. Synthesis of an N-substituted 4-hydroxy-5-(3-hydroxyphenyl)morphan with high affinity and selective μ-antagonist activity. |
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. |
AID1221964 | Transporter substrate index ratio of permeability from basolateral to apical side in human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of P-gp inhibitor LY335979 | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2 | Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model. |
AID149989 | Effective concentration for half-maximal stimulation was determined by [35S]GTP-gamma-S, assay | 2003 | Journal of medicinal chemistry, May-22, Volume: 46, Issue:11 | Structure-activity relationships of dynorphin a analogues modified in the address sequence. |
AID76241 | Opioid agonistic activity was measured in guinea pig ileum; infinite | 1981 | Journal of medicinal chemistry, Feb, Volume: 24, Issue:2 | Some 14 beta-substituted analogues of N-(cyclopropylmethyl)normorphine. |
AID148078 | Binding affinity against delta-opiate receptor (human) using [3H]-DPDPE radioligand | 2001 | Journal of medicinal chemistry, Oct-11, Volume: 44, Issue:21 | From hit to lead. Combining two complementary methods for focused library design. Application to mu opiate ligands. |
AID1820168 | Displacement of [125I]-43RFa from human QRFP receptor expressed in CHO cells by TopCount scintillation counting method | 2021 | Journal of medicinal chemistry, 06-10, Volume: 64, Issue:11 | Identification of an |
AID745767 | Displacement of [3H]-U-69593 from human kappa opioid receptor transfected in CHOK1 cells at 10 uM after 60 mins relative to control | 2013 | Journal of natural products, 05-24, Volume: 76, Issue:5 | Neocosmospora sp.-derived resorcylic acid lactones with in vitro binding affinity for human opioid and cannabinoid receptors. |
AID170062 | Opioid antagonist activity (5 mg/kg, peripherally) was determined by measuring the analgesia produced by morphine given 10 mins (after the compound) at a dose of 5 mg/kg; no effect | 2004 | Bioorganic & medicinal chemistry letters, Feb-23, Volume: 14, Issue:4 | A highly toxic morphine-3-glucuronide derivative. |
AID1437781 | Analgesic activity in Swiss albino mouse assessed as inhibition of formalin-induced paw flinching at 80 ug/kg administered for 30 mins followed by formalin challenge measured during 10 to 30 mins post formalin challenge | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Rationally designed benzopyran fused isoxazolidines and derived β |
AID1211278 | Clearance in iv dosed human | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4 | Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin. |
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. |
AID1604701 | Antagonist activity at human DOR expressed in CHO cell membranes assessed as reduction in SNC80-induced response incubated for 1 hr by [35S]-GTPgammaS coupling assay | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5 | Potent, Efficacious, and Stable Cyclic Opioid Peptides with Long Lasting Antinociceptive Effect after Peripheral Administration. |
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. |
AID1211241 | Fraction unbound in human intestinal microsomes at 1 uM after 30 to 60 mins by LC-MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4 | Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin. |
AID27559 | Partition coefficient (logP) | 1985 | Journal of medicinal chemistry, Dec, Volume: 28, Issue:12 | Factors affecting binding of trans-N-[2-(methylamino)cyclohexyl]benzamides at the primary morphine receptor. |
AID1255653 | Displacement of [3H]-DPDPE from delta opioid receptor in rat brain membrane after 120 mins by scintillation counting | 2015 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22 | Conformationally restricted κ-opioid receptor agonists: Synthesis and pharmacological evaluation of diastereoisomeric and enantiomeric decahydroquinoxalines. |
AID148427 | Antagonistic activity (Ke) at Opioid receptor kappa 1 was determined against ethylketocyclazocine in the mouse vas deferens (MVD) | 1990 | Journal of medicinal chemistry, Apr, Volume: 33, Issue:4 | Synthesis and biological evaluation of 14-alkoxymorphinans. 3. Extensive study on cyprodime-related compounds. |
AID148151 | Agonist activity towards human Opioid receptor kappa 1 mediated [35S]GTP-gamma-S, binding calculated as maximum inhibition | 2003 | Journal of medicinal chemistry, May-22, Volume: 46, Issue:11 | Structure-activity relationships of dynorphin a analogues modified in the address sequence. |
AID1167045 | Displacement of [3H]DPDPE from human DOR expressed in HEK293 cells after 60 mins by scintillation counting analysis | 2014 | Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21 | Nonpeptide small molecule agonist and antagonist original leads for neuropeptide FF1 and FF2 receptors. |
AID148928 | Binding affinity was evaluated by measuring the ability to displace DPDPE radioligand binding from delta opioid receptor in mouse vas deferens preparation | 1995 | Journal of medicinal chemistry, Aug-04, Volume: 38, Issue:16 | Synthesis and biological evaluation of 14-alkoxymorphinans. 11. 3-Hydroxycyprodime and analogues: opioid antagonist profile in comparison to cyprodime. |
AID1230325 | Displacement of [3H]U69593 from kappa opioid receptor (unknown origin) transfected into HEK293 cells at 10 uM by microplate scintillation counting | 2015 | Journal of natural products, Jun-26, Volume: 78, Issue:6 | Flavonoids from Perovskia atriplicifolia and Their in Vitro Displacement of the Respective Radioligands for Human Opioid and Cannabinoid Receptors. |
AID229192 | Inhibition of specific binding of [3H]NANM of sigma binding site in Guinea pig brain membranes | 1992 | Journal of medicinal chemistry, Dec-11, Volume: 35, Issue:25 | Radiosynthesis, cerebral distribution, and binding of [125I]-1-(p-iodophenyl)-3-(1-adamantyl)guanidine, a ligand for sigma binding sites. |
AID296738 | Antagonist activity at human mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S assay | 2007 | Journal of medicinal chemistry, Aug-09, Volume: 50, Issue:16 | Probes for narcotic receptor mediated phenomena. 34. Synthesis and structure-activity relationships of a potent mu-agonist delta-antagonist and an exceedingly potent antinociceptive in the enantiomeric C9-substituted 5-(3-hydroxyphenyl)-N-phenylethylmorph |
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. |
AID600437 | Antagonist activity at human recombinant delta-type opioid receptor coupled Galphaqi5 chimeric protein expressed in CHO cell membranes assessed as inhibition of DPDPE-stimulated calcium mobilization | 2009 | Bioorganic & medicinal chemistry, Jul-15, Volume: 17, Issue:14 | Structure-activity studies on the nociceptin/orphanin FQ receptor antagonist 1-benzyl-N-{3-[spiroisobenzofuran-1(3H),4'-piperidin-1-yl]propyl} pyrrolidine-2-carboxamide. |
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. |
AID128498 | Analgesic activity in mice by the tail-flick method | 1981 | Journal of medicinal chemistry, Feb, Volume: 24, Issue:2 | Structure-activity studies on narcotic antagonists. 2. N-substituted ethyl 3-(m- or p-hydroxyphenyl) nipecotates. |
AID224567 | Tested for the opioid antagonist effect at mu-opioid receptor in isolated guinea pig ileum at 20 nM | 1993 | Journal of medicinal chemistry, Oct-01, Volume: 36, Issue:20 | 3,4-Dimethyl-4-(3-hydroxyphenyl)piperidines: opioid antagonists with potent anorectant activity. |
AID443796 | Displacement of [125I]OXY from human kappa opioid receptor expressed in CHO cells | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3 | Synthesis and opioid activity of enantiomeric N-substituted 2,3,4,4a,5,6,7,7a-octahydro-1H-benzofuro[3,2-e]isoquinolines. |
AID1633368 | Displacement of [3H]-diprenorphine from human delta opioid receptor expressed in CHO cell membranes incubated for 1 hr by micro beta2 scintillation counting method | 2019 | ACS medicinal chemistry letters, Apr-11, Volume: 10, Issue:4 | Novel Cyclic Biphalin Analogues by Ruthenium-Catalyzed Ring Closing Metathesis: |
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. |
AID624621 | Specific activity of expressed human recombinant UGT2B7Y | 2000 | Annual review of pharmacology and toxicology, , Volume: 40 | Human UDP-glucuronosyltransferases: metabolism, expression, and disease. |
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. |
AID226060 | Inhibition of [3H]-Naloxone binding to rat brain membrane without NaCl | 1983 | Journal of medicinal chemistry, Jan, Volume: 26, Issue:1 | Synthesis and pharmacological studies of 4,4-disubstituted piperidines: a new class of compounds with potent analgesic properties. |
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. |
AID1562920 | Displacement of [3H]JWH-018 from CB1R/CB2R in Wistar rat brain membranes at 10 uM after 60 mins by liquid scintillation analysis | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Preparation of bivalent agonists for targeting the mu opioid and cannabinoid receptors. |
AID131245 | Narcotic antagonism was measured by using Anti-Straub tail (AST) test after subcutaneous administration | 1994 | Journal of medicinal chemistry, Sep-16, Volume: 37, Issue:19 | Synthesis and opioid activity of 7-oxygenated 2,3,4,4a,5,6,7,7a-octahydro-1H-benzofuro[3,2-e]isoquinolin-9-ols. |
AID496826 | Antimicrobial activity against Entamoeba histolytica | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
AID1358123 | Displacement of [3H]diprenorphine from human DOR expressed in African green monkey COS1 cell membranes at 1 uM incubated for 1 hr by scintillation counting method | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Synthesis of 7β-hydroxy-8-ketone opioid derivatives with antagonist activity at mu- and delta-opioid receptors. |
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. |
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. |
AID496824 | Antimicrobial activity against Toxoplasma gondii | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
AID286239 | Displacement of [125I]deltorphin 2 from human recombinant delta opioid receptor expressed in HEK cell membrane | 2007 | Journal of natural products, May, Volume: 70, Issue:5 | Habbemines A and B, pyrrolidine alkaloids with human delta-opioid receptor binding affinity from the leaves of Elaeocarpus habbemensis. |
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). |
AID235328 | Selectivity ratio of kappa opioid receptor to delta opioid receptor | 1988 | Journal of medicinal chemistry, Feb, Volume: 31, Issue:2 | Application of the message-address concept in the design of highly potent and selective non-peptide delta opioid receptor antagonists. |
AID612053 | Antagonist activity against human recombinant kappa opioid receptor expressed in CHO cells assessed as inhibition of [35S]GTP-gamma-S binding after 3 hrs by liquid scintillation counting | 2011 | Bioorganic & medicinal chemistry, Jun-01, Volume: 19, Issue:11 | Probes for narcotic receptor mediated phenomena. Part 42: synthesis and in vitro pharmacological characterization of the N-methyl and N-phenethyl analogues of the racemic ortho-c and para-c oxide-bridged phenylmorphans. |
AID165434 | Tested in rabbit for percentage analgesia after treatment with compound | 1989 | Journal of medicinal chemistry, Mar, Volume: 32, Issue:3 | New 4-(heteroanilido)piperidines, structurally related to the pure opioid agonist fentanyl, with agonist and/or antagonist properties. |
AID1186504 | Displacement of [3H]-naloxone from rat mu opioid receptor expressed in HEK cells after 60 mins | 2014 | Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17 | Discovery, structure-activity relationship studies, and anti-nociceptive effects of 1-phenyl-3,6,6-trimethyl-1,5,6,7-tetrahydro-4H-indazol-4-one as novel opioid receptor agonists. |
AID150821 | Concentration required to inhibit agonist (loperamide) stimulated [35S]GTP-gamma-S, binding to membranes containing the cloned human mu opioid receptor | 2003 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 13, Issue:24 | trans-3,4-dimethyl-4-(3-carboxamidophenyl)piperidines: a novel class of micro-selective opioid antagonists. |
AID1137263 | Analgesic activity in sc dosed rat assessed as inhibition of morphine-induced effect | 1979 | Journal of medicinal chemistry, Oct, Volume: 22, Issue:10 | (2,6-Methano-3-benzazocin-11 beta-yl)alkanones. 1. Alkylalkanones: a new series of N-methyl derivatives with novel opiate activity profiles. |
AID148018 | Inhibition of [3H]U-69593 binding to human Opioid receptor kappa 1 expressed in HEK 293 cells | 2000 | Bioorganic & medicinal chemistry letters, Mar-20, Volume: 10, Issue:6 | Design, synthesis and biological evaluation of 3-amino-3-phenylpropionamide derivatives as novel mu opioid receptor ligands. |
AID229186 | Inhibition of specific binding of [125I]-PIPAG to sigma binding site in Guinea pig brain membranes | 1992 | Journal of medicinal chemistry, Dec-11, Volume: 35, Issue:25 | Radiosynthesis, cerebral distribution, and binding of [125I]-1-(p-iodophenyl)-3-(1-adamantyl)guanidine, a ligand for sigma binding sites. |
AID357082 | Antinociceptive effect in icv dosed sickle cell anemic NY1DD transgenic mouse after 10 mins 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. |
AID357089 | Binding affinity to CCR5 in NY1DD transgenic mouse brain membrane | 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. |
AID481095 | Displacement of [3H]U69593 from kappa opioid receptor in guinea pig brain membrane after 150 mins by scintillation counting | 2010 | Journal of medicinal chemistry, May-27, Volume: 53, Issue:10 | Conformationally constrained kappa receptor agonists: stereoselective synthesis and pharmacological evaluation of 6,8-diazabicyclo[3.2.2]nonane derivatives. |
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AID1820166 | Displacement of [3H]-PrRP-20 from human PrRP receptor expressed in CHO cells by TopCount scintillation counting method | 2021 | Journal of medicinal chemistry, 06-10, Volume: 64, Issue:11 | Identification of an |
AID1458127 | Antagonist activity at recombinant human MOR expressed in HEK293T cells assessed as reduction in DAMGO-induced inhibition of forskolin-stimulated cAMP level at 10 uM preincubated for 15 to 20 mins followed by DAMGO and forskolin addition by GloSensor assa | 2017 | Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15 | Opioid Receptor Modulators with a Cinnamyl Group. |
AID111970 | Maximum percent analgesia using tail flick test in mice | 1980 | Journal of medicinal chemistry, Jun, Volume: 23, Issue:6 | 14-(Arylhydroxyamino)codeinones and derivatives as analgetics and antagonists. |
AID149152 | Compound was evaluated for the percent recovery of 1.0 nM of [3H]- DAGO binding to opioid receptor mu in un washed guinea pig brain membranes at 1000(nM) concentration | 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. |
AID148929 | Binding potency of D-ala2,D-Leu5-enkephalin to Opioid receptor delta 1 in the mouse vas deferens | 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. |
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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. |
AID1458129 | Antagonist activity at recombinant human DOR expressed in HEK293T cells assessed as reduction in DADLE-induced inhibition of forskolin-stimulated cAMP level at 10 uM preincubated for 15 to 20 mins followed by DADLE and forskolin addition by GloSensor assa | 2017 | Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15 | Opioid Receptor Modulators with a Cinnamyl Group. |
AID443812 | Antagonist activity at human delta opioid receptor expressed in CHO cells assessed as inhibition of agonist-induced [35S]GTPgammaS binding | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3 | Synthesis and opioid activity of enantiomeric N-substituted 2,3,4,4a,5,6,7,7a-octahydro-1H-benzofuro[3,2-e]isoquinolines. |
AID176827 | Tested for concentration required to reduce the food consumption by 20 % 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. |
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AID148813 | Antagonistic activity against Opioid receptor delta 1 using [D-Ala2,D-Leu5]enkephalin in mouse vas deferens preparation | 1988 | Journal of medicinal chemistry, Feb, Volume: 31, Issue:2 | Application of the message-address concept in the design of highly potent and selective non-peptide delta opioid receptor antagonists. |
AID1465638 | AUC (0 to t) in Beagle dog at 10 mg/kg, po by LC-MS/MS analysis | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20 | Oral Delivery of Propofol with Methoxymethylphosphonic Acid as the Delivery Vehicle. |
AID496832 | Antimicrobial activity against Trypanosoma brucei rhodesiense | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
AID1441546 | Displacement of [3H]DAMGO from mu-type opioid receptor in guinea pig brain membranes after 120 mins by solid scintillation counting | 2017 | Journal of medicinal chemistry, 03-23, Volume: 60, Issue:6 | Design and Synthesis of Enantiomerically Pure Decahydroquinoxalines as Potent and Selective κ-Opioid Receptor Agonists with Anti-Inflammatory Activity in Vivo. |
AID132612 | In vivo analgesic activity was measured by using Antiphenyl quinone Writhing(PQW) test after subcutaneous administration; Inactive | 1994 | Journal of medicinal chemistry, Sep-16, Volume: 37, Issue:19 | Synthesis and opioid activity of 7-oxygenated 2,3,4,4a,5,6,7,7a-octahydro-1H-benzofuro[3,2-e]isoquinolin-9-ols. |
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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. |
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. |
AID152401 | Irreversible inhibition of 0.5 nM [3H]bremazocine binding against Opioid receptors from washed bovine caudate membranes at 1 nM in presence of NaCl | 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. |
AID152057 | Inhibition of [3H]naloxone binding to Opioid receptor mu 1 of rat brain membrane | 1985 | Journal of medicinal chemistry, Dec, Volume: 28, Issue:12 | Factors affecting binding of trans-N-[2-(methylamino)cyclohexyl]benzamides at the primary morphine receptor. |
AID1221959 | Efflux ratio of permeability from apical to basolateral over basolateral to apical side of MDCK cells expressing MDR1 | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2 | Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model. |
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AID148836 | Antagonistic activity against Opioid receptor kappa 1 using ethylketazocine in guinea pig ileum preparation | 1988 | Journal of medicinal chemistry, Feb, Volume: 31, Issue:2 | Application of the message-address concept in the design of highly potent and selective non-peptide delta opioid receptor antagonists. |
AID1210069 | Inhibition of human recombinant CYP2J2 assessed as reduction in astemizole O-demethylation by LC-MS/MS method | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1 | Discovery and characterization of novel, potent, and selective cytochrome P450 2J2 inhibitors. |
AID165438 | Percentage of respirations per minute after treatment in rabbit | 1989 | Journal of medicinal chemistry, Mar, Volume: 32, Issue:3 | New 4-(heteroanilido)piperidines, structurally related to the pure opioid agonist fentanyl, with agonist and/or antagonist properties. |
AID749673 | Antagonist activity at human recombinant mu opioid receptor expressed in CHO cell membranes assessed as inhibition of DAMGO-induced [35S]GTPgammaS binding by liquid scintillation counting analysis | 2013 | Bioorganic & medicinal chemistry, Jun-01, Volume: 21, Issue:11 | Probes for narcotic receptor mediated phenomena. 47. Novel C4a- and N-substituted-1,2,3,4,4a,9a-hexahydrobenzofuro[2,3-c]pyridin-6-ols. |
AID1211249 | Unbound intrinsic glucuronidation clearance in human liver microsomes at 1 uM after 30 to 60 mins by LC-MS/MS analysis in presence of UDP-glucuronosyltransferase and 2% bovine serum albumin | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4 | Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin. |
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. |
AID1255651 | Displacement of [3H]-U-69593 from kappa opioid receptor in guinea pig brain membrane after 120 mins by scintillation counting | 2015 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22 | Conformationally restricted κ-opioid receptor agonists: Synthesis and pharmacological evaluation of diastereoisomeric and enantiomeric decahydroquinoxalines. |
AID150030 | In vivo binding affinity against delta Opioid receptor was measured by using labeled ligand [3H]DADLE (1 nM) with 4 nM sufentanil | 1994 | Journal of medicinal chemistry, Sep-16, Volume: 37, Issue:19 | Synthesis and opioid activity of 7-oxygenated 2,3,4,4a,5,6,7,7a-octahydro-1H-benzofuro[3,2-e]isoquinolin-9-ols. |
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AID152211 | Opioid receptor mu 2 affinity against the receptor site model site 2(mu2) | 1986 | Journal of medicinal chemistry, Apr, Volume: 29, Issue:4 | N-substituent modulation of opiate agonist/antagonist activity in resolved 3-methyl-3-(m-hydroxyphenyl)piperidines. |
AID1146261 | Narcotic antagonist activity in morphine-dependent monkey by single dose suppression test | 1977 | Journal of medicinal chemistry, Nov, Volume: 20, Issue:11 | Synthesis and pharmacological activity of some N-alkyl-substituted 9alpha-ethyl-2'-hydroxy-5-methyl-6,7-benzomorphans. |
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. |
AID149048 | Inhibition of [3H]naloxone receptor binding to opioid receptor in the absence of 100 mM NaCl | 1986 | Journal of medicinal chemistry, Apr, Volume: 29, Issue:4 | N-substituent modulation of opiate agonist/antagonist activity in resolved 3-methyl-3-(m-hydroxyphenyl)piperidines. |
AID745763 | Displacement of [3H]-CP55940 from human recombinant CB1 receptor transfected in HEK293 cells at 10 uM after 90 mins relative to control | 2013 | Journal of natural products, 05-24, Volume: 76, Issue:5 | Neocosmospora sp.-derived resorcylic acid lactones with in vitro binding affinity for human opioid and cannabinoid receptors. |
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. |
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). |
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AID1197355 | Antagonist activity against human recombinant opioid mu receptor expressed in CHO cell membranes assessed as reduction in DAMGO-induced response after 3 hrs by [35S]GTP-gamma-S binding assay | 2015 | European journal of medicinal chemistry, Mar-06, Volume: 92 | Probes for narcotic receptor mediated phenomena 49. N-substituted rac-cis-4a-arylalkyl-1,2,3,4,4a,9a-hexahydrobenzofuro[2,3-c]pyridin-6-ols. |
AID338191 | Displacement of [3H]DPDPE from delta opioid receptor assessed as specific binding relative to total binding | 1993 | Journal of natural products, Apr, Volume: 56, Issue:4 | The role of receptor binding in drug discovery. |
AID610903 | Binding affinity at human kappa opioid receptor expressed in CHO-K1 cells at 10 uM | 2011 | Journal of natural products, Jul-22, Volume: 74, Issue:7 | Benzyl derivatives with in vitro binding affinity for human opioid and cannabinoid receptors from the fungus Eurotium repens. |
AID496827 | Antimicrobial activity against Leishmania amazonensis | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
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. |
AID1562933 | Antagonist activity at MOR in Wistar rat brain membranes at 10 uM in presence of Tyr-D-Ala-Gly-Phe-NH2 after 60 mins by [35S]-GTPgammaS binding assay relative to control | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Preparation of bivalent agonists for targeting the mu opioid and cannabinoid receptors. |
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. |
AID1633367 | Displacement of [3H]-diprenorphine from human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by micro beta2 scintillation counting method | 2019 | ACS medicinal chemistry letters, Apr-11, Volume: 10, Issue:4 | Novel Cyclic Biphalin Analogues by Ruthenium-Catalyzed Ring Closing Metathesis: |
AID233698 | Selectivity ratio is the ratio of the binding affinities against delta and mu opioid receptors. | 1995 | Journal of medicinal chemistry, Aug-04, Volume: 38, Issue:16 | Synthesis and biological evaluation of 14-alkoxymorphinans. 11. 3-Hydroxycyprodime and analogues: opioid antagonist profile in comparison to cyprodime. |
AID1135646 | Antagonist activity at opioid receptor in mouse/rat NG108-15 cells assessed as reversal of morphine-induced inhibition of adenylate cyclase activity at 0.5 uM | 1978 | Journal of medicinal chemistry, Apr, Volume: 21, Issue:4 | Studies in the (+)-morphinan series. 5. Synthesis and biological properties of (+)-naloxone. |
AID1137259 | Analgesic activity in sc dosed mouse by acetylcholine writhing test | 1979 | Journal of medicinal chemistry, Oct, Volume: 22, Issue:10 | (2,6-Methano-3-benzazocin-11 beta-yl)alkanones. 1. Alkylalkanones: a new series of N-methyl derivatives with novel opiate activity profiles. |
AID293128 | Inhibition of morphine-induced antinociception in mouse at 2.38 ng, icv after 10 mins by hot plate test | 2007 | Bioorganic & medicinal chemistry, Feb-01, Volume: 15, Issue:3 | Transformation of mu-opioid receptor agonists into biologically potent mu-opioid receptor antagonists. |
AID277678 | Activity at mu opioid receptor assessed as increase in calcium level in CHO cells by aequorin luminescence based calcium assay | 2007 | Journal of medicinal chemistry, Feb-08, Volume: 50, Issue:3 | Synthesis and characterization of potent and selective mu-opioid receptor antagonists, [Dmt(1), D-2-Nal(4)]endomorphin-1 (Antanal-1) and [Dmt(1), D-2-Nal(4)]endomorphin-2 (Antanal-2). |
AID148019 | Binding affinity at cloned human kappa opioid receptor by [3H]diprenorphine displacement. | 2003 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 13, Issue:24 | trans-3,4-dimethyl-4-(3-carboxamidophenyl)piperidines: a novel class of micro-selective opioid antagonists. |
AID231774 | Ratio for 50% inhibition of [3H]naloxone (1 M) binding to opioid receptor in rat brain membrane was determined in the absence of NaCl to that of presence of NaCl | 1984 | Journal of medicinal chemistry, Dec, Volume: 27, Issue:12 | Synthesis and biological evaluation of 14-alkoxymorphinans. 1. Highly potent opioid agonists in the series of (-)-14-methoxy-N-methylmorphinan-6-ones. |
AID132267 | The Effective dose was measured by using mouse writhing assay after the compound administered subcutaneously; IA means inactive | 1980 | Journal of medicinal chemistry, Feb, Volume: 23, Issue:2 | Analgesic narcotic antagonists. 2. 8-Alkymorphinan-6-ones. |
AID496823 | Antimicrobial activity against Trichomonas vaginalis | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
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. |
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. |
AID596638 | Displacement of [3H]naltrindole from human delta-opioid receptor expressed in CHO cells after 3 hrs by scintillation counting | 2011 | Bioorganic & medicinal chemistry, May-01, Volume: 19, Issue:9 | Synthesis and binding affinity of novel mono- and bivalent morphinan ligands for κ, μ, and δ opioid receptors. |
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. |
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. |
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. |
AID443809 | Antagonist activity at human mu opioid receptor expressed in CHO cells assessed as inhibition of agonist-induced [35S]GTPgammaS binding | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3 | Synthesis and opioid activity of enantiomeric N-substituted 2,3,4,4a,5,6,7,7a-octahydro-1H-benzofuro[3,2-e]isoquinolines. |
AID443801 | Displacement of [3H]di-O-tolyguanidine from sigma2 receptor in rat brain homogenate | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3 | Synthesis and opioid activity of enantiomeric N-substituted 2,3,4,4a,5,6,7,7a-octahydro-1H-benzofuro[3,2-e]isoquinolines. |
AID1221960 | Apparent permeability from apical to basolateral side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of P-gp inhibitor LY335979 | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2 | Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model. |
AID114537 | Tested for effective dose required to produce diarrhea in morphine dependent mice after subcutaneous administration | 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. |
AID107605 | Compound was tested in vivo for narcotic agonist activity (dose in sc, mg/kg) in mice using phenylquinone assay; I = Inactive at 1,10, 30 mg/kg | 1986 | Journal of medicinal chemistry, Nov, Volume: 29, Issue:11 | Comparison of (-)-eseroline with (+)-eseroline and dihydroseco analogues in antinociceptive assays: confirmation of rubreserine structure by X-ray analysis. |
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. |
AID600432 | Displacement of [3H]DPN from human recombinant delta-type opioid receptor expressed in CHO cell membranes | 2009 | Bioorganic & medicinal chemistry, Jul-15, Volume: 17, Issue:14 | Structure-activity studies on the nociceptin/orphanin FQ receptor antagonist 1-benzyl-N-{3-[spiroisobenzofuran-1(3H),4'-piperidin-1-yl]propyl} pyrrolidine-2-carboxamide. |
AID1655378 | Displacement of [3H]diprenorphine human MOR expressed in CHO cell membranes after 1 hr by micro beta2 scintillation counting method | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5 | Developing Cyclic Opioid Analogues: Fluorescently Labeled Bioconjugates of Biphalin. |
AID148313 | Binding affinity was evaluated by measuring the ability to displace CI977 radioligand binding from Opioid receptor kappa 1 in mouse vas deferens preparation | 1995 | Journal of medicinal chemistry, Aug-04, Volume: 38, Issue:16 | Synthesis and biological evaluation of 14-alkoxymorphinans. 11. 3-Hydroxycyprodime and analogues: opioid antagonist profile in comparison to cyprodime. |
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. |
AID357085 | Antinociceptive effect in icv dosed sickle cell anemic hBERK1 transgenic mouse after 10 mins 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. |
AID314189 | Antagonist activity at mu opioid receptor expressed in CHO cells assessed as release of intracellular calcium ions by aequorin luminescence-based calcium assay | 2008 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 18, Issue:4 | Novel highly potent mu-opioid receptor antagonist based on endomorphin-2 structure. |
AID149445 | Inhibition of 0.5 nM [3H]- Bremazocine binding to Opioid receptor mu 1 of bovine striatum membrane | 1990 | Journal of medicinal chemistry, Aug, Volume: 33, Issue:8 | Electrophilic alpha-methylene-gamma-lactone and isothiocyanate opioid ligands related to etorphine. |
AID1562932 | Antagonist activity at MOR in Wistar rat brain membranes at 10 uM in presence of oxycodone after 60 mins by [35S]-GTPgammaS binding assay relative to control | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Preparation of bivalent agonists for targeting the mu opioid and cannabinoid receptors. |
AID170061 | Opioid antagonist activity (30 mg/kg, peripherally) was determined by measuring the analgesia produced by morphine given 10 mins (after the compound) at a dose of 5 mg/kg; no effect | 2004 | Bioorganic & medicinal chemistry letters, Feb-23, Volume: 14, Issue:4 | A highly toxic morphine-3-glucuronide derivative. |
AID413920 | Antagonist activity at human mu opioid receptor expressed in CHO cells assessed as inhibition of DAMGO-induced [35S]GTPgammaS binding | 2008 | Journal of medicinal chemistry, Dec-25, Volume: 51, Issue:24 | Probes for narcotic receptor mediated phenomena. 37. Synthesis and opioid binding affinity of the final pair of oxide-bridged phenylmorphans, the ortho- and para-b-isomers and their N-phenethyl analogues, and the synthesis of the N-phenethyl analogues of |
AID600431 | Displacement of [3H]DPN from human recombinant mu-type opioid receptor expressed in CHO cell membranes | 2009 | Bioorganic & medicinal chemistry, Jul-15, Volume: 17, Issue:14 | Structure-activity studies on the nociceptin/orphanin FQ receptor antagonist 1-benzyl-N-{3-[spiroisobenzofuran-1(3H),4'-piperidin-1-yl]propyl} pyrrolidine-2-carboxamide. |
AID128014 | Compound was evaluated in vivo for the antagonist activity by the tail flick assay using morphine as the agonist in mice. | 1984 | Journal of medicinal chemistry, Dec, Volume: 27, Issue:12 | Opioid agonists and antagonists. 6,6-Hydrazi and 6-oximino derivatives of 14-hydroxydihydromorphinones. |
AID7783 | Unbound fraction (plasma) | 2004 | Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5 | Prediction of human volume of distribution values for neutral and basic drugs. 2. Extended data set and leave-class-out statistics. |
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. |
AID149367 | Evaluation for the ability of delta opioid to protect the [3H]-DAMGO binding site from alkylation | 1994 | Journal of medicinal chemistry, May-27, Volume: 37, Issue:11 | 14 alpha,14' beta-[Dithiobis[(2-oxo-2,1-ethanediyl)imino]]bis (7,8-dihydromorphinone) and 14 alpha,14' beta-[dithiobis[(2-oxo-2,1- ethanediyl)imino]]bis[7,8-dihydro-N-(cyclopropylmethyl)normorphinone]: chemistry and opioid binding properties. |
AID311996 | Displacement of [125I]deltorphin 2 from human recombinant delta opioid receptor expressed in HEK cells | 2007 | Journal of natural products, Dec, Volume: 70, Issue:12 | Alkaloids with human delta-opioid receptor binding affinity from the Australian rainforest tree Peripentadenia mearsii. |
AID1255661 | Intrinsic activity at kappa opioid receptor in human HEK293 cells at 1 uM after 30 mins by [35S]GTPgammaS binding assay relative to U-69593 | 2015 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22 | Conformationally restricted κ-opioid receptor agonists: Synthesis and pharmacological evaluation of diastereoisomeric and enantiomeric decahydroquinoxalines. |
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. |
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. |
AID1587571 | Displacement of [3H]DPDPE from delta opioid receptor in rat membranes after 120 mins by scintillation counting analysis | |||
AID179386 | Concentration of drug required to inhibit the stereospecific binding of [3H]naloxone (5 nM) to homogenates of rat brain minus cerebellum in the presence of 100 mM NaCl | 1984 | Journal of medicinal chemistry, May, Volume: 27, Issue:5 | 5-Aryl-3-azabicyclo[3.2.0]heptan-6-one ketals, compounds with morphine-like analgesic activity. |
AID325959 | Antagonist activity at human cloned mu opioid receptor assessed as inhibition of loperamide-stimulated [35S]GTP-gamma-S binding | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6 | Novel trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidines as mu opioid receptor antagonists with improved opioid receptor selectivity profiles. |
AID1358124 | Displacement of [3H]diprenorphine from human DOR expressed in African green monkey COS1 cell membranes at 10 uM incubated for 1 hr by scintillation counting method | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Synthesis of 7β-hydroxy-8-ketone opioid derivatives with antagonist activity at mu- and delta-opioid receptors. |
AID496817 | Antimicrobial activity against Trypanosoma cruzi | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
AID127051 | Compound was evaluated for antinociceptive activity in mouse using tail flick vs morphine assay | 2000 | Bioorganic & medicinal chemistry letters, Nov-06, Volume: 10, Issue:21 | N-Cyclohexylethyl-N-noroxymorphindole: a mu-opioid preferring analogue of naltrindole. |
AID680023 | TP_TRANSPORTER: inhibition of Deltorphin II uptake (Deltorphin II: 50 uM, Naloxone: 1500 uM) in Xenopus laevis oocytes | 2000 | The Journal of pharmacology and experimental therapeutics, Jul, Volume: 294, Issue:1 | Organic anion-transporting polypeptides mediate transport of opioid peptides across blood-brain barrier. |
AID314198 | Antinociceptive activity in mouse assessed as rearing latency at 5 ug, icv in presence of endomorphin-2 by hot plate test | 2008 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 18, Issue:4 | Novel highly potent mu-opioid receptor antagonist based on endomorphin-2 structure. |
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. |
AID1820170 | Displacement of [3H]-Diprenorphine from human DOP receptor expressed in HEK293 cells by scintillation counting method | 2021 | Journal of medicinal chemistry, 06-10, Volume: 64, Issue:11 | Identification of an |
AID496830 | Antimicrobial activity against Leishmania major | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
AID107479 | Compound was tested in vivo for narcotic agonist activity (dose in sc, mg/kg) in mice using hot plate assay; I = Inactive at 1,10, 30 mg/kg | 1986 | Journal of medicinal chemistry, Nov, Volume: 29, Issue:11 | Comparison of (-)-eseroline with (+)-eseroline and dihydroseco analogues in antinociceptive assays: confirmation of rubreserine structure by X-ray analysis. |
AID607797 | Antagonist activity at human mu opioid receptor expressed in CHO cells coexpressing human recombinant MOR after 3 hrs by [35S]GTPgammaS binding assay | 2011 | Bioorganic & medicinal chemistry, Jul-15, Volume: 19, Issue:14 | Probes for narcotic receptor mediated phenomena. 43. Synthesis of the ortho-a and para-a, and improved synthesis and optical resolution of the ortho-b and para-b oxide-bridged phenylmorphans: compounds with moderate to low opioid-receptor affinity. |
AID204005 | In vivo binding affinity against sigma Opioid receptor was measured by using labeled ligand [3H]-SKF- 10,047 (1 nM) | 1994 | Journal of medicinal chemistry, Sep-16, Volume: 37, Issue:19 | Synthesis and opioid activity of 7-oxygenated 2,3,4,4a,5,6,7,7a-octahydro-1H-benzofuro[3,2-e]isoquinolin-9-ols. |
AID1167044 | Displacement of [3H]DAMGO from human MOR expressed in HEK293 cells after 60 mins by scintillation counting analysis | 2014 | Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21 | Nonpeptide small molecule agonist and antagonist original leads for neuropeptide FF1 and FF2 receptors. |
AID1574664 | Displacement of [3H]DAMGO from MOR in guinea pig brain membranes after 120 mins by scintillation counting method | 2019 | Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2 | Development of Novel Quinoxaline-Based κ-Opioid Receptor Agonists for the Treatment of Neuroinflammation. |
AID1458128 | Agonist activity at recombinant human DOR expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP level at 10 uM preincubated for 15 to 20 mins followed by forskolin addition by GloSensor assay relative to control | 2017 | Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15 | Opioid Receptor Modulators with a Cinnamyl Group. |
AID148988 | Affinity to opioid receptor kappa 1 using [3H]U-69593 as radioligand in homogenates of guinea pig brain membranes | 2001 | Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17 | Methylated analogues of methyl (R)-4-(3,4-dichlorophenylacetyl)- 3-(pyrrolidin-1-ylmethyl)piperazine-1-carboxylate (GR-89,696) as highly potent kappa-receptor agonists: stereoselective synthesis, opioid-receptor affinity, receptor selectivity, and functio |
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. |
AID149533 | Affinity against the Opioid receptor delta 1 | 1986 | Journal of medicinal chemistry, Apr, Volume: 29, Issue:4 | N-substituent modulation of opiate agonist/antagonist activity in resolved 3-methyl-3-(m-hydroxyphenyl)piperidines. |
AID1230326 | Displacement of [3H]DAMGO from mu opioid receptor (unknown origin) transfected into HEK293 cells at 10 uM by microplate scintillation counting | 2015 | Journal of natural products, Jun-26, Volume: 78, Issue:6 | Flavonoids from Perovskia atriplicifolia and Their in Vitro Displacement of the Respective Radioligands for Human Opioid and Cannabinoid Receptors. |
AID1211204 | Drug metabolism in human liver microsomes assessed as UGT1A8/2B7-mediated unbound intrinsic glucuronidation clearance at 1 uM after 30 to 60 mins by LC-MS/MS analysis in presence of 2% bovine serum albumin | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4 | Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin. |
AID409954 | Inhibition of mouse brain MAOA | 2008 | Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21 | Quantitative structure-activity relationship and complex network approach to monoamine oxidase A and B inhibitors. |
AID1604691 | Displacement of [3H]-diprenorphine from human MOR expressed in CHO cell membranes incubated for 1 hr by scintillation counting method | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5 | Potent, Efficacious, and Stable Cyclic Opioid Peptides with Long Lasting Antinociceptive Effect after Peripheral Administration. |
AID165734 | Percent change of volume in the respiratory activity was measured in rabbit at the 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. |
AID1197360 | Agonist activity against human recombinant opioid kappa receptor expressed in CHO cell membranes after 3 hrs by [35S]GTP-gamma-S binding assay relative to 500 nM (-)-U50,488 | 2015 | European journal of medicinal chemistry, Mar-06, Volume: 92 | Probes for narcotic receptor mediated phenomena 49. N-substituted rac-cis-4a-arylalkyl-1,2,3,4,4a,9a-hexahydrobenzofuro[2,3-c]pyridin-6-ols. |
AID1211213 | Unbound intrinsic glucuronidation clearance in human intestinal microsomes at 1 uM after 30 to 60 mins by LC-MS/MS analysis in presence of UDP-glucuronosyltransferase | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4 | Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin. |
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. |
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. |
AID294050 | Antinociceptive activity in mouse assessed as licking latency at 1 mg/kg, ip by hot plate method | 2007 | Bioorganic & medicinal chemistry, Mar-15, Volume: 15, Issue:6 | Structure-activity relationships of methoctramine-related polyamines as muscarinic antagonist: effect of replacing the inner polymethylene chain with cyclic moieties. |
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. |
AID624611 | Specific activity of expressed human recombinant UGT1A8 | 2000 | Annual review of pharmacology and toxicology, , Volume: 40 | Human UDP-glucuronosyltransferases: metabolism, expression, and disease. |
AID1215671 | Drug metabolism in pooled human hepatocytes assessed as aldehyde oxidase-mediated drug metabolism at 10 uM up to 120 mins by HPLC analysis in presence of 25 uM of hydralazine | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7 | Hydralazine as a selective probe inactivator of aldehyde oxidase in human hepatocytes: estimation of the contribution of aldehyde oxidase to metabolic clearance. |
AID147859 | Binding affinity against opioid receptor kappa 1 using [3H]- U-69,593 radioligand | 2001 | Journal of medicinal chemistry, Oct-11, Volume: 44, Issue:21 | From hit to lead. Combining two complementary methods for focused library design. Application to mu opiate ligands. |
AID150414 | Ability to displace [3H]DHM from Opioid receptors in the absence of sodium ion(Na+) | 1980 | Journal of medicinal chemistry, Jun, Volume: 23, Issue:6 | 14-(Arylhydroxyamino)codeinones and derivatives as analgetics and antagonists. |
AID220522 | Tested for the opioid antagonist effect at delta-opioid receptor in isolated mouse vas deferens at 20 nM | 1993 | Journal of medicinal chemistry, Oct-01, Volume: 36, Issue:20 | 3,4-Dimethyl-4-(3-hydroxyphenyl)piperidines: opioid antagonists with potent anorectant activity. |
AID1224135 | Displacement of [3H]U-69593 from kappa-opioid receptor in guinea pig brain membrane | 2014 | Bioorganic & medicinal chemistry, Jul-01, Volume: 22, Issue:13 | Combination of cyclohexane and piperazine based κ-opioid receptor agonists: Synthesis and pharmacological evaluation of trans,trans-configured perhydroquinoxalines. |
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. |
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. |
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. |
AID165436 | Tested in rabbit for percentage analgesia after treatment with morphine | 1989 | Journal of medicinal chemistry, Mar, Volume: 32, Issue:3 | New 4-(heteroanilido)piperidines, structurally related to the pure opioid agonist fentanyl, with agonist and/or antagonist properties. |
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. |
AID1633374 | Antagonist activity at human delta opioid receptor expressed in CHO cell membranes assessed as reduction in SNC80-induced [35S]GTPgammaS binding incubated for 1 hr | 2019 | ACS medicinal chemistry letters, Apr-11, Volume: 10, Issue:4 | Novel Cyclic Biphalin Analogues by Ruthenium-Catalyzed Ring Closing Metathesis: |
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. |
AID1777977 | Binding affinity to mu-opioid receptor (unknown origin) | |||
AID148761 | Compound was evaluated for the percent recovery of 0.5 nM of [3H]- bremazocine binding to total opioid receptor in washed guinea pig brain membranes at 1000 (nM) concentration of the compound | 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. |
AID338190 | Displacement of [3H]DAGO from mu opioid receptor assessed as specific binding relative to total binding | 1993 | Journal of natural products, Apr, Volume: 56, Issue:4 | The role of receptor binding in drug discovery. |
AID151464 | Opioid receptor mu 1 affinity against the receptor site model site 1 (mu1) | 1986 | Journal of medicinal chemistry, Apr, Volume: 29, Issue:4 | N-substituent modulation of opiate agonist/antagonist activity in resolved 3-methyl-3-(m-hydroxyphenyl)piperidines. |
AID610905 | Binding affinity at human CB1 receptor expressed in CHO-K1 cells at 10 uM | 2011 | Journal of natural products, Jul-22, Volume: 74, Issue:7 | Benzyl derivatives with in vitro binding affinity for human opioid and cannabinoid receptors from the fungus Eurotium repens. |
AID147920 | Compound was evaluated for the percent recovery of 1.0 nM of [3H]- DPDPE binding to Opioid receptor delta 1 in un washed guinea pig brain membranes at 1000(nM) concentration | 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. |
AID1221956 | Apparent permeability from apical to basolateral side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2 | Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model. |
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. |
AID170059 | Opioid antagonist activity (1 mg/kg, peripherally) was determined by measuring the analgesia produced by morphine given 10 mins (after the compound) at a dose of 5 mg/kg; no effect | 2004 | Bioorganic & medicinal chemistry letters, Feb-23, Volume: 14, Issue:4 | A highly toxic morphine-3-glucuronide derivative. |
AID601796 | Displacement of [3H]DAMGO from mu opioid receptor in guinea pig brain membranes | 2011 | European journal of medicinal chemistry, Jun, Volume: 46, Issue:6 | Synthesis of 7,9-diazabicyclo[4.2.2]decanes as conformationally restricted κ receptor agonists: fine tuning of the dihedral angle of the ethylenediamine pharmacophore. |
AID148255 | Evaluation for the ability of kappa opioid to protect the [3H]U-69593 binding site from alkylation | 1994 | Journal of medicinal chemistry, May-27, Volume: 37, Issue:11 | 14 alpha,14' beta-[Dithiobis[(2-oxo-2,1-ethanediyl)imino]]bis (7,8-dihydromorphinone) and 14 alpha,14' beta-[dithiobis[(2-oxo-2,1- ethanediyl)imino]]bis[7,8-dihydro-N-(cyclopropylmethyl)normorphinone]: chemistry and opioid binding properties. |
AID1211211 | Unbound intrinsic glucuronidation clearance in human kidney microsomes at 1 uM after 30 to 60 mins by LC-MS/MS analysis in presence of UDP-glucuronosyltransferase and 2% bovine serum albumin | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4 | Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin. |
AID21856 | In vivo clearance in human | 1999 | Journal of medicinal chemistry, Dec-16, Volume: 42, Issue:25 | Combining in vitro and in vivo pharmacokinetic data for prediction of hepatic drug clearance in humans by artificial neural networks and multivariate statistical techniques. |
AID601799 | Displacement of [3H]di-o-toylguanidine from sigma 2 receptor in rat liver homogenates | 2011 | European journal of medicinal chemistry, Jun, Volume: 46, Issue:6 | Synthesis of 7,9-diazabicyclo[4.2.2]decanes as conformationally restricted κ receptor agonists: fine tuning of the dihedral angle of the ethylenediamine pharmacophore. |
AID1574665 | Displacement of [3H]DPDPE from DOR in Sprague-Dawley rat brain membranes after 120 mins by scintillation counting method | 2019 | Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2 | Development of Novel Quinoxaline-Based κ-Opioid Receptor Agonists for the Treatment of Neuroinflammation. |
AID26362 | Ionization constant (pKa) | 2004 | Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5 | Prediction of human volume of distribution values for neutral and basic drugs. 2. Extended data set and leave-class-out statistics. |
AID152056 | Inhibition of [3H]naloxone binding to Opioid receptor mu 1 of rat brain membrane | 1985 | Journal of medicinal chemistry, Dec, Volume: 28, Issue:12 | Factors affecting binding of trans-N-[2-(methylamino)cyclohexyl]benzamides at the primary morphine receptor. |
AID187178 | Inhibition constant of compound on R-(+)-125[I]-8 radioligand binding to rat striatal membranes | 1991 | Journal of medicinal chemistry, Mar, Volume: 34, Issue:3 | Synthesis and resolution of (+-)-7-chloro-8-hydroxy-1-(3'-iodophenyl)-3-methyl-2,3,4,5-tetrahydro- 1H-3- benzazepine (TISCH): a high affinity and selective iodinated ligand for CNS D1 dopamine receptor. |
AID232509 | Selectivity ratio of EKC and normorphine(NM) in mouse vas deferens | 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. |
AID148902 | Tested for irreversible inhibition of [3H]- Naltrexone binding with in the presence of NaCl (unwashed) | 1984 | Journal of medicinal chemistry, Dec, Volume: 27, Issue:12 | Diastereomeric 6-desoxy-6-spiro-alpha-methylene-gamma-butyrolactone derivatives of naltrexone and oxymorphone. Selective irreversible inhibition of naltrexone binding in an opioid receptor preparation by a conformationally restricted michael acceptor liga |
AID425653 | Renal clearance in human | 2009 | Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15 | Physicochemical determinants of human renal clearance. |
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. |
AID1211176 | Drug metabolism in human intestinal microsomes assessed as UGT1A8/2B7-mediated unbound intrinsic glucuronidation clearance at 1 uM after 30 to 60 mins by LC-MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4 | Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin. |
AID1441545 | Displacement of [3H]U-69,593 from kappa-type opioid receptor in guinea pig brain membranes after 120 mins by solid scintillation counting | 2017 | Journal of medicinal chemistry, 03-23, Volume: 60, Issue:6 | Design and Synthesis of Enantiomerically Pure Decahydroquinoxalines as Potent and Selective κ-Opioid Receptor Agonists with Anti-Inflammatory Activity in Vivo. |
AID233879 | Selectivity ratio was determined using the Ke value of Opioid receptor delta 1 to that of Opioid receptor mu 1 | 1990 | Journal of medicinal chemistry, Apr, Volume: 33, Issue:4 | Synthesis and biological evaluation of 14-alkoxymorphinans. 3. Extensive study on cyprodime-related compounds. |
AID1358126 | Displacement of [3H]diprenorphine from human KOR expressed in African green monkey COS1 cell membranes at 10 uM incubated for 1 hr by scintillation counting method | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Synthesis of 7β-hydroxy-8-ketone opioid derivatives with antagonist activity at mu- and delta-opioid receptors. |
AID148006 | In vitro binding affinity towards human Opioid receptor kappa 1 on CHO cell membranes using [3H]diprenorphine displacement. | 2003 | Journal of medicinal chemistry, May-22, Volume: 46, Issue:11 | Structure-activity relationships of dynorphin a analogues modified in the address sequence. |
AID600433 | Displacement of [3H]DPN from human recombinant kappa-type opioid receptor expressed in CHO cell membranes | 2009 | Bioorganic & medicinal chemistry, Jul-15, Volume: 17, Issue:14 | Structure-activity studies on the nociceptin/orphanin FQ receptor antagonist 1-benzyl-N-{3-[spiroisobenzofuran-1(3H),4'-piperidin-1-yl]propyl} pyrrolidine-2-carboxamide. |
AID152397 | Irreversible inhibition of 0.5 nM [3H]bremazocine binding against Opioid receptors from unwashed bovine caudate membranes at 1 nM in presence of NaCl | 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. |
AID1777978 | Binding affinity to delta-opioid receptor (unknown origin) | |||
AID624620 | Specific activity of expressed human recombinant UGT2B7H | 2000 | Annual review of pharmacology and toxicology, , Volume: 40 | Human UDP-glucuronosyltransferases: metabolism, expression, and disease. |
AID151916 | Inhibition of [3H]naloxone binding to Opioid receptor mu 1 of rat brain membrane | 1985 | Journal of medicinal chemistry, Dec, Volume: 28, Issue:12 | Factors affecting binding of trans-N-[2-(methylamino)cyclohexyl]benzamides at the primary morphine receptor. |
AID138825 | Evaluation for the ability of mu opioid to protect the [3H]DAMGO binding site from alkylation | 1994 | Journal of medicinal chemistry, May-27, Volume: 37, Issue:11 | 14 alpha,14' beta-[Dithiobis[(2-oxo-2,1-ethanediyl)imino]]bis (7,8-dihydromorphinone) and 14 alpha,14' beta-[dithiobis[(2-oxo-2,1- ethanediyl)imino]]bis[7,8-dihydro-N-(cyclopropylmethyl)normorphinone]: chemistry and opioid binding properties. |
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. |
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. |
AID1820171 | Displacement of [3H]-Diprenorphine from human KOP receptor expressed in HEK293 cells by scintillation counting method | 2021 | Journal of medicinal chemistry, 06-10, Volume: 64, Issue:11 | Identification of an |
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). |
AID150975 | In vitro binding affinity to human Opioid receptor mu 1 on CHO cell membranes using [3H]diprenorphine displacement. | 2003 | Journal of medicinal chemistry, May-22, Volume: 46, Issue:11 | Structure-activity relationships of dynorphin a analogues modified in the address sequence. |
AID1185657 | Displacement of [3H]-naloxone from human mu opioid receptor expressed in CHO-K1 cells by scintillation counting analysis | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15 | Synthesis and pharmacological evaluation of 5-pyrrolidinylquinoxalines as a novel class of peripherally restricted κ-opioid receptor agonists. |
AID295930 | Displacement of [3H]U-69593 from kappa opioid receptor in guinea pig brain membrane | 2007 | European journal of medicinal chemistry, Oct, Volume: 42, Issue:10 | Synthesis of bridged piperazines with sigma receptor affinity. |
AID1146570 | Antiwrithing activity in sc dosed mouse assessed as prevention of acetylcholine-induced abdominal constriction response | 1978 | Journal of medicinal chemistry, Dec, Volume: 21, Issue:12 | (2-exo-3-endo)-2-Aryltropane-3-carboxylic esters, a new class of narcotic antagonists. |
AID515780 | Intrinsic solubility of the compound in water | 2010 | Bioorganic & medicinal chemistry, Oct-01, Volume: 18, Issue:19 | QSAR-based solubility model for drug-like compounds. |
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. |
AID596552 | Displacement of [3H]U69563 from human kappa-opioid receptor expressed in CHO cells after 60 mins by scintillation counting | 2011 | Bioorganic & medicinal chemistry, May-01, Volume: 19, Issue:9 | Synthesis and binding affinity of novel mono- and bivalent morphinan ligands for κ, μ, and δ opioid receptors. |
AID437482 | Antagonist activity at mu opioid receptor expressed in CHO-K1 cells assessed as cAMP accumulation | 2009 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 19, Issue:23 | Design, synthesis and biological evaluation of a bivalent micro opiate and adenosine A1 receptor antagonist. |
AID1211284 | Glucuronidation clearance in human liver microsomes | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4 | Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin. |
AID327870 | Activation of human mu opioid receptor expressed in HEK293a cells coexpressing YFP-labelled alphai1 and CFP-labelled beta-1-gamma-2 Gi subunits assessed as decrease in fluorescence resonance energy transfer signal | 2007 | The Journal of biological chemistry, Sep-14, Volume: 282, Issue:37 | Live cell monitoring of mu-opioid receptor-mediated G-protein activation reveals strong biological activity of close morphine biosynthetic precursors. |
AID1823682 | Antagonist activity at human mu opioid receptor expressed in HEK293T cells assessed as Galphai2 activation preincubated with compound in D-PBS for 3 hrs followed by coelenterazine addition for 5 mins once again compound addition for 10 mins by BRET assay | |||
AID1528330 | Antagonist activity at mouse mu opioid receptor expressed in CHO cells cotransfected with Galphaqi5 assessed as inhibition of DAMGO-induced increase in intracellular calcium concentration preincubated for 60 mins in Fluo4AM solution followed by compound a | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24 | Application of Bivalent Bioisostere Concept on Design and Discovery of Potent Opioid Receptor Modulators. |
AID437483 | Binding affinity to adenosine receptor A1 | 2009 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 19, Issue:23 | Design, synthesis and biological evaluation of a bivalent micro opiate and adenosine A1 receptor antagonist. |
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. |
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. |
AID381424 | Inhibition of U50488-induced analgesic activity against C57BL/6 mouse assessed as tail withdrawal latency at 10 mg/kg, ip | 2007 | The Journal of biological chemistry, Oct-12, Volume: 282, Issue:41 | Long-acting kappa opioid antagonists disrupt receptor signaling and produce noncompetitive effects by activating c-Jun N-terminal kinase. |
AID286936 | Displacement of [125I]deltorphin 2 from human recombinant delta opioid receptor expressed in HEK cell membranes | 2007 | Journal of natural products, May, Volume: 70, Issue:5 | Indolizidine alkaloids with delta-opioid receptor binding affinity from the leaves of Elaeocarpus fuscoides. |
AID1587572 | Displacement of [3H]U69,593 from kappa opioid receptor in guinea pig brain membrane after 120 mins by scintillation counting analysis | |||
AID1135637 | Displacement of [3H]-(-)-naloxone from opiate receptor in rat brain membrane | 1978 | Journal of medicinal chemistry, Apr, Volume: 21, Issue:4 | Studies in the (+)-morphinan series. 5. Synthesis and biological properties of (+)-naloxone. |
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. |
AID150012 | Antagonistic activity against Opioid receptor mu 1 using morphine in guinea pig ileum preparation | 1988 | Journal of medicinal chemistry, Feb, Volume: 31, Issue:2 | Application of the message-address concept in the design of highly potent and selective non-peptide delta opioid receptor antagonists. |
AID137458 | Ability of compound for reversal of morphine and analgesia was determined; 2= reversal of both morphine respiratory depression and analgesia | 1989 | Journal of medicinal chemistry, Mar, Volume: 32, Issue:3 | New 4-(heteroanilido)piperidines, structurally related to the pure opioid agonist fentanyl, with agonist and/or antagonist properties. |
AID1777979 | Binding affinity to kappa-opioid receptor (unknown origin) | |||
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). |
AID1221982 | Fraction absorbed in human | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2 | Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model. |
AID1211244 | Fraction unbound in human liver microsomes at 1 uM after 30 to 60 mins by LC-MS/MS analysis in presence of 2% bovine serum albumin | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4 | Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin. |
AID1137258 | Analgesic activity in sc dosed rat assessed as inhibition of phenazocine-induced effect | 1979 | Journal of medicinal chemistry, Oct, Volume: 22, Issue:10 | (2,6-Methano-3-benzazocin-11 beta-yl)alkanones. 1. Alkylalkanones: a new series of N-methyl derivatives with novel opiate activity profiles. |
AID496821 | Antimicrobial activity against Leishmania | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
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. |
AID1146574 | Narcotic analgesic activity in sc dosed rat assessed as inhibition of phenazocine-induced effect by D'Amour-Smith tail flick test | 1978 | Journal of medicinal chemistry, Dec, Volume: 21, Issue:12 | (2-exo-3-endo)-2-Aryltropane-3-carboxylic esters, a new class of narcotic antagonists. |
AID128025 | Compound was tested for analgesia in mouse writhing assay by subcutaneous administration; IA means inactive | 1980 | Journal of medicinal chemistry, Dec, Volume: 23, Issue:12 | Analgesic narcotic antagonists. 4. 7-Methyl-N-(cycloalkylmethyl)-3-hydroxymorphinan-6-ones and -isomorphinan-6-ones. |
AID226729 | Relative potency calculated from the ratio of IC50 of [Leu]-enkephalin to that of the compound | 1984 | Journal of medicinal chemistry, Jul, Volume: 27, Issue:7 | A photoaffinity reagent to label the opiate receptors of guinea pig ileum and mouse vas deferens. |
AID1443980 | Inhibition of human BSEP expressed in fall armyworm sf9 cell plasma membrane vesicles assessed as reduction in vesicle-associated [3H]-taurocholate transport preincubated for 10 mins prior to ATP addition measured after 15 mins in presence of [3H]-tauroch | 2010 | Toxicological sciences : an official journal of the Society of Toxicology, Dec, Volume: 118, Issue:2 | Interference with bile salt export pump function is a susceptibility factor for human liver injury in drug development. |
AID624606 | Specific activity of expressed human recombinant UGT1A1 | 2000 | Annual review of pharmacology and toxicology, , Volume: 40 | Human UDP-glucuronosyltransferases: metabolism, expression, and disease. |
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. |
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. |
AID624636 | Drug glucuronidation reaction catalyzed by human recombinant UGT1A8 | 2005 | Pharmacology & therapeutics, Apr, Volume: 106, Issue:1 | UDP-glucuronosyltransferases and clinical drug-drug interactions. |
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. |
AID1472423 | Stability in human hepatocytes after 120 mins by HPLC-MS/MS analysis | 2018 | Journal of medicinal chemistry, 01-11, Volume: 61, Issue:1 | The Magic of Crystal Structure-Based Inhibitor Optimization: Development of a Butyrylcholinesterase Inhibitor with Picomolar Affinity and in Vivo Activity. |
AID149052 | Compound was evaluated for opioid receptor affinity against the receptor site model site 5 | 1986 | Journal of medicinal chemistry, Apr, Volume: 29, Issue:4 | N-substituent modulation of opiate agonist/antagonist activity in resolved 3-methyl-3-(m-hydroxyphenyl)piperidines. |
AID147854 | Antagonistic activity in the Opioid receptor kappa 1-mediated [35S]GTP-gamma-S, binding assay against 50 nM U-50,488 | 2003 | Journal of medicinal chemistry, May-22, Volume: 46, Issue:11 | Structure-activity relationships of dynorphin a analogues modified in the address sequence. |
AID1458123 | Agonist activity at recombinant human KOR expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP level at 10 uM preincubated for 15 to 20 mins followed by forskolin addition by GloSensor assay relative to control | 2017 | Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15 | Opioid Receptor Modulators with a Cinnamyl Group. |
AID1465635 | Cmax in Beagle dog at 10 mg/kg, po by LC-MS/MS analysis | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20 | Oral Delivery of Propofol with Methoxymethylphosphonic Acid as the Delivery Vehicle. |
AID601797 | Displacement of [3H]DPDPE from delta opioid receptor in rat brain membranes | 2011 | European journal of medicinal chemistry, Jun, Volume: 46, Issue:6 | Synthesis of 7,9-diazabicyclo[4.2.2]decanes as conformationally restricted κ receptor agonists: fine tuning of the dihedral angle of the ethylenediamine pharmacophore. |
AID1211221 | Ratio of unbound intrinsic glucuronidation clearance in human kidney microsomes in presence of 2% bovine serum albumin to unbound intrinsic glucuronidation clearance in human kidney microsomes in absence of bovine serum albumin | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4 | Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin. |
AID1465653 | Cmax in Beagle dog at 1 mg/kg, iv administered as single bolus dose by LC-MS/MS analysis | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20 | Oral Delivery of Propofol with Methoxymethylphosphonic Acid as the Delivery Vehicle. |
AID114397 | Tested for antagonistic activity using Straub tail test in mice at 20 mg/kg upon subcutaneous administration | 1980 | Journal of medicinal chemistry, Jun, Volume: 23, Issue:6 | 14-(Arylhydroxyamino)codeinones and derivatives as analgetics and antagonists. |
AID610904 | Binding affinity at human mu opioid receptor expressed in CHO-K1 cells at 10 uM | 2011 | Journal of natural products, Jul-22, Volume: 74, Issue:7 | Benzyl derivatives with in vitro binding affinity for human opioid and cannabinoid receptors from the fungus Eurotium repens. |
AID21852 | In vitro clearance in rat in 1000000 cells | 1999 | Journal of medicinal chemistry, Dec-16, Volume: 42, Issue:25 | Combining in vitro and in vivo pharmacokinetic data for prediction of hepatic drug clearance in humans by artificial neural networks and multivariate statistical techniques. |
AID496819 | Antimicrobial activity against Plasmodium falciparum | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
AID1441548 | Displacement of [3H]DPDPE from delta-type opioid receptor in guinea pig brain membranes after 120 mins by solid scintillation counting | 2017 | Journal of medicinal chemistry, 03-23, Volume: 60, Issue:6 | Design and Synthesis of Enantiomerically Pure Decahydroquinoxalines as Potent and Selective κ-Opioid Receptor Agonists with Anti-Inflammatory Activity in Vivo. |
AID425652 | Total body clearance in human | 2009 | Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15 | Physicochemical determinants of human renal clearance. |
AID496831 | Antimicrobial activity against Cryptosporidium parvum | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
AID496825 | Antimicrobial activity against Leishmania mexicana | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
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. |
AID443800 | Selectivity index, ratio of Ki for human delta opioid receptor to human mu opioid receptor | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3 | Synthesis and opioid activity of enantiomeric N-substituted 2,3,4,4a,5,6,7,7a-octahydro-1H-benzofuro[3,2-e]isoquinolines. |
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. |
AID223593 | Tested for the opioid antagonist effect at kappa-opioid receptor in isolated guinea pig ileum at 20 nM | 1993 | Journal of medicinal chemistry, Oct-01, Volume: 36, Issue:20 | 3,4-Dimethyl-4-(3-hydroxyphenyl)piperidines: opioid antagonists with potent anorectant activity. |
AID443799 | Selectivity index, ratio of Ki for human kappa opioid receptor to human mu opioid receptor | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3 | Synthesis and opioid activity of enantiomeric N-substituted 2,3,4,4a,5,6,7,7a-octahydro-1H-benzofuro[3,2-e]isoquinolines. |
AID496829 | Antimicrobial activity against Leishmania infantum | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
AID745766 | Displacement of [3H]-DAMGO from human mu opioid receptor transfected in CHOK1 cells at 10 uM after 60 mins relative to control | 2013 | Journal of natural products, 05-24, Volume: 76, Issue:5 | Neocosmospora sp.-derived resorcylic acid lactones with in vitro binding affinity for human opioid and cannabinoid receptors. |
AID1211255 | Drug metabolism in human intestinal microsomes assessed as UGT1A9-mediated unbound intrinsic glucuronidation clearance at 5 uM after 30 to 60 mins by LC-MS/MS analysis in presence of 2% bovine serum albumin | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4 | Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin. |
AID151900 | Displacement [3H]-naloxone from the Opioid receptor mu 1 isolated from rat brain membrane. | 1989 | Journal of medicinal chemistry, Mar, Volume: 32, Issue:3 | New 4-(heteroanilido)piperidines, structurally related to the pure opioid agonist fentanyl, with agonist and/or antagonist properties. |
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. |
AID224714 | Tested for its antagonist activity against mu receptor using DAMGO as radioligand in isolated guinea pig ileum | 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. |
AID150990 | Inhibition of binding of the non-selective opioid antagonist, [3H]diprenorphine, to cloned human mu opioid receptor | 2003 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 13, Issue:24 | trans-3,4-dimethyl-4-(3-carboxamidophenyl)piperidines: a novel class of micro-selective opioid antagonists. |
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). |
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. |
AID1465632 | Half life in Beagle dog at 10 mg/kg, po by LC-MS/MS analysis | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20 | Oral Delivery of Propofol with Methoxymethylphosphonic Acid as the Delivery Vehicle. |
AID1854007 | Antagonist activity at human MOR expressed in CHO-K1 cells assessed as reduction in fentanyl induced cAMP production incubated for 30 mins by Lance ultra cAMP assay | 2022 | RSC medicinal chemistry, Feb-23, Volume: 13, Issue:2 | Design, synthesis, and biological evaluation of C |
AID151286 | Irreversible occupancy of Opioid receptor mu 1 from rat brain membrane using specific [3H]-sufentanil binding assay, irradiation carried out with monochromatic light (+ hr nu) | 1990 | Journal of medicinal chemistry, Sep, Volume: 33, Issue:9 | Photoactivatable opiate derivatives as irreversible probes of the mu-opioid receptor. |
AID1211197 | Ratio of UGT1A8/2B7-mediated unbound intrinsic glucuronidation clearance in human kidney microsomes to UGT1A8/2B7-mediated unbound intrinsic glucuronidation clearance in human intestinal microsomes at 1 uM | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4 | Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin. |
AID601795 | Displacement of [3H]U69593 from kappa opioid receptor in guinea pig brain membranes after 150 mins by scintillation counting | 2011 | European journal of medicinal chemistry, Jun, Volume: 46, Issue:6 | Synthesis of 7,9-diazabicyclo[4.2.2]decanes as conformationally restricted κ receptor agonists: fine tuning of the dihedral angle of the ethylenediamine pharmacophore. |
AID745762 | Displacement of [3H]-CP55940 from human recombinant CB2 receptor transfected in HEK293 cells at 10 uM after 90 mins relative to control | 2013 | Journal of natural products, 05-24, Volume: 76, Issue:5 | Neocosmospora sp.-derived resorcylic acid lactones with in vitro binding affinity for human opioid and cannabinoid receptors. |
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. |
AID347315 | Inhibition of morphine-induced antinociception in sc dosed Swiss Webster mouse assessed as dose producing 50% antagonism of morphine response preincubated for 5 mins before the addition of morphine assessed after 20 mins by warm water tail immersion test | 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. |
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. |
AID151287 | Irreversible occupancy of Opioid receptor mu 1 from rat brain membrane using specific [3H]sufentanil binding assay in non irradiated experiment (-h nu) | 1990 | Journal of medicinal chemistry, Sep, Volume: 33, Issue:9 | Photoactivatable opiate derivatives as irreversible probes of the mu-opioid receptor. |
AID1211251 | Unbound intrinsic glucuronidation clearance in human kidney microsomes at 1 uM after 30 to 60 mins by LC-MS/MS analysis in presence of UDP-glucuronosyltransferase | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4 | Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin. |
AID1437779 | Analgesic activity in Swiss albino mouse assessed as inhibition of acetic acid-induced abdominal constriction at 80 ug/kg administered for 30 mins followed by acetic acid challenge measured after 30 mins | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Rationally designed benzopyran fused isoxazolidines and derived β |
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). |
AID1137264 | Analgesic activity in sc dosed rat assessed as inhibition of meperidine-induced effect | 1979 | Journal of medicinal chemistry, Oct, Volume: 22, Issue:10 | (2,6-Methano-3-benzazocin-11 beta-yl)alkanones. 1. Alkylalkanones: a new series of N-methyl derivatives with novel opiate activity profiles. |
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. |
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. |
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. |
AID151759 | Inhibition of [3H]DAMGO binding to rat Opioid receptor mu 1 | 2000 | Bioorganic & medicinal chemistry letters, Mar-20, Volume: 10, Issue:6 | Design, synthesis and biological evaluation of 3-amino-3-phenylpropionamide derivatives as novel mu opioid receptor ligands. |
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). |
AID230027 | Ratio of Kt value to that of Kp value of the compound. | 1985 | Journal of medicinal chemistry, Dec, Volume: 28, Issue:12 | Factors affecting binding of trans-N-[2-(methylamino)cyclohexyl]benzamides at the primary morphine receptor. |
AID1197359 | Agonist activity against human recombinant opioid kappa receptor expressed in CHO cell membranes after 3 hrs by [35S]GTP-gamma-S binding assay | 2015 | European journal of medicinal chemistry, Mar-06, Volume: 92 | Probes for narcotic receptor mediated phenomena 49. N-substituted rac-cis-4a-arylalkyl-1,2,3,4,4a,9a-hexahydrobenzofuro[2,3-c]pyridin-6-ols. |
AID601798 | Displacement of [3H]-(+)-pentazocine from sigma 1 receptor in guinea pig brain membranes | 2011 | European journal of medicinal chemistry, Jun, Volume: 46, Issue:6 | Synthesis of 7,9-diazabicyclo[4.2.2]decanes as conformationally restricted κ receptor agonists: fine tuning of the dihedral angle of the ethylenediamine pharmacophore. |
AID1473741 | Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay | 2013 | Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1 | A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. |
AID148153 | Agonist activity towards human Opioid receptor kappa 1 mediated [35S]GTP-gamma-S, binding calculated as maximum stimulation | 2003 | Journal of medicinal chemistry, May-22, Volume: 46, Issue:11 | Structure-activity relationships of dynorphin a analogues modified in the address sequence. |
AID1211223 | Ratio of unbound intrinsic glucuronidation clearance in human intestinal microsomes in presence of 2% bovine serum albumin to unbound intrinsic glucuronidation clearance in human intestinal microsomes in absence of bovine serum albumin | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4 | Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin. |
AID325965 | Ratio of Ki for human cloned mu opioid receptor to Ki for human cloned delta opioid receptor | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6 | Novel trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidines as mu opioid receptor antagonists with improved opioid receptor selectivity profiles. |
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. |
AID141512 | In vivo binding affinity against mu opioid receptor was measured by using labeled ligand [3H]naloxone (0.5 nM) | 1994 | Journal of medicinal chemistry, Sep-16, Volume: 37, Issue:19 | Synthesis and opioid activity of 7-oxygenated 2,3,4,4a,5,6,7,7a-octahydro-1H-benzofuro[3,2-e]isoquinolin-9-ols. |
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. |
AID29359 | Ionization constant (pKa) | 2000 | Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13 | QSAR model for drug human oral bioavailability. |
AID1185659 | Displacement of [3H]-deltorphine from human delta opioid receptor expressed in CHO-K1 cells by scintillation counting analysis | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15 | Synthesis and pharmacological evaluation of 5-pyrrolidinylquinoxalines as a novel class of peripherally restricted κ-opioid receptor agonists. |
AID450513 | Displacement of [3H]DADLE from delta opioid receptor in rat brain measured total binding per mg of protein at 5 uM | 2009 | Bioorganic & medicinal chemistry, Aug-15, Volume: 17, Issue:16 | Synthesis and characterizations of novel quinoline derivatives having mixed ligand activities at the kappa and mu receptors: Potential therapeutic efficacy against morphine dependence. |
AID1820169 | Displacement of [3H]-Diprenorphine from human MOP receptor expressed in HEK293 cells by scintillation counting method | 2021 | Journal of medicinal chemistry, 06-10, Volume: 64, Issue:11 | Identification of an |
AID1146100 | Displacement of [3H]naloxone from opiate receptor (unknown origin) after 10 mins | 1977 | Journal of medicinal chemistry, Aug, Volume: 20, Issue:8 | 3-Hydroxy-17-aralkylmorphinans as potential opiate receptor-site-directed alkylating agents. |
AID1129816 | Antagonist activity at delta opioid receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation at 100 uM after 30 mins in presence of agonist U69593 | 2014 | Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7 | Endomorphin analogues with mixed μ-opioid (MOP) receptor agonism/δ-opioid (DOP) receptor antagonism and lacking β-arrestin2 recruitment activity. |
AID325962 | Displacement of [3H]diprenorphine from human cloned delta opioid receptor | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6 | Novel trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidines as mu opioid receptor antagonists with improved opioid receptor selectivity profiles. |
AID1901075 | Displacement of [3H]-DPDPE from DOR in rat brain membranes measured by competitive radioligand receptor binding assay | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Synthesis of 8-aminomorphans with high KOR affinity. |
AID496818 | Antimicrobial activity against Trypanosoma brucei brucei | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
AID148202 | Negative logarithm of the molar concentration of Opioid receptor mu 1 was determined in guinea pig ileum | 2000 | Bioorganic & medicinal chemistry letters, Dec-18, Volume: 10, Issue:24 | Assessment of substitution in the second pharmacophore of Dmt-Tic analogues. |
AID1465643 | Half life in Beagle dog at 1 mg/kg, iv administered as single bolus dose by LC-MS/MS analysis | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20 | Oral Delivery of Propofol with Methoxymethylphosphonic Acid as the Delivery Vehicle. |
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. |
AID357083 | Antinociceptive effect in intratracheally dosed sickle cell anemic NY1DD transgenic mouse after 10 mins 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. |
AID314197 | Antinociceptive activity in mouse assessed as paw licking latency at 5 ug, icv in presence of endomorphin-2 by hot plate test | 2008 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 18, Issue:4 | Novel highly potent mu-opioid receptor antagonist based on endomorphin-2 structure. |
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. |
AID148250 | Inhibition of [3H]naltrindole binding to human Opioid receptor delta 1 in CHO cells | 2000 | Bioorganic & medicinal chemistry letters, Mar-20, Volume: 10, Issue:6 | Design, synthesis and biological evaluation of 3-amino-3-phenylpropionamide derivatives as novel mu opioid receptor ligands. |
AID151585 | Inhibition against binding of radioligand [N-allyl-2-3-3H]-naloxone to membrane of baby hamster kidney cells infected with forest virus encoding the cDNAs for rat Opioid receptor mu 1 | 2000 | Bioorganic & medicinal chemistry letters, Apr-17, Volume: 10, Issue:8 | ORL1 receptor ligands: structure-activity relationships of 8-cycloalkyl-1-phenyl-1,3,8-triaza-spiro[4.5]decan-4-ones. |
AID1655377 | Displacement of [3H]diprenorphine human delta opioid receptor expressed in CHO cell membranes after 1 hr by micro beta2 scintillation counting method | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5 | Developing Cyclic Opioid Analogues: Fluorescently Labeled Bioconjugates of Biphalin. |
AID1358125 | Displacement of [3H]diprenorphine from human KOR expressed in African green monkey COS1 cell membranes at 1 uM incubated for 1 hr by scintillation counting method | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Synthesis of 7β-hydroxy-8-ketone opioid derivatives with antagonist activity at mu- and delta-opioid receptors. |
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. |
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. |
AID233881 | Selectivity ratio was determined using the Ke value of kappa receptor to that of mu receptor | 1990 | Journal of medicinal chemistry, Apr, Volume: 33, Issue:4 | Synthesis and biological evaluation of 14-alkoxymorphinans. 3. Extensive study on cyprodime-related compounds. |
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. |
AID1536061 | Induction of withdrawal symptoms in morphine-pelleted Swiss Webster mouse model assessed as paw tremors jumps at 1 mg/kg, sc measured after 72 hrs post dose for 20 mins | 2019 | Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2 | Design, Synthesis, and Biological Evaluation of the Third Generation 17-Cyclopropylmethyl-3,14β-dihydroxy-4,5α-epoxy-6β-[(4'-pyridyl)carboxamido]morphinan (NAP) Derivatives as μ/κ Opioid Receptor Dual Selective Ligands. |
AID149036 | Concentration for 50% inhibition of [3H]naloxone (1 M) binding to opioid receptor in rat brain membrane was determined in the absence of NaCl | 1984 | Journal of medicinal chemistry, Dec, Volume: 27, Issue:12 | Synthesis and biological evaluation of 14-alkoxymorphinans. 1. Highly potent opioid agonists in the series of (-)-14-methoxy-N-methylmorphinan-6-ones. |
AID234027 | The sodium index is the ratio of the IC50 value for the inhibition of [3H]naloxone binding to homogenates of rat brain minus cerebellum in presence of 100 mM of NaCl. | 1984 | Journal of medicinal chemistry, May, Volume: 27, Issue:5 | 5-Aryl-3-azabicyclo[3.2.0]heptan-6-one ketals, compounds with morphine-like analgesic activity. |
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. |
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. |
AID165439 | Percentage of respirations per minute after treatment with morphine when compared to control in rabbit | 1989 | Journal of medicinal chemistry, Mar, Volume: 32, Issue:3 | New 4-(heteroanilido)piperidines, structurally related to the pure opioid agonist fentanyl, with agonist and/or antagonist properties. |
AID1211285 | Glucuronidation clearance in human liver microsomes in presence of bovine serum albumin | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4 | Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin. |
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. |
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. |
AID1135643 | Antagonist activity at opioid receptor in electrically stimulated guinea pig ileum assessed as reversal of (-)-normorphine-induced inhibition of contraction at 10 nM | 1978 | Journal of medicinal chemistry, Apr, Volume: 21, Issue:4 | Studies in the (+)-morphinan series. 5. Synthesis and biological properties of (+)-naloxone. |
AID148901 | Tested for irreversible inhibition of [3H]- Naltrexone binding with in the absence of NaCl (washed) | 1984 | Journal of medicinal chemistry, Dec, Volume: 27, Issue:12 | Diastereomeric 6-desoxy-6-spiro-alpha-methylene-gamma-butyrolactone derivatives of naltrexone and oxymorphone. Selective irreversible inhibition of naltrexone binding in an opioid receptor preparation by a conformationally restricted michael acceptor liga |
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. |
AID21851 | In vitro clearance in human in 1000000 cells | 1999 | Journal of medicinal chemistry, Dec-16, Volume: 42, Issue:25 | Combining in vitro and in vivo pharmacokinetic data for prediction of hepatic drug clearance in humans by artificial neural networks and multivariate statistical techniques. |
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. |
AID338154 | Displacement of [3H]DPDPE from delta opioid receptor | 1993 | Journal of natural products, Apr, Volume: 56, Issue:4 | The role of receptor binding in drug discovery. |
AID1820172 | Displacement of [3H]nociceptin from human recombinant NOP receptor expressed in HEK293 cells by scintillation counting analysis | 2021 | Journal of medicinal chemistry, 06-10, Volume: 64, Issue:11 | Identification of an |
AID178158 | Antagonist activity in rat tail flick assay by intraperitoneal administration | 1980 | Journal of medicinal chemistry, Dec, Volume: 23, Issue:12 | Analgesic narcotic antagonists. 4. 7-Methyl-N-(cycloalkylmethyl)-3-hydroxymorphinan-6-ones and -isomorphinan-6-ones. |
AID1473740 | Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 10 mins by membrane vesicle transport assay | 2013 | Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1 | A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. |
AID196435 | Inhibition constant on radiolabeled [125 I] FIDA1 binding to rat striatal membranes | 1993 | Journal of medicinal chemistry, Jan-22, Volume: 36, Issue:2 | Fluorinated and iodinated dopamine agents: D2 imaging agents for PET and SPECT. |
AID1458130 | Antagonist activity at recombinant human MOR expressed in HEK293T cells assessed as reduction in DAMGO-induced inhibition of forskolin-stimulated cAMP level preincubated for 15 to 20 mins followed by DAMGO and forskolin addition by GloSensor assay | 2017 | Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15 | Opioid Receptor Modulators with a Cinnamyl Group. |
AID596551 | Displacement of [3H]DAMGO from human mu-opioid receptor expressed in CHO cells after 60 mins by scintillation counting | 2011 | Bioorganic & medicinal chemistry, May-01, Volume: 19, Issue:9 | Synthesis and binding affinity of novel mono- and bivalent morphinan ligands for κ, μ, and δ 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. |
AID624613 | Specific activity of expressed human recombinant UGT1A10 | 2000 | Annual review of pharmacology and toxicology, , Volume: 40 | Human UDP-glucuronosyltransferases: metabolism, expression, and disease. |
AID325964 | Ratio of Ki for human cloned mu opioid receptor to Ki for human cloned kappa opioid receptor | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6 | Novel trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidines as mu opioid receptor antagonists with improved opioid receptor selectivity profiles. |
AID167702 | Percent change of rate in the respiratory activity was measured in rabbit at the 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. |
AID149233 | Tested for inhibitory activity against (DPDE)delta receptor in mouse vas deferens | 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. |
AID1211228 | Drug metabolism in human liver microsomes assessed as UGT1A8/2B7-mediated unbound intrinsic glucuronidation clearance at 1 uM after 30 to 60 mins by LC-MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4 | Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin. |
AID357098 | Reduction of analgesic activity in NY1DD transgenic mouse pretreated with Met-RANTES 2 hrs before drug administration | 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. |
AID487867 | Displacement of [3H]DAMGO from mu opioid receptor in guinea pig forebrain by beta plate scintillation counting | 2010 | Journal of natural products, Jun-25, Volume: 73, Issue:6 | A bastadin with potent and selective delta-opioid receptor binding affinity from the Australian sponge Ianthella flabelliformis. |
AID1211268 | Ratio of UGT1A8/2B7-mediated unbound intrinsic glucuronidation clearance in human intestinal microsomes to UGT1A8/2B7-mediated unbound intrinsic glucuronidation clearance in human liver microsomes at 1 uM in presence of 2% bovine serum albumin | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4 | Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin. |
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. |
AID1528335 | Inhibition of opioid-withdrawal symptom in morphine-pelleted Swiss Webster mouse assessed as reduction in wet dog shakes at 1 mg/kg, sc observed after 20 mins | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24 | Application of Bivalent Bioisostere Concept on Design and Discovery of Potent Opioid Receptor Modulators. |
AID1901076 | Displacement of [3H]-U69593 from KOR in guinea pig brain membranes measured by competitive radioligand receptor binding assay | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Synthesis of 8-aminomorphans with high KOR affinity. |
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. |
AID357084 | Antinociceptive effect in sc dosed sickle cell anemic NY1DD transgenic mouse after 60 mins 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. |
AID1146262 | Narcotic antagonist activity in morphine-dependent monkey by precipitated withdrawl test | 1977 | Journal of medicinal chemistry, Nov, Volume: 20, Issue:11 | Synthesis and pharmacological activity of some N-alkyl-substituted 9alpha-ethyl-2'-hydroxy-5-methyl-6,7-benzomorphans. |
AID197675 | Compound was evaluated for the binding strength to receptor Mimetic peptide (RMP) at 5 degree celsius, Ki was determined from its potency in displacing [Leu]-enkephalin binding. | 1984 | Journal of medicinal chemistry, Feb, Volume: 27, Issue:2 | Design, synthesis, and binding characteristics of an opiate receptor mimetic peptide. |
AID497005 | Antimicrobial activity against Pneumocystis carinii | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
AID1574663 | Displacement of [3H]U-69,593 from KOR in guinea pig brain membranes after 120 mins by scintillation counting method | 2019 | Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2 | Development of Novel Quinoxaline-Based κ-Opioid Receptor Agonists for the Treatment of Neuroinflammation. |
AID1211239 | Fraction unbound in human kidney microsomes at 1 uM after 30 to 60 mins by LC-MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4 | Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin. |
AID600436 | Antagonist activity at human recombinant mu-type opioid receptor coupled Galphaqi5 chimeric protein expressed in CHO cell membranes assessed as inhibition of dermorphin-stimulated calcium mobilization | 2009 | Bioorganic & medicinal chemistry, Jul-15, Volume: 17, Issue:14 | Structure-activity studies on the nociceptin/orphanin FQ receptor antagonist 1-benzyl-N-{3-[spiroisobenzofuran-1(3H),4'-piperidin-1-yl]propyl} pyrrolidine-2-carboxamide. |
AID1465640 | Oral bioavailability in Beagle dog at 10 mg/kg by LC-MS/MS analysis | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20 | Oral Delivery of Propofol with Methoxymethylphosphonic Acid as the Delivery Vehicle. |
AID114416 | Tested for effective dose required to produce diarrhea in morphine dependent mice after peroral administration | 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. |
AID610902 | Binding affinity at human delta opioid receptor expressed in CHO-K1 cells at 10 uM | 2011 | Journal of natural products, Jul-22, Volume: 74, Issue:7 | Benzyl derivatives with in vitro binding affinity for human opioid and cannabinoid receptors from the fungus Eurotium repens. |
AID1211216 | Unbound intrinsic glucuronidation clearance in human intestinal microsomes at 1 uM after 30 to 60 mins by LC-MS/MS analysis in presence of UDP-glucuronosyltransferase and 2% bovine serum albumin | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4 | Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin. |
AID1221958 | Efflux ratio of permeability from apical to basolateral side over basolateral to apical side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2 | Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model. |
AID443806 | Antagonist activity at human kappa opioid receptor expressed in CHO cells assessed as inhibition of agonist-induced [35S]GTPgammaS binding | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3 | Synthesis and opioid activity of enantiomeric N-substituted 2,3,4,4a,5,6,7,7a-octahydro-1H-benzofuro[3,2-e]isoquinolines. |
AID148459 | Inhibition against binding of radioligand [N-allyl-2-3-3H]-naloxone to membrane of baby hamster kidney cells infected with forest virus encoding the cDNAs for rat Opioid receptor kappa 1 | 2000 | Bioorganic & medicinal chemistry letters, Apr-17, Volume: 10, Issue:8 | ORL1 receptor ligands: structure-activity relationships of 8-cycloalkyl-1-phenyl-1,3,8-triaza-spiro[4.5]decan-4-ones. |
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. |
AID1536326 | Antinociceptive activity in Kunming mouse model of thermal-induced nociception assessed as increase in latency to tail withdrawal at 5 nmol, icv measured up to 60 mins by tail flick test | |||
AID592681 | Apparent permeability across human Caco2 cell membrane after 2 hrs by LC-MS/MS analysis | 2011 | Bioorganic & medicinal chemistry, Apr-15, Volume: 19, Issue:8 | QSAR-based permeability model for drug-like compounds. |
AID381423 | Inhibition of U50488-induced analgesic activity against C57BL/6 mouse assessed as tail withdrawal latency at 10 mg/kg, ip after 2 days | 2007 | The Journal of biological chemistry, Oct-12, Volume: 282, Issue:41 | Long-acting kappa opioid antagonists disrupt receptor signaling and produce noncompetitive effects by activating c-Jun N-terminal kinase. |
AID596649 | Selectivity ratio of Ki for human kappa opioid receptor over Ki for human mu opioid receptor | 2011 | Bioorganic & medicinal chemistry, May-01, Volume: 19, Issue:9 | Synthesis and binding affinity of novel mono- and bivalent morphinan ligands for κ, μ, and δ opioid receptors. |
AID1528337 | Inhibition of opioid-withdrawal symptom in morphine-pelleted Swiss Webster mouse assessed as reduction in paw tremors at 1 mg/kg, sc observed after 20 mins | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24 | Application of Bivalent Bioisostere Concept on Design and Discovery of Potent Opioid Receptor Modulators. |
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. |
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. |
AID1211280 | Fraction unbound in human plasma | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4 | Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin. |
AID1146102 | Displacement of [3H]naloxone from opiate receptor (unknown origin) after 10 mins in presence of NaCl | 1977 | Journal of medicinal chemistry, Aug, Volume: 20, Issue:8 | 3-Hydroxy-17-aralkylmorphinans as potential opiate receptor-site-directed alkylating agents. |
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. |
AID21858 | In vivo clearance in rat | 1999 | Journal of medicinal chemistry, Dec-16, Volume: 42, Issue:25 | Combining in vitro and in vivo pharmacokinetic data for prediction of hepatic drug clearance in humans by artificial neural networks and multivariate statistical techniques. |
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. |
AID152239 | Binding affinity against mu-opiate receptor (human) using [3H]DAMGO radioligand | 2001 | Journal of medicinal chemistry, Oct-11, Volume: 44, Issue:21 | From hit to lead. Combining two complementary methods for focused library design. Application to mu opiate ligands. |
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. |
AID437485 | Binding affinity to mu opioid receptor | 2009 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 19, Issue:23 | Design, synthesis and biological evaluation of a bivalent micro opiate and adenosine A1 receptor antagonist. |
AID600526 | Antagonist activity at human recombinant kappa-type opioid receptor coupled Galphaqi5 chimeric protein expressed in CHO cell membranes assessed as inhibition of dynorphin-stimulated calcium mobilization | 2009 | Bioorganic & medicinal chemistry, Jul-15, Volume: 17, Issue:14 | Structure-activity studies on the nociceptin/orphanin FQ receptor antagonist 1-benzyl-N-{3-[spiroisobenzofuran-1(3H),4'-piperidin-1-yl]propyl} pyrrolidine-2-carboxamide. |
AID233699 | Selectivity ratio is the ratio of the binding affinities against kappa and mu opioid receptors. | 1995 | Journal of medicinal chemistry, Aug-04, Volume: 38, Issue:16 | Synthesis and biological evaluation of 14-alkoxymorphinans. 11. 3-Hydroxycyprodime and analogues: opioid antagonist profile in comparison to cyprodime. |
AID149050 | Inhibition of [3H]naloxone receptor binding to opioid receptor in the presence of 100 mM NaCl | 1986 | Journal of medicinal chemistry, Apr, Volume: 29, Issue:4 | N-substituent modulation of opiate agonist/antagonist activity in resolved 3-methyl-3-(m-hydroxyphenyl)piperidines. |
AID1211190 | Ratio of UGT1A8/2B7-mediated unbound intrinsic glucuronidation clearance in human intestinal microsomes to UGT1A8/2B7-mediated unbound intrinsic glucuronidation clearance in human liver microsomes at 1 uM | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4 | Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin. |
AID107480 | Compound was tested in vivo for narcotic agonist activity (dose in sc, mg/kg) in mice using tail flick assay; I = Inactive at 1,10, 30 mg/kg | 1986 | Journal of medicinal chemistry, Nov, Volume: 29, Issue:11 | Comparison of (-)-eseroline with (+)-eseroline and dihydroseco analogues in antinociceptive assays: confirmation of rubreserine structure by X-ray analysis. |
AID107609 | Compound was tested in vivo for narcotic antagonist activity (dose in sc, mg/kg) in mice using tail flick antagonism assay | 1986 | Journal of medicinal chemistry, Nov, Volume: 29, Issue:11 | Comparison of (-)-eseroline with (+)-eseroline and dihydroseco analogues in antinociceptive assays: confirmation of rubreserine structure by X-ray analysis. |
AID1221957 | Apparent permeability from basolateral to apical side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2 | Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model. |
AID1211283 | Fraction metabolized glucuronidation in human liver microsomes in presence of UDP-glucuronosyltransferase and bovine serum albumin | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4 | Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin. |
AID596650 | Selectivity ratio of Ki for human kappa opioid receptor over Ki for human delta opioid receptor | 2011 | Bioorganic & medicinal chemistry, May-01, Volume: 19, Issue:9 | Synthesis and binding affinity of novel mono- and bivalent morphinan ligands for κ, μ, and δ opioid receptors. |
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. |
AID1536060 | Induction of withdrawal symptoms in morphine-pelleted Swiss Webster mouse model assessed as escape jumps at 1 mg/kg, sc measured after 72 hrs post dose for 20 mins | 2019 | Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2 | Design, Synthesis, and Biological Evaluation of the Third Generation 17-Cyclopropylmethyl-3,14β-dihydroxy-4,5α-epoxy-6β-[(4'-pyridyl)carboxamido]morphinan (NAP) Derivatives as μ/κ Opioid Receptor Dual Selective Ligands. |
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. |
AID1211281 | Ratio of drug level blood to plasma in human | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4 | Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin. |
AID378465 | Displacement of [125I]deltorphin 2 from human recombinant delta opioid receptor expressed in HEK293 cells | 2006 | Journal of natural products, Sep, Volume: 69, Issue:9 | Grandisines C-G, indolizidine alkaloids from the Australian rainforest tree Elaeocarpus grandis. |
AID1211237 | Fraction unbound in human liver microsomes at 1 uM after 30 to 60 mins by LC-MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4 | Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin. |
AID1458125 | Antagonist activity at recombinant human KOR expressed in HEK293T cells assessed as reduction in U50488-induced inhibition of forskolin-stimulated cAMP level at 10 uM preincubated for 15 to 20 mins followed by U50488 and forskolin addition by GloSensor as | 2017 | Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15 | Opioid Receptor Modulators with a Cinnamyl Group. |
AID180325 | Inhibitory effect on the binding of 2 nM [3H]naloxone to rat brain membrane | 1984 | Journal of medicinal chemistry, Jul, Volume: 27, Issue:7 | A photoaffinity reagent to label the opiate receptors of guinea pig ileum and mouse vas deferens. |
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). |
AID1221963 | Transporter substrate index ratio of permeability from apical to basolateral side in human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of P-gp inhibitor LY335979 | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2 | Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model. |
AID1592241 | Antinociceptive activity in C57BL/6 mouse model of thermal-induced nociception at 100 mg/kg, sc measured up to 30 to 180 mins by tail flick test | |||
AID65625 | Tested for binding affinity against dopamine receptor D3 expressed in Sf9 cells. | 1993 | Journal of medicinal chemistry, May-14, Volume: 36, Issue:10 | Synthesis of (R,S)-2'-trans-7-hydroxy-2-[N-n-propyl-N-(3'-iodo-2'- propenyl)-amino]tetralin (trans-7-OH-PIPAT): a new D3 dopamine receptor ligand. |
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. |
AID220524 | Binding affinity towards delta-opioid receptor by displacement of [3H]DADL 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. |
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. |
AID1820167 | Displacement of [125I]-Kp-10 from human Kiss1 receptor by TopCount scintillation counting method | 2021 | Journal of medicinal chemistry, 06-10, Volume: 64, Issue:11 | Identification of an |
AID325960 | Displacement of [3H]diprenorphine from human cloned kappa opioid receptor | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6 | Novel trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidines as mu opioid receptor antagonists with improved opioid receptor selectivity profiles. |
AID1211288 | Drug metabolism in human kidney microsomes assessed as UGT1A8/2B7-mediated unbound intrinsic glucuronidation clearance at 1 uM after 30 to 60 mins by LC-MS/MS analysis in presence of 2% bovine serum albumin | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4 | Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin. |
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. |
AID148812 | Antagonistic activity (Ke) at Opioid receptor delta 1 was determined against DADLE in the mouse vas deferens (MVD) method. | 1990 | Journal of medicinal chemistry, Apr, Volume: 33, Issue:4 | Synthesis and biological evaluation of 14-alkoxymorphinans. 3. Extensive study on cyprodime-related compounds. |
AID1604692 | Displacement of [3H]-diprenorphine from human DOR expressed in CHO cell membranes incubated for 1 hr by scintillation counting method | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5 | Potent, Efficacious, and Stable Cyclic Opioid Peptides with Long Lasting Antinociceptive Effect after Peripheral Administration. |
AID196436 | Inhibition constant on radiolabeled [125 I] FIDA2 binding to rat striatal membranes | 1993 | Journal of medicinal chemistry, Jan-22, Volume: 36, Issue:2 | Fluorinated and iodinated dopamine agents: D2 imaging agents for PET and SPECT. |
AID1185653 | Displacement of [3H]U-69593 from kappa opioid receptor in guinea pig brain membranes after 2 hrs by scintillation counting analysis | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15 | Synthesis and pharmacological evaluation of 5-pyrrolidinylquinoxalines as a novel class of peripherally restricted κ-opioid receptor agonists. |
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AID179385 | Concentration of drug required to inhibit the stereospecific binding of [3H]-naloxone (5 nM) to homogenates of rat brain minus cerebellum in the absence of 100 mM NaCl | 1984 | Journal of medicinal chemistry, May, Volume: 27, Issue:5 | 5-Aryl-3-azabicyclo[3.2.0]heptan-6-one ketals, compounds with morphine-like analgesic activity. |
AID476929 | Human intestinal absorption in po dosed human | 2010 | European journal of medicinal chemistry, Mar, Volume: 45, Issue:3 | Neural computational prediction of oral drug absorption based on CODES 2D descriptors. |
AID1211275 | Ratio of UGT1A8/2B7-mediated unbound intrinsic glucuronidation clearance in human kidney microsomes to UGT1A8/2B7-mediated unbound intrinsic glucuronidation clearance in human intestinal microsomes at 1 uM in presence of 2% bovine serum albumin | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4 | Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin. |
AID1221962 | Efflux ratio of permeability from apical to basolateral side over basolateral to apical side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of P-gp inhibitor LY335979 | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2 | Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model. |
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AID1473739 | Inhibition of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay | 2013 | Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1 | A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. |
AID255309 | Percent inhibition against Opioid receptor at 1 uM | 2005 | Journal of medicinal chemistry, Nov-03, Volume: 48, Issue:22 | 2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization. |
AID149157 | Compound was evaluated for the percent recovery of 1.0 nM of [3H]- DAGO binding to opioid receptor mu in washed guinea pig brain membranes at 1000(nM) concentration | 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. |
AID487865 | Displacement of [3H]DPDPE from delta opioid receptor in guinea pig forebrain by beta plate scintillation counting | 2010 | Journal of natural products, Jun-25, Volume: 73, Issue:6 | A bastadin with potent and selective delta-opioid receptor binding affinity from the Australian sponge Ianthella flabelliformis. |
AID147927 | Compound was evaluated for the percent recovery of 1.0 nM of [3H]- DPDPE binding to Opioid receptor delta 1 in washed guinea pig brain membranes at 1000(nM) concentration | 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. |
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. |
AID21853 | In vivo clearance in dog | 1999 | Journal of medicinal chemistry, Dec-16, Volume: 42, Issue:25 | Combining in vitro and in vivo pharmacokinetic data for prediction of hepatic drug clearance in humans by artificial neural networks and multivariate statistical techniques. |
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. |
AID186973 | Binding of [3H]diprenorphine to rat brain membranes was evaluated and the dissociation constant (KD) was determined. | 1990 | Journal of medicinal chemistry, May, Volume: 33, Issue:5 | N-(3-[18F]fluoropropyl)-N-nordiprenorphine: synthesis and characterization of a new agent for imaging opioid receptors with positron emission tomography. |
AID443797 | Displacement of [125I]OXY from human mu opioid receptor expressed in CHO cells | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3 | Synthesis and opioid activity of enantiomeric N-substituted 2,3,4,4a,5,6,7,7a-octahydro-1H-benzofuro[3,2-e]isoquinolines. |
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). |
AID338153 | Displacement of [3H]DAGO from mu opioid receptor | 1993 | Journal of natural products, Apr, Volume: 56, Issue:4 | The role of receptor binding in drug discovery. |
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). |
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. |
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. |
AID443798 | Displacement of [125I]OXY from human delta opioid receptor expressed in CHO cells | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3 | Synthesis and opioid activity of enantiomeric N-substituted 2,3,4,4a,5,6,7,7a-octahydro-1H-benzofuro[3,2-e]isoquinolines. |
AID138523 | Opioid antagonist activity of compound was measured as inhibiting the binding of normorphine to mouse vas deferens | 1981 | Journal of medicinal chemistry, Feb, Volume: 24, Issue:2 | Some 14 beta-substituted analogues of N-(cyclopropylmethyl)normorphine. |
AID151146 | Binding affinity was evaluated by measuring the ability to displace [3H]-DAMGO radioligand binding from Opioid receptor mu 1 in mouse vas deferens preparation | 1995 | Journal of medicinal chemistry, Aug-04, Volume: 38, Issue:16 | Synthesis and biological evaluation of 14-alkoxymorphinans. 11. 3-Hydroxycyprodime and analogues: opioid antagonist profile in comparison to cyprodime. |
AID1215672 | Drug metabolism in pooled human hepatocytes assessed as aldehyde oxidase-mediated drug metabolism at 10 uM up to 120 mins by HPLC analysis in presence of 50 uM of hydralazine | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7 | Hydralazine as a selective probe inactivator of aldehyde oxidase in human hepatocytes: estimation of the contribution of aldehyde oxidase to metabolic clearance. |
AID1211183 | Ratio of UGT1A8/2B7-mediated unbound intrinsic glucuronidation clearance in human kidney microsomes to UGT1A8/2B7-mediated unbound intrinsic glucuronidation clearance in human liver microsomes at 1 uM | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4 | Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin. |
AID1230324 | Displacement of [3H]DPDPE from delta opioid receptor (unknown origin) transfected into HEK293 cells at 10 uM by microplate scintillation counting | 2015 | Journal of natural products, Jun-26, Volume: 78, Issue:6 | Flavonoids from Perovskia atriplicifolia and Their in Vitro Displacement of the Respective Radioligands for Human Opioid and Cannabinoid Receptors. |
AID286308 | Agonist activity at human opioid kappa receptor expressed in CHO cells assessed as stimulation of [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. |
AID232504 | Selectivity ratio of DADLE and normorphine(NM) in mouse vas deferens | 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. |
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). |
AID325957 | Displacement of [3H]diprenorphine from human cloned mu opioid receptor | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6 | Novel trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidines as mu opioid receptor antagonists with improved opioid receptor selectivity profiles. |
AID450625 | Agonist activity at mouse delta opioid receptor expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding at 10 uM after 90 mins by liquid scintillation counting relative to control | 2009 | Bioorganic & medicinal chemistry, Sep-01, Volume: 17, Issue:17 | Novel delta opioid receptor agonists exhibit differential stimulation of signaling pathways. |
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. |
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. |
AID1055367 | Displacement of radiolabeled DAMGO from human recombinant mu opioid receptor expressed in OPRM1 cells | 2013 | Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22 | Structure-activity relationship of imidazopyridinium analogues as antagonists of neuropeptide s receptor. |
AID152225 | Affinity to mu-receptor, using [3H]DAMGO as radioligand in homogenates of guinea pig brain membranes | 2001 | Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17 | Methylated analogues of methyl (R)-4-(3,4-dichlorophenylacetyl)- 3-(pyrrolidin-1-ylmethyl)piperazine-1-carboxylate (GR-89,696) as highly potent kappa-receptor agonists: stereoselective synthesis, opioid-receptor affinity, receptor selectivity, and functio |
AID125892 | Compound was evaluated for antinociceptive activity in mouse | 2000 | Bioorganic & medicinal chemistry letters, Nov-06, Volume: 10, Issue:21 | N-Cyclohexylethyl-N-noroxymorphindole: a mu-opioid preferring analogue of naltrindole. |
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. |
AID496828 | Antimicrobial activity against Leishmania donovani | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
AID1669028 | Antagonist activity at human delta opioid receptor expressed in CHO cell membranes assessed as reduction in SNC80-induced [35S]GTPgammaS binding preincubated for 5 mins followed by SNC80 addition and measured after 1 hr | |||
AID228143 | Binding affinity towards human kappa,mu,delta receptors was calculated as the ratio; 1/0.34/3.5 | 2003 | Journal of medicinal chemistry, May-22, Volume: 46, Issue:11 | Structure-activity relationships of dynorphin a analogues modified in the address sequence. |
AID357095 | Down-regulation of CCR5 mRNA expression in sickle cell anemic NY1DD transgenic mouse | 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. |
AID624608 | Specific activity of expressed human recombinant UGT1A4 | 2000 | Annual review of pharmacology and toxicology, , Volume: 40 | Human UDP-glucuronosyltransferases: metabolism, expression, and disease. |
AID1465647 | AUC (0 to t) in Beagle dog at 1 mg/kg, iv administered as single bolus dose by LC-MS/MS analysis | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20 | Oral Delivery of Propofol with Methoxymethylphosphonic Acid as the Delivery Vehicle. |
AID226059 | Inhibition of [3H]naloxone binding to rat brain membrane with 100 mM NaCl. | 1983 | Journal of medicinal chemistry, Jan, Volume: 26, Issue:1 | Synthesis and pharmacological studies of 4,4-disubstituted piperidines: a new class of compounds with potent analgesic properties. |
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). |
AID1536059 | Induction of withdrawal symptoms in morphine-pelleted Swiss Webster mouse model assessed as dog shakes at 1 mg/kg, sc measured after 72 hrs post dose for 20 mins | 2019 | Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2 | Design, Synthesis, and Biological Evaluation of the Third Generation 17-Cyclopropylmethyl-3,14β-dihydroxy-4,5α-epoxy-6β-[(4'-pyridyl)carboxamido]morphinan (NAP) Derivatives as μ/κ Opioid Receptor Dual Selective Ligands. |
AID139383 | Number of writhings 10 min after intracerebroventricular administration of 10 microg 3 and ip administration of naloxone (10 min before compound is administered). | 1983 | Journal of medicinal chemistry, Jan, Volume: 26, Issue:1 | New carboxyalkyl inhibitors of brain enkephalinase: synthesis, biological activity, and analgesic properties. |
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. |
AID612052 | Antagonist activity against human recombinant mu opioid receptor expressed in CHO cells assessed as inhibition of [35S]GTP-gamma-S binding after 3 hrs by liquid scintillation counting | 2011 | Bioorganic & medicinal chemistry, Jun-01, Volume: 19, Issue:11 | Probes for narcotic receptor mediated phenomena. Part 42: synthesis and in vitro pharmacological characterization of the N-methyl and N-phenethyl analogues of the racemic ortho-c and para-c oxide-bridged phenylmorphans. |
AID151915 | Inhibition of [3H]naloxone binding to Opioid receptor mu 1 of rat brain membrane | 1985 | Journal of medicinal chemistry, Dec, Volume: 28, Issue:12 | Factors affecting binding of trans-N-[2-(methylamino)cyclohexyl]benzamides at the primary morphine receptor. |
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. |
AID148757 | Compound was evaluated for the percent recovery of 0.5 nM of [3H]- bremazocine binding to total opioid receptor in unwashed guinea pig brain membranes at 1000(nM) concentration of the compound | 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. |
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. |
AID149842 | Tested for its antagonist activity against kappa receptor using U-69,593 as radioligand in isolated guinea pig ileum | 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. |
AID150415 | Ability to displace [3H]naloxone from Opioid receptors in the presence of sodium ion(Na+) | 1980 | Journal of medicinal chemistry, Jun, Volume: 23, Issue:6 | 14-(Arylhydroxyamino)codeinones and derivatives as analgetics and antagonists. |
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. |
AID610906 | Binding affinity at human CB2 receptor expressed in CHO-K1 cells at 10 uM | 2011 | Journal of natural products, Jul-22, Volume: 74, Issue:7 | Benzyl derivatives with in vitro binding affinity for human opioid and cannabinoid receptors from the fungus Eurotium repens. |
AID1146101 | Displacement of [3H]naloxone from opiate receptor (unknown origin) after 2 hrs | 1977 | Journal of medicinal chemistry, Aug, Volume: 20, Issue:8 | 3-Hydroxy-17-aralkylmorphinans as potential opiate receptor-site-directed alkylating agents. |
AID1211261 | Ratio of UGT1A8/2B7-mediated unbound intrinsic glucuronidation clearance in human kidney microsomes to UGT1A8/2B7-mediated unbound intrinsic glucuronidation clearance in human liver microsomes at 1 uM in presence of 2% bovine serum albumin | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4 | Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin. |
AID150253 | Ability (10 ug/kg) to inhibit binding of [125I]iododexetimide to opioid receptor mice | 1989 | Journal of medicinal chemistry, May, Volume: 32, Issue:5 | Synthesis and biological evaluation of [125I]- and [123I]-4-iododexetimide, a potent muscarinic cholinergic receptor antagonist. |
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. |
AID233531 | The ratio between [3H]naloxone binding in the presence and absence of 100 mM NaCl | 1986 | Journal of medicinal chemistry, Apr, Volume: 29, Issue:4 | N-substituent modulation of opiate agonist/antagonist activity in resolved 3-methyl-3-(m-hydroxyphenyl)piperidines. |
AID148251 | Concentration required to inhibit the binding of the non-selective opioid antagonist, [3H]diprenorphine, to cloned human delta opioid receptor | 2003 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 13, Issue:24 | trans-3,4-dimethyl-4-(3-carboxamidophenyl)piperidines: a novel class of micro-selective opioid antagonists. |
AID148900 | Tested for irreversible inhibition of [3H]- Naltrexone binding with in the absence of NaCl (unwashed) | 1984 | Journal of medicinal chemistry, Dec, Volume: 27, Issue:12 | Diastereomeric 6-desoxy-6-spiro-alpha-methylene-gamma-butyrolactone derivatives of naltrexone and oxymorphone. Selective irreversible inhibition of naltrexone binding in an opioid receptor preparation by a conformationally restricted michael acceptor liga |
AID149037 | Concentration for 50% inhibition of [3H]naloxone (1 M) binding to opioid receptor in rat brain membrane was determined in the presence of NaCl | 1984 | Journal of medicinal chemistry, Dec, Volume: 27, Issue:12 | Synthesis and biological evaluation of 14-alkoxymorphinans. 1. Highly potent opioid agonists in the series of (-)-14-methoxy-N-methylmorphinan-6-ones. |
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. |
AID149425 | In vivo binding affinity against kappa opioid receptor was measured by using labeled ligand [3H]ethylketocyclazocine (1 nM) with 500 nM DADLE and 20 nM sufentanil | 1994 | Journal of medicinal chemistry, Sep-16, Volume: 37, Issue:19 | Synthesis and opioid activity of 7-oxygenated 2,3,4,4a,5,6,7,7a-octahydro-1H-benzofuro[3,2-e]isoquinolin-9-ols. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
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. |
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. |
AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | |||
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Timeframe | Studies, This Drug (%) | All Drugs % |
---|---|---|
pre-1990 | 8546 (45.27) | 18.7374 |
1990's | 4162 (22.05) | 18.2507 |
2000's | 2607 (13.81) | 29.6817 |
2010's | 2509 (13.29) | 24.3611 |
2020's | 1055 (5.59) | 2.80 |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.
| This Compound (98.87) All Compounds (24.57) |
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 1,257 (6.24%) | 5.53% |
Reviews | 766 (3.80%) | 6.00% |
Case Studies | 688 (3.42%) | 4.05% |
Observational | 58 (0.29%) | 0.25% |
Other | 17,365 (86.25%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Trial | Phase | Enrollment | Study Type | Start Date | Status | ||
---|---|---|---|---|---|---|---|
The Effect of Universal Pre-hospital Naloxone Education on Patient and Family Safety, Attitudes and Experience in the Surgical Patient: a Prospective Randomized Trial [NCT04868552] | 500 participants (Anticipated) | Interventional | 2021-09-30 | Not yet recruiting | |||
Buprenorphine Loading in the Emergency Department [NCT04283500] | Phase 4 | 15 participants (Actual) | Interventional | 2020-11-01 | Completed | ||
The Safety and Tolerability of Methadone/Naloxone Combination in Opioid Substitution Treatment [NCT01160432] | 0 participants (Actual) | Interventional | 2013-05-31 | Withdrawn | |||
A Phase III Randomized Controlled Trial to Evaluate the Efficacy of Drug Treatment in Prevention of HIV Infection and Death Among Opiate Dependent Injectors [NCT00270257] | Phase 3 | 1,251 participants (Actual) | Interventional | 2008-05-31 | Terminated(stopped due to DSMB halted the study due to futility as a result of lower than anticipated HIV incidence rates) | ||
Clinical Controlled Trial on Extinction of Opioidergic Binge Eating Disorder (BED) With Intranasal Naloxone Administration [NCT01567670] | Phase 2/Phase 3 | 138 participants (Anticipated) | Interventional | 2011-08-31 | Active, not recruiting | ||
Clinical Outcomes From Injectable Nalmefene in the Emergency Department (COINED) [NCT05808881] | Phase 4 | 0 participants (Actual) | Interventional | 2023-06-30 | Withdrawn(stopped due to Due to changes in research objectives and methodological approach.) | ||
A Pilot, Phase 1, Open-Labelled, 4 Period, Randomised, Crossover Study to Evaluate the Pharmacokinetics of Naloxone When Given by the IV, IM and Buccal Routes of Administration in Healthy Male Subjects [NCT02733822] | Phase 1 | 4 participants (Anticipated) | Interventional | 2016-06-30 | Not yet recruiting | ||
Clinical Study to Investigate the Pharmacokinetics of Multiple Repeated Doses of Intranasal Naloxone [NCT04764630] | Phase 1 | 21 participants (Actual) | Interventional | 2021-03-01 | Completed | ||
Randomised, Double-blind, Placebo-controlled, Parallel-group, Multi-centre, Phase III Trial to Investigate the Efficacy, Safety and Tolerability of Naloxone HCl PR Tablets in Patients With Opioid Induced Constipation [NCT03687268] | Phase 3 | 1,500 participants (Anticipated) | Interventional | 2017-07-31 | Recruiting | ||
Naloxone Treatment in Skåne County - Effect on Drug-related Mortality and Overdose-related Complications [NCT03570099] | 2,000 participants (Anticipated) | Observational [Patient Registry] | 2018-06-11 | Active, not recruiting | |||
[NCT01109511] | Phase 4 | 85 participants (Actual) | Interventional | 2010-03-01 | Completed | ||
Overdose Risk Management and Compensation in the Era of Naloxone [NCT03933345] | 600 participants (Anticipated) | Observational | 2019-04-05 | Recruiting | |||
Suboxone and Methadone for HIV Risk Reduction in Subutex Injectors [NCT01131273] | Phase 3 | 68 participants (Actual) | Interventional | 2010-06-30 | Completed | ||
A Study to Assess the Pharmacokinetic Profile of an Investigational Formulation of Buprenorphine HCl/Naloxone HCl 8mg/2mg Capsules Relative to the Pharmacokinetic Profile of Suboxone® (Buprenorphine HCl/Naloxone HCl 8mg/2mg Sublingual Tablets). [NCT01260675] | 12 participants (Actual) | Observational | 2010-12-31 | Completed | |||
An Open Study With OXN to Evaluate the Patient Preference for Pain Treatment With Respect to Quality of Life After WHO Stap I or Step II Analgesics for Patients With Moderate to Severe Non-malignant Pain [NCT01167699] | Phase 3 | 174 participants (Actual) | Interventional | 2009-06-30 | Completed | ||
A Randomized, Double-blind, Double-dummy, Active-drug-controlled, Parallel-group, Multicentre Acceptability and Safety Study of the Transfer From Subutex/Suboxone to RBP-6300 in Opioid-dependent Subjects [NCT01582347] | Phase 2 | 143 participants (Actual) | Interventional | 2012-03-31 | Completed | ||
Can Opioid Induced Effects on Esophageal Motility and Lower Esophageal Sphincter be Counteracted by a Dopamine Receptor Antagonist? [NCT01191645] | Phase 4 | 14 participants (Actual) | Interventional | 2010-10-31 | Completed | ||
An Exploratory, Randomised, Double-blind, Placebo-controlled, Parallel Group, Pilot Study to Assess the Analgesic Efficacy of Oxycodone/Naloxone Prolonged Release Tablets (OXN PR) Compared to Placebo in Opioid-naive Subjects Suffering From Severe Pain Due [NCT01197261] | Phase 2 | 120 participants (Actual) | Interventional | 2010-09-30 | Completed | ||
Phase 1b Randomized, Placebo-controlled Study to Assess the Effect of a Single Dose of ASP8062 on the Multiple Dose Safety, Tolerability and Pharmacokinetics of Buprenorphine/Naloxone in Subjects With Opioid Use Disorder [NCT04447287] | Phase 1 | 23 participants (Actual) | Interventional | 2020-06-29 | Completed | ||
A Double Blind Randomized Vehicle Controlled Crossover Study to Evaluate the Safety and Efficacy of Topical Naloxone Hydrochloride Lotion 0.5% for the Relief of Pruritus in Patients With the MF or SS Forms of Cutaneous T-Cell Lymphoma [NCT02811783] | Phase 3 | 59 participants (Actual) | Interventional | 2017-01-31 | Terminated(stopped due to Sponsor decision) | ||
Bioavailability of Nasal Naloxone and Injected Naloxone Compared. A Randomized, Open Label, 4-way Cross-over Study [NCT02598856] | Phase 1 | 22 participants (Actual) | Interventional | 2016-03-31 | Completed | ||
Time to Detox: A Patient-Centered Comparison of Length of Detoxification Treatment and Time to Naltrexone Maintenance Therapy in Opioid-Dependent Individuals [NCT03678792] | Phase 3 | 0 participants (Actual) | Interventional | 2019-11-15 | Withdrawn(stopped due to Infeasible to conduct at this time.) | ||
Buprenorphine Treatment for Prescription Opioid Dependence [NCT02187198] | Phase 3 | 9 participants (Actual) | Interventional | 2015-03-31 | Completed | ||
A Method to Increase Buprenorphine Treatment Capacity [NCT03580902] | Phase 1/Phase 2 | 51 participants (Actual) | Interventional | 2019-01-22 | 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 | ||
Effects of a Kappa Agonist on Hot Flashes in Menopausal Women [NCT02070718] | Phase 1 | 12 participants (Actual) | Interventional | 2013-01-31 | Completed | ||
Rapid Reversal of CNS-Depressant Drug Effect Prior to Brain Death Determination [NCT03743805] | Early Phase 1 | 0 participants (Actual) | Interventional | 2019-01-01 | Withdrawn(stopped due to Insufficient patients) | ||
The Role of the Opioid System in Placebo Effects on Pain and Social Rejection [NCT04650841] | Early Phase 1 | 60 participants (Anticipated) | Interventional | 2024-09-01 | Not yet recruiting | ||
Addiction, HIV and Tuberculosis in Malaysian Criminal Justice Settings [NCT03089983] | 1,129 participants (Actual) | Interventional | 2017-08-21 | Active, not recruiting | |||
Measures to Improve Outcomes After an Opioid Overdose [NCT03968237] | 200 participants (Anticipated) | Observational | 2019-08-01 | Recruiting | |||
Increasing Patient Knowledge of the Signs of Opioid Overdose and Naloxone in a Suburban Treatment Program [NCT02120612] | 100 participants (Actual) | Observational | 2014-04-30 | Completed | |||
A Comparison of PR Oxycodone/Naloxone and PR Oxycodone After Cardiac Surgery [NCT01374763] | Phase 4 | 165 participants (Actual) | Interventional | 2011-07-31 | Completed | ||
Study of Routs of Naloxone Administration for Opioid Overdosed Patients [NCT01293058] | Phase 2 | 100 participants (Actual) | Interventional | 2007-03-31 | Completed | ||
A Randomized, Double-blind, Placebo-controlled, Multicenter Trial With an Enriched Study Design to Assess the Efficacy and Safety of Oxycodone/Naloxone Controlled-release Tablets (OXN) Compared to Placebo in Opioid-experienced Subjects With Moderate to Se [NCT01358526] | Phase 3 | 1,095 participants (Actual) | Interventional | 2011-05-31 | Completed | ||
Biology and Experience of Eating in Women With Obesity [NCT02805972] | Phase 2 | 41 participants (Actual) | Interventional | 2017-05-20 | Completed | ||
Opioid Use Disorder Treatment Linkage at Sexual Health Clinics Using Buprenorphine [NCT04991974] | Phase 2/Phase 3 | 360 participants (Anticipated) | Interventional | 2021-09-17 | Enrolling by invitation | ||
Effect of Ultra-low Dose Naloxone on Remifentanil-Induced Hyperalgesia [NCT03066739] | Phase 2 | 105 participants (Anticipated) | Interventional | 2023-02-25 | Recruiting | ||
Neural Correlates of Hypoalgesia Driven by Observation [NCT03897998] | Phase 2 | 182 participants (Anticipated) | Interventional | 2021-11-01 | Recruiting | ||
Adolescent Community Reinforcement Approach (A-CRA) Implementation in Combination With Buprenorphine/Naloxone for Young Adults Ages 18 to 25 With Severe Opioid Use Disorder [NCT03287180] | 0 participants (Actual) | Interventional | 2019-01-01 | Withdrawn(stopped due to unable to enroll any participants) | |||
Ultra Small Dose of Intrathecal Naloxone to Minimize Morphine Induced Side- Effects in Patients Undergoing Minor Anal Surgery Under Spinal Anesthesia. A Randomized Double Blind Study [NCT03230474] | 100 participants (Actual) | Interventional | 2016-05-31 | Completed | |||
"GREAT (Good Response With Appropriate Treatment) Factors Influencing the Analgesic Response Over Time of the Oxycodone-Naloxone Association in Painful Cancer Patients" [NCT02293785] | 200 participants (Actual) | Observational | 2014-11-30 | Completed | |||
Randomised, Double-blind, Double-dummy, Cross-over Multicenter Study to Demonstrate Equivalence in Analgesic Efficacy & Bowel Function Taking Oxycodone Equivalents of 120 & 160 mg Per Day as Achieved With the Higher OXN PR Tablet Strengths (OXN60/30 mg PR [NCT02321397] | Phase 2/Phase 3 | 155 participants (Actual) | Interventional | 2014-11-30 | Completed | ||
An Open-label, Single Centre Prospective Cohort Study to Determine the Effectiveness and Safety of Targin® for Pain Management and Opioid-induced Constipation in Patients With Spinal Cord Injury: Can we Improve Pain and Ameliorate Secondary Complications [NCT03179475] | Phase 4 | 1 participants (Actual) | Interventional | 2019-09-05 | Completed | ||
Opioid Antagonism in Individuals Ascertained Through the Partners HealthCare Biobank [NCT04975347] | Phase 1 | 23 participants (Anticipated) | Interventional | 2022-06-03 | Enrolling by invitation | ||
A COMPARATIVE STUDY BETWEEN TWO PHARMACOLOGICAL ASSOCIATIONS OXYCODONE/NALOXONE AND CODEINE / PARACETAMOL IN TREATMENT OF MODERATE-SEVERE CHRONIC PAIN DUE TO OSTEOARTHRITIS OF KNEE AND/OR HIP [NCT02032927] | Phase 4 | 0 participants (Actual) | Interventional | 2013-06-30 | Withdrawn | ||
Feasibility of Pediatric Emergency Department-Initiated Treatment for Adolescents With Opioid Use Disorder [NCT04737603] | Phase 2 | 24 participants (Anticipated) | Interventional | 2024-07-30 | Not yet recruiting | ||
Naloxone Administration Via Auto-injection in Healthy Volunteers [NCT05099614] | Early Phase 1 | 20 participants (Actual) | Interventional | 2021-03-10 | Completed | ||
Pilot Study to Look at Feasibility of Testing and Treatment of Combination Fentanyl and Opioid Dependent Individuals With Different Buprenorphine Induction Methods [NCT04794790] | Early Phase 1 | 30 participants (Anticipated) | Interventional | 2022-05-09 | Recruiting | ||
Opioid Antagonism in Hypogonadotropic Hypogonadism [NCT04975334] | Phase 2 | 23 participants (Anticipated) | Interventional | 2023-12-31 | Enrolling by invitation | ||
Etude Comparative Monocentrique, randomisée, en Cross Over, en Double Aveugle, Contre Placebo, de l'Action de la Morphine et de la Naloxone Dans un modèle Cognitif de Gestion Des Efforts Physiques [NCT02267304] | Phase 2 | 37 participants (Actual) | Interventional | 2013-10-30 | Completed | ||
The Role of Endogenous Opioidergic Systems in Breathing Based Analgesia [NCT03419858] | Early Phase 1 | 60 participants (Actual) | Interventional | 2017-03-13 | Completed | ||
A Randomised, Double-blind, Placebo-controlled, Parallel-group, Multicenter Study to Demonstrate Improvement of Symptoms of RLS in Subjects With Moderate to Severe Idiopathic RLS With Daytime Symptoms Who Take OXN PR Compared to Subjects Taking Placebo (P [NCT01112644] | Phase 3 | 205 participants (Actual) | Interventional | 2010-04-30 | Completed | ||
A Single-Dose, Bioequivalence Study of FMXIN001 4 mg Microspheres Powder and Narcan® 4 mg/0.1 mL Nasal Spray Under Fasting Conditions [NCT04713709] | Phase 1 | 46 participants (Actual) | Interventional | 2021-01-31 | Completed | ||
Houston Emergency Engagement System for Youths and Adolescents [NCT04811014] | Phase 4 | 15 participants (Anticipated) | Interventional | 2021-04-19 | Recruiting | ||
A Multi-national, Prospective Mixed Methods Study of the Effectiveness of Naloxone (Including Intranasal Nyxoid) Administration by Lay People in Reversing Opioid Overdose [NCT05072249] | 6,000 participants (Anticipated) | Observational | 2021-06-08 | Recruiting | |||
An Open Study to Observe OXN Treatment for Patients With Moderate to Severe Non-malignant Pain [NCT01167127] | Phase 3 | 113 participants (Actual) | Interventional | 2009-06-30 | Completed | ||
Subjective Analgesic Effects of Naloxone and Virtual Reality [NCT01105871] | 50 participants (Anticipated) | Interventional | 2010-08-31 | Active, not recruiting | |||
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 | ||
Increasing Naloxone Access for Persons Who Use Opioids: An Online Recruitment and Training Approach to Opioid Overdose Education and Naloxone Distribution [NCT04303000] | Phase 4 | 111 participants (Actual) | Interventional | 2021-07-11 | Completed | ||
Comparison of Buprenorphine vs Buprenorphine/Naloxone on the Effects of Maternal Symptomatology [NCT03740243] | Phase 4 | 0 participants (Actual) | Interventional | 2018-11-30 | Withdrawn(stopped due to No enrollment) | ||
Double-blind, Placebo-controlled Randomised Study on the Efficacy of Naloxone Nasal Spray for the Treatment of Gambling Disorder [NCT03430180] | Phase 2 | 126 participants (Anticipated) | Interventional | 2018-02-22 | Enrolling by invitation | ||
Treatment of Chronic Itch in Patients Under Arsenic Exposure With Sublingual Naloxone: A Single-blind Randomized Trial [NCT03751111] | Phase 1/Phase 2 | 100 participants (Actual) | Interventional | 2019-02-13 | Completed | ||
A PHASE 1 RANDOMIZED, OPEN-LABEL, SINGLE-DOSE, 3-TREATMENT CROSS-OVER STUDY TO EVALUATE RELATIVE BIOAVAILABILITY OF INTRAMUSCULAR INJECTION OF NALOXONE HCL 5 Milligrams (mg) [5mg/0.5 Milliliters (mL] USING A QUICKSHOT™ AUTOINJECTOR COMPARED TO 2 mg NALOXO [NCT05264493] | Phase 1 | 13 participants (Actual) | Interventional | 2020-10-06 | Completed | ||
An Open-Label, Single-Center Study to Evaluate the Exposure-Response Relationship Between the Plasma Drug Concentrations and the Change From Baseline in QTc at Steady State Following Once-daily Administration of CASSIPA® in Opioid Dependent Subjects. [NCT04088266] | Phase 4 | 0 participants (Actual) | Interventional | 2020-01-31 | Withdrawn(stopped due to Study delayed indefinetly) | ||
A Single-Center, Randomized, Open-Label, Single-Dose Study to Evaluate the Pharmacokinetics, Safety, and Tolerability of Depot Buprenorphine (RBP-6000) Using Poly (DL-lactide-co-glycolide) Polymer of Two Different Molecular Weights (Low and High Molecular [NCT02559973] | Phase 1 | 47 participants (Actual) | Interventional | 2015-09-30 | Completed | ||
Evaluation of Transfer From Subutex or Other Treatment for Opioid Drug Dependence to Suboxone: Acceptability, Safety and Impact on Medication Dispensing [NCT00725608] | 339 participants (Actual) | Observational | 2008-05-31 | Completed | |||
Providing A Resource: Telemedicine at Needle Exchanges to Reach Under-served Populations - Greensboro [NCT05108935] | 17 participants (Actual) | Interventional | 2022-02-17 | Completed | |||
A Pilot Study of the Bioavailability of Nasal Naloxone [NCT01939444] | Phase 2 | 5 participants (Actual) | Interventional | 2013-08-31 | Completed | ||
A Prospective, Randomized Trial of Enteral Naloxone Versus a Traditional Bowel Regimen in Prevention of Constipation and Decreased Gastric Motility in Critically Ill Trauma Patients [NCT00799201] | Phase 4 | 3 participants (Actual) | Interventional | 2007-08-31 | Terminated(stopped due to Naloxone became unavailable due to manufacturing shortatges requiring the study to be terminated.) | ||
A Phase-I, Two-Stage, Double-Blind, Placebo-Controlled, Pharmacokinetic and Pharmacodynamic Trial of Low Doses of Intravenous 6β-Naltrexol (AIKO-150) in Opioid-Dependent Subjects. [NCT00829777] | Phase 1 | 8 participants (Anticipated) | Interventional | 2009-03-31 | Completed | ||
Evaluating the Pharmacokinetics and Patient Outcomes of Buprenorphine Microdosing [NCT05307458] | 20 participants (Anticipated) | Observational | 2022-07-01 | Recruiting | |||
Phase Ib/2a Drug-drug Interaction Study of Lemborexant as an Adjunctive Treatment for Buprenorphine/Naloxone for Opioid Use Disorder [NCT04818086] | Phase 1/Phase 2 | 48 participants (Actual) | Interventional | 2021-05-03 | Completed | ||
Effect of High-dose Naloxone Infusion on Pain and Hyperalgesia in Patients Following Groin-Hernia Repair. A Randomized, Placebo-controlled, Double-blind Crossover Study [NCT01992146] | Phase 2 | 16 participants (Anticipated) | Interventional | 2015-11-30 | Recruiting | ||
Pharmacist-Led Interventions to Increase Access to Medications for Opioid Use Disorder [NCT05776823] | 240 participants (Anticipated) | Interventional | 2023-05-05 | Enrolling by invitation | |||
A Prospective, Randomized Trial of the Effect of Standard of Care Reduced Dose Versus Full Dose Buprenorphine/Naloxone in the Perioperative Period on Pain Control and Post Operative Opioid Use Disorder Symptoms [NCT03266445] | Phase 4 | 76 participants (Anticipated) | Interventional | 2018-10-05 | Not yet recruiting | ||
Oral Naloxone for Treatment of Opioid-induced Constipation in Patients Receiving Methadone Maintenance Treatment [NCT02137213] | Phase 2 | 20 participants (Actual) | Interventional | 2014-08-31 | Completed | ||
Bioavailability of a New Formulation of Nasal Naloxone for Prehospital Use [NCT02158117] | Phase 1 | 12 participants (Actual) | Interventional | 2014-03-31 | Completed | ||
The Impact of a Web-Based Naloxone Intervention Under Standing Orders to Patients Prescribed Chronic Opioid Therapy [NCT03337009] | 1,004 participants (Actual) | Interventional | 2017-12-21 | Active, not recruiting | |||
Impact of Direct Outreach to Expand Access to Naloxone in the Context of Standing Orders [NCT03241771] | 325 participants (Actual) | Interventional | 2017-08-14 | Completed | |||
Behavioral Pharmacological Examination of a Novel Buprenorphine Induction Method Among Individuals Who Use Fentanyl [NCT06089707] | Phase 3 | 25 participants (Anticipated) | Interventional | 2024-01-15 | Not yet recruiting | ||
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 Confirmatory, Placebo-controlled, Randomised, Double-blind, Single-dummy, Parallel Group, Ratio-finding Study in Constipated Pain Patients to Establish an Optimal Hydromorphone - Naloxone Ratio With an Improved Bowel Function and a Comparable Analgesic [NCT00992576] | Phase 2/Phase 3 | 600 participants (Anticipated) | Interventional | 2010-01-31 | Completed | ||
A 4-week Multicentre, Randomized, Open Label, Parallel Group, Active Control Phase IV Study to Evaluate Efficacy and Safety of Oxycodone/Naloxone in Comparison With Oxycontin in Korean Patients With Cancer Pain(TOP) [NCT01313780] | Phase 4 | 128 participants (Actual) | Interventional | 2011-05-31 | Completed | ||
A Phase 2 Multi-Center Open-label Study to Assess the Safety and Tolerability of a Buprenorphine/Naloxone Film Strip Administered by the Sublingual and Buccal Routes [NCT00640835] | Phase 2 | 382 participants (Actual) | Interventional | 2008-02-29 | Completed | ||
Comparative Effectiveness of Patient-Centered Strategies to Improve Pain Management and Opioid Safety for Veterans [NCT03026790] | Phase 2 | 820 participants (Actual) | Interventional | 2017-10-19 | Completed | ||
Rapid Initiation of Buprenorphine/Naloxone to Optimize MAT Utilization in Philadelphia [NCT03908437] | Phase 4 | 104 participants (Actual) | Interventional | 2019-07-15 | Completed | ||
Buprenorphine Stabilization and Induction Onto Vivitrol for Heroin-dependent Individuals [NCT03711318] | Phase 3 | 8 participants (Actual) | Interventional | 2018-11-01 | Terminated(stopped due to continuing study was no longer feasible) | ||
A Randomized Controlled Trial Comparing Buprenorphine and Methadone for Opioid Dependent Chronic Pain Patients [NCT00879996] | Phase 4 | 54 participants (Actual) | Interventional | 2009-04-30 | Completed | ||
A Randomized, Double-blind, Cross-over Trial Comparing the Analgesic Potency and Side Effects of Buprenorphine and Ultra-low-dose Naloxone to Buprenorphine Alone [NCT00679458] | 12 participants (Anticipated) | Interventional | 2008-09-30 | Completed | |||
The Effect of the Combined Use of Naloxone and Tramacet on Postoperative Analgesia in Elderly Patients Having Joint Replacement Surgery: a Randomized Controlled Study. [NCT00679614] | Phase 3 | 45 participants (Actual) | Interventional | 2007-12-17 | Completed | ||
Evaluating the Specific Role of Endogenous Opioids as the Mechanism Underlying tAN-based Analgesia in Healthy Individuals [NCT05490134] | Early Phase 1 | 136 participants (Anticipated) | Interventional | 2023-03-22 | Recruiting | ||
A Single-Dose, 1-Period, 1-Treatment Pilot Study of an Investigational Capsule Formulation of 2 mg/.05 mg Buprenorphine/Naloxone Under Fasting Conditions [NCT00880841] | 6 participants (Actual) | Observational | 2009-04-30 | Completed | |||
Randomised, Double-blind, Double-dummy, Parallel-group Multicentre Study to Demonstrate Non-inferiority in Pain & Locomotor Function & Improvement in Symptoms of Constipation in Subjects With Moderate to Severe Pain Due to Osteoarthritis (OA) of the Knee [NCT00902837] | Phase 3 | 181 participants (Actual) | Interventional | 2009-05-31 | Completed | ||
A Randomized Acceptability and Safety Study of the Transfer From Subutex to Suboxone in Opioid- Dependent Subjects [NCT00605033] | Phase 4 | 241 participants (Actual) | Interventional | 2008-03-31 | Completed | ||
A Randomized, Double-Blind, Placebo-Controlled, Dose-Ranging Study To Determine The Efficacy and Safety of Buprenorphine (as NTC-510 and NTC-510A) in Subjects With Pain Following Surgical Extraction of 1 or 2 Third Molars. [NCT02161354] | Phase 2 | 52 participants (Actual) | Interventional | 2014-06-30 | Terminated(stopped due to safety and efficacy after cohort 5 did not warrant further dose escalation) | ||
Study of Efficacy of OXN PR, Compared to Oxy PR, for Reduction of Intensity of Opioid-induced Constipation Symptoms in Pts Treated for Cancer or Non-cancer Pain: A Randomised, Double-blind, Controlled, Multicentre Study [NCT01014559] | Phase 3 | 225 participants (Actual) | Interventional | 2010-02-28 | Terminated(stopped due to Lack of recruitment) | ||
Effect of High-dose Target-controlled Naloxone Infusion on Pain and Hyperalgesia During a Burn Injury. A Randomized, Placebo-controlled, Double-blind Crossover Study [NCT02684669] | Phase 2 | 80 participants (Actual) | Interventional | 2016-02-29 | Completed | ||
Phase 1, Pharmacokinetic Evaluation of Intranasal and Intramuscular Naloxone in Healthy Volunteers [NCT02572089] | Phase 1 | 30 participants (Actual) | Interventional | 2014-10-31 | Completed | ||
Drug Discrimination in Methadone-Maintained Humans Study 2 [NCT00733239] | Phase 1 | 15 participants (Actual) | Interventional | 2008-08-31 | Completed | ||
Reinforcing Effects of Intravenous Buprenorphine Versus Buprenorphine/Naloxone in Buprenorphine-maintained Intravenous Drug Users (P05207) [NCT00710385] | Phase 3 | 19 participants (Actual) | Interventional | 2007-09-30 | Completed | ||
Reversal of Opioid-induced Respiratory Depression With Opioid Antagonists - a Study in Opioid naïve Individuals and Chronic Opioid Users Under Real-life Conditions [NCT05338632] | Phase 1 | 24 participants (Anticipated) | Interventional | 2022-06-24 | Recruiting | ||
Naloxone Block of Low-dose (Analgetic Dose) Ketamine [NCT00921765] | Phase 4 | 3 participants (Actual) | Interventional | 2009-12-31 | Terminated(stopped due to Problems with patient recruitment) | ||
The Impact of Intravenous Heroin Use on Immune Activation in Treated HIV [NCT03976258] | 190 participants (Actual) | Observational | 2017-07-14 | Completed | |||
A Phase I Urodynamic Study of the Opioid Antagonist, Naloxone and Intravenous Methylnaltrexone Reverse Opioid Effects on Bladder Function in Healthy Volunteers [NCT01367561] | Phase 1 | 15 participants (Actual) | Interventional | 2002-10-31 | Completed | ||
Opioid Induced Bowel Dysfunction in Patients Undergoing Spinal Surgery [NCT02573922] | Phase 4 | 180 participants (Actual) | Interventional | 2012-05-31 | Completed | ||
CSP #2014 - Comparative Effectiveness of Two Formulations of Buprenorphine for Treating Opioid Use Disorder in Veterans (VA-BRAVE) [NCT04375033] | Phase 4 | 952 participants (Anticipated) | Interventional | 2020-11-03 | Recruiting | ||
The Effect of Ultra-low-dose Naloxone on Remifentanil-induced Postoperative Hyperalgesia - A Randomized Controlled Study [NCT02856087] | 92 participants (Actual) | Interventional | 2014-11-30 | Completed | |||
Mechanisms of Hypoglycemia Associated Autonomic Failure [NCT00678145] | Phase 2 | 116 participants (Anticipated) | Interventional | 2008-03-31 | Active, not recruiting | ||
Functional Brain Mechanisms Underlying the Anti-suicidal Effects of Buprenorphine in Opioid Use Disorder [NCT04234516] | Phase 4 | 0 participants (Actual) | Interventional | 2020-01-20 | Withdrawn(stopped due to PI leaving the institute) | ||
An Exploratory, Randomised, Double-blind, Single-dummy, Placebo Controlled, Parallel Group Study to Demonstrate the Analgesic Efficacy of Oxycodone/Naloxone Prolonged Release Tablets in Addition to Pregabalin Compared to Pregabalin Alone in Opioid-naïve S [NCT00944697] | Phase 2 | 98 participants (Actual) | Interventional | 2009-07-31 | Completed | ||
Impact of Naloxone on the Analgesic Effect of Paracetamol in Healthy Volunteers [NCT00750048] | Phase 1 | 12 participants (Actual) | Interventional | 2008-09-30 | Completed | ||
A Multicentre, Randomised, Open-label, Active-controlled Trial of the Effectiveness of Buprenorphine/Naloxone in Reducing Intravenous Buprenorphine Misuse in France [NCT00955162] | Phase 4 | 270 participants (Actual) | Interventional | 2009-08-31 | Completed | ||
Assessment of Cannabinoid-opiate Interactions in Humans With a Cannabis Use Disorder and Healthy Subjects [NCT01591629] | Early Phase 1 | 6 participants (Actual) | Interventional | 2011-11-04 | Completed | ||
An Open Multi-center Trial of Suboxone® (Buprenorphine/Naloxone) Treatment Among Opiate-Dependent Subjects [NCT00901875] | Phase 4 | 127 participants (Actual) | Interventional | 2009-03-31 | Completed | ||
Efficacy of Intramuscular Naloxone 0.4mg. in Prophylaxis of Intrathecal [NCT00890942] | 60 participants (Actual) | Interventional | 2009-05-31 | Completed | |||
The Optimal Dose of Prophylactic Naloxone in Ameliorating Opioid Induced Side Effects in Children and Adolescents Receiving Intravenous Patient Controlled Analgesia (IVPCA) Morphine for Moderate to Severe Pain: A Pharmacodynamic, Pharmacokinetic, and Phar [NCT00330343] | Phase 2 | 75 participants (Actual) | Interventional | 2004-05-31 | Completed | ||
Novel Approach for the Prevention of Hypoglycemia Associated Autonomic Failure (HAAF) [NCT03608163] | Phase 4 | 17 participants (Actual) | Interventional | 2018-08-10 | Active, not recruiting | ||
Drug Discrimination in Methadone-Maintained Humans Study 3 [NCT01068847] | Phase 1 | 9 participants (Actual) | Interventional | 2010-02-28 | Completed | ||
Effect of a High-dose Naloxone Infusion on Secondary Hyperalgesia After a First-degree Burn [NCT01935206] | Phase 1 | 15 participants (Actual) | Interventional | 2013-06-30 | Completed | ||
A Phase1, Open-Label, Drug-Drug Interaction Study Between Methadone and Daclatasvir/Asunaprevir/BMS-791325 3 DAA FDC + 75mg BMS-791325 and Between Buprenorphine/Naloxone and Daclatasvir/Asunaprevir/BMS-791325 3 DAA FDC +75mg BMS-791325 [NCT02045693] | Phase 1 | 32 participants (Actual) | Interventional | 2014-02-28 | Completed | ||
A Prospective, Randomized Trial of the Effect of Standard of Care Reduced Dose Versus Full Dose Buprenorphine/Naloxone in the Perioperative Period on Pain Control and Post-Operative Opioid Use Disorder Symptoms [NCT04091009] | Phase 4 | 76 participants (Anticipated) | Interventional | 2020-01-31 | Not yet recruiting | ||
CS1008A Efficacy/Safety Trial of Buprenorphine/Naloxone [NCT00015028] | Phase 2 | 0 participants | Interventional | 1996-11-30 | Completed | ||
Buprenorphine/Nx Treatment of Heroin Dependence-A Compassionate Use Study [NCT00015340] | Phase 4 | 582 participants (Actual) | Interventional | 1999-08-31 | Completed | ||
Developing and Testing the Opioid Rapid Response System [NCT04589676] | 400 participants (Actual) | Interventional | 2020-12-01 | Completed | |||
Intra-nasal Naloxone for Treatment of Impaired Awareness of Hypoglycemia [NCT02700048] | Phase 1/Phase 2 | 11 participants (Actual) | Interventional | 2016-06-30 | Terminated(stopped due to research grant for the trial was not funded) | ||
Explorative, Double-blind Study on Dose Effectiveness of DUROGESIC D-Trans 12 Mcg/h and 25mcg/h Compared to Transtec and Placebo in Acute Pain Models in Healthy Volunteers. [NCT00886002] | Phase 1 | 20 participants (Actual) | Interventional | 2004-11-30 | Completed | ||
Naloxone for the Treatment of Opioid-Induced Pruritus: A Double-Blind, Prospective, Randomized, Controlled Study [NCT01071057] | Phase 2/Phase 3 | 92 participants (Actual) | Interventional | 2010-12-31 | Completed | ||
Nasal Naloxone for Narcotic Overdose [NCT01912573] | Phase 4 | 236 participants (Anticipated) | Interventional | 2013-09-30 | Not yet recruiting | ||
A Randomized, Double-blind, Double-dummy, Parallel-group, Multicenter Study to Demonstrate Improvement in Symptoms of Constipation in Subjects With Moderate to Severe Non-malignant Pain Taking Oxycodone Equivalent of ≥10 mg/Day and ≤50 mg/Day as Oxycodone [NCT01918098] | Phase 3 | 230 participants (Actual) | Interventional | 2013-09-01 | Completed | ||
A Randomsied, Double-blind, Double-dummy, Parallel-group Multicentre Study to Demonstrate Improvement in Symptoms of Constipation in Subjects With Non-malignant Pain Taking Oxycodone Equivalent of 60-80 mg/Day as Oxycodone/Naloxone Prolonged Release Compa [NCT00412100] | Phase 3 | 0 participants | Interventional | 2006-04-30 | Completed | ||
Assessing a Clinically-meaningful Opioid Withdrawal Phenotype [NCT05027919] | Phase 2 | 60 participants (Anticipated) | Interventional | 2022-02-01 | Recruiting | ||
[NCT01971632] | Phase 3 | 463 participants (Actual) | Interventional | 2005-01-31 | Completed | ||
The Efficacy, With Regard to Pain Relief, of Targinact® Treatment for Patients With Severe Pain Compared to Previous Analgesic Treatment; a Non-interventional Study. [NCT01983137] | 1,338 participants (Actual) | Observational | 2011-04-30 | Completed | |||
Hypoglycemia After Exercise in Type 1 Diabetes: Intranasal Naloxone as a Novel Therapy to Preserve Hypoglycemia Counterregulation [NCT03149770] | Phase 2 | 36 participants (Actual) | Interventional | 2017-09-18 | 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 | ||
A Multicenter Safety Trial of Buprenorphine/Naloxone for the Treatment of Opiate Dependence [NCT00007527] | Phase 4 | 600 participants | Interventional | 1999-08-31 | Completed | ||
A Randomised, Double-blind, Parallel Group Multicentre Study to Demonstrate Non-inferiority of the Analgesic Efficacy of Oxycodone/Naloxone 10/5 or 20/10 mg Prolonged Release Tablets (OXN PR) BID Compared to Oxycodone 10 or 20 mg Prolonged Release Tablets [NCT01083485] | Phase 4 | 137 participants (Actual) | Interventional | 2010-03-31 | Completed | ||
Evaluating Specific and Non-Specific Mechanisms in Two Distinct Complementary/Integrative Interventions for Chronic Pain [NCT04744883] | Early Phase 1 | 240 participants (Anticipated) | Interventional | 2020-08-10 | Recruiting | ||
Drug Discrimination in Methadone-Maintained Humans Study 1 [NCT00593463] | Phase 1 | 40 participants (Anticipated) | Interventional | 2006-09-30 | Completed | ||
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 | ||
A Pilot Implementation Project of Methadone and Suboxone® for Injecting Drug Users in Ho Chi Minh City, Vietnam [NCT05368675] | Phase 4 | 448 participants (Actual) | Interventional | 2013-12-18 | Completed | ||
The NAPRESSIM Trial. The Use of Low Dose Prophylactic Naloxone Infusion to Prevent Respiratory Depression With Intrathecal Morphine. [NCT02885948] | Phase 4 | 96 participants (Actual) | Interventional | 2016-04-30 | Completed | ||
A Two-part Open Label Study of the Pharmacodynamic Effects of Intranasal Nalmefene Compared to Intranasal Naloxone in Healthy Volunteers Under Steady State Opioid Agonism [NCT04828005] | Phase 1 | 84 participants (Actual) | Interventional | 2021-03-30 | Completed | ||
Protocol for a Mixed Methods Feasibility Study for the Surviving Opioid Overdose With Naloxone Education and Resuscitation (SOONER) Trial [NCT03821649] | 90 participants (Actual) | Interventional | 2019-01-23 | Completed | |||
A Randomized, Double-blind, Double-dummy, Placebo-controlled, Active-controlled, Parallel-group, Multicenter Trial of Oxycodone/Naloxone Controlled-release Tablets (OXN) to Assess the Analgesic Efficacy (Compared to Placebo) and the Management of Opioid-i [NCT01427270] | Phase 3 | 455 participants (Actual) | Interventional | 2011-08-31 | Completed | ||
A Randomized, Double-blind, Double-dummy, Placebo-controlled, Active-controlled, Parallel-group, Multicenter Trial of Oxycodone/Naloxone Controlled-release Tablets (OXN) to Assess the Analgesic Efficacy (Compared to Placebo) and the Management of Opioid-i [NCT01427283] | Phase 3 | 450 participants (Actual) | Interventional | 2011-08-31 | Completed | ||
The Effect of Chronic Pain on Delay Discounting in Methadone Patients [NCT04473950] | Phase 1 | 29 participants (Actual) | Interventional | 2020-01-08 | Terminated(stopped due to The COVID-19 Pandemic prevented us from meeting target goals.) | ||
Comparing Rapid Micro-Induction and Standard Induction of Buprenorphine/Naloxone for Treatment of Opioid Use Disorder: A Randomized Controlled Trial [NCT04234191] | Phase 2 | 50 participants (Anticipated) | Interventional | 2021-08-18 | Recruiting | ||
A Double-blind, Double-dummy, Parallel Group, Randomised Study to Compare the Efficacy & Tolerability of Oxycodone/Naloxone Prolonged Release (OXN PR) & Codeine/Paracetamol in the Treatment of Moderate to Severe Chronic Low Back Pain or Pain Due to Osteoa [NCT00784810] | Phase 4 | 247 participants (Actual) | Interventional | 2009-02-28 | Completed | ||
Addressing the Opioid Epidemic Through Community Pharmacy Engagement: Randomized Controlled Trial (Aim 2) [NCT04677387] | 47 participants (Actual) | Interventional | 2021-07-01 | Completed | |||
[NCT01851486] | 0 participants (Actual) | Interventional | 2013-01-31 | Withdrawn(stopped due to Labortory focus was changed and study was not opened at all) | |||
Evaluating Microdosing in Emergency Departments: A Randomized Controlled Trial Comparing the Effectiveness of Buprenorphine/Naloxone Microdosing vs. Standard Dosing (EMED Study) [NCT04893525] | Phase 2/Phase 3 | 658 participants (Anticipated) | Interventional | 2021-07-23 | Recruiting | ||
The Role of Endogenous Opioids in Mindfulness-based Chronic Pain Relief [NCT04034004] | Early Phase 1 | 88 participants (Actual) | Interventional | 2021-01-01 | Completed | ||
Buprenorphine/Naloxone Stabilization and Induction Onto Injection Naltrexone: An Outpatient Detoxification for Opioid Dependence. [NCT02294253] | Phase 2/Phase 3 | 30 participants (Actual) | Interventional | 2014-09-30 | Completed | ||
The Effect of Adding Ultra-low Dose of Naloxone to Fentanyl on the Incidence of Pruritis After Spinal Anesthesia for Cesarean Section: Prospective Randomized Double-blind Study ÏÑÇÓÉ [NCT04518618] | 96 participants (Actual) | Interventional | 2020-09-11 | Completed | |||
Randomized Controlled Pilot Trial of Extended-released Buprenorphine vs. Sublingual Buprenorphine-naloxone in Rural Settings [NCT06023459] | Phase 3 | 144 participants (Anticipated) | Interventional | 2024-01-01 | Not yet recruiting | ||
HCV Treatment of IDUs After Buprenorphine Stabilization [NCT00249574] | 10 participants (Anticipated) | Interventional | 2003-06-30 | Completed | |||
Maternal Buprenorphine-naloxone Treatment During the Perinatal Period: Fetal and Infant Effects [NCT03291847] | Phase 2 | 42 participants (Actual) | Interventional | 2018-06-01 | Active, not recruiting | ||
Neuropeptides in Human Reproduction [NCT01952782] | Phase 1 | 128 participants (Anticipated) | Interventional | 2014-04-30 | Recruiting | ||
Withdrawal Suppression Efficacy of Tramadol [NCT00142896] | Phase 2 | 16 participants (Actual) | Interventional | 2005-02-28 | Completed | ||
Characterization of Pain Processing Mechanisms in Irritable Bowel Syndrome [NCT00108446] | Phase 2 | 0 participants | Interventional | 2003-10-31 | Completed | ||
Naltrexone and CBT for Problem-drinking MSM [NCT00444418] | Phase 3 | 200 participants (Actual) | Interventional | 2006-04-30 | Completed | ||
Role of Endorphins in the Perception of Dyspnea in Patients With Chronic Obstructive Pulmonary Disease [NCT00458419] | 17 participants (Actual) | Interventional | 2005-09-30 | Completed | |||
The Acute and Protracted Blockade Efficacy of Buprenorphine/Naloxone [NCT00134888] | 8 participants (Actual) | Interventional | 2000-12-31 | Completed | |||
Optimizing Patient Centered-Care: A Pragmatic Randomized Control Trial Comparing Models of Care in the Management of Prescription Opioid Misuse (OPTIMA Trial) [NCT03033732] | Phase 4 | 272 participants (Actual) | Interventional | 2017-10-02 | Completed | ||
Biobehavioral Studies of Opioid Seeking: Effects of Buprenorphine/Naloxone Dose on Experimental Stress Reactivity and Opioid Abstinence [NCT03015246] | Phase 1/Phase 2 | 26 participants (Actual) | Interventional | 2016-12-31 | 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 | ||
Differences in the Pharmacokinetic and Pharmacodynamic Profile of Ticagrelor and Its Active Metabolite AR-C124900XX Between Patients With Unstable Angina Pectoris Treated With Crushed Ticagrelor and a Combination of Morphine and Naloxone or Morphine Alone [NCT02939248] | Phase 4 | 30 participants (Actual) | Interventional | 2016-10-31 | Completed | ||
Opioid Induced Acute Preconditioning [NCT00184938] | 40 participants (Anticipated) | Interventional | 2005-01-31 | Suspended | |||
A Randomized Controlled Trial Testing Buprenorphine as a Treatment in Opiate Dependent Pain Patients [NCT00552578] | Phase 4 | 12 participants (Actual) | Interventional | 2007-10-31 | Terminated(stopped due to "Tapering doses protocol arm was not effective for treatment retention outcome.") | ||
A Randomised, Double-blind, Active-controlled, Double-dummy, Parallel Group Study to Determine the Safety and Efficacy of Oxycodone/Naloxone Prolonged Release Tablets in Subjects With Moderate to Severe, Chronic Cancer Pain [NCT00513656] | Phase 2 | 230 participants (Anticipated) | Interventional | 2007-09-30 | Completed | ||
A Multicenter, Randomized, Double-Blind, Placebo-controlled, Phase IIB Study of Oral Naloxone for the Treatment of Opioid-Induced Constipation in Patients With Chronic, Non-malignant Pain or Malignant Pain [NCT00020605] | Phase 3 | 0 participants | Interventional | 2000-05-31 | Active, not recruiting | ||
Buprenorphine/Naloxone Versus Clonidine For Out-patient Opiate Detoxification [NCT00032968] | Phase 3 | 341 participants | Interventional | 2001-01-31 | Completed | ||
CS1008 A&B Eff/Safety Trial of BUP/NX for the Treatment of Opiate Dependence [NCT00015171] | Phase 3 | 0 participants | Interventional | 1996-04-30 | Completed | ||
PK0496 Pharmacokinetics of Buprenorphine [NCT00015288] | Phase 1 | 0 participants | Interventional | 1996-11-30 | Completed | ||
A Tailored, Peer-delivered Intervention to Reduce Recurring Opioid Overdoses [NCT02922959] | 80 participants (Actual) | Interventional | 2017-02-07 | Completed | |||
Bup/Nx - Facilitated Rehab for Opioid Dependent Adolescents [NCT00078130] | Phase 3 | 223 participants | Interventional | 2003-07-31 | Completed | ||
Buprenorphine/Naloxone Versus Clonidine for Inpatient Opiate Detoxification [NCT00032955] | Phase 3 | 163 participants | Interventional | 2001-02-28 | Completed | ||
Opioid Induced Bowel Dysfunction in Patients Undergoing Cesarean Section [NCT02571881] | Phase 4 | 57 participants (Actual) | Interventional | 2012-10-31 | Active, not recruiting | ||
Single Dose, Crossover, Pharmacokinetic Evaluation of a New Naloxone Nasal Swab, Naloxone Nasal Spray, and Intramuscular Naloxone Injection in Healthy Volunteers [NCT05363501] | Phase 1 | 76 participants (Actual) | Interventional | 2021-01-21 | Completed | ||
Abuse Potential of Parenteral Buprenorphine/Naloxone in Non-Dependent Opioid Abusers [NCT00134875] | 9 participants (Actual) | Interventional | 2000-12-31 | Terminated | |||
Abuse Potential of Buprenorphine/Naloxone as a Function of Maintenance Dose of Buprenorphine/Naloxone [NCT00149539] | Phase 2 | 12 participants (Actual) | Interventional | 2004-06-30 | Terminated(stopped due to Funding ended for the study) | ||
Effects of Buprenorphine/Naloxone in Non-Dependent Opioid Abusers [NCT00158236] | 7 participants | Interventional | 1997-01-31 | Completed | |||
Starting Treatment With Agonist Replacement Therapies (START) [NCT00315341] | Phase 4 | 1,269 participants (Actual) | Interventional | 2006-04-30 | Completed | ||
Pilot for Improved Office Based Treatment of Opioid-Dependence [NCT03586466] | 80 participants (Anticipated) | Interventional | 2018-12-01 | Recruiting | |||
A Placebo Controlled, Double-blind, Randomized, Multicenter Study to Evaluate the Efficacy and Safety of Naloxone HCl IV in Patients With Stroke [NCT05301712] | Phase 4 | 446 participants (Actual) | Interventional | 2018-08-07 | Completed | ||
Pharmacokinetics and Pharmacodynamics of a New Formulation of Nasal Naloxone for Prehospital Use [NCT02307721] | Phase 1/Phase 2 | 12 participants (Actual) | Interventional | 2014-12-31 | Completed | ||
A Multi-center, Open-Label, 24-Week, Follow-Up Study to Assess Safety, Efficacy, and Treatment Adherence For Maintenance Treatment of Opioid Dependence With OX219 [NCT01903005] | Phase 4 | 668 participants (Actual) | Interventional | 2013-07-31 | Completed | ||
Post-marketing Surveillance Study (Paper-AWB) for GPs and Clinics: Treatment of Opioid-dependent Patients With SUBOXONE® 2 mg / 8 mg Sublingual Tablets - Acceptability and Safety Data From a Real Life Scenario. [NCT00723749] | 384 participants (Actual) | Observational | 2008-03-31 | Completed | |||
A Phase 1, Open-Label, Single-Sequence Study to Examine the Effect of Telaprevir on the Pharmacokinetics of Buprenorphine in Subjects on Stable Buprenorphine/Naloxone Maintenance Therapy [NCT01275599] | Phase 1 | 16 participants (Anticipated) | Interventional | 2011-01-31 | Completed | ||
A Phase 1, Open Label, Randomized Study to Investigate the Pharmacokinetics and Safety of Multiple Doses of Intranasal Naloxone in Healthy Adult Participants [NCT05377255] | Phase 1 | 24 participants (Actual) | Interventional | 2022-03-28 | Completed | ||
Novel Induction to Buprenorphine/Naloxone: A Quasi-Experimental Study With Comparison Group [NCT05644587] | Phase 4 | 170 participants (Anticipated) | Interventional | 2023-02-06 | Enrolling by invitation | ||
Pilot Study of a Multi-System Analysis of Opioid Receptor Binding [NCT05528848] | Phase 1 | 60 participants (Anticipated) | Interventional | 2022-09-20 | Recruiting | ||
A Randomized, Blinded, Active-controlled Non-inferiority Study of the Efficacy and Safety of OX219 for the Induction of Treatment of Opioid Dependence [NCT01848054] | Phase 3 | 313 participants (Actual) | Interventional | 2013-06-30 | Completed | ||
Buprenorphine for Probationers and Parolees: Bridging the Gap Into Treatment [NCT03616236] | Phase 3 | 320 participants (Anticipated) | Interventional | 2019-03-01 | Active, not recruiting | ||
SPNS - An Evaluation of Innovative Methods for Integrating Buprenorphine Opioid Abuse Treatment in HIV Primary Care [NCT00227357] | 101 participants (Actual) | Observational | 2005-07-31 | Completed | |||
Influence Of Low Dose Intrathecal Naloxone On Bupivacaine - Fentanyl Spinal Anaesthesia For Lower Limb Orthopedic Surgery In Elderly Patients [NCT04673812] | 92 participants (Actual) | Interventional | 2020-12-10 | Completed | |||
The Impact of Concomitant Ultra Low Dose Infusion Naloxone and Therapeutic Infusion Opioid on Opioid Requirements in Pediatric ICU Patients [NCT00286052] | Phase 3 | 128 participants | Interventional | 2002-12-31 | Completed | ||
Improving Equitable Access to Naloxone to Prevent Opioid Overdose Deaths Within Syringe Service Programs [NCT05886712] | 32 participants (Anticipated) | Interventional | 2023-07-01 | Recruiting | |||
Buprenorphine Maintenance vs. Detoxification in Prescription Opioid Dependence [NCT00555425] | Phase 4 | 113 participants (Actual) | Interventional | 2008-07-31 | Completed | ||
A Phase I Single Dose, Open Label, Randomized, Three Period Crossover Pilot Study to Compare the Pharmacokinetics, Safety and Tolerability of MVP005 Intranasal Spray With Intranasal Administration of Naloxone Solution for Injection in Healthy Adult Subjec [NCT01622504] | Phase 1 | 6 participants (Anticipated) | Interventional | 2012-06-30 | Not yet recruiting | ||
HIV, Buprenorphine, and the Criminal Justice System [NCT01550341] | 50 participants (Actual) | Interventional | 2012-02-23 | Completed | |||
The Evaluation of Targinact® in Daily Practice, With Regards to Pain Relief and Constipation, in Chronic Severe Pain Patients Compared to Previous Prolonged Release Oxycodone Treatment: a Non-interventional, Observational Study. [NCT01710904] | 68 participants (Actual) | Observational | 2012-09-30 | Completed | |||
Evaluation of BEMA® Buprenorphine NX for Buprenorphine Induction of Opioid Dependent Subjects [NCT01713803] | Phase 3 | 0 participants (Actual) | Interventional | Withdrawn(stopped due to FDA did not require a clinical trial for indication.) | |||
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 | ||
Efficacy of Naloxone in Reducing Postictal Central Respiratory Dysfunction in Patients With Epilepsy [NCT02332447] | Phase 3 | 485 participants (Actual) | Interventional | 2015-01-31 | Completed | ||
Prospective, Randomized Clinical Pilot Study: Oral Opiate Targin In Treatment Of Postoperative Pain After Major Cardiac Surgery [NCT01816581] | Phase 4 | 50 participants (Actual) | Interventional | 2011-07-31 | Completed | ||
Induction of Opioid-Dependent Individuals Onto Buprenorphine and Buprenorphine/Naloxone [NCT00637000] | Phase 2 | 38 participants (Actual) | Interventional | 2008-03-31 | Completed | ||
A Randomized Pilot Study of Long Acting Buprenorphine Injection Compared to Sublingual Buprenorphine/Naloxone Films [NCT03744663] | Phase 2 | 0 participants (Actual) | Interventional | 2022-06-30 | Withdrawn(stopped due to Funding for uninsured subjects could not be realized and staffing after COVID hit was also a problem.) | ||
Evaluation of the Effectiveness, Safety, and Tolerability of Tapentadol PR Versus Oxycodone/Naloxone PR in Non-opioid Pre-treated Subjects With Uncontrolled Severe Chronic Low Back Pain With a Neuropathic Pain Component. [NCT01838616] | Phase 4 | 367 participants (Actual) | Interventional | 2013-04-30 | Completed | ||
A Multicenter, Phase IV, Interventional Study to Assess the Efficacy and Safety of TARGIN(R) (Oxycodone/Naloxone) in Korean Patients With Spinal Disorders [NCT01811238] | Phase 4 | 240 participants (Actual) | Interventional | 2012-09-30 | Completed | ||
CTN-0051: Extended-Release Naltrexone vs. Buprenorphine for Opioid Treatment [NCT02032433] | Phase 4 | 570 participants (Actual) | Interventional | 2014-01-29 | Completed | ||
Prescription Opioid Abuse Among Pain Patients: Predictors of Relapse [NCT01967641] | Phase 2 | 51 participants (Actual) | Interventional | 2005-11-30 | Completed | ||
Buprenorphine Tx:A Safe Alternative for Opioid Dependent Pain Patients [NCT01841931] | 4 participants (Actual) | Interventional | 2013-02-28 | Terminated(stopped due to Principal Investigator is no longer at this site) | |||
An Evaluation of a Social Network Intervention for Primary and Secondary Prevention of Opioid Overdoses [NCT04212364] | 300 participants (Anticipated) | Interventional | 2019-03-15 | Recruiting | |||
A Randomised, Double-blind, Double-dummy, Parallel-group Multicenter Study to Demonstrate Improvement in Symptoms of Constipation and Non-inferiority in Analgesic Efficacy in Subjects With Non-malignant or Malignant Pain That Require Around-the-clock Opio [NCT01438567] | Phase 3 | 270 participants (Actual) | Interventional | 2011-09-30 | Completed | ||
[NCT01439100] | Phase 3 | 172 participants (Anticipated) | Interventional | 2011-10-31 | Completed | ||
A Phase 1, Open-Label, Randomized, Crossover, Comparative Bioavailability Study of Naloxone Nasal Spray and Naloxone Hydrochloride Intravenous and Intramuscular Injection in Healthy Volunteers [NCT03827642] | Phase 1 | 24 participants (Actual) | Interventional | 2018-04-23 | Completed | ||
Medications Development for Drug Abuse Disorders [NCT01188421] | Phase 1/Phase 2 | 106 participants (Actual) | Interventional | 2010-10-31 | Completed | ||
Effect of Kappa Opioid Agonist-Antagonists in the Heat/Capsaicin Sensitization Model [NCT00947284] | 3 participants (Actual) | Interventional | 2010-01-31 | Terminated(stopped due to Experimental pain model didn't work as anticipated.) | |||
Buprenorphine Combination Tablet Feasibility [NCT00000298] | Phase 2 | 0 participants | Interventional | 1995-08-31 | Completed | ||
Does Duloxetine Reduce Chronic Pain After Total Knee Arthroplasty? [NCT02307305] | Phase 2 | 168 participants (Anticipated) | Interventional | 2014-08-31 | Recruiting | ||
The Effect of Naloxone and Mehtylnaltrexone on Esophageal Sensitivity in Healthy Volunteers: a Randomized, Double-blind, Placebo-controlled Study [NCT03014843] | 12 participants (Actual) | Interventional | 2013-10-31 | Completed | |||
Evaluation of Preference for a Buprenorphine-based Maintenance Therapy, After a Switch From Buprenorphine Alone (Subutex®) to the Buprenorphine/Naloxone Combination (Suboxone®), in Opioid-dependent Patients With Buprenorphine Maintenance Therapy [NCT00684073] | Phase 4 | 60 participants (Actual) | Interventional | 2007-07-31 | Completed | ||
A Usability Assessment of Intramuscular, Atomized Intranasal, and Nasal Spray Administration of Naloxone by Untrained Community Members [NCT04025671] | 208 participants (Actual) | Interventional | 2017-08-23 | Completed | |||
Neural Mechanisms of Immersive Virtual Reality in Chronic Pain [NCT04851301] | Phase 1/Phase 2 | 259 participants (Anticipated) | Interventional | 2021-11-01 | Recruiting | ||
A Phase 1, Open-Label, Randomized, Crossover, Comparative Bioavailability Study of Naloxone Nasal Spray and Naloxone Hydrochloride Intramuscular Injection in Healthy Volunteers [NCT03827629] | Phase 1 | 24 participants (Actual) | Interventional | 2017-08-07 | Completed | ||
Comparison of Naloxone Pharmacokinetics Using Marketed Naloxone Devices [NCT03386591] | Phase 1 | 30 participants (Actual) | Interventional | 2018-01-03 | Completed | ||
The Use of Oral Naloxone to Prevent Post Spinal Fusion Ileus [NCT03176316] | Phase 4 | 150 participants (Anticipated) | Interventional | 2018-01-02 | Recruiting | ||
Pharmacokinetics of Buprenorphine and Naloxone in Subjects With Mild to Severe Hepatic Impairment (Child-Pugh Classes, A, B, and C), in HCV-Seropositive Subjects, and in Healthy Volunteers [NCT01846455] | Phase 4 | 43 participants (Actual) | Interventional | 2012-09-30 | 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 | ||
A Pilot Study Comparing a Low-dose Versus a High-dose Sublingual Buprenorphine Induction Dosing Scheme in Fentanyl Using Patients With Opioid Use Disorder (OUD) [NCT05944952] | Phase 4 | 40 participants (Anticipated) | Interventional | 2023-10-01 | Not yet recruiting | ||
The Role of Endorphins in the Perception of Dyspnea With Resistive Loading in Patients With COPD [NCT00958919] | 14 participants (Actual) | Interventional | 2009-08-31 | Completed | |||
Effects of Extended Release Methylnaltrexone Bromide (150 mg b.i.d.) in Comparison to Extended Release Naloxone Hydrochloride (20 mg b.i.d.) on Loperamide-induced Delay of the Oro-cecal, Whole-gut and Colon Transit Time in Healthy Subjects. [NCT01596764] | Phase 1 | 16 participants (Actual) | Interventional | 2011-05-31 | Completed | ||
Pilot Study: Treatment of Gambling Disorder With Fast Acting Opiate Antagonist, Naloxone Nasal Spray [NCT03223896] | Phase 2 | 20 participants (Actual) | Interventional | 2017-02-14 | Completed | ||
Buprenorphine Physician-Pharmacist Collaboration in the Management of Patients With Opioid Use Disorder: Clinical Trials Network 0075 [NCT03248947] | Early Phase 1 | 71 participants (Actual) | Interventional | 2018-03-28 | Completed | ||
Buprenorphine Pharmacology Related to Addiction Treatment [NCT00000236] | Phase 2 | 0 participants | Interventional | Completed | |||
Modeling Kappa Opioid Analgesic Mechanisms in Chronic Orofacial Pain Disorders [NCT00716807] | 46 participants (Actual) | Interventional | 2008-01-31 | Terminated(stopped due to Unable to recruit a sufficient number of subjects.) | |||
Efficacy/Safety Trial of Buprenorphine/Nx for Opiate Dependence [NCT00000353] | Phase 2 | 0 participants | Interventional | 1996-10-31 | Completed | ||
A Phase 2, Randomized, Double-Blind, Placebo-Controlled Study to Assess the Safety and Efficacy of ASP8062 as an Add-on Therapy to Buprenorphine/Naloxone in Participants With Opioid Use Disorder [NCT05062577] | Phase 2 | 0 participants (Actual) | Interventional | 2021-11-08 | Withdrawn(stopped due to Due to corporate strategic considerations) | ||
Sensory and Opioid Mechanisms of Affective Touch [NCT03096353] | Early Phase 1 | 29 participants (Actual) | Interventional | 2017-08-01 | Completed | ||
The Ability of Vaped Marijuana to Reduce the Severity of Naloxone-Precipitated Withdrawal [NCT05114460] | Phase 2 | 32 participants (Anticipated) | Interventional | 2021-11-01 | Suspended(stopped due to The U.S. Department of Health and Human Services Office of Human Research Protections issued an FWA restriction on NYSPI research that included a pause of human subjects research as of June 23, 2023.) | ||
Efficacy of Buprenorphine and XR-Naltrexone Combination for Relapse Prevention in Opioid Use Disorder [NCT05011266] | Phase 2/Phase 3 | 180 participants (Anticipated) | Interventional | 2022-08-01 | Recruiting | ||
A Multicentre, Randomised, Double-Blind, Placebo-Controlled, Multiple Ascending Dose Study Evaluating the Safety, Tolerability and Efficacy of Naloxone SR Capsules in Subjects With Constipation Due to Opioids, Taken for Persistent Non-Cancer Pain [NCT00984334] | Phase 2 | 40 participants (Actual) | Interventional | 2009-10-31 | Completed | ||
Mechanism of Analgesic Effect on Prolonged Continuous Theta Burst Stimulation [NCT05360030] | 45 participants (Actual) | Interventional | 2022-05-14 | Completed | |||
Randomized Placebo-controlled Trial of Intravenous Naloxone to Improve Oxygenation in Hypoxemic Lung-Eligible Brain-Dead Organ Donors [NCT02581111] | Phase 2/Phase 3 | 199 participants (Actual) | Interventional | 2015-09-30 | Completed | ||
A Pivotal, Phase 1, Open-Label, Randomized, Crossover, Single-Dose, Comparative Bioavailability Study of Buprenorphine-Naloxone Sublingual Spray and Suboxone® Sublingual Film in Healthy Volunteers [NCT02477267] | Phase 1 | 47 participants (Actual) | Interventional | 2015-06-30 | Completed | ||
Trial of Buprenorphine/Naloxone for Treatment of Opiate Dependence [NCT00000344] | Phase 2 | 40 participants | Interventional | Completed | |||
Anti Emetic Efficacy of Combination of Ramosetron and Premixture of Naloxone With Patient-controlled Analgesia After Gynecologic Surgery [NCT02416115] | 90 participants (Actual) | Interventional | 2014-07-31 | Completed | |||
Surviving Opioid Overdose With Naloxone Education and Resuscitation Trial (SOONER): Randomized Trial and Embedded Qualitative Study to Compare the Effectiveness of point-of Care Overdose Education and Naloxone Distribution Versus Referral to an Existing C [NCT04740099] | 0 participants (Actual) | Interventional | 2021-12-31 | Withdrawn(stopped due to The study never started due to COVID-19.) | |||
5HT3 Antagonists to Treat Opioid Withdrawal and to Prevent the Progression of Physical Dependence [NCT01549652] | 133 participants (Actual) | Interventional | 2011-04-30 | Completed | |||
Comparison of Two Naloxone Infusion Rates on the Postoperative Recovery of Patients Undergoing Spine Fusion Surgery [NCT01531439] | 84 participants (Actual) | Interventional | 2011-11-30 | Completed | |||
Health Promotion and Public Safety: Community-based Collaborative Services to Addicted Offenders [NCT01843751] | Phase 3 | 24 participants (Actual) | Interventional | 2013-03-31 | Completed | ||
Buprenorphine vs. Opioid Dose Escalation Among Patients With Chronic Pain [NCT01875848] | Phase 4 | 7 participants (Actual) | Interventional | 2013-12-31 | Terminated(stopped due to Data safety monitoring board recommended due to low recruitment yield.) | ||
An Interventional Study to Compare the Efficacy and Tolerability of Current and Slow Titration With Targin® in the Treatment of Moderate to Severe Non-malignant Chronic Pain (GLORY) [NCT01811186] | Phase 4 | 261 participants (Actual) | Interventional | 2012-12-31 | Completed | ||
Evaluation of a Community-based Education, Navigation, and Support (CENS) Intervention to Reduce Opioid-related Harms Among Military Veterans [NCT05343169] | 300 participants (Anticipated) | Interventional | 2022-10-21 | Recruiting | |||
NTNU Intranasal Naloxone Trial - a Double Blinded, Double Dummy, Randomized Controlled Trial of Intranasal Naloxone for Pre-hospital Use [NCT03518021] | Phase 3 | 286 participants (Actual) | Interventional | 2018-05-15 | Completed | ||
Randomized Trial of Buprenorphine Microdose Initiation for Ambulatory Settings [NCT05450718] | Phase 4 | 70 participants (Anticipated) | Interventional | 2024-01-31 | Not yet recruiting | ||
Reduced Opioid Analgesic Requirements Via Improved Endogenous Opioid Function [NCT02469077] | 117 participants (Actual) | Interventional | 2015-08-31 | Completed | |||
A Randomized Blinded Pilot Study to Compare Targinact vs. Oxycodone in Early Return of Gastrointestinal Function After Colorectal Surgery [NCT02109640] | Phase 3 | 50 participants (Actual) | Interventional | 2014-10-31 | Completed | ||
An Open-Label, One-Period Study in Patients Receiving Methadone or Buprenorphine/Naloxone Maintenance Therapy to Evaluate the Effect of SCH 503034 (Boceprevir) on Either Methadone or Buprenorphine/Naloxone Plasma Concentrations (Protocol No. P08123) [NCT01396005] | Phase 1 | 21 participants (Actual) | Interventional | 2011-09-30 | Completed | ||
A Pharmacokinetic/Pharmacodynamic (PK/PD) Evaluation of Naloxone Following Intradermal Injection in Humans [NCT05876572] | Phase 4 | 3 participants (Anticipated) | Interventional | 2024-01-31 | Not yet recruiting | ||
A 4-week, Open Label, Multi-center, Prospective, Single-arm, Non-interventional Phase IV Study to Evaluate the Efficacy of Targin for the Treatment of Korean Patients With Cancer Pain Under Conditions of Daily Practice [NCT01719757] | Phase 4 | 359 participants (Actual) | Interventional | 2012-07-31 | Completed | ||
A Multicenter, Phase IV, Interventional Study to Assess the Efficacy and Safety of Oxycodone/Naloxone in Korean Patients With Chemotherapy-Induced Peripheral Neuropathy Who Need Opioid Combination Treatment With Existing Pregabalin Treatment [NCT01675531] | Phase 4 | 73 participants (Actual) | Interventional | 2012-12-31 | Completed | ||
A Phase I Double-Blind, Placebo-Controlled Randomized Study to Assess Repeated Doses of INDV-2000 (C4X_3256) up to 28 Days in Healthy Volunteers, and an Open-Label Study of INDV-2000 up to 11 Days in Treatment Seeking Individuals With Opioid Use Disorder [NCT04976855] | Phase 1 | 64 participants (Actual) | Interventional | 2022-08-17 | Completed | ||
A Randomized Controlled Trial Comparing Buprenorphine and Methadone for Treatment in Opioid Dependent Chronic Back Pain Patients [NCT01559454] | Phase 4 | 19 participants (Actual) | Interventional | 2012-02-29 | Completed | ||
A Phase III, Randomized, Double-blind, Double-dummy, Parallel Group Study to Determine the Safety and Efficacy of Oxy/Nal Prolonged Release Tablets Compared to Oxy PR in Subjects With Moderate to Severe, Chronic Cancer Pain [NCT01885182] | Phase 3 | 232 participants (Actual) | Interventional | 2013-06-01 | Completed | ||
Cocaine Use Reduction With Buprenorphine (CURB) [NCT01402492] | Phase 2/Phase 3 | 302 participants (Actual) | Interventional | 2011-09-30 | Completed | ||
Effect of Ultra-low Dose Naloxone During Supraclavicular Brachial Plexus Block on the Anti-nociceptive Criteria of Post-operative Opioid in Orthopedic Upper Limb Surgeries [NCT03372486] | 64 participants (Actual) | Interventional | 2017-12-18 | 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 | ||
Naloxone Auto-injector as a Universal Precaution for Patients With Opioid Substance Use Disorder [NCT02669901] | 402 participants (Actual) | Interventional | 2016-04-04 | Completed | |||
Justice Community Opioid Innovation Network (JCOIN): Reducing Opioid Mortality in Illinois [NCT04925427] | 1,500 participants (Anticipated) | Interventional | 2021-08-10 | Recruiting | |||
Topical Naloxone Hydrochloride as a Diagnostic Tool for Ocular Neuropathic Pain [NCT04454281] | Phase 1 | 1 participants (Actual) | Interventional | 2020-10-01 | Completed | ||
Assess the Efficacy of Buprenorphine/Naloxone Micro-Dosing for Postoperative Pain Management in Opioid-Tolerant Patients [NCT04771689] | Phase 4 | 60 participants (Anticipated) | Interventional | 2022-07-01 | Not yet recruiting | ||
Interim Buprenorphine Treatment to Bridge Waitlist Delays: Stage II Evaluation [NCT03420313] | Phase 2 | 100 participants (Anticipated) | Interventional | 2018-03-01 | Recruiting | ||
Buprenorphine to Improve HIV Care Engagement and Outcomes: A Randomized Trial (BRAVO) [NCT01936857] | Phase 4 | 281 participants (Actual) | Interventional | 2015-07-31 | Completed | ||
Effect of High-dose Target-controlled Naloxone Infusion on Pain and Hyperal-gesia in Patients Following Recovery From Impacted Mandibular Third Molar Extraction. A Randomized, Placebo-controlled, Double-blind Crossover Study. [NCT02976337] | Phase 2 | 14 participants (Anticipated) | Interventional | 2017-10-12 | Recruiting | ||
A Multiple-Dose Study of Blockade of Subjective Opioid Effects, Plasma Levels, and Safety of Subcutaneous Injections of Depot Buprenorphine (RBP-6000) in Subjects With Opioid Use Disorder [NCT02044094] | Phase 2 | 39 participants (Actual) | Interventional | 2013-11-30 | Completed | ||
A Single Center, Randomized, 2 Way Cross-Over, Phase 4 Study Comparing Usability of Zubsolv Sublingual Tablets 5.7/1.4 to Suboxone Sublingual Film 8/2 Including Ease of Use, Taste Preference, Dissolution Time, Desire to Abuse, and Overall Acceptance In Bu [NCT02038790] | Phase 4 | 33 participants (Actual) | Interventional | 2013-11-30 | Completed | ||
Does Postoperative Administration of Oral Oxycodone With/Without Naloxone, Reduce the Duration of Epidural Analgesia in Patients Undergoing Cystectomy Without Impairing Its Benefits? A Randomized, Double Blind Controlled Trial [NCT02516059] | Phase 4 | 90 participants (Actual) | Interventional | 2015-09-14 | Completed | ||
Stress and Opioid Misuse Risk: The Role of Endogenous Opioid and Endocannabinoid Mechanisms [NCT05142267] | 120 participants (Anticipated) | Interventional | 2022-03-02 | Recruiting | |||
Pharmacodynamics and Arteriovenous Differences of Naloxone in Healthy Participants Exposed to an Opioid [NCT02405988] | 12 participants (Actual) | Interventional | 2015-04-30 | Completed | |||
[information is prepared from clinicaltrials.gov, extracted Sep-2024] |