Cocaine: An alkaloid ester extracted from the leaves of plants including coca. It is a local anesthetic and vasoconstrictor and is clinically used for that purpose, particularly in the eye, ear, nose, and throat. It also has powerful central nervous system effects similar to the amphetamines and is a drug of abuse. Cocaine, like amphetamines, acts by multiple mechanisms on brain catecholaminergic neurons; the mechanism of its reinforcing effects is thought to involve inhibition of dopamine uptake. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
cocaine : A tropane alkaloid obtained from leaves of the South American shrub Erythroxylon coca. [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]
| Flora | Rank | Flora Definition | Family | Family Definition |
|---|---|---|---|---|
| Cola | genus | A plant genus of the family STERCULIACEAE. This is the source of the kola nut which contains CAFFEINE and is used in popular beverages.[MeSH] | Malvaceae | The mallow family of the order MALVALES, subclass Dilleniidae, class Magnoliopsida. The common names of hollyhock and mallow are used for several genera of Malvaceae.[MeSH] |
| ID Source | ID |
|---|---|
| PubMed CID | 2826 |
| CHEMBL ID | 32363 |
| SCHEMBL ID | 21931 |
| SCHEMBL ID | 23086019 |
| MeSH ID | M0004670 |
| PubMed CID | 446220 |
| CHEMBL ID | 370805 |
| CHEBI ID | 27958 |
| SCHEMBL ID | 21930 |
| MeSH ID | M0004670 |
| Synonym |
|---|
| AC-16037 |
| allococaine |
| methyl 3-(benzoyloxy)-8-methyl-8-azabicyclo[3.2.1]octane-2-carboxylate |
| KBIO1_000975 |
| DIVK1C_000975 |
| IDI1_000975 |
| (+)-cocaine |
| 8-azabicyclo(3.2.1)octane-2-carboxylic acid, 3-(benzoyloxy)-8-methyl-, methyl ester, (1r-(exo,exo))- |
| NCGC00159467-02 |
| NINDS_000975 |
| MLS002320697 |
| smr001338843 |
| (-)-cocaine base |
| L000836 |
| NCGC00159467-03 |
| CHEMBL32363 |
| bdbm86207 |
| cas_50-36-2 |
| nsc_446220 |
| HMS2272A05 |
| SCHEMBL21931 |
| 21206-60-0 |
| pseudococaine - |
| ZPUCINDJVBIVPJ-UHFFFAOYSA-N |
| methyl 3-(benzoyloxy)-8-methyl-8-azabicyclo[3.2.1]octane-2-carboxylate # |
| AKOS025401423 |
| cocainzusatze |
| methyl 8-methyl-3-[(phenylcarbonyl)oxy]-8-azabicyclo[3.2.1]octane-2-carboxylate |
| STL565195 |
| SCHEMBL23086019 |
| 8-azabicyclo[3.2.1]octane-2-carboxylicacid,3-(benzoyloxy)-8-methyl-,methyl ester,(1r,2r,3s,5s)-rel- |
| neurocaine |
| cocainum |
| methyl [1r-(exo,exo)]-3-(benzoyloxy)-8-methyl-8-azabicyclo[3.2.1]octane-2-carboxylate |
| 2-methyl-3beta-hydroxy-1alphah,5alphah-tropane-2beta-carboxylate benzoate (ester) |
| (1r,2r,3s,5s)-2-(methoxycarbonyl)tropan-3-yl benzoate |
| CHEBI:27958 , |
| methyl (1r,2r,3s,5s)-3-(benzoyloxy)-8-methyl-8-azabicyclo[3.2.1]octane-2-carboxylate |
| [1r-(exo,exo)]-3-(benzoyloxy)-8-methyl-8-azabicyclo[3.2.1]octane-2-carboxylic acid, methyl ester |
| gtpl2286 |
| methyl (1r,2r,3s,5s)-8-methyl-3-[(phenylcarbonyl)oxy]-8-azabicyclo[3.2.1]octane-2-carboxylate |
| bdbm22418 |
| cocaine (-) |
| COC , |
| methyl benzoylecgonine |
| (-)-cocaine |
| badrock |
| g-rock |
| (1r,2r,3s,5s)-2-methoxycarbonyltropan-3-yl benzoate |
| goofball |
| snow (birds) |
| coca |
| ecgonine, methyl ester, benzoate (ester) |
| lady |
| foo foo |
| girl |
| sleighride |
| toot |
| toke |
| 3beta-hydroxy-2beta-tropanecarboxylic acid methyl ester benzoate (ester) |
| happy dust |
| white girl or lady |
| moonrocks |
| yeyo |
| star-spangled powder |
| flake |
| hell |
| cocain |
| eritroxilina |
| 1-alpha-h,5-alpha-h-tropane-2-beta-carboxylic acid, 3-beta-hydroxy-, methyl ester, benzoate |
| florida snow |
| cocaine, l- |
| green gold |
| snort |
| methyl 3-beta-hydroxy-1-alpha-h,5-alpha-h-tropane-2-beta-carboxylate benzoate (ester) |
| blow |
| jam |
| cholly |
| 2-beta-tropanecarboxylic acid, 3-beta-hydroxy-, methyl ester, benzoate (ester) |
| 1-cocaine |
| dama blanca |
| caviar |
| burese |
| bouncing powder |
| kokan |
| kibbles n' bits |
| happy powder |
| 3-tropanylbenzoate-2-carboxylic acid methyl ester |
| happy trails |
| gold dust |
| l-cocaine |
| c carrie |
| erytroxylin |
| bernice |
| blast |
| blizzard |
| cocktail |
| cola |
| 1-alpha-h,5-alpha-h-tropane-2-beta-carboxylic acid, 3-beta-hydroxy-, methyl ester, benzoate (ester) (8ci) |
| star dust |
| 3beta-hydroxy-1alphah,5alphah-tropane-2beta-carboxylic acid methyl ester benzoate |
| 8-azabicyclo[3.2.1]octane-2-carboxylic acid, 3-(benzoyloxy)-8-methyl-, methyl ester, (1r,2r,3s,5s)- (9ci) |
| pimp's drug |
| kokayeen |
| 2-beta-carbomethoxy-3-beta-benzoxytropane |
| sweet stuff |
| leaf |
| kokain |
| charlie |
| cecil |
| cocaine free base |
| candy |
| chicken scratch |
| benzoylmethylecgonine |
| coke |
| trails |
| methyl 3beta-hydroxy-1alphah,5alphah-tropane-2beta-carboxylate benzoate (ester) |
| cocaina |
| prime time |
| heaven |
| freeze |
| bazooka |
| 3-(benzoyloxy)-8-methyl-8-azabicyclo-(3.2.1)octane-2-carboxylic acid methyl ether |
| corine |
| bernies |
| cabello |
| hsdb 6469 |
| beta-cocain |
| cocaine |
| C01416 |
| l-cocain |
| 1Q72 |
| DB00907 |
| 1I7Z |
| dea no. 9041 |
| 2beta-carbomethoxy-3beta-benzoxytropane |
| snow |
| einecs 200-032-7 |
| nose candy |
| ecgonine methyl ester benzoate (ester) |
| crack cocaine |
| (r)-(-)-cocaine |
| CHEMBL370805 |
| ids-nc-004 |
| rx-0041 |
| rx0041 |
| AKOS015965554 |
| cecil [street name] |
| i5y540lhvr , |
| crack |
| bernice [street name] |
| unii-i5y540lhvr |
| gold dust [street name] |
| girl [street name] |
| toot [street name] |
| flake [street name] |
| cholly [street name] |
| lady [street name] |
| rock [street name] |
| green gold [street name] |
| happy dust [street name] |
| star dust [street name] |
| cocaine [usp:ban] |
| blow [street name] |
| happy trails [street name] |
| ecgonine methyl ester benzoate |
| [1r-(exo,exo)]-3-(benzoyloxy)-8-methyl-8-azabicyclo[3.2.1]octane-2-carboxylic acid |
| cocaine [mart.] |
| cocaine [vandf] |
| cocaine [usp monograph] |
| cocaine [mi] |
| cocaine [hsdb] |
| 3.beta.-hydroxy-2.beta.-tropanecarboxylic acid methyl ester benzoate (ester) |
| methyl 3b-hydroxy-1.alpha.h,5.alpha.h-tropane-2.beta.-carboxylate benzoate (ester) |
| methyl (1r,2r,3s,5s)-3-(benzoyloxy)-8-methyl-8-azabicyclo(3.2.1) octane-2-carboxylate |
| cocainum [hpus] |
| cocaine [who-dd] |
| EPITOPE ID:158626 |
| SCHEMBL21930 |
| beta-cocaine |
| DTXSID2038443 , |
| cocaine 1.0 mg/ml in acetonitrile |
| cocaine 0.1 mg/ml in acetonitrile |
| ZPUCINDJVBIVPJ-LJISPDSOSA-N |
| Q41576 |
| star dust (street name) |
| dtxcid501030562 |
| cocaine (usp:ban) |
| toot (street name) |
| methyl (1r-(exo,exo))-3-(benzoyloxy)-8-methyl-8-azabicyclo(3.2.1)octane-2-carboxylate |
| lady (street name) |
| methyl 3b-hydroxy-1alphah,5alphah-tropane-2beta-carboxylate benzoate (ester) |
| bernice (street name) |
| (1r-(exo,exo))-3-(benzoyloxy)-8-methyl-8-azabicyclo(3.2.1)octane-2-carboxylic acid, methyl ester |
| methyl (1r,2r,3s,5s)-3-(benzoyloxy)-8-methyl-8-azabicyclo(3.2.1)octane-2-carboxylate |
| happy trails (street name) |
| cocaine (mart.) |
| rock (street name) |
| cecil (street name) |
| happy dust (street name) |
| cholly (street name) |
| green gold (street name) |
| flake (street name) |
| gold dust (street name) |
| cocaine (usp monograph) |
| girl (street name) |
| blow (street name) |
| cocaine, 1mg/ml in acetonitrile |
Cocaine use during pregnancy has become increasingly recognized. There also has been increased concern about the toxic and teratogenic properties of cocaine on the fetus. These observations confirm that the drug metabolites generated after CocH gene transfer therapy are safe.
| Excerpt | Reference | Relevance |
|---|---|---|
| " These data suggest that monoamines are involved in mediating the motor activity of cocaine but not implicated in the toxic effect of the drug." | ( [Attempt at modification of the pharmacological and toxic effects of cocaine]. Lallemant, AM, 1979) | 0.26 |
| "Comparative experiments were performed on female rats given pregnenolone-16 alpha-carbonitrile (PCN), spironolactone, triamcinolone, estradiol or diethylstilbestrol to study correlations between the toxic effect of cocaine, its blood clearance and its urinary excretion." | ( Effect of steroids and diethylstilbestrol on cocaine toxicity, plasma concentrations and urinary excretion. Kourounakis, P; Rapp, U; Selye, H, 1979) | 0.26 |
| " The 20 mg dose of cocaine dissolved in 2 ml of saline without adrenaline was found to be safe and produced adequate nasal decongestion in the absence of other predominant factors." | ( Topical cocaine and general anaesthesia: an investigation of the efficacy and side effects of cocaine on the nasal mucosae. Anderton, JM; Nassar, WY, 1975) | 0.25 |
| " Based on this study, Caramel Colour II was not toxic in F344 rats treated for 13 wk." | ( Subchronic toxicity study of Caramel Colour II in F344 rats. Carter, JL; Chappel, CI; Emerson, JL; MacKenzie, KM; Petsel, SR; Stanley, J, 1992) | 0.28 |
| " The toxic effects of ethanol and cocaine were not reduced by the ingestion of vitamin E during short-term exposure of 21 days of treatment." | ( Chronic ethanol and cocaine-induced hepatotoxicity: effects of vitamin E supplementation. Eskelson, CD; Pirozhkov, SV; Watson, RR, 1992) | 0.28 |
| "A putative role for endogenous excitatory amino acid systems in the mediation of the cardiovascular and toxic responses to acute administration of cocaine, was examined in spontaneously hypertensive and normal Wistar-Kyoto rats." | ( Antagonism of the toxicity of cocaine by MK-801: differential effects in spontaneously hypertensive and Wistar-Kyoto rats. Acuff, CG; Ho, IK; Hoskins, B; Rockhold, RW; Surrett, RS; Zhang, T, 1992) | 0.28 |
| "As cocaine use during pregnancy has become increasingly recognized, there also has been increased concern about the toxic and teratogenic properties of cocaine on the fetus." | ( Cocaine and development: mechanisms of fetal toxicity and neonatal consequences of prenatal cocaine exposure. Gingras, JL; Hume, RF; O'Donnell, KJ; Weese-Mayer, DE, 1992) | 0.28 |
| "Local anaesthetics are responsible for 5 to 10% of all reported adverse reactions to anaesthetic drugs." | ( Adverse effects of local anaesthetics. McCaughey, W, ) | 0.13 |
| " In addition, when these drugs are used concomitantly such as in polydrug abuse, it has been suggested that they may cause synergistic adverse effects on the myocardium." | ( A primary culture system of postnatal rat heart cells for the study of cocaine and methamphetamine toxicity. Welder, AA, 1992) | 0.28 |
| " Thirty minutes later, rats were anesthetized with 40 mg/kg of sodium pentobarbital intraperitoneally and were then given 10 mg/kg (least toxic dose) cocaine intravenously." | ( Inhibition of pseudocholinesterase activity protects from cocaine-induced cardiorespiratory toxicity in rats. Berman, ML; Kambam, JR; Naukam, R, 1992) | 0.28 |
| " On the basis of these studies, Caramel Colour IV was not toxic or carcinogenic in F344 rats or B6C3F1 mice." | ( Toxicity and carcinogenicity studies of Caramel Colour IV in F344 rats and B6C3F1 mice. Boysen, BG; Chappel, CI; Emerson, JL; Field, WE; MacKenzie, KM; Petsel, SR; Stanley, J, 1992) | 0.28 |
| "Chronically instrumented, conscious, unrestrained rats subjected to an LD50 dose (1." | ( Pharmacologic interventions after an LD50 cocaine insult in a chronically instrumented rat model: are beta-blockers contraindicated? Garner, D; Niemann, JT; Smith, M, 1991) | 0.28 |
| "In this conscious animal model subjected to an LD50 IV cocaine insult, chlorpromazine and diazepam, previously shown to be of value in other animal models, had no effect on survival." | ( Pharmacologic interventions after an LD50 cocaine insult in a chronically instrumented rat model: are beta-blockers contraindicated? Garner, D; Niemann, JT; Smith, M, 1991) | 0.28 |
| "61 mg/kg while the LD50 of cocaine in buprenorphine (0." | ( Antagonism of acute cocaine toxicity by buprenorphine. Bansinath, M; Goldfrank, LR; Shukla, VK; Turndorf, H, 1991) | 0.28 |
| " In the present study, significant genetic differences were found in cocaine-induced lethality, with a two-fold difference in LD50 values seen between the most sensitive (NBR) and least sensitive (LEW) strains." | ( Cocaine toxicity: genetic differences in cocaine-induced lethality in rats. George, FR, 1991) | 0.28 |
| " Conversely, no significant differences in cocaine LD50 values were found, being 100." | ( Cocaine toxicity: genetic evidence suggests different mechanisms for cocaine-induced seizures and lethality. George, FR, 1991) | 0.28 |
| "The toxic effects of cocaine are enhanced in the presence of lidocaine." | ( Lidocaine potentiation of cocaine toxicity. Albertson, TE; Derlet, RW; Tharratt, RS, 1991) | 0.28 |
| " This paper reviews epidemiological research on the extent of use as well as reports of adverse effects." | ( Crack cocaine use: a review of prevalence and adverse effects. Smart, RG, 1991) | 0.28 |
| " The theorized toxic metabolite of cocaine is thought to be generated by a multistep pathway mediated primarily by cytochrome P-450." | ( Potentiation of cocaine-mediated hepatotoxicity by acute and chronic ethanol. Boyer, CS; Petersen, DR, 1990) | 0.28 |
| " These data offer insight into future approaches for the treatment of patients with the acute toxic effects of cocaine." | ( Anticonvulsant modification of cocaine-induced toxicity in the rat. Albertson, TE; Derlet, RW, 1990) | 0.28 |
| " These data suggest that the enzyme, or enzymes, responsible for the production of the toxic metabolite are absent, or at very low levels, in female and immature male mice, and that they are either inducible by androgens or are repressed by estrogens or progestins." | ( Developmental expression of cocaine hepatotoxicity in the mouse. Smolen, A; Smolen, TN, 1990) | 0.28 |
| " The serum cocaine values and the incidence of toxic effects of cocaine were compared between the 2 groups." | ( Cocaine and adrenaline: a safe or necessary combination in the nose? A study to determine the effect of adrenaline on the absorption and adverse side effects of cocaine. Brockbank, M; Pfleiderer, AG, 1988) | 0.27 |
| " This effect does not appear to result from an inhibition of the toxic metabolite(s) of cocaine, as a 10-fold molar excess of yohimbine failed to antagonize lipid peroxidation caused by in vitro incubation of cocaine with hepatic microsomes." | ( Antagonism of cocaine-induced hepatotoxicity by the alpha adrenergic antagonists phentolamine and yohimbine. Harbison, RD; James, RC; Roberts, SM; Schiefer, MA, 1987) | 0.27 |
| " The comprehensive toxic screen, which provides multiple modalities of drug analysis, will be a key diagnostic tool in the further investigation of these inherently toxic agents and their impact on syndromes of cocaine intoxication." | ( Clinical toxicity of cocaine adulterants. Shannon, M, 1988) | 0.27 |
| " Children reported that candy was safe to eat, even in large amounts." | ( Perception of toxicity and dose by 3- and 4-year-old children. Garrettson, LK; Osborne, SC, 1985) | 0.27 |
| "" REsults showed a high incidence and wide range of adverse consequences including: impairment of job functioning, interpersonal relationships, and financial status; disturbances of mood and cognitive functioning; psychiatric symptoms of depression, paranoia, and increased suicidal/violent tendencies; and physical symptoms of exhaustion, weight loss, sleep problems, and seizures." | ( Adverse effects of cocaine abuse. Tatarsky, A; Washton, AM, 1984) | 0.27 |
| " The symptoms include mydriasis, seizures, acute toxic psychosis, and coma in various combinations." | ( The "body packer syndrome"-toxicity following ingestion of illicit drugs packaged for transportation. Mittlemann, RE; Wetli, CV, 1981) | 0.26 |
| " The present study was undertaken to determine whether nitric oxide synthase inhibitors block the development of sensitization to the toxic effects of cocaine in mice." | ( Blockade of sensitization to the toxic effects of cocaine in mice by nitric oxide synthase inhibitors. Itzhak, Y, 1994) | 0.29 |
| " The animals pretreated with lidocaine were compared with the control animals for the number of adverse effects from cocaine at each dose tested." | ( The effects of lidocaine pretreatment on cocaine neurotoxicity and lethality in mice. Goldfrank, LR; Heit, J; Hoffman, RS, ) | 0.13 |
| " The results showed that: a) the extracts were mutagenic only to strain TA98 (without and after metabolic activation); b) there was a similar efficiency of applied solvents in extraction of mutagenic substances detectable with TA98, and c) the toluene extracts were most toxic towards test bacteria TA98." | ( [Impact of different solvents on results of genotoxicity studies of airborne dust taken from work environments]. Mielzyńska, D; Siwińska, E; Smolik, E; Szaciłło, H, 1995) | 0.29 |
| " Our results showed that a large, acute dose of morphine given to drug-naive male rats 24 hr before the initiation of breeding had no effect on fertility rates, but produced several adverse effects on fetal outcome." | ( Adverse effects of paternal opiate exposure on offspring development and sensitivity to morphine-induced analgesia. Adams, M; Cicero, TJ; Meyer, ER; Nock, B; O'Connor, L, 1995) | 0.29 |
| "Cocaine use is accompanied by a high risk of serious adverse effects involving the cardiovascular system." | ( The pathophysiology of cocaine cardiotoxicity. Klaus, W; Rump, AF; Theisohn, M, 1995) | 0.29 |
| " Synthetic local anesthetics such as tetracaine and proparacaine were developed which were more potent and less toxic than cocaine, but still produced corneal epithelium defects if used chronically." | ( Comparative toxicity of tetracaine, proparacaine and cocaine evaluated with primary cultures of rabbit corneal epithelial cells. Acosta, D; Grant, RL, 1994) | 0.29 |
| " Relief of chest pain and/or adverse hemodynamic outcome were the primary endpoints." | ( Nitroglycerin in the treatment of cocaine associated chest pain--clinical safety and efficacy. DiSano, MJ; Dyer, S; Fairweather, P; Feldman, JA; Fish, SS; Gennis, P; Hoffman, RS; Hollander, JE; Schumb, DA; Wax, P, 1994) | 0.29 |
| "Although cocaine abuse has been a major drug problem in the United States for over 100 years, it has only been in the last decade that the adverse effects of cocaine on the cardiovascular system have become a serious health issue." | ( Cellular mechanisms of cocaine cardiotoxicity. Grammas, P; Melchert, RB; Welder, AA, 1993) | 0.29 |
| " Intracellular lactate dehydrogenase activity, free calcium levels ([Ca2+]i), reduced glutathione (GSH) and lipid peroxidation were investigated to evaluate the toxic effect of cocaine on hepatocytes." | ( Cocaine hepatotoxicity: two different toxicity mechanisms for phenobarbital-induced and non-induced rat hepatocytes. Castell, JV; Gómez-Lechón, J; Jover, R; Ponsoda, X, 1993) | 0.29 |
| " Because cocaine and anabolic-androgenic steroids are used improperly, more focus needs to be paid to the toxic mechanisms of their adverse effects." | ( Cardiotoxic effects of cocaine and anabolic-androgenic steroids in the athlete. Melchert, RB; Welder, AA, 1993) | 0.29 |
| " Arterial blood was withdrawn at the onset of the toxic signs or symptoms for determination of cocaine concentrations." | ( Gender-related differences in cocaine toxicity in the rat. Abe, Y; Akiba, K; Cooper, TB; Masaoka, T; Matsuo, M; Morishima, HO, 1993) | 0.29 |
| " Using a potent and selective ligand of sigma binding sites, 6-[6-(4-hydroxypiperidinyl)hexyloxy]-3-methylflavone (NPC 16377), we further investigated the influence of sigma ligands on additional behavioral and toxic effects of cocaine in mice." | ( Effects of the selective sigma receptor ligand, 6-[6-(4-hydroxypiperidinyl)hexyloxy]-3-methylflavone (NPC 16377), on behavioral and toxic effects of cocaine. Ferkany, J; Hickey, P; Katz, JL; Menkel, M; Pontecorvo, M; Terry, P; Witkin, JM, 1993) | 0.29 |
| " Since expression of the inducible 72 kDa heat shock protein (HSP72) is a sensitive indicator of potentially toxic neuronal stress, we next determined if cocaine evoked HSP72 expression." | ( Cocaine neurotoxicity and altered neuropeptide Y immunoreactivity in the rat hippocampus; a silver degeneration and immunocytochemical study. Goodman, JH; Sloviter, RS, 1993) | 0.29 |
| " These data suggest that daily maintenance on buprenorphine is not associated with adverse side effects or toxic interactions with a single acute dose of intravenous cocaine or morphine." | ( Acute interactions of buprenorphine with intravenous cocaine and morphine: an investigational new drug phase I safety evaluation. Kuehnle, J; Mello, NK; Mendelson, JH; Rhoades, EM; Sintavanarong, P; Teoh, SK, 1993) | 0.29 |
| "The nervous system is vulnerable to a wide range of toxic insults." | ( Alcohol- and drug-related neurotoxicity. Filley, CM; Kelly, JP, 1993) | 0.29 |
| " Preclinical studies were conducted to assess the behavioral and toxic effects of benztropine alone and in conjunction with cocaine." | ( Effects of benztropine on behavioral and toxic effects of cocaine: comparison with atropine and the selective dopamine uptake inhibitor 1-[2-(diphenylmethoxy)ethyl]-4-(3-phenyl-propyl)-piperazine. Acri, JB; Siedleck, BK; Witkin, JM, 1996) | 0.29 |
| " No patient exhibited an adverse reaction related to TAC." | ( Safe and effective method for application of tetracaine, adrenaline, and cocaine to oral lacerations. Bonadio, WA, 1996) | 0.29 |
| "This TAC application technique was safe and highly effective in providing anesthesia for minor oral lacerations." | ( Safe and effective method for application of tetracaine, adrenaline, and cocaine to oral lacerations. Bonadio, WA, 1996) | 0.29 |
| " However, no data currently exist concerning potential interactions between toxic levels of cocaine and volatile anesthetic agents." | ( Cocaine toxicity and isoflurane anesthesia: hemodynamic, myocardial metabolic, and regional blood flow effects in swine. Boylan, JF; Boylen, P; Carmichael, FJ; Cheng, DC; Feindel, C; Koren, G; Sandler, AN, 1996) | 0.29 |
| " The cardiac and cardiovascular toxic effects of cocaine include various degrees of myocardial ischemia, cardiac arrhythmias, cardiotoxicity, hypertensive effects, cerebrovascular effects and a hypercoagulable state." | ( Pathophysiology and treatment of cocaine toxicity: implications for the heart and cardiovascular system. Kavanagh, KM; Teo, KK; Williams, RG, 1996) | 0.29 |
| "A sample of drug users (n = 158) were contacted and interviewed in non-clinical community settings about their use of Ecstasy, cocaine powder, and amphetamines and the adverse effects of these drugs." | ( Adverse effects of stimulant drugs in a community sample of drug users. Fountain, J; Gossop, M; Griffiths, P; Powis, B; Strang, J; Williamson, S, 1997) | 0.3 |
| "In this preliminary report from a placebo-controlled, double-blind, dose-response study on the use of pergolide mesylate for cocaine dependence in outpatients 8 out of 235 subjects noted adverse events requiring breaking of the blind." | ( Pergolide mesylate. Adverse events occurring in the treatment of cocaine dependence. Cochrane, CE; Kajdasz, DK; Malcolm, R; Moore, JW, 1997) | 0.3 |
| "The aim of the present study was to assess the toxic potential of drugs of abuse and other neuropharmacological agents in the pathogenesis of AIDS dementia complex (ADC), the neurological complication of AIDS." | ( Regulation of glutathione and cell toxicity following exposure to neurotropic substances and human immunodeficiency virus-1 in vitro. Demuth, M; Götz, ME; Koutsilieri, E; Riederer, P; Sauer, U; Sopper, S; ter Meulen, V, 1997) | 0.3 |
| " The LD50 values were about 20 mg and 5 mg for mice and rats, respectively." | ( Toxicity, mutagenicity, and behavioral effects of beta-CIT, a ligand for dopamine transporter exploration by SPECT. Belzung, C; Besnard, JC; Chalon, S; Chiron, JP; Emond, P; Farde, L; Guilloteau, D; Halldin, C; Mauclaire, V, 1998) | 0.3 |
| " Evidence for direct toxic effects is next presented." | ( Selective direct toxicity of cocaine on fetal mouse neurons. Teratogenic implications of neurite and apoptotic neuronal loss. Courtoy, PJ; Evrard, P; Nassogne, MC, 1998) | 0.3 |
| " These toxic effects are thought to be due to oxidative stress." | ( Melatonin attenuates methamphetamine-induced toxic effects on dopamine and serotonin terminals in mouse brain. Asanuma, M; Cadet, JL; Hirata, H, 1998) | 0.3 |
| "Cocaine, norcocaine, cocaethylene, benzoylecgonine, and ecgonine methyl ester were infused intravenously to produce sequential behavioral alterations and central nervous system and cardiovascular toxic effects." | ( The comparative toxicity of cocaine and its metabolites in conscious rats. Cooper, TB; Iso, A; Morishima, HO; Whittington, RA, 1999) | 0.3 |
| "The dose of norcocaine necessary to produce toxic effects was smaller than that of cocaine and cocaethylene." | ( The comparative toxicity of cocaine and its metabolites in conscious rats. Cooper, TB; Iso, A; Morishima, HO; Whittington, RA, 1999) | 0.3 |
| "These results indicate that benzoylecgonine and ecgonine methyl ester are not as toxic as cocaine, norcocaine, or cocaethylene when administered intravenously to pharmacologically naive rats." | ( The comparative toxicity of cocaine and its metabolites in conscious rats. Cooper, TB; Iso, A; Morishima, HO; Whittington, RA, 1999) | 0.3 |
| " Ethanol might exacerbate cocaine hepatocyte toxicity by three different pathways: a) by increasing the oxidative metabolism of cocaine and hence the oxidative damage; b) by the formation of a more toxic metabolite, namely cocaethylene; or c) by decreasing the defence mechanisms of the cell (i." | ( Increased toxicity of cocaine on human hepatocytes induced by ethanol: role of GSH. Bort, R; Castell, JV; Gómez-Lechón, MJ; Jover, R; Ponsoda, X, 1999) | 0.3 |
| " However, many antidepressants considered for treatment of cocaine addiction target these monoamine systems and may thus amplify these toxic effects during relapse." | ( Antidepressant drugs appear to enhance cocaine-induced toxicity. George, FR; O'Dell, LE; Ritz, MC, 2000) | 0.31 |
| " On account of several experimental and clinical studies reporting effectiveness against the toxic effects of heroin and methamphetamine, chlormethiazole was systematically tested in the present study for its effectiveness against cocaine-induced seizures and lethality in mice." | ( Chlormethiazole: effectiveness against toxic effects of cocaine in mice. Gasior, M; Ungard, JT; Witkin, JM, 2000) | 0.31 |
| "The purpose of the present investigation was to determine whether the sensitivity to systemic toxic effects of cocaine is altered in genetically epilepsy-prone rats (GEPRs)." | ( Phenotypic expression of the systemic toxicity of cocaine in genetically epilepsy-prone rats. Heavner, JE; Kao, YJ; Kaye, AD; Reigel, CE; Shi, B, 2000) | 0.31 |
| "rad;OH concentration in embryonic tissues after COC exposure and toxic interactions of COC and NaSAL can also occur at an earlier stage of development." | ( Salicylate and cocaine: interactive toxicity during chicken mid-embryogenesis. Sparber, SB; Venturini, L, 2001) | 0.31 |
| " However, an acceleration of behavioral despair in the Porsolt test similar to that observed in the IM group was observed in the COCA group after the disappearance of the acute toxic symptoms (5 hours after the COCA treatment)." | ( Stress-related behavioral alterations accompanying cocaine toxicity: the effects of mixed opioid drugs. Hayase, T; Yamamoto, K; Yamamoto, Y, 2000) | 0.31 |
| " The present study demonstrated that cocaine is toxic to multiple organs, and at low dose can induce hepatic damage without gross pathological injury to the heart." | ( Differential patterns of cocaine-induced organ toxicity in murine heart versus liver. Amende, I; DeAngelis, J; Hampton, TG; Min, J; Morgan, JP; Ren, X; Wang, JF; Zhang, Y, 2001) | 0.31 |
| "This study shows that concomitant use of cocaine and adrenaline in the proper concentration and volume and in a carefully screened patient group was safe for the cardiovascular system." | ( Cardiovascular safety of cocaine anaesthesia in the presence of adrenaline during septal surgery. Atalay, H; Kaftan, A; Kara, CO; Oğmen, G; Pinar, HS, 2001) | 0.31 |
| " The vaccine was well-tolerated and had no serious drug-related adverse events, although three subjects at the highest dose experienced brief post injection twitching." | ( Human therapeutic cocaine vaccine: safety and immunogenicity. Bond, J; Fox, B; Jack, L; Kosten, TR; Roberts, JS; Rosen, M; Settles, M; Shields, J, 2002) | 0.31 |
| " Using the activity-counting instrument Supermex, the relationship between the toxic signs and the corresponding behavioral alterations could be assessed." | ( Antidotal effects of buprenorphine on the behavioral alterations accompanying cocaine and combined cocaine-ethanol toxicity. Hayase, T; Yamamoto, K; Yamamoto, Y, ) | 0.13 |
| " There have been reports indicating that, in the presence of toxic doses of cocaine, the CCBs could actually potentiate cocaine toxicity in rats." | ( Nifedipine potentiates the toxic effects of cocaine in mice. Ansah, TA; Kopsombut, P; Shockley, DC; Wade, LH, 2002) | 0.31 |
| " Serious adverse effects have been described in several series of women consuming pure cocaine, but in recent years articles questioning some of the damaging effects of cocaine on the fetus and newborn have been published." | ( [Cocaine toxicity in the newborn. Detection and prevalence]. García-Algar, O; López Segura, N; Mur Sierra, A, 2002) | 0.31 |
| "An assay for computerized scoring of the DNA content of the protozoan Tetrahymena pyriformis has been used for the detection of toxic responses to cocaine, since DNA is responsible for the replication of the genetic material and also reflects closely the number of chromosomes in the nucleus." | ( DNA toxicity of cocaine hydrochloride and cocaine freebase by means of DNA image analysis on Tetrahymena pyriformis. Alevisopoulos, G; Chatziioannou, A; Koutselinis, A; Livaditou, A; Rellaki, A; Spiliopoulou, H; Stefanidou, M, 2002) | 0.31 |
| "In this 6-month placebo-controlled trial, herbal ephedra/caffeine (90/192 mg/day) promoted body weight and body fat reduction and improved blood lipids without significant adverse events." | ( Herbal ephedra/caffeine for weight loss: a 6-month randomized safety and efficacy trial. Blanchard, D; Boozer, CN; Daly, PA; Homel, P; Meredith, T; Nasser, JA; Solomon, JL; Strauss, R, 2002) | 0.31 |
| " Our data show that opioid drugs (heroin and morphine) are more toxic than stimulant drugs (d-amphetamine and cocaine)." | ( Toxic effects of opioid and stimulant drugs on undifferentiated PC12 cells. Macedo, TR; Morgadinho, MT; Oliveira, CR; Oliveira, MT; Rego, AC, 2002) | 0.31 |
| "To investigate the toxic effects of mid-pregnancy cocaine exposure on embryo-fetus." | ( Developmental toxicity of cocaine exposure in mid-pregnancy mice. Guan, XW; He, W; Ren, JQ; Song, J, 2002) | 0.31 |
| " Since information is not available on the effects of their concomitant abuse, and taking into account that cocaine and testosterone, when singly abused, are known to induce severe adverse effects on vascular system, our purpose was to evaluate in vitro the combined effect of these drugs on platelet and endothelial functions." | ( Testosterone and cocaine: vascular toxicity of their concomitant abuse. Franconi, M; Graziani, M; Togna, AR; Togna, GI, 2003) | 0.32 |
| "The paper presented the effects of cocaine on the human, particularly toxic effects induced by chronic use of cocaine." | ( [Cocaine toxicity]. Kiszka, M, ) | 0.13 |
| " Autopsy studies suggest that multidrug intoxication is a major risk factor for adverse outcomes after acute heroin overdose in patients." | ( Do co-intoxicants increase adverse event rates in the first 24 hours in patients resuscitated from acute opioid overdose? Christenson, J; Innes, GD; Mirakbari, SM; Tilley, J; Wong, H, 2003) | 0.32 |
| " Patients were followed to identify prespecified adverse outcome events occurring within 24 h, and multiple logistic regression was used to determine the association of concomitant drug use on short-term adverse event rates." | ( Do co-intoxicants increase adverse event rates in the first 24 hours in patients resuscitated from acute opioid overdose? Christenson, J; Innes, GD; Mirakbari, SM; Tilley, J; Wong, H, 2003) | 0.32 |
| " Overall, out of 1056 patients with known outcome status there were 123 major adverse events (11." | ( Do co-intoxicants increase adverse event rates in the first 24 hours in patients resuscitated from acute opioid overdose? Christenson, J; Innes, GD; Mirakbari, SM; Tilley, J; Wong, H, 2003) | 0.32 |
| " (2) No toxic side effects were seen but the protocol was updated in line with evidence." | ( Topical adrenaline and cocaine gel for anaesthetising children's lacerations. An audit of acceptability and safety. Crean, SV; Evans, RJ; Fardy, MJ; Kennedy, DW; Shaikh, Z, 2004) | 0.32 |
| "In mice, the recreational drug (+/-)3,4-methylenedioxymethamphetamine [MDMA ("ecstasy")] produces a selective toxic effect on brain dopamine (DA) neurons." | ( Identification and characterization of metallothionein-1 and -2 gene expression in the context of (+/-)3,4-methylenedioxymethamphetamine-induced toxicity to brain dopaminergic neurons. Becker, KG; Cheadle, C; Donovan, DM; McCann, UD; Mechan, AO; Ricaurte, GA; Tong, L; Xie, T; Yuan, J, 2004) | 0.32 |
| " Other adverse effects associated with ROS comprise teratogenesis and apoptosis." | ( Role of oxidative metabolites of cocaine in toxicity and addiction: oxidative stress and electron transfer. Kovacic, P, 2005) | 0.33 |
| " The clinical manifestations of toxic nephropathy vary from a mild reduction in renal function to hematuria, proteinuria, and urolithiasis to a severe progressive toxicity culminating in end-stage renal disease." | ( Nephrotoxicity of over-the-counter analgesics, natural medicines, and illicit drugs. Blowey, DL, 2005) | 0.33 |
| "Gender is known to play a role in the bioavailability, metabolism, and lethality of many toxic substances." | ( Influence of gender on cocaine hepatotoxicity in CF-1 mice. Abdel-Rahman, MS; Turkall, R; Visalli, T, ) | 0.13 |
| " Tat is neurotoxic and a constantly growing body of evidence suggests that the toxic effects of Tat are oxidative stress-dependent." | ( Cocaine-mediated enhancement of Tat toxicity in rat hippocampal cell cultures: the role of oxidative stress and D1 dopamine receptor. Aksenov, MY; Aksenova, MV; Booze, RM; Mactutus, CF; Nath, A; Ray, PD, 2006) | 0.33 |
| " The combination was more toxic than cocaine alone." | ( Inhibition of nitric oxide synthase enhances cocaine's developmental toxicity: vascular and CNS effects. Mendoza-Baumgart, MI; Pravetoni, M; Sparber, SB, 2007) | 0.34 |
| " Together with previous studies showing that cocaine suppresses BDNF expression, the present data suggest that the drug-induced reduction of BDNF productions may make neurons more vulnerable to cocaine's toxic effects and precipitate cocaine-induced central nervous system damages." | ( RNA interference-mediated inhibition of brain-derived neurotrophic factor expression increases cocaine's cytotoxicity in cultured cells. Feng, MJ; Yan, QS; Yan, SE, 2007) | 0.34 |
| " Second, based on preliminary investigations, an approximate intraperitoneal LD50 dose of cocaine (110 mg/kg) was identified and used as the cocaine dose in this study." | ( The effect of amiodarone pretreatment on survival of mice with cocaine toxicity. Cleveland, N; Dart, RC; DeWitt, CR; Heard, K, 2005) | 0.33 |
| " Its application in this context is controversial due to the potential associated adverse effects." | ( Cardiovascular toxicity of cocaine of iatrogenic origin. Case report. Azevedo, P; Correia, A; Costa, J; Magalhães, S; Marques, J; Nabais, S; Rebelo, A; Rocha, S; Torres, M, 2007) | 0.34 |
| " The present findings provide, for the first time, details of a synergistic toxic effect of the cocaine/atropine mixture and of the potential of diazepam for treating cocatropine-related hospital emergencies." | ( Diazepam protects against the enhanced toxicity of cocaine adulterated with atropine. Braida, D; Capurro, V; Gori, E; Pegorini, S; Rossoni, G; Sala, M; Zani, A, 2008) | 0.35 |
| " In this study, we determined if subacute administration of the atypical antipsychotic ziprasidone altered the toxic effects of cocaine in mice." | ( Administration of ziprasidone for 10 days increases cocaine toxicity in mice. Heard, K; Krier, S; Zahniser, NR, 2008) | 0.35 |
| "Aripiprazole (15 mg/day) is safe and tolerable when combined with cocaine; however, the usefulness of aripiprazole as a treatment for cocaine-use disorders remains to be determined." | ( The safety, tolerability, and subject-rated effects of acute intranasal cocaine administration during aripiprazole maintenance II: increased aripipirazole dose and maintenance period. Hays, LR; Lile, JA; Rush, CR; Stoops, WW, 2008) | 0.35 |
| " These effects were not clinically significant and no unexpected or serious adverse events were observed." | ( Cocaine effects during D-amphetamine maintenance: a human laboratory analysis of safety, tolerability and efficacy. Hays, LR; Rush, CR; Stoops, WW, 2009) | 0.35 |
| " Although the patient's response to GZA resolved spontaneously, emergency physician awareness of the toxic effects of natural licorice extract may avert symptom progression in early-identified cases." | ( Glycyrrhizic acid toxicity caused by consumption of licorice candy cigars. Johns, C, 2009) | 0.35 |
| " consumers have a history of safe consumption of cola-type beverages containing kola nut extract that dates at least to the late 19th Century, with a significant global history of exposure to the intact kola nuts that date centuries longer." | ( Safety assessment of kola nut extract as a food ingredient. Burdock, GA; Carabin, IG; Crincoli, CM, 2009) | 0.35 |
| " The toxic effects of cocaine can be attenuated by antagonists of serotonin, muscarinic cholinergic, and dopamine receptors." | ( The effect of olanzapine pretreatment on acute cocaine toxicity in mice. Cleveland, NR; Heard, KJ; Krier, S, 2009) | 0.35 |
| " Toxicity test results revealed that whole coke leachates (100% v/v) were acutely toxic to Ceriodaphnia dubia; the 7-day LC50 values were always <25% v/v coke leachate." | ( Variation in toxicity response of Ceriodaphnia dubia to Athabasca oil sands coke leachates. Liber, K; Puttaswamy, N; Turcotte, D, 2010) | 0.36 |
| "With an increasing focus on the risk of pollution resulting from coking wastewater, it is important to check its toxic effects on organisms." | ( Investigating the bio-toxicity of coking wastewater using Zea mays L. assay. Dong, Y; Han, M; Li, G; Sang, N, 2011) | 0.37 |
| "In the present study, AC927 (1-(2-phenethyl)piperidine oxalate), a selective sigma receptor ligand, was tested against the behavioral and toxic effects of cocaine in laboratory animals." | ( Effects of the selective sigma receptor ligand, 1-(2-phenethyl)piperidine oxalate (AC927), on the behavioral and toxic effects of cocaine. Coop, A; Fantegrossi, WE; Katz, JL; Li, SM; Matsumoto, RR, 2011) | 0.37 |
| " Further studies showed that these sugar-free lollipops are safe and their antimicrobial activity is stable." | ( Development and evaluation of a safe and effective sugar-free herbal lollipop that kills cavity-causing bacteria. Anderson, MH; Bauer, J; Eckert, R; Gelman, F; He, J; Hu, CH; Li, LN; Lux, R; Mentes, J; Shi, WY; Shuffer, JA; Spackman, S; Tian, Y; Wu, XY, 2011) | 0.37 |
| " A reduction in endogenous levels of BChE may result in increased metabolism by hepatic carboxylesterase to produce norcocaine, a toxic product." | ( Prolonged toxic effects after cocaine challenge in butyrylcholinesterase/plasma carboxylesterase double knockout mice: a model for butyrylcholinesterase-deficient humans. Duysen, EG; Lockridge, O, 2011) | 0.37 |
| " In contrast, ethanol produced adverse ECG changes including QTc prolongation and a DER consisting of hypotension, tachycardia, nausea, and flushing in disulfiram-treated subjects." | ( A double-blind, placebo-controlled assessment of the safety of potential interactions between intravenous cocaine, ethanol, and oral disulfiram. Anderson, A; De La Garza, R; Elkashef, A; Kahn, R; Mojsiak, J; Murff, WL; Newton, TF; Rivera, O; Roache, JD; Wallace, CL, 2011) | 0.37 |
| " Therefore, σ receptors provide a viable target for the development of pharmacotherapeutics against the adverse effects of METH." | ( CM156, a high affinity sigma ligand, attenuates the stimulant and neurotoxic effects of methamphetamine in mice. Kaushal, N; Matsumoto, RR; McCurdy, CR; Medina, MA; Mesangeau, C; Seminerio, MJ; Shaikh, J; Wilson, LL, ) | 0.13 |
| "A previous study found that coke leachates (CL) collected from oil sands field sites were acutely toxic to Ceriodaphnia dubia; however, the cause of toxicity was not known." | ( Identifying the causes of oil sands coke leachate toxicity to aquatic invertebrates. Liber, K; Puttaswamy, N, 2011) | 0.37 |
| " These compounds accelerate cocaine metabolism and antagonize the behavioral and toxic effects of cocaine in animal models." | ( Accelerating cocaine metabolism as an approach to the treatment of cocaine abuse and toxicity. Goldberg, SR; Schindler, CW, 2012) | 0.38 |
| " A humanized mAb should minimize adverse events related to the immunogenicity of the mAb protein, and the specificity for cocaine should avoid adverse events related to interactions with physiologically relevant endogenous proteins." | ( Predicting the clinical efficacy and potential adverse effects of a humanized anticocaine monoclonal antibody. Ball, WJ; Norman, AB, 2012) | 0.38 |
| " Cocaine dependence and pathological gambling share neurobiological vulnerabilities related to addiction, but PG are relatively free of the toxic consequences, such that any additional deficits observed in CDI may be interpreted as pertaining to specific drug effects." | ( Comparison of impulsivity and working memory in cocaine addiction and pathological gambling: Implications for cocaine-induced neurotoxicity. Albein-Urios, N; Clark, L; Lozano, O; Martinez-González, JM; Verdejo-García, A, 2012) | 0.38 |
| " Misuse of cocaine can induce severe toxic effects, including neurotoxicity, cardiotoxicity, hepatotoxicity." | ( Cocaine toxicity and hepatic oxidative stress. Vitcheva, V, 2012) | 0.38 |
| " Most of the direct toxic effects are mediated by oxidative stress and by mitochondrial dysfunction produced during the metabolism of noradrenaline or during the metabolism of norcocaina, as in cocaine-induced hepathotoxicity." | ( Side effects of cocaine abuse: multiorgan toxicity and pathological consequences. De Carlo, D; Fineschi, V; Fiore, C; Neri, M; Pascale, N; Riezzo, I; Turillazzi, E, 2012) | 0.38 |
| " During snowmelt, yearlings were exposed to a gradient of pH and inorganic monomeric Al (Al(i)) in humic streams to study the toxic effects and mortality." | ( Toxicity of inorganic aluminium at spring snowmelt--in-stream bioassays with brown trout (Salmo trutta L.). Andrén, CM; Rydin, E, 2012) | 0.38 |
| " The changes in the ability of the refractory organic compounds to bind with enzyme proteins, combined with the analysis of the organic components by GC/MS, show that in the process of coking wastewater treatment no new toxic chemicals were produced." | ( The effect of treatment stages on the coking wastewater hazardous compounds and their toxicity. Fan, QL; Guo, DS; Wei, XX; Yuan, XY; Zhang, ZY, 2012) | 0.38 |
| "Cocaine has been associated with acute hemodynamic changes, causing anesthesia providers to be concerned about adverse hemodynamic events during general anesthesia." | ( Utility of cocaine drug screens to predict safe delivery of general anesthesia for elective surgical patients. Alexandrov, AW; Baxter, JL, 2012) | 0.38 |
| " In addition, four thematic processes are described: (a) establishing a safe physical space, (b) building trusting relationships, (c) learning about safer crack use, and (d) accessing safer equipment." | ( The process of safer crack use among women in Vancouver's Downtown Eastside. Bungay, V; Handlovsky, IE; Johnson, J; Phillips, JC, 2013) | 0.39 |
| " The biotoxicity test indicated that the effluent of MBR was very safe for the environment." | ( Biotoxicity evaluation of coking wastewater treated with different technologies using Japanese medaka (Oryzias latipes). Chen, L; Liu, C; Liu, R; Pan, Z; Zhu, X, 2013) | 0.39 |
| " A 5-point (1-5 mM) dose-response curve of NAC clearly indicated no adverse effect on astroglial cell viability." | ( Attenuating effect of N-acetyl-L-cysteine against acute cocaine toxicity in rat C6 astroglial cells. Badisa, RB; Fitch-Pye, CA; Goodman, CB, 2013) | 0.39 |
| " Neither vector caused adverse reactions such as motor weakness, elevated liver enzymes, or disturbance in spontaneous activity." | ( Gene transfer of mutant mouse cholinesterase provides high lifetime expression and reduced cocaine responses with no evident toxicity. Brimijoin, S; Chen, X; Gao, Y; Geng, L; Hou, S; Parks, RJ; Pham, L; Radic, Z; Russell, SJ; Zhan, CG, 2013) | 0.39 |
| " However, to date the knowledge on their adverse effects to non-target organisms is inadequate." | ( Adverse effects induced by ecgonine methyl ester to the zebra mussel: a comparison with the benzoylecgonine. Binelli, A; Parolini, M, 2013) | 0.39 |
| " A pharmaceutical developed from these concepts will need to be expedient in onset and effective with minimal adverse effects while at the same time being economical." | ( Experimental treatments for cocaine toxicity: a difficult transition to the bedside. Connors, NJ; Hoffman, RS, 2013) | 0.39 |
| " In contrast to these short-term benefits, prolonged adrenergic stress is detrimental to the cardiovascular system by initiating a series of adverse effects triggering significant cardiotoxicity, whose pathophysiological mechanisms are complex and only partially elucidated." | ( Pathophysiological mechanisms of catecholamine and cocaine-mediated cardiotoxicity. Calderari, B; Liaudet, L; Pacher, P, 2014) | 0.4 |
| " Despite high vector doses (up to 10(13) particles per mouse) and high levels of transgene protein in the plasma (∼1500-fold above baseline), the CLAMS apparatus revealed no adverse physiologic or metabolic effects." | ( Physiologic and metabolic safety of butyrylcholinesterase gene therapy in mice. Brimijoin, S; Gao, Y; Geng, L; LeBrasseur, NK; Murthy, V; Parks, RJ; White, TA, 2014) | 0.4 |
| " These toxic effects include hyperthermia, hypotonic hyponatremia due to its arginine vasopressin secretagogue-like effects, rhabdomyolysis, and cardiovascular collapse." | ( Nephrotoxic effects of common and emerging drugs of abuse. Herlitz, LC; Niles, JL; Pendergraft, WF; Rosner, M; Thornley-Brown, D, 2014) | 0.4 |
| " The raw influent displayed the highest toxicity to the test species, with toxic units ranging from 16." | ( Multispecies acute toxicity evaluation of wastewaters from different treatment stages in a coking wastewater-treatment plant. Jiang, YX; Wei, C; Yan, B; Ying, GG; Zhang, LJ; Zhao, JL, 2014) | 0.4 |
| " TV-1380 was found to be safe and well tolerated with a long half-life (43-77 hours) and showed a dose-proportional increase in systemic exposure." | ( Safety, pharmacokinetics, and pharmacodynamics of TV-1380, a novel mutated butyrylcholinesterase treatment for cocaine addiction, after single and multiple intramuscular injections in healthy subjects. Bassan, M; Clark, S; Cohen-Barak, O; Gilgun-Sherki, Y; Gross, A; Hettinga, J; Mendzelevski, B; Schuilenga-Hut, P; Spiegelstein, O; van de Wetering, J; Wildeman, J, 2015) | 0.42 |
| " These findings, coupled with the fact that astrocytes maintain neuronal integrity, suggest that compounds which target and mitigate these early toxic changes in astrocytes could have a potentially broad therapeutic role in cocaine-induced CNS damage." | ( N-acetyl cysteine mitigates the acute effects of cocaine-induced toxicity in astroglia-like cells. Allen, JR; Badisa, RB; Davidson, MW; Fitch-Pye, CA; Goodman, CB; Haughbrook, RD; Kumar, SS; Mazzio, E, 2015) | 0.42 |
| " The most toxic snowmelt samples were found to be high acute hazard (class IV), while the remaining samples were rated as slight acute hazard (class II)." | ( The microbiotest battery as an important component in the assessment of snowmelt toxicity in urban watercourses--preliminary studies. Mankiewicz-Boczek, J; Stolarska, M; Szklarek, S; Wagner, I, 2015) | 0.42 |
| " The WOOD extract was most toxic and the GAS extract least toxic." | ( Aryl hydrocarbon receptor activation and developmental toxicity in zebrafish in response to soil extracts containing unsubstituted and oxygenated PAHs. Bottai, M; Dreij, K; Jönsson, ME; Lundstedt, S; Wincent, E, 2015) | 0.42 |
| " These observations confirm that the drug metabolites generated after CocH gene transfer therapy are safe even after a dose of cocaine that would ordinarily be lethal." | ( Reward and Toxicity of Cocaine Metabolites Generated by Cocaine Hydrolase. Brimijoin, S; Gao, Y; Geng, L; Miller, JD; Murthy, V; Reyes, S; Zhang, B, 2015) | 0.42 |
| " This review aims to discuss metabolomics of cocaine, namely by presenting all known metabolites of cocaine and their roles in the cocaine-mediated toxic effects." | ( Metabolomics of cocaine: implications in toxicity. Dinis-Oliveira, RJ, 2015) | 0.42 |
| " Adverse effects on ferns agree with the allelophathic role described for alkaloids and their unspecific interference with plant germination." | ( Environmental concentrations of the cocaine metabolite benzoylecgonine induced sublethal toxicity in the development of plants but not in a zebrafish embryo-larval model. Catalá, M; García-Cambero, JP; García-Cortés, H; Valcárcel, Y, 2015) | 0.42 |
| "Huperzine A was safe and well-tolerated and compared with placebo, treatment with huperzine A did not cause significant changes in any cocaine pharmacokinetic parameters (all P>." | ( Safety and Preliminary Efficacy of the Acetylcholinesterase Inhibitor Huperzine A as a Treatment for Cocaine Use Disorder. De La Garza, R; Mahoney, JJ; Newton, TF; Thompson-Lake, DG; Verrico, CD, 2015) | 0.42 |
| " The aim of the present study was to further explore potential toxic consequences of chronic exposure to cocaine, caffeine, and their combination on testicular physiology." | ( Psychostimulant-Induced Testicular Toxicity in Mice: Evidence of Cocaine and Caffeine Effects on the Local Dopaminergic System. Bisagno, V; Cadet, JL; Garcia-Rill, E; González, B; González, CR; Matzkin, ME; Muñiz, JA; Urbano, FJ; Vitullo, AD, 2015) | 0.42 |
| "Cardiotoxicity is a broad term that refers to the negative effects of toxic substances on the heart." | ( Mechanisms of Cardiotoxicity and the Development of Heart Failure. Lee, CS, 2015) | 0.42 |
| " Since atropine prevented AEME-induced neurotoxicity, it has been suggested that its toxic effects may involve the muscarinic cholinergic receptors (mAChRs)." | ( M1 and M3 muscarinic receptors may play a role in the neurotoxicity of anhydroecgonine methyl ester, a cocaine pyrolysis product. Abdalla, FM; Afeche, SC; Camarini, R; Conn, PJ; da Costa, JL; da Silva, MA; Dati, LM; Garcia, RC; Gorjão, R; Marcourakis, T; Niswender, CM; Sandoval, MR; Torres, LH; Udo, MS; Yonamine, M, 2015) | 0.42 |
| "Oxidative stress (OS) is thought to play an important role in the pharmacological and toxic effects of various drugs of abuse." | ( Cardiovascular and Hepatic Toxicity of Cocaine: Potential Beneficial Effects of Modulators of Oxidative Stress. Antonilli, L; Badiani, A; Grassi, MC; Graziani, M; Saso, L; Togna, AR, 2016) | 0.43 |
| " Special attention was given to adverse drug events or treatment failure." | ( Treatment of cocaine cardiovascular toxicity: a systematic review. Albertson, TE; Amsterdam, EA; Derlet, RW; Garber, D; Lange, RA; Laurin, EG; Olson, KR; Ramoska, EA; Richards, JR, 2016) | 0.43 |
| "Cocaine was safe and well tolerated during maintenance on a threefold range of phendimetrazine doses." | ( Safety and tolerability of intranasal cocaine during phendimetrazine maintenance. Hays, LR; Lile, JA; Rayapati, AO; Rush, CR; Stoops, WW; Strickland, JC, 2016) | 0.43 |
| "This study investigated the changes of toxic compounds in coking wastewater with biological treatment (anaerobic reactor, anoxic reactor and aerobic-membrane bioreactor, A1/A2/O-MBR) and advanced physicochemical treatment (Fenton oxidation and activated carbon adsorption) stages." | ( Acute toxicity and chemical evaluation of coking wastewater under biological and advanced physicochemical treatment processes. Cong, L; Dehua, M; Lujun, C; Rui, L; Xiaobiao, Z, 2016) | 0.43 |
| "Despite the critical need, no previous research has substantiated safe opioid analgesics without abuse liability in primates." | ( A novel orvinol analog, BU08028, as a safe opioid analgesic without abuse liability in primates. Cami-Kobeci, G; Czoty, PW; Ding, H; Husbands, SM; Kiguchi, N; Ko, MC; Nader, MA; Sukhtankar, DD, 2016) | 0.43 |
| " To directly counter these adverse hyperadrenergic effects, the patient was given 10 mg intravenous labetalol, a mixed β- and α-blocker." | ( Acute Toxicity from Topical Cocaine for Epistaxis: Treatment with Labetalol. Lange, RA; Laurin, EG; Richards, JR; Tabish, N, 2017) | 0.46 |
| " In this review, all adverse effects associated with therapeutic levamisole and levamisole-adulterated cocaine are described." | ( Adverse effects of levamisole in cocaine users: a review and risk assessment. Brunt, TM; Pennings, E; van den Berg, J; Venhuis, B, 2017) | 0.46 |
| " Thus, the present study was aimed at investigating the potential adverse effects induced by the exposure to environmental concentrations (0." | ( Environmental concentrations of cocaine and its main metabolites modulated antioxidant response and caused cyto-genotoxic effects in zebrafish embryo cells. Binelli, A; Calvagno, M; Del Giacco, L; Della Torre, C; Ghilardi, A; Magni, S; Parolini, M; Prosperi, L, 2017) | 0.46 |
| " The mechanism(s) of toxic action are discussed and treatment modalities are briefly mentioned in relevant cases." | ( Comprehensive review of cardiovascular toxicity of drugs and related agents. Applová, L; Costa, VM; Jahodář, L; Karlíčková, J; Mladěnka, A; Mladěnka, P; Patočka, J; Pourová, J; Remiao, F; Štěrba, M; Varner, KJ; Vopršalová, M, 2018) | 0.48 |
| "The relative toxicity of these toxic drugs can be ranked in this order: norcocaethylene > norcocaine > cocaethylene > cocaine." | ( In vivo characterization of toxicity of norcocaethylene and norcocaine identified as the most toxic cocaine metabolites in male mice. Shang, L; Zhan, CG; Zheng, F; Zheng, X, 2019) | 0.51 |
| "This project offers new epidemiological estimates for DSM-IV cocaine dependence among sub-groups of newly incident cocaine users in the United States (US), including estimated attack rates for 21 dependence-related cocaine side effect problems and experiences occurring <12 months after onset." | ( Cocaine dependence: "Side effects" and syndrome formation within 1-12 months after first cocaine use. Anthony, JC; Chandra, M, 2020) | 0.56 |
| " For several cocaine side effect problems and experiences (e." | ( Cocaine dependence: "Side effects" and syndrome formation within 1-12 months after first cocaine use. Anthony, JC; Chandra, M, 2020) | 0.56 |
| ", pre-dating onset); (2) Powder-using initiates become cocaine dependent and then start using crack; (3) The cocaine delivery variant of 'crack-smoking' is more toxic than powder insufflation." | ( Cocaine dependence: "Side effects" and syndrome formation within 1-12 months after first cocaine use. Anthony, JC; Chandra, M, 2020) | 0.56 |
| " Benzoylecgonine (BE) is the main toxic metabolite after cocaine consumption, with a longer retention time in the body and environment than cocaine itself." | ( Sub-lethal toxicity and elimination of the cocaine metabolite, benzoylecgonine: a narrative review. Chen, X; Deng, X; Hou, S; Huang, Y; Qiu, T; Tong, J; Wang, J; Wu, Y; Zhang, Y, 2021) | 0.62 |
| " Little is known about the toxic effects of etizolam overdose." | ( Toxicity of designer benzodiazepines: A case of etizolam and cocaine intoxication. Abbara, C; Briet, M; Drevin, G; Ferec, S, 2022) | 0.72 |
| "The four main themes emerging from the study were related to cocaine characteristics and use, e-psychonauts' knowledge and experience, desired effects and adverse events." | ( Exploring e-psychonauts perspectives towards cocaine effects and toxicity. Al Hamid, A; Assi, S; Keenan, A, 2022) | 0.72 |
| " Not only it informed about the sources and modalities of use of cocaine but also about the adverse events and social harm associated with cocaine use." | ( Exploring e-psychonauts perspectives towards cocaine effects and toxicity. Al Hamid, A; Assi, S; Keenan, A, 2022) | 0.72 |
| " By early 2021, MADDS detected shifts in cocaine purity, alerted communities of a new toxic fentanyl analogue and a synthetic cannabinoid contaminant, and confirmed the increase of xylazine (a veterinary sedative) in Massachusetts." | ( Implementation and Uptake of the Massachusetts Drug Supply Data Stream: A Statewide Public Health-Public Safety Partnership Drug Checking Program. Consigli, A; Del Pozo, B; Erowid, E; Erowid, F; Green, TC; Jarczyk, C; Michelson, L; Olson, R; Reilly, B; Ruiz, S; Thyssen, S; Wightman, R, ) | 0.13 |
| " Targeted interventions are necessary to prevent death associated with toxic drug use during hot weather." | ( Hot weather and death related to acute cocaine, opioid and amphetamine toxicity in British Columbia, Canada: a time-stratified case-crossover study. Ding, Y; Henderson, SB; Kosatsky, T; McLean, KE; McVea, D; Turna, NS; Yao, J, ) | 0.13 |
Albu-CocH enzyme has effects on the pharmacokinetic and behavioral effects of cocaine in squirrel monkeys. Doses of cocaine, methylphenidate (MP), cocaine analogs and MP analogs were substituted for cocaine. There were no differences between men and women in pharmacokinetics measures.
| Excerpt | Reference | Relevance |
|---|---|---|
| "The pharmacodynamic actions of (S)-2-[4,5-dihydro-5-propyl-2(3H)-furylidene]-1,3-cyclopentanedione (oudenone) were studied in both anesthetized animals and isolated organs." | ( Pharmacodynamic actions of (S)-2-[4,5-dihydro-5-propyl-2-(3H)-furylidene]-1,3-cyclopentanedione (oudenone). Koide, T; Ozawa, H, 1976) | 0.26 |
| " The quantities applied in this case are so small that pharmacodynamic effects do not occur." | ( [Applications of positron emission tomography (PET) to the measurement of regional cerebral pharmacokinetics]. Stöcklin, G, 1992) | 0.28 |
| " Although no significant differences between the strains were seen in the pharmacokinetics of cocaine, the half-life of both norcocaine and N-hydroxynorcocaine was significantly longer in DBA mice." | ( Pharmacokinetic analysis of the metabolism of cocaine to norcocaine and N-hydroxynorcocaine in mice. Boyer, CS; Petersen, DR, ) | 0.13 |
| " Volume of distribution at steady state (Vdss), mean resident time (MRT) and elimination half-life (T1/2) were dose-dependent over this dose range with changes occurring between the 2 and the 4 mg/kg dose of COC." | ( Cocaine pharmacokinetics in the pregnant guinea pig. Olsen, GD; Sandberg, JA, 1991) | 0.28 |
| " The mean half-life of cocaine in the fetus across doses (4." | ( Disposition of cocaine in pregnant sheep. I. Pharmacokinetics. Abrams, RM; Braun, SB; Burchfield, DJ; DeVane, CL; Miller, RL, 1991) | 0.28 |
| " Changes in LM rates and motor control performance over the postadministration period were related to the pharmacokinetic features (maximum serum concentration, time to maximum serum concentration and elimination half-life) of cocaine observed for the routes explored (i." | ( Acute effects of cocaine on spontaneous and discriminative motor functions: relation to route of administration and pharmacokinetics. Falk, JL; Imam, A; Lau, CE; Ma, F, 1991) | 0.28 |
| " The pharmacokinetic properties that presumably contribute to self-administration and drug abuse include rapid delivery of the drug into the central nervous system and high free drug clearance." | ( Clinical pharmacokinetics of non-opiate abused drugs. Bendayan, R; Busto, U; Sellers, EM, 1989) | 0.28 |
| "As a preface to the pharmacokinetic analysis of cocaine in pregnant and lactating rats (using oral administration of drug), young Long-Evans rats were used to compare the relative concentrations of cocaine in blood, brain, and liver after administering cocaine by iv or oral routes." | ( Pharmacokinetics of cocaine: basic studies of route, dosage, pregnancy and lactation. Davis, CM; Rolsten, C; Ruiz, B; Wiggins, RC, 1989) | 0.28 |
| "A general theoretical framework is constructed for the relationship between a pharmacokinetic response r (e." | ( A system approach to pharmacodynamics. I: Theoretical framework. Gillespie, WR; Veng-Pedersen, P, 1988) | 0.27 |
| " injection of either 10 or 25 mg/kg of cocaine, cocaine disappeared from plasma and brain with a half-life of 16 min and benzoylecgonine disappeared from plasma with a half-life of 62 min." | ( Pharmacokinetics of systemically administered cocaine and locomotor stimulation in mice. Benuck, M; Lajtha, A; Reith, ME, 1987) | 0.27 |
| " Many pharmacokinetic parameters were found to have a strong dose dependence over the range 1 - 3 mg/kg." | ( Cocaine pharmacokinetics in humans. Barnett, G; Hawks, R; Resnick, R, ) | 0.13 |
| "9 l/kg, mean resident time (MRT) was 42 and 57 min, and elimination half-life was 34 and 49 min at the 2 and 4 mg/kg dose of COC, respectively." | ( Pharmacokinetics and metabolism of cocaine in maternal and fetal guinea pigs. Murphey, LJ; Olsen, GD; Sandberg, JA, 1995) | 0.29 |
| "67 l/h), had a longer elimination half-life (1." | ( Comparison in humans of the potency and pharmacokinetics of intravenously injected cocaethylene and cocaine. Cook, CE; Jeffcoat, AR; Myers, M; Perez-Reyes, M; Sihler, K, 1994) | 0.29 |
| "The time course of change in plasma levels of cocaine and its major metabolite benzoylecgonine following 3 mg/kg IV cocaine and the pharmacokinetic interaction between cocaine and several monoamine uptake inhibitors were investigated in conscious rats implanted with arterial and venous cannulae." | ( Monoamine uptake inhibitors alter cocaine pharmacokinetics. Goldberg, SR; Tella, SR, 1993) | 0.29 |
| " A pharmacokinetic study was therefore conducted to characterize the disposition of cocaine and a major metabolite benzoylecgonine (BE) using piglets as an animal model." | ( Effects of labetalol on cocaine pharmacokinetics in neonatal piglets. Badger, TM; Burge, LJ; Creer, MH; Karba, R; Nehus, C; Primozic, S; Scalzo, FM, 1993) | 0.29 |
| "kg-1, is rapidly eliminated with a half-life of 29 min and a total body clearance of 77 ml." | ( In vivo pharmacokinetics and in vitro production of cocaethylene in pregnant guinea pigs. Konkol, RJ; Kron, JE; Olsen, GD, 1996) | 0.29 |
| " Pharmacodynamic modeling techniques may be used to describe relationships between plasma cocaine concentrations and specific cardiovascular effects of cocaine." | ( Electrophysiologic and electrocardiographic pharmacodynamics of cocaine. Ducharme, MP; Edwards, DJ; Sabbah, HN; Shimoyama, H; Tisdale, JE; Webb, CR, ) | 0.13 |
| " Fetal-placental cocaine clearance rate was independent of dose (337 +/- 39 mL/kg/minute), indicating that it is a first-order pharmacokinetic process." | ( Ovine fetal-placental cocaine pharmacokinetics during continuous cocaine infusion. Blount, L; Chan, K; Downs, T; Kashiwai, K; Padbury, J, ) | 0.13 |
| "Fetal-placental clearance of cocaine is a rapid, first-order pharmacokinetic process." | ( Ovine fetal-placental cocaine pharmacokinetics during continuous cocaine infusion. Blount, L; Chan, K; Downs, T; Kashiwai, K; Padbury, J, ) | 0.13 |
| " This study examined the influences exerted by changes in the route of administration on pharmacokinetic parameters and drug-induced behavioral and physiological effects of cocaine." | ( Pharmacokinetics and pharmacodynamics of cocaine. Cone, EJ, 1995) | 0.29 |
| " These data may be useful in investigating the pharmacokinetic profiles of COC and CE in humans and may also help to explain the longer plasma half-life of CE relative to that of COC." | ( Cocaine- and cocaethylene-creatinine clearance ratios in humans. Bailey, DN; Bessler, JB; Sawrey, BA, ) | 0.13 |
| " These pharmacokinetic changes were not due to the changes in the rate of MAP metabolism." | ( Effects of haloperidol and cocaine pretreatments on brain distribution and kinetics of [11C]methamphetamine in methamphetamine sensitized dog: application of PET to drug pharmacokinetic study. Fujiwara, T; Funaki, Y; Hishinuma, T; Ido, T; Ishiwata, S; Itoh, M; Iwata, R; Mizugaki, M; Nakamura, H; Numachi, Y; Sato, M; Tomioka, Y; Yanai, K; Yoshida, S, 1997) | 0.3 |
| " This analytical method was designed for use in pharmacokinetic experiments studying the formation of cocaethylene following ethanol pretreatment in rats administered cocaine." | ( Quantitation of cocaine and cocaethylene in small volumes of rat whole blood using gas chromatography-mass spectrometry. Boni, RL; Burdick, JD; Fochtman, FW, 1997) | 0.3 |
| " In late September to early October, there was a pronounced peak concentration of most of the elements together with non-sea salt sulfate." | ( Springtime peaks of trace metals in Antarctic snow. Fujii, Y; Honda, K; Ikegawa, M; Itokawa, Y; Kimura, M; Makita, K, 1997) | 0.3 |
| " Pharmacokinetic analysis showed that the t(max) (observed time to maximum concentration) values for cocaine (6." | ( Concurrent pharmacokinetic analysis of plasma cocaine and adrenocorticotropic hormone in men. Cohen, BM; Kaufman, MJ; Levin, JM; Mello, NK; Mendelson, JH; Renshaw, PF; Sholar, MB; Siegel, AJ, 1998) | 0.3 |
| " There were no correlations between either maternal cocaine Cmax or AUC0-infinity and maternal and infant hair cocaine or benzoylecgonine concentrations." | ( Transplacental pharmacokinetics of cocaine and benzoylecgonine in plasma and hair of rhesus monkeys. Bailey, B; Binienda, Z; Duhart, HM; Gillam, MP; Klein, J; Koren, G; McMartin, KI; Morris, P; Paule, MG; Slikker, W, ) | 0.13 |
| "We investigated dose-response cocaine pharmacokinetic and metabolite profiles in a within-subject design after intravenous bolus cocaine administration (1-4 mg/kg) in rats under a food-limited regimen." | ( Pharmacokinetic-pharmacodynamic modeling of the psychomotor stimulant effect of cocaine after intravenous administration: timing performance deficits. Falk, JL; Foster, DM; Lau, CE; Ma, F, 1999) | 0.3 |
| " Alcohol inhibition of cocaine metabolism caused an increase in cocaine elimination half-life from 26." | ( Cocaine and alcohol interactions in the rat: effect on cocaine pharmacokinetics and pharmacodynamics. Hedaya, MA; Pan, WJ, 1999) | 0.3 |
| " There were no differences between men and women in pharmacokinetic measures [peak plasma cocaine levels (Cmax), elimination half-life (T 1/2 min), area under the curve (AUC)] or cardiovascular or subjective effects "high" measures." | ( Cocaine pharmacokinetics in men and in women during the follicular and luteal phases of the menstrual cycle. Cohen, BM; Kaufman, MJ; Levin, JM; Mello, NK; Mendelson, JH; Renshaw, PF; Sholar, MB; Siegel, AJ, 1999) | 0.3 |
| " Bolus dose cocaine administration, simultaneously with catecholamine infusion, resulted in significantly higher Cmax levels for cocaine (3." | ( Influence of infused catecholamines on the pharmacokinetics of cocaine and benzoylecgonine formation after bolus dose or continuous cocaine administration in the rat. Diaz, J; Jamdar, S; Mets, B, 1999) | 0.3 |
| " The pharmacokinetic profile of these congeners was not dose dependent when the two doses administered were compared." | ( Cocaine, norcocaine, ecgonine methylester and benzoylecgonine pharmacokinetics in the rat. Diaz, J; Jamdar, S; Mets, B; Soo, E, 1999) | 0.3 |
| " We integrated effect-time profiles of the two behaviors with concentration-time profiles simulated from our previously published pharmacokinetic parameters to derive cocaine's pharmacodynamic parameters." | ( Pharmacokinetic determinants of cocaine's differential effects on locomotor and operant behavior. Falk, JL; Lau, CE; Lobarinas, E; Nguyen, KN; Sun, L; Wang, Q; Wang, Y, 1999) | 0.3 |
| " A sigmoid-E(max) model was used to describe the brain cocaine concentration-neurochemical effect (dopamine) relationship, and an indirect pharmacodynamic response model was used to describe the plasma cocaine concentration-cardiovascular effect relationships." | ( Cocaine and alcohol interactions in the rat: effect of cocaine and alcohol pretreatments on cocaine pharmacokinetics and pharmacodynamics. Hedaya, MA; Pan, WJ, 1999) | 0.3 |
| "Two experiments examined the influence of time of day on the intravenous self-administration of cocaine and its associated pharmacokinetic profile in male Sprague-Dawley rats." | ( Characterization of cocaine self-administration and pharmacokinetics as a function of time of day in the rat. Baird, TJ; Gauvin, D, 2000) | 0.31 |
| " Blood concentration-time effect profiles of ibogaine and noribogaine obtained for individual subjects after single oral dose administrations demonstrate complex pharmacokinetic profiles." | ( Ibogaine: complex pharmacokinetics, concerns for safety, and preliminary efficacy measures. Ervin, FD; Kovera, CA; Mash, DC; Mayor, M; Pablo, J; Singleton, EG; Tyndale, RF; Williams, IC, 2000) | 0.31 |
| "The present study was conducted to investigate whether individuals with a positive family history of alcoholism (FHP) differ from individuals without a history (FHN) in their pharmacokinetic profile, subjective and physiological response to an acute intranasal dose of cocaine (0." | ( Impact of family history of alcoholism on cocaine-induced subjective effects and pharmacokinetic profile. Kouri, EM; Lukas, SE; McNeil, JF; Raga, JM, 2000) | 0.31 |
| "Oral cocaine is more effective than IV cocaine by pharmacokinetic and pharmacodynamic analysis." | ( Contribution of the active metabolite, norcocaine, to cocaine's effects after intravenous and oral administration in rats: pharmacodynamics. Falk, JL; Lau, CE; Simpao, A; Sun, L; Wang, Q, 2001) | 0.31 |
| " The present study was conducted to investigate whether nicotine pretreatment via a transdermal patch alters the behavioral, physiological, and pharmacokinetic effects of an acute dose of cocaine in nondependent human volunteers." | ( Nicotine alters some of cocaine's subjective effects in the absence of physiological or pharmacokinetic changes. Kouri, EM; Lukas, SE; Stull, M, ) | 0.13 |
| "This article outlines the main pharmacokinetic and toxicokinetic parameters of selected addicting compounds often being abused." | ( [Pharmacokinetic and toxicokinetic parameters of some drugs of abuse]. Panas, M, 2001) | 0.31 |
| " This 8-week inpatient study examined the ability of enadoline, a selective and high-efficacy kappa-agonist, and butorphanol, a mixed agonist with intermediate efficacy at both mu- and kappa-receptors, to reduce the direct pharmacodynamic effects and self-administration of intravenous cocaine in humans (n = 8)." | ( Enadoline and butorphanol: evaluation of kappa-agonists on cocaine pharmacodynamics and cocaine self-administration in humans. Bigelow, GE; Geter-Douglas, B; Strain, EC; Walsh, SL, 2001) | 0.31 |
| " A published behavioral effect was used to investigate the effects of arteriovenous serum concentration differences on pharmacodynamic estimates for the 2 mg/kg dose." | ( Arteriovenous serum cocaine concentration difference after intravenous bolus injection and constant-rate infusions: relation to pharmacodynamic estimates in rats. Lau, CE; Sun, L, 2001) | 0.31 |
| " When more than one drug is present simultaneously, the potential for drug--drug interaction exists, which can be pharmacokinetic, pharmacodynamic or both in nature." | ( The role of ketamine on plasma cocaine pharmacokinetics in rat. Abdel-Rahman, MS; Rofael, HZ, 2002) | 0.31 |
| " The validation data support the use of this method for human pharmacokinetic studies of modafinil in patients with known or suspected use of common antidepressants, psychostimulants, and drugs of abuse." | ( Chiral analysis of d- and l-modafinil in human serum: application to human pharmacokinetic studies. DeVane, CL; Donovan, JL; Malcolm, RJ; Markowitz, JS, 2003) | 0.32 |
| " Doses of cocaine, methylphenidate (MP), cocaine analogs [(+/-)-2beta-propanoyl-3beta-(2-naphthyl)-tropane (WF-23), HD-23; (+/-)-2beta-propanoyl-3beta-(2-isopropenyl)tropane (WF-60), HD-60; and 2beta-propanoyl-3beta-(4-tolyl)-tropane (HD-11, WF-11), and 2beta-propanoyl-3beta-(4-tolyl)-tropane (HD-11, WF-11), PTT], and MP analogs [(alphaR,2R)-alpha-(2-naphthalenyl)-2-piperidineacetic acid methyl ester, HDMP-28; and (alphaR,2S)-alpha-(2-naphthalenyl)-2-pyrrolideneacetic acid methyl ester, HDMP-29] that varied in their pharmacokinetic and pharmacodynamic properties were substituted for cocaine." | ( The reinforcing efficacy of psychostimulants in rhesus monkeys: the role of pharmacokinetics and pharmacodynamics. Davies, HM; France, JE; Gregg, TC; Lile, JA; Nader, MA; Wang, Z; Woolverton, WL, 2003) | 0.32 |
| " The BZT analogs displayed a > or =8-fold higher elimination half-life (4." | ( Evaluation of the blood-brain barrier transport, population pharmacokinetics, and brain distribution of benztropine analogs and cocaine using in vitro and in vivo techniques. Cao, J; Eddington, ND; Gao, H; Newman, AH; Raje, S, 2003) | 0.32 |
| " A comparison is also presented between several methods based on animal pharmacokinetic data, using the same set of proprietary compounds, and it lends further support for the use of this method, as opposed to methods that require the gathering of pharmacokinetic data in laboratory animals." | ( Prediction of human volume of distribution values for neutral and basic drugs. 2. Extended data set and leave-class-out statistics. Gao, F; Lombardo, F; Obach, RS; Shalaeva, MY, 2004) | 0.32 |
| " There were few differences in the pharmacokinetic profile of cocaine across the menstrual cycle." | ( Pharmacokinetics of intravenous cocaine across the menstrual cycle in rhesus monkeys. Evans, SM; Foltin, RW, 2004) | 0.32 |
| " The results demonstrated that the plasma elimination half-life of cocaine is nearly three times longer in males versus females." | ( Gender differences in cocaine pharmacokinetics in CF-1 mice. Abdel-Rahman, MS; Turkall, R; Visalli, T, 2005) | 0.33 |
| "The technique of microdialysis utilizing three simultaneously implanted probes in the anaesthetized rat enables monitoring of pharmacokinetic (PK) profiles of a tested drug both in blood (1st probe) and brain (2nd probe) compartments and the pharmacodynamic (PD) response of neurotransmitters (3rd probe) released into, or accumulating within the brain extracellular fluid (ECF)." | ( Application of triple-probe microdialysis for fast pharmacokinetic/pharmacodynamic evaluation of dopamimetic activity of drug candidates in the rat brain. Egestad, B; Kehr, J; Weikop, P, 2004) | 0.32 |
| "The benztropine (BZT) analogues bind with high affinity to the dopamine transporter (DAT) and demonstrate a behavioral and pharmacokinetic profile unlike that of cocaine." | ( Pharmacodynamic assessment of the benztropine analogues AHN-1055 and AHN-2005 using intracerebral microdialysis to evaluate brain dopamine levels and pharmacokinetic/pharmacodynamic modeling. Cao, J; Cornish, J; Eddington, ND; Katz, JL; Newman, AH; Raje, S, 2005) | 0.33 |
| "Human pharmacokinetic parameters are often predicted prior to clinical study from in vivo preclinical pharmacokinetic data." | ( Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure. Jolivette, LJ; Ward, KW, 2005) | 0.33 |
| " There were no significant changes in total AUC, clearance or elimination half-life of cocaine." | ( Modafinil influences the pharmacokinetics of intravenous cocaine in healthy cocaine-dependent volunteers. Chiang, CN; DeVane, CL; Donovan, JL; Elkashef, A; Malcolm, RJ; Mojsiak, J; Taylor, RM, 2005) | 0.33 |
| "This study did not find evidence for a harmful pharmacokinetic interaction between modafinil and cocaine." | ( Modafinil influences the pharmacokinetics of intravenous cocaine in healthy cocaine-dependent volunteers. Chiang, CN; DeVane, CL; Donovan, JL; Elkashef, A; Malcolm, RJ; Mojsiak, J; Taylor, RM, 2005) | 0.33 |
| " Here, we examined the pharmacokinetic profile of MDMA in squirrel monkeys after different routes of administration, and explored the relationship between acute plasma MDMA concentrations after repeated oral dosing and subsequent brain serotonin deficits." | ( Pharmacokinetic profile of single and repeated oral doses of MDMA in squirrel monkeys: relationship to lasting effects on brain serotonin neurons. Hatzidimitriou, G; Irvine, RJ; McCann, UD; Mechan, A; Ricaurte, GA; Yuan, J, 2006) | 0.33 |
| " After oral administration of DA-8159 at a dose of 30 mg/kg to rats without or with cola beverage, the pharmacokinetic parameters of DA-8159 and DA-8164 were not significantly different between two groups of rats." | ( Effects of omeprazole or cola beverage on the pharmacokinetics of oral DA-8159, a new erectogenic, in rats. Bae, SK; Kim, WB; Kwon, JW; Lee, JH; Lee, MG, 2005) | 0.33 |
| " These findings suggest that while progesterone has an impact on locomotor behavior, pharmacokinetic effects may have a limited role in mediating behavioral responses to cocaine." | ( Estrogen and progesterone affect cocaine pharmacokinetics in female rats. Akhavan, A; Festa, ED; Foltz, R; Lamm, L; Lin, SN; Niyomchai, T; Quiñones-Jenab, V, 2006) | 0.33 |
| "AHN 1-055, a benztropine (BZT) analog, binds with high affinity to the dopamine transporter (DAT), possesses behavioral, pharmacokinetic (PK) and brain microdialysate dopamine (DA) profiles distinct from cocaine." | ( Investigation of the potential pharmacokinetic and pharmaco-dynamic drug interaction between AHN 1-055, a potent benztropine analog used for cocaine abuse, and cocaine after dosing in rats using intracerebral microdialysis. Cao, J; Cornish, J; Eddington, ND; Katz, JL; Newman, AH; Raje, S, 2006) | 0.33 |
| " The period of escalating doses (EDs) is likely associated with development of tolerance to aspects of METH's pharmacologic and toxic effects but the relative contributions of pharmacokinetic and pharmacodynamic factors have not been well defined." | ( Escalating dose pretreatment induces pharmacodynamic and not pharmacokinetic tolerance to a subsequent high-dose methamphetamine binge. Cho, AK; Kuczenski, R; Lacan, G; Melega, WP; O'Neil, ML; Segal, DS, 2006) | 0.33 |
| " We therefore examined the pharmacokinetic properties of cocaine in this model." | ( Pharmacokinetic profile of cocaine following intravenous administration in the female rabbit. Levitt, P; Parlaman, JP; Stanwood, GD; Thompson, BL, 2007) | 0.34 |
| " The present study was designed to extend the understanding of the involvement of both pharmacokinetic and pharmacodynamic factors in mediating the behavioral differences among these analogs." | ( Applicability of the dopamine and rate hypotheses in explaining the differences in behavioral pharmacology of the chloro-benztropine analogs: studies conducted using intracerebral microdialysis and population pharmacodynamic modeling. Eddington, ND; Newman, AH; Othman, AA, 2007) | 0.34 |
| " pharmacokinetic data on 670 drugs representing, to our knowledge, the largest publicly available set of human clinical pharmacokinetic data." | ( Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds. Lombardo, F; Obach, RS; Waters, NJ, 2008) | 0.35 |
| "The primary aim of the current study is to test a possible pharmacokinetic explanation for the attenuated locomotor stimulation seen in adolescents." | ( Evaluation of a pharmacokinetic hypothesis for reduced locomotor stimulation from methamphetamine and cocaine in adolescent versus adult male C57BL/6J mice. Gupta, T; Rhodes, JS; Zombeck, JA, 2009) | 0.35 |
| " Developmental differences within the brain that effect pharmacodynamic properties of psychostimulants (e." | ( Evaluation of a pharmacokinetic hypothesis for reduced locomotor stimulation from methamphetamine and cocaine in adolescent versus adult male C57BL/6J mice. Gupta, T; Rhodes, JS; Zombeck, JA, 2009) | 0.35 |
| " Our data suggest that thioperamide, at least at 10 mg/kg, increases cocaine-induced locomotion through the combination of pharmacokinetic effects and the blockade of H3 receptors located on non-histaminergic neurons." | ( Effects of the H3 receptor inverse agonist thioperamide on cocaine-induced locomotion in mice: role of the histaminergic system and potential pharmacokinetic interactions. Alleva, L; Brabant, C; Grisar, T; Jatlow, P; Lakaye, B; Lin, JS; Ohtsu, H; Picciotto, MR; Quertemont, E; Tirelli, E, 2009) | 0.35 |
| " Pharmacokinetic and pharmacodynamic parameters were compared between the two treatment phases by a paired t test." | ( Pharmacodynamic evaluation of the cardiovascular effects after the coadministration of cocaine and ethanol. Laizure, SC; Parker, RB, 2009) | 0.35 |
| "We report the first pharmacokinetic data associated with a severe cocaine intoxication in a body packer, resulting in cardiac arrest." | ( Blood cocaine and metabolite pharmacokinetics after cardiac arrest in a body-packer case. Bertaux, DC; Bloch, V; de Prost, N; Mégarbane, B; Pourriat, JL; Questel, F; Rabbat, A, 2010) | 0.36 |
| "A prolonged apparent cocaine elimination half-life has been observed." | ( Blood cocaine and metabolite pharmacokinetics after cardiac arrest in a body-packer case. Bertaux, DC; Bloch, V; de Prost, N; Mégarbane, B; Pourriat, JL; Questel, F; Rabbat, A, 2010) | 0.36 |
| " The magnitude of the proportional increase in satiety threshold (agonist concentration ratio) as a function of antagonist dose should reflect the antagonist pharmacodynamic potency." | ( Using the self-administration of apomorphine and cocaine to measure the pharmacodynamic potencies and pharmacokinetics of competitive dopamine receptor antagonists. Norman, AB; Norman, MK; Tabet, MR; Tsibulsky, VL, 2011) | 0.37 |
| "These results confirm the study hypothesis that central dopamine transporter occupancy parallels peripheral pharmacokinetic findings in orally administered long-acting dexmethylphenidate in later hours after administration." | ( Understanding the central pharmacokinetics of spheroidal oral drug absorption system (SODAS) dexmethylphenidate: a positron emission tomography study of dopamine transporter receptor occupancy measured with C-11 altropane. Bonab, AA; Clarke, A; Dougherty, DD; Fischman, AJ; Martin, J; Mirto, T; Spencer, TJ, 2012) | 0.38 |
| " Here we report on effects of one such enzyme (Albu-CocH) on the pharmacokinetic and behavioral effects of cocaine in squirrel monkeys." | ( Modification of pharmacokinetic and abuse-related effects of cocaine by human-derived cocaine hydrolase in monkeys. Bergman, J; Goldberg, SR; Hallak, H; Justinova, Z; Lafleur, D; Redhi, GH; Roschke, V; Schindler, CW; Sklair-Tavron, L; Woods, D; Yasar, S, 2013) | 0.39 |
| " The validated method was applied to a pilot intravenous pharmacokinetic study in rats." | ( Determination of a highly selective mixed-affinity sigma receptor ligand, in rat plasma by ultra performance liquid chromatography mass spectrometry and its application to a pharmacokinetic study. Avery, BA; Jamalapuram, S; McCurdy, CR; Mesangeau, C; Vuppala, PK, 2012) | 0.38 |
| " In the present study, we have developed a pharmacokinetic model through a combined use of in vitro kinetic parameters and positron emission tomography data in human to examine the effects of a cocaine-metabolizing enzyme in plasma on the time course of cocaine in plasma and brain of human." | ( Modeling of pharmacokinetics of cocaine in human reveals the feasibility for development of enzyme therapies for drugs of abuse. Zhan, CG; Zheng, F, 2012) | 0.38 |
| " This study examined the behavioral and pharmacokinetic profile of the Schedule III compound phendimetrazine, which may serve as a prodrug for the N-demethylated metabolite and potent dopamine/norepinephrine releaser phenmetrazine." | ( Role of phenmetrazine as an active metabolite of phendimetrazine: evidence from studies of drug discrimination and pharmacokinetics in rhesus monkeys. Banks, ML; Blough, BE; Fennell, TR; Negus, SS; Snyder, RW, 2013) | 0.39 |
| " Parallel pharmacokinetic studies in the same monkeys examined plasma phenmetrazine and phendimetrazine levels for correlation with cocaine-like discriminative stimulus effects." | ( Role of phenmetrazine as an active metabolite of phendimetrazine: evidence from studies of drug discrimination and pharmacokinetics in rhesus monkeys. Banks, ML; Blough, BE; Fennell, TR; Negus, SS; Snyder, RW, 2013) | 0.39 |
| "The current study aimed to elucidate the role of pharmacokinetic (PK) parameters and neurotransmitter efflux in explaining variability in (±) 3, 4-methylenedioxymethamphetamine (MDMA) self-administration in rats." | ( Acquisition of MDMA self-administration: pharmacokinetic factors and MDMA-induced serotonin release. Bird, J; Bradbury, S; Colussi-Mas, J; Mueller, M; Ricaurte, G; Schenk, S, 2014) | 0.4 |
| " In dose response sessions, all doses were given 1 hr apart in ascending order for pharmacodynamic and pharmacokinetic assessment." | ( Aripiprazole effects on self-administration and pharmacodynamics of intravenous cocaine and cigarette smoking in humans. Campbell, C; Lofwall, MR; Nuzzo, PA; Walsh, SL, 2014) | 0.4 |
| " TV-1380 was found to be safe and well tolerated with a long half-life (43-77 hours) and showed a dose-proportional increase in systemic exposure." | ( Safety, pharmacokinetics, and pharmacodynamics of TV-1380, a novel mutated butyrylcholinesterase treatment for cocaine addiction, after single and multiple intramuscular injections in healthy subjects. Bassan, M; Clark, S; Cohen-Barak, O; Gilgun-Sherki, Y; Gross, A; Hettinga, J; Mendzelevski, B; Schuilenga-Hut, P; Spiegelstein, O; van de Wetering, J; Wildeman, J, 2015) | 0.42 |
| "This randomized, double-blind, placebo-controlled, parallel-group study in nondependent cocaine users was conducted to evaluate the effect of a single intramuscular dose of Albu-BChE (50, 100, and 300 mg) on the pharmacokinetic and metabolic profile of intravenous cocaine infusions (40 mg) administered at baseline and at 24, 96, and 168 hours after Albu-BChE dosing, to assess safety of coadministering Albu-BChE and cocaine, and to explore the subjective responses to cocaine infusions after Albu-BChE dosing." | ( Assessment of Pharmacokinetic and Pharmacodynamic Interactions Between Albumin-Fused Mutated Butyrylcholinesterase and Intravenously Administered Cocaine in Recreational Cocaine Users. Bassan, M; Chakraborty, B; Cohen-Barak, O; Eyal, E; Faulknor, J; Gilgun, Y; Gilgun-Serki, Y; Hallak, H; Schoedel, KA; Sellers, EM; Shram, MJ; Spiegelstein, O; Weiss, S, 2015) | 0.42 |
| " Despite the critical nature of these variables, the drug addiction field often ignores pharmacokinetic issues, which we argue can lead to false conclusions." | ( How fast and how often: The pharmacokinetics of drug use are decisive in addiction. Allain, F; Minogianis, EA; Roberts, DC; Samaha, AN, 2015) | 0.42 |
| "No controlled cocaine administration data describe cocaine and metabolite disposition in oral fluid (OF) collected with commercially-available collection devices, OF-plasma ratios, and pharmacodynamic relationships with plasma and OF cocaine and metabolite concentrations." | ( Pharmacodynamic effects and relationships to plasma and oral fluid pharmacokinetics after intravenous cocaine administration. Concheiro, M; Ellefsen, KN; Gorelick, DA; Huestis, MA; Pirard, S, 2016) | 0.43 |
| " Peak subjective effects ("Rush," "Good drug effect" and "Bad drug effect") occurred prior to peak OF cocaine concentration, whereas observed peak plasma concentrations and subjective measures occurred simultaneously, most likely due to significantly earlier plasma Tmax compared to OF Tmax." | ( Pharmacodynamic effects and relationships to plasma and oral fluid pharmacokinetics after intravenous cocaine administration. Concheiro, M; Ellefsen, KN; Gorelick, DA; Huestis, MA; Pirard, S, 2016) | 0.43 |
| "OF offers advantages as an alternative matrix to blood and plasma for identifying cocaine intake, defining pharmacokinetic parameters at different confirmation cutoffs, and aiding different drug testing programs to best achieve their monitoring goals." | ( Pharmacodynamic effects and relationships to plasma and oral fluid pharmacokinetics after intravenous cocaine administration. Concheiro, M; Ellefsen, KN; Gorelick, DA; Huestis, MA; Pirard, S, 2016) | 0.43 |
| "The pharmacokinetic profile of oral cocaine has not been fully characterized and prospective data on oral bioavailability are limited." | ( Bioavailability and Pharmacokinetics of Oral Cocaine in Humans. Coe, MA; Cone, EJ; Jufer Phipps, RA; Walsh, SL, 2018) | 0.48 |
| " Peak cocaine values did not differ according to age or sex, but cocaine half-life in brain was approximately 2 times longer in PD 5 and PD 10 rats than adults." | ( Ontogeny of cocaine-induced behaviors and cocaine pharmacokinetics in male and female neonatal, preweanling, and adult rats. Apodaca, MG; Crawford, CA; Garcia-Carachure, I; Katz, CG; McDougall, SA; Mendez, AD; Mohd-Yusof, A; Quiroz, AT; Teran, A, 2018) | 0.48 |
| "Differences in the cocaine-induced behavioral responsiveness of very young rats (PD 5 and PD 10) and adults may be attributable, at least in part, to pharmacokinetic factors; whereas, age-dependent behavioral differences between the late preweanling period and adulthood cannot readily be ascribed to cocaine pharmacokinetics." | ( Ontogeny of cocaine-induced behaviors and cocaine pharmacokinetics in male and female neonatal, preweanling, and adult rats. Apodaca, MG; Crawford, CA; Garcia-Carachure, I; Katz, CG; McDougall, SA; Mendez, AD; Mohd-Yusof, A; Quiroz, AT; Teran, A, 2018) | 0.48 |
| " Here, we ask whether such temporal pharmacokinetic factors matter, by comparing and contrasting the neuropsychological consequences of intermittent vs." | ( The transition to cocaine addiction: the importance of pharmacokinetics for preclinical models. Allain, F; Kawa, AB; Robinson, TE; Samaha, AN, 2019) | 0.51 |
| " The aim of this study was to investigate the pharmacokinetic interactions of Cola nitida and metoclopramide in rabbits." | ( The effects of oral administration of Cola nitida on the pharmacokinetic profile of metoclopramide in rabbits. Amadi, CN; Nwachukwu, WI, 2020) | 0.56 |
| " The following pharmacokinetic parameters were also decreased: area under the curve (51%), peak plasma concentration (39%), half-life (51%); while an increase in elimination rate constant (113%) and clearance rate (98%) were noted indicating rapid elimination of the drug." | ( The effects of oral administration of Cola nitida on the pharmacokinetic profile of metoclopramide in rabbits. Amadi, CN; Nwachukwu, WI, 2020) | 0.56 |
| " Initial locomotor sensitivity to COC was used as a pharmacodynamic endpoint." | ( Pharmacokinetic and pharmacodynamic analyses of cocaine and its metabolites in behaviorally divergent inbred mouse strains. Beechinor, RJ; Crona, DJ; Schorzman, AN; Tarantino, LM; Thompson, T; Weiner, DL; Zamboni, W; Zhu, J, 2021) | 0.62 |
The PK parameters of AHN 1-055 were not changed, however, the effect on DA levels was affected when cocaine was administered with AHNDA profile is affected when dosed with cocaine. These results, taken together, suggest that NaB treatment in combination with the extinction training may facilitate the extinction of the cocaine-supported memory.
| Excerpt | Reference | Relevance |
|---|---|---|
| " The effects of cocaine alone and in combination with d-amphetamine, caffeine, morphine or delta-9-tetrahydrocannabinol were determined in five male white Carneaux pigeons responding under a multiple fixed-ratio 30, fixed-interval 600 schedule (mult FR FI)." | ( The effects of cocaine in combination with other drugs of abuse on schedule-controlled behavior in the pigeon. Evans, EB; Wenger, GR, 1990) | 0.28 |
| "Effects of cocaine, alone and in combination with the dopaminergic antagonists, SCH 23390 and haloperidol were studied in squirrel monkeys trained to respond under fixed-interval schedules of electric-shock presentation." | ( Behavioral effects of cocaine alone and in combination with selective dopamine antagonists in the squirrel monkey. Katz, JL; Witkin, JM, 1991) | 0.28 |
| "Published data confirm the substantial presence of alcohol in combination with cocaine, heroin and methadone among ME cases." | ( Alcohol use in combination with cocaine, heroin and methadone by medical examiner cases. Dufour, MC; Haberman, PW; Noble, JA, 1995) | 0.29 |
| " The present study was designed to evaluate PD 128483 ((+)-4,5,5a,6,7,8-hexahydro-6-methyl-thiazolo[4,5-f]quinoline-2-amine) alone and in combination with cocaine in three behavioral paradigms." | ( Behavioral effects of the dopamine autoreceptor agonist PD 128483 alone and in combination with cocaine. Vanover, KE; Woolverton, WL, 1994) | 0.29 |
| ") was administered in combination with mazindol (0, 1 and 2 mg given orally 2 hr before the cocaine injection)." | ( Effects of cocaine alone and in combination with mazindol in human cocaine abusers. Berger, P; Bigelow, GE; Preston, KL; Sullivan, JT, 1993) | 0.29 |
| " When combined with saline, partial substitution for cocaine was seen in one of three monkeys with AJ and in none with CLZ." | ( Evaluation of the reinforcing and discriminative stimulus effects of cocaine in combination with (+)-AJ76 or clozapine. Piercey, MF; Vanover, KE; Woolverton, WL, 1993) | 0.29 |
| " The results suggest that the interactive effects of COC in combination with ETOH or MJ, after acute administration, are subtle and in need of further analyses to better understand polydrug abuse." | ( Behavioral effects of cocaine alone and in combination with ethanol or marijuana in humans. Fischman, MW; Foltin, RW; Kelly, TH; Pippen, PA, 1993) | 0.29 |
| " These results suggest that, under these conditions, relatively high levels of cocaine (120 mg/kg, SC), given alone or in combination with subteratogenic doses of ethanol late in pregnancy, are not teratogenic in mice." | ( Acute gestational cocaine exposure alone or in combination with low-dose ethanol does not influence prenatal mortality or fetal weight in mice. Becker, HC; Patrick, KS; Randall, CL; Salo, AL, ) | 0.13 |
| " The drugs 7-OH-DPAT, quinpirole and RU24213 were studied alone and in combination with cocaine for their effects on locomotor activity in non-habituated mice." | ( Dopamine 'D2-like' receptor agonists in combination with cocaine: absence of interactive effects on locomotor activity. Reggers, J; Terry, P; Tirelli, E, 1997) | 0.3 |
| "The effect of amphetamine sulfate (AMPH) on beta-phenylethylamine (PEA) and 3-methoxytyramine (3MT) levels in the rat frontal and cingulate cortices, the nucleus accumbens, and the striatum were evaluated after the administration of either cocaine or reserpine alone and in combination with AMPH." | ( Effects of the administration of amphetamine, either alone or in combination with reserpine or cocaine, on regional brain beta-phenylethylamine and dopamine release. Karoum, F; Mosnaim, AD; Wolf, ME, ) | 0.13 |
| "The effects of the dopamine transporter (DAT) inhibitors cocaine and GBR12909 on DAT and dopamine D(2) receptors were evaluated in the brains under awake and isoflurane-anesthetized monkeys using high-resolution positron emission tomography (PET) in combination with microdialysis." | ( Isoflurane anesthesia enhances the inhibitory effects of cocaine and GBR12909 on dopamine transporter: PET studies in combination with microdialysis in the monkey brain. Harada, N; Kakiuchi, T; Nakanishi, S; Nishiyama, S; Ohba, H; Sato, K; Tsukada, H, 1999) | 0.3 |
| "The dose-response and duration effects of acute administration of the dopamine transporter (DAT) blocker cocaine and GBR12909 on dopamine synthesis and transporter availability were evaluated in the brains of conscious monkeys using high-resolution positron emission tomography (PET) in combination with microdialysis." | ( Dose-response and duration effects of acute administrations of cocaine and GBR12909 on dopamine synthesis and transporter in the conscious monkey brain: PET studies combined with microdialysis. Harada, N; Kakiuchi, T; Nishiyama, S; Ohba, H; Tsukada, H, 2000) | 0.31 |
| "The effects of ketamine, a noncompetitive antagonist of NMDA receptors, on the striatal dopaminergic system were evaluated multiparametrically in the monkey brain using high-resolution positron emission tomography (PET) in combination with microdialysis." | ( Ketamine decreased striatal [(11)C]raclopride binding with no alterations in static dopamine concentrations in the striatal extracellular fluid in the monkey brain: multiparametric PET studies combined with microdialysis analysis. Fukumoto, D; Harada, N; Kakiuchi, T; Nishiyama, S; Ohba, H; Sato, K; Tsukada, H, 2000) | 0.31 |
| " The effects of ethanol combined with cocaine on the exocrine pancreas are not known." | ( Ethanol combined with cocaine inhibits amylase release in guinea pig pancreatic lobules. Antonilli, L; Linari, G; Nencini, P; Nucerito, V, 2001) | 0.31 |
| " Since cocaine-dependent subjects might use cocaine during a clinical trial with modafinil, this study tested the safety of intravenous cocaine (30 mg) in combination with modafinil." | ( Modafinil and cocaine: a double-blind, placebo-controlled drug interaction study. Cornish, JW; Dackis, CA; Kampman, KM; Lynch, KG; O'Brien, CP; Poole, S; Rowan, A; Samaha, FF; White, L; Yu, E, 2003) | 0.32 |
| " Thus, oral MPH-SR is safe in combination with repeated cocaine doses and decreases some of the positive and reinforcing effects of cocaine in cocaine abusers with ADHD." | ( Response to cocaine, alone and in combination with methylphenidate, in cocaine abusers with ADHD. Collins, SL; Evans, SM; Foltin, RW; Kleber, HD; Levin, FR, 2006) | 0.33 |
| "The PK parameters of AHN 1-055 were not changed, however, the effect on DA levels was affected when cocaine was administered with AHNDA profile is affected when dosed with cocaine." | ( Investigation of the potential pharmacokinetic and pharmaco-dynamic drug interaction between AHN 1-055, a potent benztropine analog used for cocaine abuse, and cocaine after dosing in rats using intracerebral microdialysis. Cao, J; Cornish, J; Eddington, ND; Katz, JL; Newman, AH; Raje, S, 2006) | 0.33 |
| " However, a PM phenotype could also be caused by drug-drug interactions with CYP2D6 inhibitors or substrates such as the co-consumed cocaine and diltiazem and/or diltiazem metabolites, respectively." | ( Proof of a 1-(3-chlorophenyl)piperazine (mCPP) intake: use as adulterant of cocaine resulting in drug-drug interactions? Paul, LD; Roider, G; Rolf, B; Schmid, D; Staack, RF, 2007) | 0.34 |
| " When given in combination with cocaine, EKC produced effects that were sub-additive, suggesting that the kappa agonists may be used safely as cocaine abuse treatments." | ( Effects of kappa opioid agonists alone and in combination with cocaine on heart rate and blood pressure in conscious squirrel monkeys. Bergman, J; Gilman, JP; Goldberg, SR; Graczyk, Z; Mello, NK; Negus, SS; Schindler, CW, 2007) | 0.34 |
| "The objective of this study was to evaluate possible changes caused by multiple cocaine administration, alone and in combination with 1,4-dihydropiridine calcium channel blocker nifedipine, on cytochrome P450 levels both in the brain and liver." | ( Changes in liver and brain cytochrome p450 after multiple cocaine administration, alone and in combination with nifedipine. Mitcheva, M; Vitcheva, V, 2007) | 0.34 |
| "Data ascertained in a study of club drug use among 450 gay and bisexual men indicate that at least one class of PDE-5 (phosphodiesterase type 5 inhibitor, sildenafil [Viagra]) is used frequently in combination with club drugs such as methamphetamine, MDMA (3,4 methylenedioxymethamphetamine [ecstasy]), ketamine, cocaine, and GHB (gamma hydroxy butyrate)." | ( Sildenafil (Viagra) and club drug use in gay and bisexual men: the role of drug combinations and context. Green, KA; Halkitis, PN, 2007) | 0.34 |
| " Indeed, there are numerous commonly prescribed drugs with significant carboxylesterase-mediated metabolism such as enalapril, lovastatin, irinotecan, clopidogrel, prasugrel, methylphenidate, meperidine, and oseltamivir that may interact with ethanol." | ( The effect of ethanol on oral cocaine pharmacokinetics reveals an unrecognized class of ethanol-mediated drug interactions. Laizure, SC; Parker, RB, 2010) | 0.36 |
| " After acquiring the discrimination, the effects of cocaine (0, 25, 50, 100 and 200 mg) administered alone and in combination with aripiprazole (15 mg) were determined." | ( Discriminative stimulus, subject-rated and cardiovascular effects of cocaine alone and in combination with aripiprazole in humans. Glaser, PE; Hays, LR; Lile, JA; Rush, CR; Stoops, WW, 2011) | 0.37 |
| "The present study examined if the decreases in cocaine self-administration are due to competition from excess behavioral activity (hyperlocomotion or stereotypy) induced by the BZT analogs alone or in combination with cocaine." | ( The stereotypy-inducing effects of N-substituted benztropine analogs alone and in combination with cocaine do not account for their blockade of cocaine self-administration. Hayashi, S; Hiranita, T; Katz, JL; Li, L; Newman, AH, 2013) | 0.39 |
| " Further, the BZT analogs alone had minimal effects on locomotor activity and stereotypies and did not appreciably change the effects of cocaine on these measures when administered in combination with cocaine." | ( The stereotypy-inducing effects of N-substituted benztropine analogs alone and in combination with cocaine do not account for their blockade of cocaine self-administration. Hayashi, S; Hiranita, T; Katz, JL; Li, L; Newman, AH, 2013) | 0.39 |
| " Thus, changes in CB1r function - alone and in combination with cocaine - affected stereotyped vigilance-related behaviors in this NHP, further implicating the eCB system in the neurobiological mechanisms of cocaine addiction." | ( Cannabinoid type-1 receptor ligands, alone or in combination with cocaine, affect vigilance-related behaviors of marmoset monkeys. Barros, M; Cagni, P; de Jesus, AG; Melo, GC, 2014) | 0.4 |
| "The objectives of this study are to determine whether ISO alters conditioned place preference (CPP) for cocaine when combined with a social cue and to determine whether ISO alters the effects of cocaine when combined with social cue on nucleus accumbens shell (NAcS) dopamine (DA) and serotonin (5-HT)." | ( Effects of cocaine combined with a social cue on conditioned place preference and nucleus accumbens monoamines after isolation rearing in rats. Bland, ST; Goodell, DJ; Grotewold, SK; Hayter, C; Wall, VL, 2014) | 0.4 |
| " The goal of this study was to investigate the reinforcing effects of quetiapine alone and in combination with intravenous cocaine in monkeys." | ( Evaluation of the Reinforcing Effect of Quetiapine, Alone and in Combination with Cocaine, in Rhesus Monkeys. Brutcher, RE; Nader, MA; Nader, SH, 2016) | 0.43 |
| " These results, taken together, suggest that NaB treatment in combination with the extinction training may facilitate the extinction of the cocaine-supported memory." | ( Effects of Sodium Benzoate Treatment in Combination with An Extinction Training on the Maintenance of Cocaine-Supported Memory. Cherng, CG; Liao, TY; Lin, JK; Tsai, YN; Tzeng, WY; Wu, HH; Yu, L, 2016) | 0.43 |
| " Changes in PO deaths in combination with other psychoactive substances may provide a partial explanation." | ( Increases from 2002 to 2015 in prescription opioid overdose deaths in combination with other substances. Griesler, P; Hu, MC; Kandel, DB; Wall, M, 2017) | 0.46 |
| " We calculated (1) changes in proportions of deaths in combination with benzodiazepines, antidepressants, heroin, alcohol, cocaine between the two periods, and (2) proportions of increase in deaths attributable to each substance among PO and synthetic opioids other than methadone (SO-M) deaths, by age, gender, race/ethnicity." | ( Increases from 2002 to 2015 in prescription opioid overdose deaths in combination with other substances. Griesler, P; Hu, MC; Kandel, DB; Wall, M, 2017) | 0.46 |
| " The largest increases occurred in combination with heroin among all PO (4." | ( Increases from 2002 to 2015 in prescription opioid overdose deaths in combination with other substances. Griesler, P; Hu, MC; Kandel, DB; Wall, M, 2017) | 0.46 |
| "Increased PO overdose deaths over the last decade may be partially explained by increased deaths in combination with other psychoactive substances." | ( Increases from 2002 to 2015 in prescription opioid overdose deaths in combination with other substances. Griesler, P; Hu, MC; Kandel, DB; Wall, M, 2017) | 0.46 |
| " We report herein, for the first time, a new strategy using the noncompetitive assay format via a biomimetic material, namely, poly(p-phenylene) β-cyclodextrin poly(ethylene glycol) (PPP-CD-g-PEG) combined with gold nanoparticle (AuNP) conjugates as the labeling agent to recognize the target cocaine molecule in the test zone." | ( Mobile Phone Sensing of Cocaine in a Lateral Flow Assay Combined with a Biomimetic Material. Arslan, M; Coskunol, H; Guler, E; Gumus, ZP; Timur, S; Yagci, Y; Yilmaz Sengel, T, 2017) | 0.46 |
| " ii) Drug-drug interactions, which come out from clinical evidences as the case of CYP450 family enzyme inhibitors or inductors modulating cocaine toxicity." | ( Drug-Drug Interactions in Cocaine-users and their Clinical Implications. Caroleo, MC; Cione, E; De Sarro, G; Gallelli, L; Gratteri, S; Seminara, P; Siniscalchi, A; Sirico, S, 2017) | 0.46 |
| " Additionally, it has been reported that serum levels of lithium and warfarin were decreased and their efficacy reduced when simultaneously administered with CCDs." | ( Drug interactions of cola-containing drinks. Emami, SA; Johnston, TP; Moghadam, AT; Mohammadpour, AH; Nomani, H; Sahebkar, A, 2019) | 0.51 |
| " Synthetic cathinones are frequently consumed in combination with other drugs of abuse." | ( Bath salts and polyconsumption: in search of drug-drug interactions. Lopez-Rodriguez, AB; Viveros, MP, 2019) | 0.51 |
| "Spectroscopic techniques combined with chemometrics are a promising tool for analysis of seized drug powders." | ( Comparison of Spectroscopic Techniques Combined with Chemometrics for Cocaine Powder Analysis. Baeten, V; Dardenne, P; De Wael, K; Eliaerts, J; Meert, N; Pierna, JF; Samyn, N; Van Durme, F, 2020) | 0.56 |
Cocaine acts by altering DA bioavailability by targeting the DAT. Initial absorption rate was rapid and, on average, the peak levels of cocaine were achieved in 10 min. Cocaine pretreatment significantly increased cocaine bioavailability, absorption rate constant, TBC, and the formation clearance of cocaethylene.
We employed a typical cocaine dosing paradigm and assessed tyrosine hydroxylase immunoreactive varicosities in five different areas of the nucleus accumbens shell. The ability of (+/-)-1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane (DOI) and ketanserin, a 5-HT(2A) receptor antagonist, to either substitute for or block the discriminative-stimulus effects of cocaine was evaluated.
| Excerpt | Relevance | Reference |
|---|---|---|
| " The l-NE dose-response curve could be resolved into two components S-shaped curves: the first had an ED50 OF 10(-5) M and reached a plateau at 10(-4) M; the second component continued above 10(-3) M without reaching a plateau." | ( Pharmacological characterization of adrenergic receptors of a rabbit cerebral artery in vitro. Bevan, JA; Duckles, SP, 1976) | 0.26 |
| " Cocaine or phentolamine shifted the dose-response curve to the left." | ( Effects of ethylephrine on the rat atrial pacemaker. Aramendía, P; De Mikulic, LE; Márquez, MT, 1977) | 0.26 |
| ", total dose) did not modify the dose-response curve to 5-HT except for the lowest dose." | ( Analysis of the contractile effect of 5-hydroxytryptamine on the isolated posterior communicating artery of the cat. Gómez, B; Lluch, S; Marco, EJ; Marín, J; Salaices, M, 1979) | 0.26 |
| " Values of KA and A50 were calculated from dose-response curves obtained for three alpha-adrenergic agonists (phenylephrine, methoxamine and norepinephrine) in the presence and absence of partial irreversible blockade by phenoxybenzamine." | ( Determination of the stimulus-response relation for three alpha-adrenergic agonists on rabbit aorta. Gero, A; Raffa, RB; Tallarida, RJ, 1979) | 0.26 |
| " The dose-response function of cocaine on lever choice was then determined." | ( Cocaine as a discriminative stimulus for responding maintained by food in squirrel monkeys. Trost, RC; Woolverton, WL, 1978) | 0.26 |
| " With the 3-h time-out the dose-breaking point function on the PR schedule was similar to the dose-response rate function on the FR schedule." | ( Progressive ratio and fixed ratio schedules of cocaine-maintained responding in baboons. Bradford, LD; Brady, JV; Griffiths, RR, 1979) | 0.26 |
| " No acitvity was detected in other brain areas at various dosed or incubation times." | ( Effects of kainic acid, a cyclic analogue of glutamic acid, on cyclic nucleotide accumulation in slices of rat cerebellum. Molloy, BB; Ryan, JJ; Schmidt, MJ, 1976) | 0.26 |
| " To evaluate this possibility, the authors devised a technique for determining the minimal arrhythmic dosage of epinephrine that permitted graded assessment of changes in the sensitivity of the heart to epinephrine-induced arrhythmias." | ( Effects of pharmacologic alterations of adrenergic mechanisms by cocaine, tropolone, aminophylline, and ketamine on epinephrine-induced arrhythmias during halothane-nitrous oxide anesthesia. Koehntop, DE; Liao, JC; Van Bergen, FH, 1977) | 0.26 |
| " Lecithinase production of the isolated strains in Kitt-Tarozi bouillon, Following 18-20 hour-long cultivation at 37 degrees C is studied, and dosed within limits ranging from 5 to 100 DMO." | ( [Distribution of Cl. perfringens in preserved food and the lecithinase activity of isolated strains]. Beleva, S; Kozareva, M, 1977) | 0.26 |
| " Propranolol (3 X 10(-8) and 10(-7) M) provoked a shift to the right of the dose-response curve for dobutamine." | ( Response of the atrial pacemaker to dobutamine. Aramendía, P; Márquez, MT; Puntoni de Mikulić, LE, 1977) | 0.26 |
| "0 Hz, the log dose-response curve for the positive inotropic effect of epinine was displaced to the left, whereas the maximum of the developed tension was not changed." | ( Studies on the mechanism of the positive inotropic action evoked by epinine on the rabbit isolated papillary muscle at different rates of beating. Brodde, OE; Motomura, S; Schümann, HJ, ) | 0.13 |
| "Using measures of locomotor activity and stereotypy, dose-response curves to several psychomotor stimulant drugs were obtained on rats reared in deprived or normal environments." | ( The effects of psychomotor stimulants on stereotypy and locomotor activity in socially-deprived and control rats. Iversen, SD; Morgan, MJ; Robbins, TW; Sahakian, BJ, 1975) | 0.25 |
| " A linear dose-response relationship was observed for the suppressive effect of cocaine on the AD." | ( Cocaine and pseudococaine: comparative effects on electrical after-discharge in the limbic system of cats. Matsuzaki, M; Misra, AL, ) | 0.13 |
| " Cocaine (2 x 10(-6) M and 10(-5) M) produced 2 and 7 fold shifts to the left of the dose-response curve to (-)-noradrenaline recorded isotonically in isolated splenic capsular strips of the cat." | ( Investigation of the role of calcium in the supersensitivity produced by cocaine in cat spleen strips. Summers, RJ; Tillman, J, 1979) | 0.26 |
| " Low concentrations of (--)-cocaine or its stereoisomer, (4)-pseudococaine, produced shifts to the right of the 5-HT dose-response curves on heart and ileum with no depression of the maximum responses to electrical stimulation or dimethylphenylpiperazinium remained unaffected." | ( Blockade of serotonin receptors on autonomic neurones by (-)-cocaine and some related compounds. Fozard, JR; Mobarok Ali, AT; Newgrosh, G, 1979) | 0.26 |
| " Dose-response curves and ED50 values were then determined in brief test sessions when no responses were reinforced." | ( Comparison of the discriminative stimulus properties of cocaine and amphetamine in rats. D'Mello, GD; Stolerman, IP, 1977) | 0.26 |
| " Propranolol (10(-8) and 10(-7) M) produced a parallel shift to the right in the log dose-response curves of ethylephrine with no decrease in the maximal response, indicating that the antagonism was competitive." | ( Positive inotropic effect of ethylephrine on the isolated rat atria. Aramendía, P; Márquez, MT; Puntoni de Mikulić, LE, 1977) | 0.26 |
| " dosage per injection, of 50 and 100 mug/kg resulted in self-administration rates significantly greater than that which occurred with saline." | ( Mazindol self-administration in the rhesus monkey. Schuster, CR; Wilson, MC, 1976) | 0.26 |
| " Dose-response differences were also revealed in "breaking point" comparisons between secobarbital on the one hand, and methylphenidate and cocaine, on the other." | ( Behavioral procedures for evaluating the relative abuse potential of CNS drugs in primates. Brady, JV; Griffiths, RR, 1976) | 0.26 |
| " Statistically significant increases in body temperature, respiration rate and heart rate occurred only after the largest dosage tested." | ( Acute pharmacological activity of intravenous cocaine in the rhesus monkey. Bedford, JA; Buelke, J; Kibbe, AH; Wilson, MC, 1976) | 0.26 |
| " Dose-response curves for stimulant agonists were obtained in isolated vasa deferentia which were depolarized by a K-rich, Na-free solution." | ( The effects of denervation, cocaine, 6-hydroxydopamine and reserpine on the characteristics of drug-induced contractions of the depolarized smooth muscle of the rat and guinea-pig vas deferens. Westfall, DP, 1977) | 0.26 |
| " Both drugs also shift to the left the dose-response curves for noradrenaline and adrenaline on isolated strips, cocaine being most potent." | ( Uptake and release of catecholamines in sympathetic nerve fibres in the spleen of the cod, Gadus morhua. Holmgren, S; Nilsson, S, 1976) | 0.26 |
| " The maximum level of concentration in the blood was seen within 4 hr after administration of Li2CO3, and a greater part of the orally dosed Li2CO3 was excreted into the urine." | ( [Pharmacokinetics and general pharmacological actions of lithium salts administered singly or repeatedly]. Aihara, H; Akiyama, F; Nozu, T; Ozawa, H; Sasajima, M, 1976) | 0.26 |
| " For higher initial contractions relaxation is slowed during the first minute of wash out, probably because of the sigmoid shape of the dose-response curve." | ( Relaxation of splenic strips during wash out with amine-free solution after an exposure to noradrenaline. Lindmark, E; Schlör, G; Trendelenburg, U, 1976) | 0.26 |
| "Changes in bath temperature caused changes in the adrenergic responsiveness of rabbit iris dilator muscle as indicated by shifts in dose-response curves along the log axis and changes in maximum responses." | ( Role of neuronal and extraneuronal factors in temperature mediated responsiveness of adrenoceptors. Ahlquist, RP; Matheny, JL, 1976) | 0.26 |
| " For example, intermittent application of a particular dosage results in lower blood levels, and allowing sufficient time between doses reduces the amount necessary to obtain the desired anesthesia." | ( Local anesthesia in otolaryngology. A re-evaluation. Schenck, NL, ) | 0.13 |
| " Dose-response curves to norepinephrine were shifted to the left along the log dose axis (enhanced potency) and the maximum degree of contraction that could be elicited was increased." | ( Influence of temperature and cocaine on responses of the isolated mouse vas deferens to adrenergic amines. Bohuski, K; Buckner, CK; Ryan, CF, 1975) | 0.25 |
| " Treatment of the strips with 5-HK in concentrations higher than 2 X 10- minus 6 M shifted the dose-response curve of serotonin to the right and downward." | ( Analysis of the effect of 5-hydroxykynurenamine,, a serotonin metabolite, on isolated cerebral arteries, aortas and atria. Toda, N, 1975) | 0.25 |
| " For the inhibition of the hypotensive action of clonidine by protriptyline a parallel shift of the dose-response curve was obtained, indicating the possibility of a competitive antagonism." | ( Interaction between centrally acting hypotensive drugs and tricyclic antidepressants. van Zwieten, PA, 1975) | 0.25 |
| " The sympathetic denervation did not influence the dose-response curve obtained with acetylcholine, supporting the specific nature of the supersensitivity reaction only to the sympathetic transmitter." | ( Sympathetic innervation of cerebral arteries: prejunctional supersensitivity to norepinephrine after sympathectomy or cocaine treatment. Aubineau, P; Edvinsson, L; Owman, C; Sercombe, R; Seylaz, J, ) | 0.13 |
| " Seven days after pretreatment with 6-hydroxydopamine there is a shift to the left and increase in maxima of the dose-response curves for norepinephrine and methoxamine." | ( The effect of pretreatment with 6-hydroxydopamine on the norepinephrine concentration and sensitivity of the rat vas deferens. Fedan, JS; Westfall, DP, ) | 0.13 |
| " In the present study, log dose-response lines were obtained for dl-isoprenaline (ISO), l-adrenaline (ADR) l-noradrenaline (NOR), salbutamol (SALB), and orciprenaline on isolated tracheal chains prepared from both the laryngeal (L) and bronchial (B) ends of the trachea." | ( The effect of cocaine on the responses of the differently innervated laryngeal and bronchial ends of the guinea pig trachea in vitro to clinically used bronchodilators. Hamilton, JT; Jones, TR; Lefcoe, NM, 1975) | 0.25 |
| " In dose-response studies on the aortic strip, trans-metanicotine was significantly less active than nicotine." | ( Nicotine-like actions of cis-metanicotine and trans-metanicotine. Bowman, ER; Chang, RS; McKennis, H; Wilson, KL, 1976) | 0.26 |
| " Adult male rats were injected with cocaine (15 mg/kg, IP) once daily for 14 days, followed by a dose-response challenge with cocaine (1-15 mg/kg, IP) either 18 hours or 7 days after the final pretreatment injection." | ( Neuroendocrine responses to cocaine do not exhibit sensitization following repeated cocaine exposure. Alvarez Sanz, MC; Kerr, JE; Levy, AD; Li, Q; Rittenhouse, PA; Van de Kar, LD, 1992) | 0.28 |
| " The dose-response curves of this tonic block of peak Na+ currents by (-)/(+) cocaine and (-)/(+) bupivacaine were well fitted by the Langmuir isotherm, suggesting that one LA isomer blocked one Na+ channel." | ( Altered stereoselectivity of cocaine and bupivacaine isomers in normal and batrachotoxin-modified Na+ channels. Wang, GK; Wang, SY, 1992) | 0.28 |
| ") of cocaine on the fifth day, which was demonstrated by parallel shifting of the dose-response and time-effect curves of the test doses of cocaine." | ( Oxytocin modulates behavioural adaptation to repeated treatment with cocaine in rats. Babarczy, E; Bíró, E; Kovács, GL; Kriván, M; Laczi, F; Sarnyai, Z; Szabó, G; Telegdy, G; Vecsernyés, M, 1992) | 0.28 |
| " Each pretreatment produced a statistically significant increase in cocaine lethality throughout the dose-response curve." | ( Decreased plasma cholinesterase activity enhances cocaine toxicity in mice. Goldfrank, LR; Henry, GC; Hoffman, RS; Howland, MA; Wax, PM; Weisman, RS, 1992) | 0.28 |
| " The CSF-to-plasma ratios for cocaine were quite similar to each other over the dosage range of cocaine that was administered; however, the CSF-to-plasma ratios for benzoylecgonine decreased as the concentrations of benzoylecgonine increased in plasma and CSF." | ( The presence of cocaine and benzoylecgonine in rat cerebrospinal fluid after the intravenous administration of cocaine. Barbieri, EJ; DiGregorio, GJ; Ferko, AP; Ruch, EK, 1992) | 0.28 |
| " Hair samples were also taken continually after the dosing was stopped until the presence of cocaine and benzoylecgonine were no longer detected in hair." | ( The accumulation and disappearance of cocaine and benzoylecgonine in rat hair following prolonged administration of cocaine. Barbieri, EJ; DiGregorio, GJ; Ferko, AP; Ruch, EK, 1992) | 0.28 |
| " PCPA pretreatment shifted the cocaine dose-response curve to the right and blocked the ability of zacopride to reverse cocaine-induced activity." | ( 5-HT3 receptor antagonists block cocaine-induced locomotion via a PCPA-sensitive mechanism. Hitzemann, R; Svingos, AL, 1992) | 0.28 |
| " In further in vivo voltammetric studies, the effects of SC cocaine on synaptic concentrations of DA and 5-HT were studied in the chloral hydrate-anesthetized paradigm in two neuroanatomic substrates, NAcc and mesoaccumbens somatodendrites, the ventral tegmental area (VTA-A10), in a dose-response fashion (10, 20, and 40 mg/kg) in six separate studies." | ( Distinguishing effects of cocaine i.v. and SC on mesoaccumbens dopamineand serotonin release with chloral hydrate anesthesia. Broderick, PA, 1992) | 0.28 |
| " Prolonged use of benzodiazepines can lead to drug dependence; successful withdrawal involves gradual dosage reduction." | ( Pharmacologic considerations in the treatment of substance abuse. Skinner, MH; Thompson, DA, 1992) | 0.28 |
| " In testing the discriminative stimulus performance of five male CP and five male CNP rats, the learning rates and dose-response relationship to cocaine were not significantly different between these two groups." | ( Rats bred for differences in preference to cocaine: other behavioral measurements. Schechter, MD, 1992) | 0.28 |
| "3-3 mg/kg); the former effect was not dose dependent (bell-shaped dose-response curve), whereas the latter effect was dose-dependent." | ( Cardiovascular effects of cocaine in conscious rats: relative significance of central sympathetic stimulation and peripheral neuronal monoamine uptake and release mechanisms. Goldberg, SR; Schindler, CW; Tella, SR, 1992) | 0.28 |
| "The time course of cocaine-induced changes in self-stimulation thresholds were used to evaluate cocaine euphoria and dysphoria as a function of the chronicity of drug treatment, dosage level, and the spacing of injections." | ( Cocaine euphoria, dysphoria, and tolerance assessed using drug-induced changes in brain-stimulation reward. Frank, RA; Kokoris, D; Manderscheid, PZ; Panicker, S; Williams, HP, 1992) | 0.28 |
| " When the FR for cocaine was differentially increased, the frequency of cocaine choice decreased, shifting the cocaine dose-response function to the right and/or downward." | ( Effects of increasing response requirement on choice between cocaine and food in rhesus monkeys. Nader, MA; Woolverton, WL, 1992) | 0.28 |
| "The complex dose-response relationship by which cocaine (Coc) directly precipitates unfavorable cardiac consequences are not known." | ( A primary culture system of adult rat heart cells for the evaluation of cocaine toxicity. Welder, AA, 1992) | 0.28 |
| " In the pair-fed controls, or rats withdrawn from the smaller dosage of either ethanol or cocaine, the test dose of saline or cocaine did not elicit the PTZ-stimulus; only 30% of rats selected the PTZ-appropriate level at the highest dose of cocaine tested (10 mg/kg)." | ( Protracted withdrawal: sensitization of the anxiogenic response to cocaine in rats concurrently treated with ethanol. Lal, H; Prather, PL, 1992) | 0.28 |
| " In addition, the effect of ITI length on the dose-response curve for pentobarbital, phencyclidine, D-amphetamine, and cocaine were determined." | ( Titrating matching-to-sample performance: effects of drugs of abuse and intertrial interval. Kimball, KA; Wenger, GR, 1992) | 0.28 |
| " Dose-response curves were similar for all three treatments on the first test, but diverged markedly on subsequent tests." | ( Differential effects of injection regimen on behavioral responses to cocaine. Terry, P, 1992) | 0.28 |
| " In both groups, a urine sample was collected before dosing and at regular intervals afterwards." | ( Effect of intranasal cocaine on the urine drug screen for benzoylecgonine. Otto, RA; Reichman, OS, 1992) | 0.28 |
| "25-5 mg/kg) did not alter the cocaine dose-response curve." | ( Effects of the putative dopamine autoreceptor antagonists (+)-AJ 76 and (+)-UH 232 on the discriminative stimulus properties of cocaine. Callahan, PM; Cunningham, KA; Piercey, MF, 1992) | 0.28 |
| " The dose-response relationship of cocaine with fetal development was established in CF-1 mice by administering cocaine sc on days 5 to 18 of gestation followed by teratologic evaluation." | ( Antagonism of cocaine-induced fetal anomalies by prazosin and diltiazem in mice. Hitner, HW; Mahalik, MP, 1992) | 0.28 |
| "5, 5, 10 or 15 g/kg for 6 wk followed, for some dose groups, by a 2-wk withdrawal period, and then re-initiation of dosing for another 2 wk." | ( Toxicity and carcinogenicity studies of Caramel Colour IV in F344 rats and B6C3F1 mice. Boysen, BG; Chappel, CI; Emerson, JL; Field, WE; MacKenzie, KM; Petsel, SR; Stanley, J, 1992) | 0.28 |
| " Methodologic weaknesses of opiate animal models, especially with respect of appropriate dosing schedules, have hampered meaningful extrapolation of these studies to human risk assessment." | ( Animal models of opiate, cocaine, and cannabis use. Dow-Edwards, D; Hutchings, DE, 1991) | 0.28 |
| " dosage of 5 mg/kg, cocaine was nonlethal, although a reduction in VE was evident during the first minute after dosing." | ( Effects of adrenergic antagonists on cocaine-induced changes in respiratory function. Culp, DA; Francomacaro, DV; Murphy, DJ; Walker, ME, 1991) | 0.28 |
| " Throughout pregnancy, the dams that received cocaine gained approximately 15% less weight than the untreated controls, but none of the dosage procedures affected the size of the litters, or the weight and growth of the offspring." | ( Elicitation and modification of the acoustic startle reflex in animals prenatally exposed to cocaine. Foss, JA; Riley, EP, ) | 0.13 |
| " Rats in one control group were pair-fed to the cocaine group and injected with the saline vehicle during the dosing period, while an untreated control group was simply weighed throughout pregnancy." | ( Failure of acute cocaine administration to differentially affect acoustic startle and activity in rats prenatally exposed to cocaine. Foss, JA; Riley, EP, ) | 0.13 |
| " The oral dosage of cocaine produced some maternal lethality and reduced maternal weight gain throughout the pregnancy by approximately 12%." | ( Exploratory behavior and locomotor activity: a failure to find effects in animals prenatally exposed to cocaine. Foss, JA; Riley, EP, ) | 0.13 |
| "5 mg/kg/infusion), and shifted the dose-response curve for cocaine self-administration to the right." | ( GR38032F, a serotonin 5-HT3 antagonist, fails to alter cocaine self-administration in rats. Peltier, R; Schenk, S, 1991) | 0.28 |
| " When milk intake was stable, dose-response functions were determined for cocaine (4." | ( Attenuation of the effects of cocaine on milk consumption in rats by dopamine antagonists. Rapoza, D; Woolverton, WL, 1991) | 0.28 |
| " The change in sensitivity was characterized by a leftward shift of the dose-response curve without a change in maximum response." | ( Specific supersensitivity of the mesenteric vascular bed of Dahl salt-sensitive rats. Fleming, WW; Kong, JQ; Kotchen, TA; Taylor, DA, 1991) | 0.28 |
| " Nonsustained monomorphic ventricular tachycardia occurred spontaneously in two dogs, and sustained ventricular tachycardia could be induced by programmed stimulation at the end of the dosing protocol in five of 11 animals." | ( Hemodynamic and electrophysiological actions of cocaine. Effects of sodium bicarbonate as an antidote in dogs. Bauman, JL; Beckman, KJ; Gallastegui, JL; Hariman, RJ; Javaid, JI; Parker, RB, 1991) | 0.28 |
| " Mean plasma concentration of desipramine in a subsample of our subjects was less than that recommended for treatment of depression, thus the dosage of desipramine may have been subtherapeutic." | ( Comparison of amantadine and desipramine combined with psychotherapy for treatment of cocaine dependence. Brown, BS; Haertzen, CA; Hess, JM; Jaffe, JH; Kolar, AF; Mahaffey, JR; Weddington, WW, 1991) | 0.28 |
| " Endogenous sex steroid levels were altered in mice via gonadectomy, via physiological or supraphysiological doses of testosterone and/or estradiol, and via tamoxifen dosing to antagonize estrogens." | ( Effect of sex steroids on cocaine lethality in male and female mice. Davis, WM; Dickerson, GA; Waters, IW; Wilson, MC, 1991) | 0.28 |
| " For rats that sustained a 70% depletion of dopamine in the medial prefrontal cortex, the dose-response curve was an inverse function across the entire dose range tested." | ( Supersensitivity to the reinforcing effects of cocaine following 6-hydroxydopamine lesions to the medial prefrontal cortex in rats. Horger, BA; Peltier, R; Schenk, S; Shelton, K, 1991) | 0.28 |
| " An examination of the descending limb of the dose-response functions revealed that lowered response rates for cocaine and ketamine were correlated with increases in run time and small and inconsistent effects on postreinforcement pause time." | ( Analysis of fixed-ratio behavior maintained by drug reinforcers. Skjoldager, P; Winger, G; Woods, JH, 1991) | 0.28 |
| " Drug interactions were studied by redetermining the cocaine dose-response curve in the presence of various fixed doses of the other drugs." | ( The effects of cocaine in combination with other drugs of abuse on schedule-controlled behavior in the pigeon. Evans, EB; Wenger, GR, 1990) | 0.28 |
| "0 micrograms) inhibited the cocaine-induced hyperactivity in an U-shaped dose-response manner." | ( Oxytocin attenuates the cocaine-induced exploratory hyperactivity in mice. Kovács, GL; Sarnyai, Z; Szabó, G; Telegdy, G, ) | 0.13 |
| " The dose-response relationships of norepinephrine and sympathetic nerve stimulation were enhanced by 10(-6) M cocaine in control muscles; this did not occur in muscles from reserpine pretreated ferrets." | ( Effects of cocaine on excitation-contraction coupling of aortic smooth muscle from the ferret. Egashira, K; Morgan, JP; Morgan, KG, 1991) | 0.28 |
| " The severity of abstinence symptoms correlated with maternal methadone dosage in both term and preterm infants." | ( Neonatal opiate abstinence syndrome in term and preterm infants. Doberczak, TM; Kandall, SR; Wilets, I, 1991) | 0.28 |
| " In addition, the rewarding efficacy of the cocaine dosing parameters was subsequently confirmed in the runway subjects by conditioned place preference." | ( Animal model for investigating the anxiogenic effects of self-administered cocaine. Ettenberg, A; Geist, TD, 1991) | 0.28 |
| " Proper dosage and route of administration are additional important factors with such treatment." | ( Emergency treatments for police dogs used for illicit drug detection. Beasley, VR; Dumonceaux, GA, 1990) | 0.28 |
| ") 20 min before cocaine resulted in a 4- to 8-fold parallel shift to the right in the cocaine dose-response function." | ( Pharmacological characterization of the discriminative stimulus effects of cocaine in rhesus monkeys. Anthony, EW; Kleven, MS; Woolverton, WL, 1990) | 0.28 |
| " Complete dose-response functions for cocaine (0." | ( The effects of cocaine on food intake of baboons before, during, and after a period of repeated desipramine. Fischman, MW; Foltin, RW; Nautiyal, C, 1990) | 0.28 |
| " For all cocaine dosage groups, no differences were observed in the number of follicles present, number of oocytes retrieved, or IVF and cleavage rates." | ( The effect of cocaine on oocyte development and the follicular microenvironment in the rabbit. Kaufmann, RA; Sacco, AG; Savoy-Moore, RT; Subramanian, MG, 1990) | 0.28 |
| " Large, transient increases in heart rate, blood pressure and self-reported 'stimulated' scores were observed during single dosing sessions." | ( Demonstration of naturalistic methods for cocaine smoking by human volunteers. Cornell, EE; Fischman, MW; Foltin, RW; Nestadt, G; Pearlson, GD; Stromberger, H, 1990) | 0.28 |
| " Minimal effects and no clear dose-response relationships were observed." | ( Cocaine hepatotoxicity in cultured liver slices: a species comparison. Brendel, K; Connors, S; Gandolfi, AJ; Koep, LJ; Krumdieck, CL; Rankin, DR, 1990) | 0.28 |
| " Each subject was then maintained on daily doses of desipramine for 3 to 4 weeks, after which a second cocaine self-administration dose-response curve was generated under desipramine maintenance." | ( Effects of desipramine maintenance on cocaine self-administration by humans. Fischman, MW; Foltin, RW; Nestadt, G; Pearlson, GD, 1990) | 0.28 |
| " When doses of morphine which had no significant effect when administered alone (1 or 3 mg/kg) were combined with cocaine, the cocaine dose-response curve for efficiency was shifted down and to the left and response rates were increased." | ( Behavioral effects of cocaine and its interaction with d-amphetamine and morphine in rats. Wenger, GR; Wright, DW, 1990) | 0.28 |
| " Norepinephrine dose-response curves and frequency-response curves for transmural nerve stimulation were obtained in the presence and absence of cocaine, a specific inhibitor of neuronal reuptake." | ( Characterization of norepinephrine sensitivity in the maternal splanchnic circulation during pregnancy. Crandall, ME; Keve, TM; McLaughlin, MK, 1990) | 0.28 |
| "In the smooth muscle of the rat vas deferens, 10(-5) M cocaine shifted the dose-response curve to norepinephrine to the left and enhanced the maximal contractions to norepinephrine and methacholine." | ( Propranolol blocks cocaine-induced potentiation of the contraction in the smooth muscle of the rat vas deferens. Gomi, Y; Inagaki, O; Kasuya, Y; Ono, K; Suzuki, N, 1990) | 0.28 |
| "Pregnant and lactating Long-Evans rats were treated daily with oral cocaine at a dosage rate of 60 mg/kg/day, which is the highest dosage tolerated during chronic treatment." | ( Development under the influence of cocaine. II. Comparison of the effects of maternal cocaine and associated undernutrition on brain myelin development in the offspring. Ruiz, B; Wiggins, RC, 1990) | 0.28 |
| " Therefore, a dosage near 60 mg/kg/day by the oral route appears to mark a useful threshold between highly lethal dosages and an acceptable, sublethal dosage for chronic studies of pregnant rats." | ( Development under the influence of cocaine. I. A comparison of the effects of daily cocaine treatment and resultant undernutrition on pregnancy and early growth in a large population of rats. Ruiz, B; Wiggins, RC, 1990) | 0.28 |
| " A biphasic dose-response curve was seen for both strains." | ( Cocaine produces low dose locomotor depressant effects in mice. George, FR, 1989) | 0.28 |
| ") shifted the dose-response curves for the positive inotropic effect of plasma-dissolved (PD) ibopamine (0." | ( Analysis of the positive inotropic effect of ibopamine in the blood-perfused canine papillary muscle. Inui, J; Kawahara, K, ) | 0.13 |
| " The ratio of cocaine to metabolites increased in all three tissues, as the dosage increased, indicating that more and more of an administered dose actually reaches the tissues as cocaine as the dosage level increases." | ( Pharmacokinetics of cocaine: basic studies of route, dosage, pregnancy and lactation. Davis, CM; Rolsten, C; Ruiz, B; Wiggins, RC, 1989) | 0.28 |
| " After dose-response determinations for cocaine had been determined, a dose of cocaine that maintained maximal rates of responding was available in daily sessions." | ( The effects of a D1 and a D2 dopamine antagonist on behavior maintained by cocaine or food. Virus, RM; Woolverton, WL, 1989) | 0.28 |
| " Experimental conditions provided several different doses of drug during each of two daily 130 min sessions; as a result, a dose-response curve relating rate of responding to dose/injection for self-administered drug was obtained within each session." | ( Drug-reinforced responding: rapid determination of dose-response functions. Palmer, RK; Winger, G; Woods, JH, 1989) | 0.28 |
| "Sperm-positive female Long-Evans hooded rats were dosed subcutaneously with 10 mg/kg/day cocaine or an equal volume of vehicle (0." | ( Alterations in offspring behavior induced by chronic prenatal cocaine dosing. Kurkjian, MF; Kurtz, SL; Mattran, KM; Smith, RF, ) | 0.13 |
| " Pimozide, a drug thought to attenuate the reinforcing effects of both cocaine and heroin, shifted the functions without disturbing the dose-response relations; pimozide reliably decreased the time between successive cocaine infusions across a 4-fold range of pimozide doses." | ( Pharmacological regulation of intravenous cocaine and heroin self-administration in rats: a variable dose paradigm. Gerber, GJ; Wise, RA, 1989) | 0.28 |
| " The presence of unmetabolized cocaine in these biofluids long after the last drug administration suggests that multiple dosing and high exposure to cocaine in man leads to accumulation in deep body compartments and subsequent slow release back into circulation and eventual excretion." | ( Prolonged occurrence of cocaine in human saliva and urine after chronic use. Cone, EJ; Weddington, WW, ) | 0.13 |
| " Dosage level, duration of treatment, and interval between injection and sacrifice were the parameters examined." | ( Effects of cocaine hydrochloride on the male reproductive system. Berul, CI; Harclerode, JE, 1989) | 0.28 |
| " Inasmuch as oral administration resulted in dose-response relationships and low toxicity while subcutaneous administration did not, these factors should be considered in future studies utilizing chronic cocaine administration." | ( Comparison of oral and subcutaneous routes of cocaine administration on behavior, plasma drug concentration and toxicity in female rats. Dow-Edwards, D; Fico, TA; Gamagaris, Z; Hutchings, DE; Osman, M, 1989) | 0.28 |
| " Both the dose-response curve and the kinetics of the cocaine-induced closures indicate that there is a single class of cocaine-binding site." | ( Cocaine-induced closures of single batrachotoxin-activated Na+ channels in planar lipid bilayers. Wang, GK, 1988) | 0.27 |
| " The pressor response to levamisole was not modified by either reserpinization, acute bilateral adrenalectomy or pretreatment with cocaine, whereas pretreatment with dexamethasone, nialamide or pyroaallol shifted the dose-response curve to the right." | ( Investigation of some effects of levamisole on dog blood pressure. Gulati, OD; Hemavathi, KG; Shah, KK, ) | 0.13 |
| " Tityustoxin caused a slight leftward shift of the dose-response curves to adrenaline and norepinephrine and a large potentiation of the frequency-response curves to electrical stimulation." | ( Effects of tityustoxin on the rat isolated tail artery. Catanzaro, OL; Savino, EA, 1985) | 0.27 |
| " After determination of these dose-response relationships, the rats were divided into two groups." | ( Effects of central dopamine depletion on the d-amphetamine discriminative stimulus in rats. Cervo, L; Woolverton, WL, 1986) | 0.27 |
| " Dosage considerations may be critical because of the differential sensitivity of various tissues to calcium channel antagonists." | ( Cocaine-calcium channel antagonist interactions. Hooker, WD; Jones, RT; Mendelson, J; Rowbotham, MC, 1987) | 0.27 |
| " Firstly, dose-response effects were studied." | ( Cocaine-induced place conditioning: importance of route of administration and other procedural variables. Nomikos, GG; Spyraki, C, 1988) | 0.27 |
| " An increase in dosage in two groups of mice, to 1000 and 2000 parts/10(6), resulted in marked lymphopenia." | ( Lymphopenic effects on mice of a component of ammonia caramel, 2-acetyl-4(5)-tetrahydroxybutylimidazole (THI). Iscaro, A; Mackay, IR; O'Brien, C, ) | 0.13 |
| " To test whether cocaine potentiated changes in sinus cycle length, conduction in the atrioventricular node (AH interval) and ventricular effective refractory period induced by infused norepinephrine and ansae subclaviae stimulation, the dose-response curves of sinus cycle length, AH interval and ventricular effective refractory period to infused norepinephrine (0." | ( Cocaine-induced supersensitivity and arrhythmogenesis. Inoue, H; Zipes, DP, 1988) | 0.27 |
| " Prior major mental disorders and increased dosage of cocaine were more common among psychotic than non-psychotic patients." | ( Characteristics of freebase cocaine psychosis. Allen, D; Humblestone, B; Laughery, JA; Manschreck, TC; Mitra, N; Neville, M; Podlewski, H; Weisstein, CC, ) | 0.13 |
| " Subsequent testing at the original dosage levels revealed no change in the magnitude of cocaine's effect." | ( The effect of chronic cocaine on self-stimulation train-duration thresholds. Frank, RA; Martz, S; Pommering, T, 1988) | 0.27 |
| " Following redetermination of the PTZ and cocaine dose-response curves, chronic cocaine injections were terminated and spontaneous withdrawal was assessed by determining its substitution for the PTZ stimulus." | ( Anxiogenic properties of cocaine withdrawal. Lal, H; Wood, DM, 1987) | 0.27 |
| " Generally, an orderly inverted U-shaped dose-response curve for rates of self-injection has been observed." | ( Animal models of intravenous phencyclinoid self-administration. Marquis, KL; Moreton, JE, 1987) | 0.27 |
| " Both compounds developed sensitization to their locomotor stimulatory effects, with similarly shaped dose-response curves." | ( Effect of repeated administration of various doses of cocaine and WIN 35,065-2 on locomotor behavior of mice. Reith, ME, 1986) | 0.27 |
| " These results provide evidence that tolerance for cocaine used as a discriminative stimulus occurs as a function of chronic dose, dosing regimen and class of drug administered." | ( Characteristics of tolerance, recovery from tolerance and cross-tolerance for cocaine used as a discriminative stimulus. Emmett-Oglesby, MW; Wood, DM, 1986) | 0.27 |
| " The major epidemiologic study that formed the basis for this standard including a review of the evidence of a dose-response relationship between exposure to coal tar pitch volatiles and lung cancer is reviewed." | ( Selection, follow-up, and analysis in the Coke Oven Study. Redmond, CK; Rockette, HE, 1985) | 0.27 |
| " This method uses fractiles of the probability distribution of responses from the assay of interest and dose-response of the mixture." | ( Estimating the mass of mutagens in indeterminate mixtures. Kerster, HW; Schaeffer, DJ, 1985) | 0.27 |
| " The dose-response lines to phenylephrine were shifted in a parallel manner by propranolol 10(-8)M and 10(-7)M, suggesting that the relaxations were mediated through beta-adrenoceptors." | ( Actions of phenylephrine on beta-adrenoceptors in guinea-pig trachea. Chahl, LA; O'Donnell, SR, 1969) | 0.25 |
| "Inhibition of neuronal uptake with cocaine had no significant effect on the dose-response curve to noradrenaline in strips of beef coronary artery." | ( Sensitization of noradrenaline responses by inhibitors of extraneuronal uptake in a coronary artery preparation. Kalsner, S, 1974) | 0.25 |
| " 6) In the presence of cocaine, the dose-response curves plotted from the mechanical activity induced by excess [K]o or by noradrenaline shifted to the left and the maximum responses evoked by either treatment were enhanced." | ( Effects of cocaine on a hypogastric nerve-vas deferens preparation of the guinea pig. Hashiguchi, T; Ito, Y; Kuriyama, H, 1974) | 0.25 |
| " In adult cats, cocaine (1 and 10 mug/ml) or denervation produced a shift to the left of dose-response curves to (-)-noradrenaline, whereas they failed to modify dose-response curves to (-)-isoprenaline." | ( Effects of cocaine or denervation on responses of isolated strips of cat spleen to (-)-noradrenaline and (-)-isoprenaline. Granata, AR; Langer, SZ, 1973) | 0.25 |
| " The slopes of dose-response curves for each pollutant were plotted for each assay to compare relative potency." | ( The induction of sister chromatid exchanges by environmental pollutants: relationship of SCE to other measures of genetic damage. Benson, JM; Brooks, AL; Dutcher, JS; Li, AP; Shimizu, RW, 1984) | 0.27 |
| " 3 Presynaptic alpha-adrenoceptor antagonist activity was assessed by studying the effect of increasing antagonist concentrations on cumulative clonidine dose-response curves on the stimulated vas deferens." | ( Pre- and postsynaptic alpha-adrenoceptor blocking activity of raubasine in the rat vas deferens. Demichel, P; Gomond, P; Roquebert, J, 1981) | 0.26 |
| " These findings indicate that to establish the actual responses to high external potassium, non cumulative dose-response curves must be performed." | ( Responses of the rat tail artery to high external potassium concentration. Polidoro, JH; Savino, EA, 1982) | 0.26 |
| " Cocaine plus reserpine shift the dose-response curve for phenylephrine to the left." | ( Mechanism of action of phenylephrine on isolated guinea-pig atria rate. Nigro, D; Scivoletto, R, 1983) | 0.27 |
| " The range of the dose-response curve is 0-400 ng ml-1 benzoylecgonine." | ( Radioimmunoassay of benzoylecgonine in samples of forensic interest. Robinson, K; Smith, RN, 1984) | 0.27 |
| " Preincubation with cocaine, 10(-5) M, shifted the inhibitory dose-response curves of Iso and Orc to the left, 16." | ( Mechanism of action of isoprenaline, isoxuprine, terbutaline and orciprenaline on gravid human isolated myometrium. Influence of the neuronal uptake process. Calixto, JB; Simas, CM, 1984) | 0.27 |
| " Four hours after sinoaortic denervation, the dose-response curve to l-norepinephrine (NE) in perfused mesenteric arteries in vitro was shifted to the right and the maximal response reduced, compared with sham-operated controls." | ( Acute sinoaortic denervation induces pre- and postsynaptic alpha-adrenergic subsensitivity in mesenteric arteries in the rat. Granata, AR, 1984) | 0.27 |
| " In both preparations only the combined application of phentolamine (10(-6) M) and pindolol (3 X 10(-8) M) shifted the entire dose-response curves for the positive inotropic effect of dopamine to the right, while either antagonist used separately had no effect." | ( The mode of direct action of dopamine on the rabbit heart. Brodde, OE; Inui, J; Motomura, S; Schümann, HJ, ) | 0.13 |
| " All three alpha antagonists employed produced in innervated glands parallel displacements of the dose-response curves to norepinephrine, prazosin being 30 and 100 times more potent than phentolamine and yohimbine, respectively." | ( Alpha-1 adrenoceptors mediate secretory responses to norepinephrine in innervated and denervated rat submaxillary glands. Elverdin, JC; Luchelli-Fortis, MA; Perec, CJ; Stefano, FJ, 1984) | 0.27 |
| " At all dosage levels, COC increased the overflow of NE into the coronary sinus blood during cardiac sympathetic stimulation." | ( The effects of neuronal uptake blockade on the cardiac responses to sympathetic nerve stimulation and norepinephrine infusion in anesthetized dogs. Levy, MN; Masuda, Y, 1984) | 0.27 |
| " There is also evidence for a consistent dose-response relationship in lung cancer mortality when duration and location of employment at the coke ovens are considered." | ( Cancer mortality among coke oven workers. Redmond, CK, 1983) | 0.27 |
| " d-Amphetamine, cocaine, and caffeine each had the effect of elevating both bite and lever press responses; nicotine, chlorpromazine, chlordiazepoxide, and diazepam each elevated lever press responding while depressing bite responding across a portion of the dosage range; phenobarbital, alcohol, and morphine had the effect of depressing both bite and lever press responses but lever pressing was selectively more depressed than biting." | ( Unique influences of ten drugs upon post-shock biting attack and pre-shock manual responding. Emley, GS; Hutchinson, RR, 1983) | 0.27 |
| " One subject who was administered dextroamphetamine did not produce a wave consistent with amphetamine with a dosage of 5 mg." | ( Qualitative measurement of drugs. Gilbert, LM; Golz, A; Komorowski, FS; Westerman, ST, 1984) | 0.27 |
| " Active compounds exhibited an inverted U-shaped dose-response curve." | ( Amnesia-reversal activity of a series of N-[(disubstituted-amino)alkyl] -2-oxo-1-pyrrolidineacetamides, including pramiracetam. Butler, DE; L'Italien, YJ; Marriott, JG; Nordin, IC; Poschel, PH; Zweisler, L, 1984) | 0.27 |
| "It has been shown that there is a dose-response relationship between blood levels of intravenously injected cocaine and magnitude of evoked heat rate (Javaid et al." | ( Acute tolerance to cocaine in humans. Fischman, MW; Schuster, CR, 1981) | 0.26 |
| " The dose-response curve for this discrimination was orderly with an ED50 of about one-half of the training dose (0." | ( A neuropharmacological analysis of the discriminative stimulus properties of fenfluramine. Appel, JB; White, FJ, 1981) | 0.26 |
| " Comparing dose-response relations, arteries from both groups were equally sensitive to NE and KCl." | ( Increased sensitivity to angiotensin in uterine arteries from pregnant rabbits. Moisey, DM; Tulenko, T, 1983) | 0.27 |
| " AM was not able to cause contraction of strips obtained from dogs pretreated with reserpine; phentolamine shifted the dose-response curve of AM to the right." | ( On the mechanism of action of amezinium methylsulphate on the dog saphenous vein. Araújo, D; Caramona, MM; Osswald, W, 1983) | 0.27 |
| " A series of dose-response functions were then determined by giving a dose of a drug or a pair of drug doses once every 4 days." | ( Effects of psychomotor stimulants, alone and in pairs, on milk drinking in the rat after intraperitoneal and intragastric administration. Foltin, RW; Schuster, CR; Woolverton, WL, 1983) | 0.27 |
| " Although the dose-response functions for rates of responding and intake under both schedules were similar, the local pattern of responding under the second-order schedule was under the control of both the brief stimulus presentations as well as drug delivery." | ( Behavior maintained under fixed-interval and second-order schedules of cocaine or pentobarbital in rhesus monkeys. Johanson, CE, 1982) | 0.26 |
| " MCI-2016 (3 X 10(-6)M) and cocaine (3 X 10(-5)M) produced a leftward shift (15 and 20 times, respectively) of the dose-response curves for the contractile effect of NA and increased the maximum contractile response to NA by approximately 7 and 14% respectively." | ( Selective potentiation of noradrenaline in the guinea-pig vas deferens by 2-(4-methylaminobutoxy) diphenylmethane hydrochloride (MCI-2016), a new psychotropic drug. Ohizumi, Y; Takahashi, M; Tobe, A, 1982) | 0.26 |
| " Maximal response rates for NPA were about 1/2 of that of A, NMA and NEA, and the dose-response curve was shifted to the right of these compounds by about 4 times." | ( Structure-activity relationships among some d-N-alkylated amphetamines. Johanson, CE; Shybut, G; Woolverton, WL, 1980) | 0.26 |
| " The high cumulative UV dosage is due to the unique geographical and climatic features of the region." | ( Aetiology of spheroidal degeneration of the cornea in Labrador. Johnson, GJ, 1981) | 0.26 |
| " Lidoncaine, 5 x 10(-4) M, and MEGX, 2 x 10(-3) M, shifted the dose-response curve of NE to the right, whereas GX, 5 x 10(-4) M, shifted the curve to the left." | ( Modifications by lidocaine and its N-dealkylated metabolites of the response of the isolated rabbit aorta to transmural electrical stimulation. Fukuda, S; Takeshita, H; Toda, N, 1980) | 0.26 |
| " Regardless of the dosing regimen, extracellular dopamine levels were tonically elevated by 200-800% within the cocaine self-administration periods, fluctuating phasically within this range between responses." | ( Fluctuations in nucleus accumbens dopamine concentration during intravenous cocaine self-administration in rats. Burnette, B; Justice, JB; Leeb, K; Newton, P; Pocock, D; Wise, RA, 1995) | 0.29 |
| " Chronic nimodipine dosing in cocaine-dependent individuals is now needed to confirm its efficacy in the treatment of cocaine dependence." | ( The effects of nimodipine on the EEG of substance abusers. Guo, X; Herning, RI; Lange, WR, 1995) | 0.29 |
| " The incidence of these events, and the influence of specific dosing routes or regimens on their occurrence is not established." | ( 12-lead and continuous ECG recordings of subjects during inpatient administration of smoked cocaine. Hatsukami, DK; Pentel, PR; Salerno, DM; Thompson, T, 1994) | 0.29 |
| " Cocaine also caused significant increases in baseline HR, MAP, LVSP, and PWI between doses given on the same day at 1-h intervals, but the absolute value of the peak response to cocaine of these hemodynamic parameters was independent of dosing regimen." | ( Systemic and coronary hemodynamic effects of repetitive cocaine administration in conscious dogs. Pagel, PS; Tessmer, JP; Warltier, DC, 1994) | 0.29 |
| "0 mg/kg) produced dose-dependent rightward shifts of the (+/-)BAY k 8644 dose-response curve." | ( Modification of the behavioral effects of (+/-)BAY k 8644, cocaine and d-amphetamine by L-type calcium channel blockers in squirrel monkeys. Barrett, JE; Rosenzweig-Lipson, S, 1995) | 0.29 |
| " The results indicate that there is a substantial treatment dose-response relationship." | ( Treatment intensity and reduction in drug use for cocaine-dependent methadone patients: a dose-response relationship. Foote, J; Handelsman, L; Lovejoy, M; Magura, S; Palij, M; Rosenblum, A; Stimmel, B, ) | 0.13 |
| "4 mg/kg) or CGS 12066B (16 mg/kg) produced a leftward shift in the cocaine dose-response curve (0." | ( Modulation of the discriminative stimulus properties of cocaine by 5-HT1B and 5-HT2C receptors. Callahan, PM; Cunningham, KA, 1995) | 0.29 |
| " Results indicate that at the dosage used (8 mg/kg of body weight, given intravenously daily) gross teratologic defects do not develop." | ( The rabbit as a model for studies of cocaine exposure in utero. Groce, MY; Hammer, JG; Harvey, JA; Jones, L; Murphy, EH; Romano, AG; Schumann, MD; Wang, XH, 1995) | 0.29 |
| " However, the response of preproenkephalin, c-fos and zif/268 mRNAs to such a dosing regimen is unknown." | ( Cocaine binges differentially alter striatal preprodynorphin and zif/268 mRNAs. Daunais, JB; McGinty, JF, 1995) | 0.29 |
| " An adult dose-response curve pattern of stereotypy and locomotion to acute cocaine treatment was observed at PND 21, and of rearing at PND 28." | ( Ontogeny of behavioral sensitization to cocaine. Akiyama, K; Fujiwara, Y; Kuroda, S; Tsuchida, K; Ujike, H, 1995) | 0.29 |
| " There were no significant differences between groups for the overall cocaine dosage or temporal pattern of infusions on days 1 and 7 of withdrawal." | ( Tolerance-like attenuation to contingent and noncontingent cocaine-induced elevation of extracellular dopamine in the ventral striatum following 7 days of withdrawal from chronic treatment. Grimm, JW; Lynch, AM; Meil, WM; Roll, JM; See, RE, 1995) | 0.29 |
| " The multiple cocaine dosing regimen produced maternal peak serum concentrations of cocaine 3 times higher than that of a single dose (approximately 1550 vs." | ( Long-term learning deficits and changes in unlearned behaviors following in utero exposure to multiple daily doses of cocaine during different exposure periods and maternal plasma cocaine concentrations. Acuff-Smith, KD; Cappon, GD; Fisher, JE; Pu, C; Reed, TM; Schilling, MA; Vorhees, CV, ) | 0.13 |
| ") was used in all experiments except the dose-response relationship study." | ( Role of the sympathoadrenal axis in the cardiovascular response to cocaine in conscious unrestrained rats. Chen, BX; Myles, J; Wilkerson, RD, 1995) | 0.29 |
| " To determine if raising the daily methadone dosage is an effective way to eliminate cocaine abuse, 74 methadone maintenance patients maintained at daily dosages between 30 and 80 mg and who chronically abused cocaine were studied by a standard protocol." | ( Cocaine abuse in methadone maintenance patients is associated with low serum methadone concentrations. Shannon, J; Tennant, F, 1995) | 0.29 |
| " Dose-response functions for all four drugs were displaced to the left and average ED50 values were reduced by 3-fold or more under the low-dose compared to the high-dose training condition." | ( Effects of N-methyl-D-aspartate antagonists in rats discriminating different doses of cocaine: comparison with direct and indirect dopamine agonists. Edwards, MA; Kantak, KM; Spealman, RD, 1995) | 0.29 |
| " Methylene Blue (which blocks production of cGMP by EDRF-NO) and Nw-nitro-L-arginine (which inhibits EDRF-NO synthesis), both shifted 5-HT dose-response curves to the left and completely abolished the differences in sensitivity to the agonist." | ( Nitric oxide and superoxide anions in vascular reactivity of renovascular hypertensive rats. Bellver, A; Celentano, MM; de la Riva, IJ; Rosón, MI; Vega, GW, 1995) | 0.29 |
| " Administration of U50,488H (3 mg/kg), in conjunction with several doses of cocaine, did not shift the cocaine dose-response curve." | ( Assessment of the discriminative stimulus effects of cocaine in the rat: lack of interaction with opioids. Broadbent, J; Dworkin, SI; Gaspard, TM, ) | 0.13 |
| "6-mg/kg doses of GBR 12909 produced downward shifts in the dose-response curves for cocaine (0." | ( Effects of monoamine reuptake inhibitors on cocaine self-administration in rats. Tella, SR, 1995) | 0.29 |
| " Additionally, bilateral injection of a fixed dose of SCH 23390 (2 micrograms) into the central amygdala resulted in a rightward shift in the cocaine dose-response curve (2." | ( Discriminative stimulus effects of cocaine: antagonism by dopamine D1 receptor blockade in the amygdala. Bryan, SK; Callahan, PM; Cunningham, KA, 1995) | 0.29 |
| " These data suggest a dose-response relation between the magnitude of prenatal cocaine exposure and impaired fetal growth." | ( Relation between meconium concentration of the cocaine metabolite benzoylecgonine and fetal growth. Cabral, H; Frank, DA; Mirochnick, M; Turner, A; Zuckerman, B, 1995) | 0.29 |
| " Dosing was double-blind and double-dummy." | ( Buprenorphine versus methadone in the treatment of opioid-dependent cocaine users. Bigelow, GE; Liebson, IA; Stitzer, ML; Strain, EC, 1994) | 0.29 |
| " Dose-response and time course experiments were performed in phenobarbitone treated male DBA/2Ha mice to study the pathogenesis of this unusual cocaine induced lesion." | ( Cocaine hepatotoxicity: a study on the pathogenesis of periportal necrosis. Charles, SJ; Mullervy, J; Powell, CJ, 1994) | 0.29 |
| " This shift in the cocaine dose-response curve was apparent when conditioning commenced either 3 or 7, but not 14, days after the cessation of cocaine pretreatment." | ( Sensitization to the conditioned rewarding effects of cocaine: pharmacological and temporal characteristics. Heidbreder, C; Shippenberg, TS, 1995) | 0.29 |
| "A retrospective, inception cohort, nonrandomized control design was employed to evaluate the effects of daily vs twice daily dosing of methadone on opiate/cocaine use, and noncompliance with urine toxicology requests in methadone-maintained pregnant women, n = 45." | ( Methadone dosing and pregnancy: impact on program compliance. DePetrillo, PB; Rice, JM, 1995) | 0.29 |
| " SPECT studies were performed at baseline, after maximum dosage was reached and after tapering off the study drug." | ( Improved regional cerebral blood flow in chronic cocaine polydrug users treated with buprenorphine. Garada, B; Holman, BL; Levin, JM; Mello, NK; Mendelson, JH; Schwartz, RB; Teoh, SK, 1995) | 0.29 |
| " Cumulative dosing with cocaine (0." | ( Role of delta opioid receptors in the reinforcing and discriminative stimulus effects of cocaine in rhesus monkeys. Lukas, SE; Mello, NK; Mendelson, JH; Negus, SS; Portoghese, PS, 1995) | 0.29 |
| " The time course of action and dosage range of cocaine that produces potentiation follows that which increases blood pressure (BP), heart rate (HR), rate-pressure product and coronary vasoconstriction." | ( Sympathetic nervous system mediated cardiovascular effects of cocaine are primarily due to a peripheral site of action of the drug. Dretchen, KL; Erzouki, HK; Gillis, RA; Hernandez, YM; Kuhn, FE; Mandal, AK; Raczkowski, VF, 1995) | 0.29 |
| " Dose-response functions for cocaine and haloperidol demonstrated both quantitative and qualitative specificity of the training stimuli." | ( A three-choice haloperidol-saline-cocaine drug discrimination task in rats. Gauvin, DV; Goulden, KL; Holloway, FA, 1994) | 0.29 |
| " Cocaine users were more likely than nonusers of cocaine to use heroin at all methadone dosage levels." | ( Heroin use during methadone maintenance treatment: the importance of methadone dose and cocaine use. Davenny, K; Friedland, GH; Hartel, DM; Klein, RS; Kline, J; Schoenbaum, EE; Selwyn, PA, 1995) | 0.29 |
| " In contrast, the dose-response to cocaine as well as the numbers and firing rates of 5-HT neurons found in rats with long-term habenula lesions did not differ from controls." | ( Habenula lesions decrease the responsiveness of dorsal raphe serotonin neurons to cocaine. Cunningham, KA; Paris, JM, 1994) | 0.29 |
| " Adult offspring prenatally exposed to cocaine were observed to exhibit a reduced sensitivity to the discriminative stimulus effects of cocaine as evidenced by a significant shift to the right in the dose-response curve of cocaine discrimination." | ( Responsiveness to cocaine challenge in adult rats following prenatal exposure to cocaine. Heyser, CJ; Rajachandran, L; Spear, LP; Spear, NE, 1994) | 0.29 |
| " Latency to acquisition of the lever discrimination for rats that had received prior exposure to amphetamine was shorter than for the saline-pretreated counterparts in each cocaine dosage group." | ( Development and expression of sensitization to cocaine's reinforcing properties: role of NMDA receptors. Bankson, MG; Gibbs, S; Higley, D; Horger, BA; House, DT; McNamara, C; Schenk, S; Valadez, A, 1993) | 0.29 |
| " Pretreatment with citalopram or fluoxetine attenuated the rate-increasing effects of cocaine and produced an overall downward shift in the cocaine dose-response function." | ( Modification of behavioral effects of cocaine by selective serotonin and dopamine uptake inhibitors in squirrel monkeys. Spealman, RD, 1993) | 0.29 |
| " These results suggest that cocaine administered prior to the reintroduction of cues associated with a conditioning episode can modulate memory processes, and that the dose-response function for this effect is U-shaped." | ( Cocaine administration prior to reactivation facilitates later acquisition of an avoidance response in rats. Martinez, JL; Phillips, MY; Rodriguez, SB; Rodriguez, WA, 1993) | 0.29 |
| " In experiment 3, a full cocaine dose-response function was examined." | ( Isolation rearing enhances the locomotor response to cocaine and a novel environment, but impairs the intravenous self-administration of cocaine. Everitt, BJ; Howes, SR; Phillips, GD; Robbins, TW; Whitelaw, RB; Wilkinson, LS, 1994) | 0.29 |
| " In experiment 2b, a full d-amphetamine dose-response function was examined." | ( Isolation rearing impairs the reinforcing efficacy of intravenous cocaine or intra-accumbens d-amphetamine: impaired response to intra-accumbens D1 and D2/D3 dopamine receptor antagonists. Everitt, BJ; Howes, SR; Phillips, GD; Robbins, TW; Whitelaw, RB, 1994) | 0.29 |
| " In contrast, the same dose of active PTX produced significant, long-lasting increases (up to 1 month) in the self-administration of both drugs, and shifted the dose-response curves to the right." | ( Inactivation of Gi and G(o) proteins in nucleus accumbens reduces both cocaine and heroin reinforcement. Nestler, EJ; Self, DW; Stein, L; Terwilliger, RZ, 1994) | 0.29 |
| ") decreased milk intake in rats (n = 9) and, when given in combination with cocaine, shifted the cocaine dose-response function (4." | ( Behavioral effects of the dopamine autoreceptor agonist PD 128483 alone and in combination with cocaine. Vanover, KE; Woolverton, WL, 1994) | 0.29 |
| " The results showed dose-response relationships for both plasma concentrations of cocaine and for the total number of overt behavioural signs." | ( Cocaine-induced rausch: overt behaviour and plasma concentrations in rhesus monkeys. Aceto, MD; Bowman, ER; Saady, JJ, ) | 0.13 |
| " Cumulative dose-response curves (10(-12)-10(-4) M) were generated for cocaine and the major cocaine metabolites in fetal sheep cerebral artery segments." | ( Effects of cocaine, benzoylecgonine, and cocaine metabolites in cannulated pressurized fetal sheep cerebral arteries. Covert, RF; Madden, JA; Schreiber, MD; Torgerson, LJ, 1994) | 0.29 |
| " Dosing was double-blind and double-dummy." | ( Comparison of buprenorphine and methadone in the treatment of opioid dependence. Bigelow, GE; Liebson, IA; Stitzer, ML; Strain, EC, 1994) | 0.29 |
| " In both groups, 56% of patients remained in treatment through the 16-week flexible dosing period." | ( Comparison of buprenorphine and methadone in the treatment of opioid dependence. Bigelow, GE; Liebson, IA; Stitzer, ML; Strain, EC, 1994) | 0.29 |
| "The results of this study provide further support for the utility of buprenorphine as a new medication in the treatment of opioid dependence and demonstrate efficacy equivalent to that of methadone when used during a clinically guided flexible dosing procedure." | ( Comparison of buprenorphine and methadone in the treatment of opioid dependence. Bigelow, GE; Liebson, IA; Stitzer, ML; Strain, EC, 1994) | 0.29 |
| ") were administered 30 min before determination of cocaine dose-response functions using a cumulative dosing method." | ( Effects of cholecystokinin antagonists on the discriminative stimulus effects of cocaine in rats and monkeys. Massey, BW; Vanover, KE; Woolverton, WL, 1994) | 0.29 |
| "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 |
| "0 mg/kg) had no significant effect on the dose-response curve for cocaine self-administration." | ( Failure of ritanserin to block the discriminative or reinforcing stimulus effects of cocaine. Emmett-Oglesby, MW; Peltier, RL; Schenk, S; Thomas, WH, 1994) | 0.29 |
| " Animals were dosed intramuscularly with cocaine hydrochloride at 1 mg/kg, supplemented with a tritiated cocaine tracer." | ( Transplacental pharmacokinetics and maternal/fetal plasma concentrations of cocaine in pregnant macaques near term. Bailey, JR; Binienda, Z; Duhart, HM; Paule, MG; Slikker, W, ) | 0.13 |
| " Furthermore, bradykinin did not modify the dose-response curves for added norepinephrine." | ( Importance of sympathetic innervation in the positive inotropic effects of bradykinin and ramiprilat. Djokovic, A; Erdös, EG; Miletich, DJ; Minshall, RD; Rabito, SF; Vogel, SM; Yelamanchi, VP, 1994) | 0.29 |
| "The previously observed association between smoking and placenta previa is supported by the dose-response relationship observed in this study." | ( The relationship between exposure during pregnancy to cigarette smoking and cocaine use and placenta previa. Davis, FG; Handler, AS; Mason, ED; Rosenberg, DL, 1994) | 0.29 |
| " This study indicates that a non-toxic dosage of cocaine stimulates uterine contractions, and pregnancy enhances this effect." | ( [The effect of cocaine on uterine contractions in the rat]. Iso, A; Morishima, HO; Nakahara, K, 1994) | 0.29 |
| " The present study examined whether the effects of these two dosing regimens are related to alterations in the functional status of dopamine (DA) D2 receptors." | ( Withdrawal from continuous or intermittent cocaine administration: changes in D2 receptor function. Caron, MG; Ellinwood, EH; Joyner, CM; King, GR; Lee, TH; Silvia, C; Xue, Z, 1994) | 0.29 |
| " Dose-response curves indicate that only one molecule of benzocaine is required to bind with one BTX-modified Na+ channel at -70 mV, whereas approximately two molecules are needed at +50 mV." | ( Binding of benzocaine in batrachotoxin-modified Na+ channels. State-dependent interactions. Wang, GK; Wang, SY, 1994) | 0.29 |
| " Addressing these concerns is important in conducting parametric studies that require examining dose-response effects." | ( Methodological issues in the administration of multiple doses of smoked cocaine-base in humans. Brauer, LH; Crosby, R; Glass, J; Hanson, K; Hatsukami, DK; Nelson, R; Pentel, PR, 1994) | 0.29 |
| " The dosage and plasma concentrations of cocaine associated with the onset of convulsions and cardiovascular depression were significantly lower in pregnant rats when compared with the nonpregnant animals." | ( Pregnancy decreases the threshold for cocaine-induced convulsions in the rat. Cooper, TB; Hara, T; Masaoka, T; Morishima, HO; Tsuji, A, 1993) | 0.29 |
| " Our experiments did not show any great differences in the overall efficacy of the two drugs, although they showed quite a different dose-response effect." | ( Effect of synthetic thymic hormones on the cocaine-induced inhibition of the primary immune response in mice. Di Francesco, P; Falchetti, R; Favalli, C; Garaci, E; Gaziano, R; Lanzilli, G; Ravagnan, G, 1993) | 0.29 |
| " When the response requirement (FR) for cocaine was differentially increased by doubling or quadrupling, the frequency of cocaine choice decreased, shifting the cocaine dose-response function to the right." | ( Behavioral economics and drug choice: effects of unit price on cocaine self-administration by monkeys. Hedeker, D; Nader, MA; Woolverton, WL, 1993) | 0.29 |
| " As expected, female offspring of dams exposed to saline in utero displayed greater activation to a 20 mg/kg SC dosage of cocaine than their male counterparts." | ( Prenatal cocaine eliminates the sex-dependent differences in activation observed in adult rats after cocaine challenge. Miller, DB; Seidler, FJ, 1994) | 0.29 |
| " Based on the present and previous results, it appears that the regulation of the DAT is fairly plastic, and is highly sensitive to cocaine dosing regimes and withdrawal intervals." | ( Cocaine use increases [3H]WIN 35428 binding sites in human striatum. Carroll, FI; Clark, TB; Duncan, GE; Kirkman, JA; Little, KY, 1993) | 0.29 |
| " However, analysis of variance revealed a statistically significant shift to the right in the cocaine dose-response curves for effects on tonic and evoked LC discharge in unanesthetized compared to anesthetized rats." | ( Cocaine effects on brain noradrenergic neurons of anesthetized and unanesthetized rats. Conti, E; Curtis, AL; Valentino, RJ, 1993) | 0.29 |
| " Correlates of neural activation in the neocortex displayed an inverse dose-response curve to that found in the hippocampus; the time-to-peak effect was shorter (6-43 min) and the maximal change was reduced." | ( Imaging of hippocampal and neocortical neural activity following intravenous cocaine administration in freely behaving cats. Harper, RM; Poe, GR; Rector, DM, 1993) | 0.29 |
| " Logistic regression indicated that alcoholism among MMTP patients was associated with years drinking, years of sharing needles, utilization of drug abuse detoxification but not alcohol detoxification, smaller increases in methadone dosage over time, and psychiatric symptomatology." | ( Correlates of alcohol use among methadone patients. el-Bassel, N; Schilling, RF; Su, KH; Turnbull, JE, 1993) | 0.29 |
| " A second set of experiments determined whether tolerance could be studied using a multi-dose method to obtain dose-response data in a single session." | ( Tolerance to self-administration of cocaine in rats: time course and dose-response determination using a multi-dose method. Depoortere, RY; Emmett-Oglesby, MW; Gong, YH; Hooper, ML; Lane, JD; Peltier, RL; Pickering, CL, 1993) | 0.29 |
| " When rats were challenged 10-14 d after discontinuing either dosage regimen of daily cocaine, the increase in both motor activity and extracellular dopamine was augmented." | ( Time course of extracellular dopamine and behavioral sensitization to cocaine. I. Dopamine axon terminals. Duffy, P; Kalivas, PW, 1993) | 0.29 |
| " Similarly, no apparent toxicity was observed in virgin animals injected with the same dosage of cocaine." | ( Alterations in biodistribution of cocaine may explain differential toxicity in pregnant and postpartum rats. Dwivedi, C; Engineer, FN; Vaughan, SL, 1993) | 0.29 |
| " By using a video-image analysis of behavior in an intact animal model and a pavlovian drug treatment protocol, new, spontaneous but environmentally contingent and stable behavior patterns emerge selectively in the paired treatment group with repeated drug administration which can be used as a behavioral marker to assess dose-response effects and drug substitution test results with a novel drug." | ( Activation of an apomorphine behavior pattern by cocaine: a new behavioral test for drug substitution. Carey, RJ; Damianopoulos, EN, 1993) | 0.29 |
| " In analyzing the dose-response curves, cocaethylene was the most potent vasoconstrictor, followed by cocaine, norcocaine and then ecogonine, benzoylecgonine and ecgonine methylester." | ( Cocaine and its metabolites constrict cerebral arterioles in newborn pigs. Albuquerque, ML; Anday, E; Feuer, P; Kurth, CD; Monitto, C; Shaw, L, 1993) | 0.29 |
| "To compare the dose effectiveness of low to moderate doses of methadone in a sample of a contemporary population of opioid abusers, because the optimal dosing of methadone in the treatment of opioid dependence remains an issue." | ( Dose-response effects of methadone in the treatment of opioid dependence. Bigelow, GE; Liebson, IA; Stitzer, ML; Strain, EC, 1993) | 0.29 |
| "All participants were initially treated with active methadone for a minimum of 5 weeks and then received 15 weeks of stable dosing at 50, 20, or 0 mg per day." | ( Dose-response effects of methadone in the treatment of opioid dependence. Bigelow, GE; Liebson, IA; Stitzer, ML; Strain, EC, 1993) | 0.29 |
| "There is a dose-response effect for methadone treatment." | ( Dose-response effects of methadone in the treatment of opioid dependence. Bigelow, GE; Liebson, IA; Stitzer, ML; Strain, EC, 1993) | 0.29 |
| " Dose-response and antagonist testing commenced once stable rates of cocaine SA were achieved." | ( Lack of involvement of delta-opioid receptors in mediating the rewarding effects of cocaine. Babovic-Vuksanovic, D; de Vries, TJ; Elmer, G; Shippenberg, TS, 1995) | 0.29 |
| " Animals were dosed with PCP (15 mg/kg, ip) its congener (+) MK-801 (0." | ( Drug-induced circling preference in rats. Correlation with monoamine levels. Ali, SF; Gough, B; Kordsmeier, KJ, ) | 0.13 |
| " Pregnant rats were dosed orally with cocaine hydrochloride (60 mg/kg/d) from gestational day (GD) 7-21." | ( Prenatal cocaine exposure revealed minimal postnatal changes in rat striatal dopamine D2 receptor sites and mRNA levels in the offspring. Choi, HL; Stadlin, A; Tsang, D; Tsim, KW, ) | 0.13 |
| " The sensitivity and specificity of the overall analysis system (immunoassay screen and GC-MS confirmation) was 86% and 97%, with known cocaine dosing of volunteers as the acceptable indicator of the true clinical state." | ( Enzyme immunoassay validation for qualitative detection of cocaine in sweat. Fay, J; Fogerson, R; Niedbala, RS; Schoendorfer, D; Spiehler, V, 1996) | 0.29 |
| " We determined the horizontal position of the dose-response curves for the positive inotropic effects exerted by noradrenaline in the absence and presence of the neuronal uptake blocker cocaine and in the absence and presence of the beta-adrenoceptor antagonist timolol and of the alpha 1-adrenoceptor antagonist prazosin." | ( Location of alpha 1-adrenoceptors relative to beta-adrenoceptors in rat myocardium. Dybvik, T; Osnes, JB; Skomedal, T, 1995) | 0.29 |
| " In a cumulative dosing procedure, five cumulative doses of cocaine (0." | ( Relationship between the discriminative stimulus effects and plasma concentrations of intramuscular cocaine in rhesus monkeys. Hall, E; Lamas, X; Mello, NK; Negus, SS, 1995) | 0.29 |
| "Pregnant Long-Evans hooded rats were dosed with 5, 10, 20, or 40 mg/kg/d cocaine from GD7 through GD20; pairfed/vehicle-injected, and uninjected controls were included." | ( Prenatal cocaine produces dose-dependent suppression of prolactin and growth hormone in neonatal rats. Coss, M; Royall, GD; Smith, RF, 1995) | 0.29 |
| "Fifty cocaine-dependent patients completed a 2-week double-blind, double-dummy, parallel-group comparison of four dosage levels of diethylpropion and placebo." | ( Diethylpropion pharmacotherapeutic adjuvant therapy for inpatient treatment of cocaine dependence: a test of the cocaine-agonist hypothesis. Alim, TN; Deutsch, SI; Lindquist, T; Rosse, RB; Vocci, FJ, 1995) | 0.29 |
| "To determine in a representative sample of full-term urban newborns of English-speaking mothers whether an immediate or late dose-response effect could be demonstrated between prenatal cocaine exposure and newborn neurobehavioral performance, controlling for confounding factors." | ( Late dose-response effects of prenatal cocaine exposure on newborn neurobehavioral performance. Cabral, H; Frank, DA; Mirochnick, M; Tronick, EZ; Zuckerman, B, 1996) | 0.29 |
| " In adults, chronic cocaine use alters neurotransmitter concentrations and receptor dose-response relationships." | ( Effect of chronic cocaine exposure on carotid artery reactivity in neonatal rabbits. Feuer, P; Kurth, CD; Loeb, AL; Monitto, CL; O'Rourke, MM, 1996) | 0.29 |
| " A clear dose-response relationship was observed between the cumulative dose of cocaine administered during gestation and the levels of both cocaine and its major metabolite, benzoylecgonine, in samples of infant hair taken at birth." | ( The effect of chronic cocaine exposure during pregnancy on maternal and infant outcomes in the rhesus monkey. Binienda, Z; Gillam, MP; Harkey, MR; Henderson, GL; Morris, P; Paule, MG; Zhou, C, ) | 0.13 |
| " When responding was stable, dose-response curves were determined for cocaine (0." | ( Self-administration of the dopamine D3 agonist 7-OH-DPAT in rhesus monkeys is modified by prior cocaine exposure. Mach, RH; Nader, MA, 1996) | 0.29 |
| "5-20 mg/kg) produced, at best, a partial substitution while mCPBG (10 mg/kg) did not alter the cocaine dose-response relationship." | ( Detailed investigations of 5-HT3 compounds in a drug discrimination model. Callahan, PM; Cunningham, KA; De La Garza, R, 1996) | 0.29 |
| " The ascending limb of the cocaine dose-response curve was shifted downward and approximately one log unit to the right during low-dose buprenorphine treatment (0." | ( Buprenorphine-induced alterations of cocaine's reinforcing effects in rhesus monkey: a dose-response analysis. Drieze, JM; Lukas, SE; Mello, NK; Mendelson, JH, 1995) | 0.29 |
| " Behavior in D2 mice relative to B6 mice also appeared to be shifted to the left of the dose-response curve measured within-subjects." | ( Genetic differences in intravenous cocaine self-administration between C57BL/6J and DBA/2J mice. Cunningham, CL; Grahame, NJ, 1995) | 0.29 |
| " Comparative results indicated that dosage of any adjunct therapy was associated with days in treatment and standard treatment sessions attended, and that standard treatment sessions attended was associated with negative urinalysis results at follow-up." | ( Effectiveness of adjunct therapies in crack cocaine treatment. Montoya, ID; Nelson, R; Richard, AJ; Spence, RT, ) | 0.13 |
| " Repeated administration of BTCP dose-dependently produced leftward and downward shifts of the cocaine dose-response curve." | ( Effects of repeated administration of N-[1-(2-benzo(b)-thiophenyl)cyclohexy]piperidine and cocaine on locomotor activity in C57BL/6 mice. Kamenka, JM; Kleven, MS; Koek, W; Prinssen, EP; Vignon, J, 1996) | 0.29 |
| " This is known to occur where frequent dosing is required as in the study of drugs of abuse." | ( Cocaine hydrochloride in poly(L-lactide) microspheres potentiates effects on the locomotion of rats+. Bertelsen, GA; Gulati, A; Hickey, AJ; Masinde, LE; Schlemmer, RF, 1995) | 0.29 |
| " The statistical distribution of the drug concentrations compared with the self-reported consumption behaviour of the users may possibly lead to a better understanding of the relationship between drug dosage and corresponding concentrations in hair." | ( Concentrations of delta 9-tetrahydrocannabinol, cocaine and 6-monoacetylmorphine in hair of drug abusers. Kauert, G; Röhrich, J, 1996) | 0.29 |
| " Testing consisted of three daily sessions of fixed cocaine dosing (four injections; 0, 16 and 48 mg/70 kg) and three daily sessions of cocaine self-administration with a choice procedure (16, 32 and 48 mg/70 kg vs." | ( Effects of methadone or buprenorphine maintenance on the subjective and reinforcing effects of intravenous cocaine in humans. Fischman, MW; Foltin, RW, 1996) | 0.29 |
| ", the dose-response functions were biphasic." | ( Parametric analysis of cocaine self-administration under a progressive-ratio schedule in rhesus monkeys. Kleven, MS; Massey, BW; Rowlett, JK; Woolverton, WL, 1996) | 0.29 |
| " However, cocaine exposed infants did not require more medication for withdrawal management either in terms of dosage or of days treated." | ( Neonatal withdrawal syndrome in infants exposed to cocaine and methadone. Carroll, KM; Mayes, LC, 1996) | 0.29 |
| " The purpose of the present study was to provide the first complete characterization of the dose-response relationships of cocaine (0." | ( Sympathetic nerve responses elicited by cocaine in anesthetized and conscious rats. Abrahams, TP; Cuntapay, M; Varner, KJ, 1996) | 0.29 |
| "Although topical intranasal cocaine remains a common anesthetic in nasal surgery, controversy surrounds its dosage and mucosal absorption." | ( Absorption of topical cocaine in rhinologic procedures. Greinwald, JH; Holtel, MR, 1996) | 0.29 |
| "3 mM), at approximately twice the equimolar dosage of cocaine, produced apneustic breathing that was indistinguishable from that produced by cocaine." | ( Cardiorespiratory effects of cocaine and procaine at the ventral brainstem. Dehkordi, O; Dennis, GC; Millis, RM; Trouth, CO, 1996) | 0.29 |
| " Following a 7-day withdrawal period, we examined the effects of these two dosing regimens on: (1) baseline dopamine efflux and uptake following single-pulse electrical stimulation, (2) inhibition of uptake by cocaine; and (3) inhibition of efflux by autoreceptor activation." | ( Effects of intermittent and continuous cocaine administration on dopamine release and uptake regulation in the striatum: in vitro voltammetric assessment. Ellinwood, EH; Jones, SR; Lee, TH; Wightman, RM, 1996) | 0.29 |
| " In order to quantify changes in sensitivity to cocaine, cumulative dose-response functions for acute cocaine were determined using a multiple schedule comprised of six 10-minute components separated by time-out periods of 3 minutes." | ( Effects of exposure regimen on changes in sensitivity to the effects of cocaine on schedule-controlled behavior in rhesus monkeys. Kleven, MS; Woolverton, WL, 1996) | 0.29 |
| " In addition, a dose-response relationship was suggested." | ( Prenatal cocaine and neonatal outcome: evaluation of dose-response relationship. Angelilli, ML; Baker, D; Covington, C; Delaney-Black, V; Hack, C; Long, J; Nordstrom-Klee, B; Ostrea, E; Romero, A; Silvestre, MA; Tagle, MT, 1996) | 0.29 |
| " A dose-response relationship was evident." | ( Prenatal cocaine and neonatal outcome: evaluation of dose-response relationship. Angelilli, ML; Baker, D; Covington, C; Delaney-Black, V; Hack, C; Long, J; Nordstrom-Klee, B; Ostrea, E; Romero, A; Silvestre, MA; Tagle, MT, 1996) | 0.29 |
| " The primary goal of this study was to determine the validity of the variables of the DEC evaluation in predicting whether research volunteers had been administered ethanol, cocaine, or marijuana; a secondary goal was to determine the accuracy of trained police officers (Drug Recognition Examiner, DRE) in detecting whether subjects had been dosed with ethanol, cocaine, or marijuana." | ( Laboratory validation study of drug evaluation and classification program: ethanol, cocaine, and marijuana. Crouch, DJ; Heishman, SJ; Singleton, EG, 1996) | 0.29 |
| " Parallel line analysis indicated that the slopes of the ascending portion of the RTI-121 and RTI-130 dose-response curves differed from that of cocaine, suggesting the involvement of mechanisms different from that of cocaine." | ( Highly potent cocaine analogs cause long-lasting increases in locomotor activity. Boja, JW; Carroll, FI; Fleckenstein, AE; Kopajtic, TA; Kuhar, MJ, 1996) | 0.29 |
| " Lesioned rats showed a cocaine dose-response function that was shifted upwards relative to control subjects." | ( Excitotoxic lesions of the basolateral amygdala impair the acquisition of cocaine-seeking behaviour under a second-order schedule of reinforcement. Everitt, BJ; Markou, A; Robbins, TW; Whitelaw, RB, 1996) | 0.29 |
| " The results indicate that nimodipine and BayK 8644 shifted the dose-response curve for cocaine's reinforcing action to the right and left, respectively." | ( Modulation of cocaine intravenous self-administration in drug-naive animals by dihydropyridine Ca2+ channel modulators. Kuzmin, A; Ramsey, NF; Semenova, S; Van Ree, JM; Zvartau, EE, 1996) | 0.29 |
| " A dose-response effect was found: higher amounts of cocaine were associated with higher neurobehavioral risk scores." | ( Neonatal neurobehavioral outcome following prenatal exposure to cocaine. Barr, HM; Martin, DC; Martin, JC; Streissguth, AP, ) | 0.13 |
| "1 for protocols 1 and 2, respectively) in stimulating the 5-HTP-induced HTR and produced a bell-shaped dose-response curve." | ( The stimulatory and inhibitory components of cocaine's actions on the 5-HTP-induced 5-HT2A receptor response. Darmani, NA; Reeves, SL, 1996) | 0.29 |
| " Each volunteer was first tested under all dosing conditions without an arterial catheter (phase I), to determine whether subjects could tolerate each cocaine dose, before testing with an arterial catheter (phase II)." | ( Arterial and venous cocaine plasma concentrations in humans: relationship to route of administration, cardiovascular effects and subjective effects. Cone, EJ; Evans, SM; Henningfield, JE, 1996) | 0.29 |
| " For example, a 20 mg/kg, intraperitoneal dosage of cocaine that was tolerated during pregnancy caused tonic-clonic convulsions and death during the postpartum period." | ( Biodistribution of cocaine during perinatal period in rats. Dwivedi, C; Eighmy, AM; Singh, KK, 1996) | 0.29 |
| "The author discussed problems arising from the use of different mathematical dose-response models for extrapolation of cancer risk from high to low doses." | ( [Methods of extrapolating risk from from high to low doses and their effect on determining MAC values]. Szymczak, W, 1996) | 0.29 |
| " Dopamine neurons in the ventral tegmental area, on the other hand, were sub- and normosensitive to apomorphine following intermittent and continuous dosing regimens, respectively." | ( Differential effects of SCH 23390 on the apomorphine subsensitivity in the substantia nigra and ventral tegmental area 1 day following withdrawal from continuous or intermittent cocaine pretreatment. Ellinwood, EH; Gao, WY; Lee, TH, 1997) | 0.3 |
| "Subcutaneous injections of cocaine hydrochloride in sterile physiological saline were administered to rats at a dosage of 20 or 40 mg." | ( Focal necrotizing panniculitis and vascular necrosis in rats given subcutaneous injections of cocaine hydrochloride. Morrell, JI; Scott, DW; Vernotica, EM, 1997) | 0.3 |
| " Following this, subjects were administered ineffective doses of alcohol prior to further dose-response assessments with cocaine and with ineffective doses of cocaine prior to further dose-response assessments with alcohol." | ( The interaction of cocaine and alcohol on schedule-controlled responding. Riley, AL; Sobel, BF, 1997) | 0.3 |
| " Self-administration of cocaine (by rats) and morphine (by mice) was readily initiated and showed an inverted U-shaped unit dose-response curve." | ( Kappa-opioid receptor agonist U50,488H modulates cocaine and morphine self-administration in drug-naive rats and mice. Gerrits, MA; Kuzmin, AV; Semenova, S; Van Ree, JM; Zvartau, EE, 1997) | 0.3 |
| " In contrast, daily injections of ondansetron with cocaine significantly blocked the development of sensitization with an inverted U-shape dose-response curve." | ( Blockade of cocaine sensitization and tolerance by the co-administration of ondansetron, a 5-HT3 receptor antagonist, and cocaine. Ellinwood, EH; King, GR; Xiong, Z, 1997) | 0.3 |
| " 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) | 0.3 |
| "In this preliminary report from a placebo-controlled, double-blind, dose-response study on the use of pergolide mesylate for cocaine dependence in outpatients 8 out of 235 subjects noted adverse events requiring breaking of the blind." | ( Pergolide mesylate. Adverse events occurring in the treatment of cocaine dependence. Cochrane, CE; Kajdasz, DK; Malcolm, R; Moore, JW, 1997) | 0.3 |
| " No gender difference in HPA axis activation was observed in a dose-response study of cocaine-induced HPA activation in 10 day old rats." | ( Gender difference in cocaine-induced HPA axis activation. Francis, R; Kuhn, C, 1997) | 0.3 |
| "5 mg/kg) produced a leftward shift in the cocaine dose-response curve (0." | ( Modulation of the discriminative stimulus properties of cocaine: comparison of the effects of fluoxetine with 5-HT1A and 5-HT1B receptor agonists. Callahan, PM; Cunningham, KA, 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 |
| " These methods can be broadly divided into two types of approaches based on their treatment of dose-response data to estimate risks." | ( Dose-response analysis in risk assessment: evaluation of behavioral specificity. Glowa, JR, 1996) | 0.29 |
| " In the present study, the effects of maternal cocaine dosage and of cocaine-elicited maternal seizures on the progeny were studied." | ( Cocaine administration in pregnant rabbits alters cortical structure and function in their progeny in the absence of maternal seizures. Fischer, I; Friedman, E; Grayson, D; Jones, L; Levitt, P; Murphy, EH; O'Brien-Jenkins, A; Wang, HY; Wang, XH, 1997) | 0.3 |
| " In particular, in a first series of experiments, we determined the effects of suppressing endogenous glucocorticoids by adrenalectomy on a full dose-response curve of cocaine-induced locomotion and the influence, on this behavioral response, of different corticosterone concentrations, by implanting different corticosterone pellets in adrenalectomized rats." | ( Glucocorticoids and behavioral effects of psychostimulants. I: locomotor response to cocaine depends on basal levels of glucocorticoids. Barrot, M; De Jésus-Oliveira, C; Deroche, V; Le Moal, M; Marinelli, M; Piazza, PV; Rougé-Pont, F, 1997) | 0.3 |
| " Forty percent of animals died in the absence of Mg2+ infusion following high dosage of cocaine." | ( Magnesium protects against cocaine-induced hemorrhagic stroke in a rat model: a 31P-NMR in-vivo study. Altura, BM; Altura, BT; Gebrewold, A; Gupta, AR, 1997) | 0.3 |
| "This study describes the results of a 'side-by-side' comparison of two measurement techniques and two dosing regimens in a discrimination study using rats trained to either 10 mg/kg cocaine or 2 mg/kg 3,4-methylenedioxymethamphetamine (MDMA)." | ( Discrete versus cumulative dosing in dose-response discrimination studies. Schechter, MD, 1997) | 0.3 |
| " Dosing began on this day." | ( Retinal lesions in rat fetuses prenatally exposed to cocaine. Barroso-Moguel, R; Méndez-Armenta, M; Ríos, C; Romero-Díaz, V; Villeda-Hernández, J, ) | 0.13 |
| "A double-blind, Latin-square, placebo-controlled, dose-response study was conducted in an inpatient general clinical research center and clinical pharmacology unit of a university teaching hospital." | ( Cocaine effects on digital blood flow and diffusing capacity for carbon monoxide among chronic cocaine users. Becker, PM; Jasinski, DR; Preston, KL; Sullivan, JT; Testa, MP; Wigely, FM; Wise, RA, 1997) | 0.3 |
| " However, both wild-type and mutant mice had similar dose-response to cocaine." | ( Intravenous cocaine self-administration in mice lacking 5-HT1B receptors. Ator, R; Emmett-Oglesby, MW; Hen, R; Rocha, BA, 1997) | 0.3 |
| " These data indicate that procedural variables can alter dose-response curves for cocaine self-administration." | ( Dose-effect functions for cocaine self-administration: effects of schedule and dosing procedure. Dworkin, SI; Gaspard, TM; Kim, SA; Sizemore, GM; Vrana, SL; Walker, LE, 1997) | 0.3 |
| " Urine specimens collected in a cocaine dosing study in non-treatment-seeking subjects (n = 5) and a cocaine treatment trial (n = 37) were analyzed for the cocaine metabolite, benzoylecgonine, with qualitative and quantitative methods." | ( Assessment of cocaine use with quantitative urinalysis and estimation of new uses. Cone, EJ; Preston, KL; Schuster, CR; Silverman, K, 1997) | 0.3 |
| " Methadone dosing was flexible, with patient participation in dose decisions." | ( The relationship of methadone dose and other variables to outcomes of methadone maintenance. Maddux, JF; Prihoda, TJ; Vogtsberger, KN, 1997) | 0.3 |
| " Atropine (10(-6) M) upwardly shifted the dose-response curves of MEG, cocaine, and carbachol but not of procaine." | ( Effect of cocaine and methylecgonidine on intracellular Ca2+ and myocardial contraction in cardiac myocytes. Huang, L; Ishiguro, Y; Morgan, JP; Woolf, JH, 1997) | 0.3 |
| " Saliva obtained 2 h after dosing appeared to be free of contamination and demonstrated S/P ratios comparable with intravenous administration." | ( Cocaine disposition in saliva following intravenous, intranasal, and smoked administration. Cone, EJ; Darwin, WD; Oyler, J, 1997) | 0.3 |
| " When administered in combination with cocaine, D1 agonists displaying relatively low efficacy (SKF 38393, SKF 75670) attenuated both the rate-altering effects of cocaine on fixed-ratio responding and the discriminative-stimulus effects of cocaine, resulting in overall rightward shifts of the cocaine dose-response functions." | ( Differential modulation of behavioral effects of cocaine by low- and high-efficacy D1 agonists. Bergman, J; Rosenzweig-Lipson, S; Spealman, RD, 1997) | 0.3 |
| " Rats were pretreated with vehicle or an agonist, then dose-response curves for d-amphetamine or cocaine were generated." | ( mu-, delta- and kappa-opioid receptor agonists do not alter the discriminative stimulus effects of cocaine or d-amphetamine in rats. Holtzman, SG; Woolfolk, DR, 1997) | 0.3 |
| " Bilateral intra-NAc infusions of the PKA inhibitor Rp-cAMPS reduced baseline cocaine self-administration, shifted the dose-response curve for cocaine self-administration to the left, and induced relapse of cocaine-seeking behavior after extinction from cocaine self-administration, consistent with an enhancement of cocaine effects in each paradigm." | ( Involvement of cAMP-dependent protein kinase in the nucleus accumbens in cocaine self-administration and relapse of cocaine-seeking behavior. Barnhart, WJ; Genova, LM; Hope, BT; Nestler, EJ; Self, DW; Spencer, JJ, 1998) | 0.3 |
| " The researcher must ensure that the patients comply with the dosing schedule and that they are trained to return medications for accurate pill counts." | ( Management of clinical trials with new medications for cocaine dependence and abuse. Kiev, A, 1997) | 0.3 |
| " The same dosing sequence was repeated in week 8 with doubled (x 2) doses." | ( Drug testing with alternative matrices I. Pharmacological effects and disposition of cocaine and codeine in plasma, sebum, and stratum corneum. Cone, EJ; Joseph, RE; Ohuoha, C; Oyler, JM; Wstadik, AT, ) | 0.13 |
| "03 mg/kg/infusion), suggesting that DM shifted the dose-response curve for cocaine self-administration to the left." | ( Dextromethorphan alters the reinforcing effect of cocaine in the rat. Hong, SY; Jhoo, WK; Kim, HC; Park, BK, 1997) | 0.3 |
| " The dose-response function of both those psychostimulants did not change in the course of the experiment." | ( The role of the nitric oxide (NO) pathway in the discriminative stimuli of amphetamine and cocaine. Filip, M; Przegaliński, E, 1998) | 0.3 |
| " ADX had no effect on thresholds for lateral hypothalamic self-stimulation (LHSS) and did not alter the cocaine dose-response curve for lowering the LHSS threshold." | ( Effect of adrenalectomy on cocaine facilitation of medial prefrontal cortex self-stimulation. Abrahamsen, GC; Carr, KD, 1998) | 0.3 |
| " Sequential blood samples were collected for up to three days, and scalp hair samples were collected at 24 and 72 h after dosing and at monthly intervals for up to 12 months." | ( Incorporation of isotopically labeled cocaine into human hair: race as a factor. Harkey, MR; Henderson, GL; Jacob, P; Jones, RT; Zhou, C, ) | 0.13 |
| " The antagonist (1-10 mg/kg) failed to engender cocaine-appropriate responding when injected alone, and failed to modify the cocaine dose-response curve when injected as a pre-treatment; however, it reduced response rates dose-dependently." | ( The dopamine D4 receptor antagonist L-745,870: effects in rats discriminating cocaine from saline. Costanza, RM; Terry, P, 1998) | 0.3 |
| " Dose-response effects of fetal cocaine exposure on fetal growth and neonatal neurobehavior are reported using quantitative methods of ascertainment." | ( Neurological correlates of fetal cocaine exposure. Chiriboga, CA, 1998) | 0.3 |
| " The primary aim of this NIDA-funded study is to determine if a relationship exists between prenatal cocaine/alcohol exposures and school behavior and, if so, to determine if the relationship is characterized by a dose-response relationship." | ( Prenatal coke: what's behind the smoke? Prenatal cocaine/alcohol exposure and school-age outcomes: the SCHOO-BE experience. Ager, J; Compton, S; Covington, C; Delaney-Black, V; Martier, S; Sokol, R; Templin, T, 1998) | 0.3 |
| " In a separate experiment, animals were dosed as described above and were sacrificed by decapitation after the 30-minute treatment period." | ( Calcium channel antagonist isradipine attenuates cocaine-induced motor activity in rats: correlation with brain monoamine levels. Ali, SF; Arsah, TA; Mills, K; Shockley, DC, 1998) | 0.3 |
| " The dose-response relationship for cocaine demonstrated a a typical inverted U-shaped function." | ( Reinforcing effects of caffeine, ephedrine, and their binary combination in rats. Baird, TJ; Briscoe, RJ; Gauvin, DV; Holloway, FA; Vallett, M; Vanecek, SA, 1998) | 0.3 |
| " Lorazepam is more likely to require repeat dosing than droperidol." | ( Chemical restraint for the agitated patient in the emergency department: lorazepam versus droperidol. Derlet, RW; Duncan, DR; Richards, JR, ) | 0.13 |
| " Dose-response curves for each drug, conducted at each drug's t1/2, indicated considerable differences in potency (EC50) at stimulating [3H]MPP+ release from C6-hSERT cells [3beta-(4-iodophenyl)tropane-2beta-carboxylic acid methyl ester (RTI-55) > imipramine > 1-[2-diphenylmethoxy]ethyl-4-(3-phenylpropyl)-piperazine (GBR-12935) threo-(+/-)-methylphenidate > cocaine > mazindol > 2-beta-carbomethoxy-3beta-(4-fluorophenyl)tropane (CFT) > (+)methamphetamine > amphetamine > DA > fenfluramine > norepinephrine (NE) > 5-HT]." | ( [3H]substrate- and cell-specific effects of uptake inhibitors on human dopamine and serotonin transporter-mediated efflux. Eshleman, AJ; Janowsky, A; Johnson, RA; Meyers, T; Neve, KA, 1998) | 0.3 |
| " Overall, plasma cocaine levels and activity were well correlated and followed a predictable dose-response pattern." | ( Plasma cocaine levels and locomotor activity after systemic injection in virgin and in lactating maternal female rats. Morrell, JI; Vernotica, EM, 1998) | 0.3 |
| " However, a shift to the left in the cocaine dose-response function was observed revealing that the lesioned group self-administered significantly higher amounts of low doses of cocaine than control rats." | ( Effects of lesions of the nucleus basalis magnocellularis on the acquisition of cocaine self-administration in rats. Everitt, BJ; Robbins, TW; Robledo, P; Weissenborn, R, 1998) | 0.3 |
| " After escalation, drug consumption was characterized by an increased early drug loading and an upward shift in the cocaine dose-response function, suggesting an increase in hedonic set point." | ( Transition from moderate to excessive drug intake: change in hedonic set point. Ahmed, SH; Koob, GF, 1998) | 0.3 |
| "The effect of corticosterone on the acquisition of cocaine-seeking behavior was investigated in rats using ascending dose-response curves for intravenous cocaine self-administration." | ( Corticosterone facilitates the acquisition of cocaine self-administration in rats: opposite effects of the type II glucocorticoid receptor agonist dexamethasone. Goeders, NE; Mantsch, JR; Saphier, D, 1998) | 0.3 |
| " Chronic oral administration of cocaine was considered a feasible route because of the ease of administration, control of dosing patterns, and possible reduction in medical risks compared with the intravenous and smoked routes." | ( Cocaine and metabolite concentrations in plasma during repeated oral administration: development of a human laboratory model of chronic cocaine use. Cone, EJ; Jufer, RA; Walsh, SL, 1998) | 0.3 |
| " Physicians must adhere to recommendations to avoid mucous membrane contact and ensure appropriate dosing with these agents." | ( Topical anesthesia. Keyes, PD; Rizos, J; Tallon, JM, 1998) | 0.3 |
| " It is concluded that blockade of the kappa-opioid receptor by nor-binaltorphimine may produce a rightward shift of the unit dose-response relationship of cocaine reward, thus decreasing the sensitivity to cocaine reward." | ( Kappa-opioid receptor blockade with nor-binaltorphimine modulates cocaine self-administration in drug-naive rats. Gerrits, MA; Kuzmin, AV; Van Ree, JM, 1998) | 0.3 |
| "To determine if there was a dose-response relationship with regard to cocaine treatment and maternal behavior exhibited by lactating rats at doses that had not been previously investigated, we examined the effects of three doses of chronic cocaine administration throughout gestation on both onset and established maternal behavior." | ( A dose-response study of chronic cocaine on maternal behavior in rats. Ayers, AA; Johns, JM; Meter, KE; Nelson, CJ; Walker, CH, ) | 0.13 |
| " Next, the drug discrimination dose-response curves were redetermined." | ( A history of postponing shock does not appear to alter the discriminative stimulus effects of cocaine. Hasling, TA; Tatham, TA, 1998) | 0.3 |
| " Cumulative dose-response curves were assessed by injecting saline at the start of the second block and increasing cocaine doses at the onset of subsequent blocks." | ( Response suppression during cumulative dosing: a role for Pavlovian conditioning. Branch, MN; Walker, DJ, 1998) | 0.3 |
| "5 mg/kg) did not modify the dose-response curves of those psychostimulants." | ( Stimulation of serotonin (5-HT)1A receptors attenuates the locomotor, but not the discriminative, effects of amphetamine and cocaine in rats. Filip, M; Przegaliñski, E, 1997) | 0.3 |
| " Similar cocaine dose-response functions were observed with the differential outcome group and the control group and there was not a statistically significant effect of differential outcomes on the cocaine generalization curve." | ( The application of differential outcomes to a cocaine--saline discrimination procedure. Baker, LE; Morgan, TB, 1997) | 0.3 |
| "01 mg/kg) prior to cumulative doses of cocaine produced dose-dependent leftward shifts in the cocaine dose-response function." | ( Opioid enhancement of the discriminative stimulus effects of cocaine: evidence for involvement of mu and delta opioid receptors. Rowlett, JK; Spealman, RD, 1998) | 0.3 |
| " Cocaine and amphetamine dose-response analyses were conducted on drug-naive mice from the tenth generation." | ( Sensitivity to cocaine and amphetamine among mice selectively bred for differential cocaine sensitivity. Arros, DM; Henricks, KK; Marley, ME; Marley, RJ; Miner, LL, 1998) | 0.3 |
| "5; 250/9, and 500/18 micrograms/infusion; n = 4) under a fixed ratio (FR) 10: 20-s time-out schedule of reinforcement/multicomponent dosing session." | ( Synergistic elevations in nucleus accumbens extracellular dopamine concentrations during self-administration of cocaine/heroin combinations (Speedball) in rats. Co, C; Dworkin, SI; Hemby, SE; Smith, JE, 1999) | 0.3 |
| ") was administered 30 min prior to a neurotoxic MeAmp dosage for this species (2 x 2 mg/kg, 4 h apart); control subjects received MeAmp." | ( Dizocilpine and reduced body temperature do not prevent methamphetamine-induced neurotoxicity in the vervet monkey: [11C]WIN 35,428 - positron emission tomography studies. Harvey, DC; Huang, SC; Lacan, G; Melega, WP; Phelps, ME, 1998) | 0.3 |
| " For example, the frequency and duration of 'moving' dose-dependently increased after cocaine, while d-amphetamine and caffeine again produced bell-shaped dose-response curves." | ( D-amphetamine, cocaine and caffeine: a comparative study of acute effects on locomotor activity and behavioural patterns in rats. Antoniou, K; Hyphantis, T; Kafetzopoulos, E; Marselos, M; Papadopoulou-Daifoti, Z, 1998) | 0.3 |
| " Other dosage regimens and response measures need to be tested to understand the full scope of acute and chronic cocaine-ethanol interactions and the possible health consequences." | ( Acute and chronic alcohol-cocaine interactions in rats. MacKinnon, K; York, JL, 1999) | 0.3 |
| " A significant dose-dependent reduction in the number of reinforcer deliveries occurred at the peak of the cocaine dose-response function (0." | ( Effects of ethanol hangover on the operant self-administration of cocaine in rats. Briscoe, RJ; Gauvin, DV, 1999) | 0.3 |
| "We conclude that adverse neonatal effects associated with fetal cocaine exposure follow a dose-response relationship: newborns with higher levels of prenatal cocaine exposure show higher rates of impairments in fetal head growth and abnormalities of muscle tone, movements, and posture." | ( Dose-response effect of fetal cocaine exposure on newborn neurologic function. Bateman, D; Brust, JC; Chiriboga, CA; Hauser, WA, 1999) | 0.3 |
| "We investigated dose-response cocaine pharmacokinetic and metabolite profiles in a within-subject design after intravenous bolus cocaine administration (1-4 mg/kg) in rats under a food-limited regimen." | ( Pharmacokinetic-pharmacodynamic modeling of the psychomotor stimulant effect of cocaine after intravenous administration: timing performance deficits. Falk, JL; Foster, DM; Lau, CE; Ma, F, 1999) | 0.3 |
| "Controlled human dosing studies with drugs of abuse have revealed the importance of the chosen route of administration on the delivery of drugs to the bloodstream and to their site of action." | ( Recent discoveries in pharmacokinetics of drugs of abuse. Cone, EJ, 1998) | 0.3 |
| " At doses of cocaine on the descending limb of the cocaine dose-response curve, the mu-selective agonist DAMGO produced a dose-related decrease in cocaine self-administration when delivered by microinfusion into the VTA." | ( The mu opioid agonist DAMGO alters the intravenous self-administration of cocaine in rats: mechanisms in the ventral tegmental area. Adamson, KL; Chow, BL; Coen, KM; Corrigall, WA, 1999) | 0.3 |
| " Rates of withdrawal symptoms were low and did not differ across dosing schedules." | ( Plasma concentrations of buprenorphine 24 to 72 hours after dosing. Chawarski, MC; O'Connor, PG; Pakes, J; Schottenfeld, RS, 1999) | 0.3 |
| " AMPH at a dosage of 1 mg/kg significantly increased PEA concentration only in the striatum." | ( Effects of the administration of amphetamine, either alone or in combination with reserpine or cocaine, on regional brain beta-phenylethylamine and dopamine release. Karoum, F; Mosnaim, AD; Wolf, ME, ) | 0.13 |
| " The nasal cavity was isolated to prevent drainage of nasally applied dosing solution to nonnasal regions." | ( Direct transport of cocaine from the nasal cavity to the brain following intranasal cocaine administration in rats. Chen, Z; Chow, HS; Matsuura, GT, 1999) | 0.3 |
| " Using the experimental model of intravenous drug self-administration with a within-session dose-response paradigm, we first studied the course of cocaine intake over 14 sessions in rats." | ( Cocaine self-administration increases the incentive motivational properties of the drug in rats. Deroche, V; Le Moal, M; Piazza, PV, 1999) | 0.3 |
| " Further, cocaethylene shifted the dose-response functions for both cocaine and alcohol to the left and down, while cocaine and alcohol shifted the dose-response function for cocaethylene to the left and down." | ( The interaction of cocaethylene and cocaine and of cocaethylene and alcohol on schedule-controlled responding in rats. Riley, AL; Sobel, BF, 1999) | 0.3 |
| " Furthermore, due to the shape of the dose-response curve, in chronic cocaine but not in acute cocaine rats, ibogaine pretreatment enhanced the locomotor response to 5 and 10 mg/kg cocaine while decreasing the locomotor response to 40 mg/kg cocaine." | ( Pretreatment with the putative anti-addictive drug, ibogaine, increases the potency of cocaine to elicit locomotor responding: a study with acute and chronic cocaine-treated rats. Glick, SD; Maisonneuve, IM; Szumlinski, KK, 1999) | 0.3 |
| " Only with haloperidol (maximum 60%), risperidone (maximal 20%), and olanzapine (maximal 20%) a partial antagonism without clearcut dose-response was observed." | ( Inability of antipsychotics to antagonize the cueing properties of cocaine in rats. De Haes, P; Meert, TF; van Campenhout, N, 1999) | 0.3 |
| " The same dosing sequence was repeated in week 8 with doubled doses (high-dose week)." | ( Drug testing with alternative matrices II. Mechanisms of cocaine and codeine deposition in hair. Cone, EJ; Höld, KM; Joseph, RE; Rollins, DE; Wilkins, DG, 1999) | 0.3 |
| " Next, a morphine dose-response curve (1." | ( Sensitization to daily morphine injections in rats with unilateral lesions of the substantia nigra. Easterling, KW; Holtzman, SG; Kimmel, HL; Volpicelli, LA, 1999) | 0.3 |
| " Cocaine dose-response curves exhibited decreasing rates of response under the FR 70 schedule but increasing locomotor activity in a dose-related fashion." | ( Pharmacokinetic determinants of cocaine's differential effects on locomotor and operant behavior. Falk, JL; Lau, CE; Lobarinas, E; Nguyen, KN; Sun, L; Wang, Q; Wang, Y, 1999) | 0.3 |
| " We determined the influence of neuronal uptake blockade by cocaine upon the horizontal position of the dose-response curves for the inotropic and lusitropic effects exerted by noradrenaline in the presence of extra neuronal uptake blockade by hydrocortisone and in the presence and absence of adrenoceptor blockers." | ( Similar localisation of alpha1- and beta-adrenoceptors in rabbit heart in relation to sympathetic nerve endings. Dybvik, T; Osnes, JB; Skomedal, T, 1999) | 0.3 |
| " Sweat specimens were collected for 30 min at various times following administration of cocaine or codeine in controlled dosing studies." | ( Sweat testing for cocaine, codeine and metabolites by gas chromatography-mass spectrometry. Cone, EJ; Huestis, MA; Joseph, RE; Oyler, JM; Schoendorfer, D; Wstadik, AT, 1999) | 0.3 |
| "125 mg/kg) produced an apparent shift of the cocaine dose-response curve to the right." | ( The GABA(B) agonist CGP 44532 decreases cocaine self-administration in rats: demonstration using a progressive ratio and a discrete trials procedure. Andrews, M; Brebner, K; Froestl, W; Phelan, R; Roberts, DC, 1999) | 0.3 |
| " Subjective and cardiovascular responses were measured and blood samples for pharmacokinetic evaluation were obtained prior to cocaine dosing and at various times after dosing." | ( Attenuation of the euphoric effects of cocaine by the dopamine D1/D5 antagonist ecopipam (SCH 39166) Clarke, L; Coffin, V; Cornish, J; Glue, P; Kampman, K; Kaplan, HL; O'Brien, CP; Poole, S; Romach, MK; Sellers, EM; Somer, GR, 1999) | 0.3 |
| "We recently conducted a dose-response study of the effects of cocaine on several activity measures in the panel of BxD/Ty recombinant inbred mice." | ( Quantitative-trait loci analysis of cocaine-related behaviours and neurochemistry. Erwin, VG; Jones, BC; McClearn, GE; Plomin, R; Reed, CL; Rodriguez, LA; Tarantino, LM, 1999) | 0.3 |
| " Increases in cocaine dose attenuated the effects of the DA antagonists, resulting in rightward shifts of the cocaine dose-response curves." | ( The effects of benzamide analogues on cocaine self-administration in rhesus monkeys. Green, KL; Luedtke, RR; Mach, RH; Nader, MA, 1999) | 0.3 |
| " During food restriction cocaine served as a reinforcer for all monkeys, whereas during free feeding cocaine functioned as a reinforcer for 3 of 4 monkeys; with these monkeys, the dose-response curve obtained under free feeding was shifted to the right of that obtained under food restriction." | ( Cocaine self-administration under conditions of restricted and unrestricted food access. Macenski, MJ; Meisch, RA, 1999) | 0.3 |
| " It is suggested that these cocaine dosing regimes cause differential and dynamic changes in dopamine autoreceptor sensitivity during the early withdrawal phase." | ( Altered sensitivity of dopamine autoreceptors in rat accumbens 1 and 7 days after intermittent or continuous cocaine withdrawal. Davidson, C; Ellinwood, EH; Lee, TH, 2000) | 0.31 |
| ", 24 hours apart; a neurotoxic dosage for this species)." | ( Long-term methamphetamine-induced decreases of [(11)C]WIN 35,428 binding in striatum are reduced by GDNF: PET studies in the vervet monkey. Desalles, AA; Lacan, G; Melega, WP; Phelps, ME, 2000) | 0.31 |
| " Combination tests of glycineB ligands demonstrated that injection of a fixed dose of ACPC (200 mg/kg) or L-701,324 (3 mg/kg) together with different doses of AMPH or COC practically did not modify dose-response curves of the psychostimulants, nor did it affect their ED50 values." | ( Lack of effects of glycineB receptor ligands on the psychostimulant-induced discriminative stimuli in rats. Filip, M; Papp, M; Przegaliński, E, 2000) | 0.31 |
| " Although neurobehavioral abnormalities have been observed among cocaine-exposed infants in several studies and in some cases dose-response effects have been found, the specific neurobehaviors affected vary from one study to the next." | ( Adverse effects of fetal cocaine exposure on neonatal auditory information processing. Papageorgiou, AN; Potter, SM; Stack, DM; Zelazo, PR, 2000) | 0.31 |
| "The dose-response and duration effects of acute administration of the dopamine transporter (DAT) blocker cocaine and GBR12909 on dopamine synthesis and transporter availability were evaluated in the brains of conscious monkeys using high-resolution positron emission tomography (PET) in combination with microdialysis." | ( Dose-response and duration effects of acute administrations of cocaine and GBR12909 on dopamine synthesis and transporter in the conscious monkey brain: PET studies combined with microdialysis. Harada, N; Kakiuchi, T; Nishiyama, S; Ohba, H; Tsukada, H, 2000) | 0.31 |
| "In the first series of experiments, three dose-response curves were generated that examined the effect of three doses of baclofen (1." | ( Effect of baclofen on cocaine self-administration in rats reinforced under fixed-ratio 1 and progressive-ratio schedules. Brebner, K; Phelan, R; Roberts, DC, 2000) | 0.31 |
| " Under both dosing procedures, within a cocaine cycle (session), shorter (<45 s) inter-response times (IRT) progressively increased with doses, and reinforced responses decreased." | ( Sensitization of operant behavior to oral cocaine with increasing- and repetitive-dose regimens. Falk, JL; Lau, CE; Lobarinas, E, 1999) | 0.3 |
| " We show that individual differences in drug self-administration originate from vertical shift in the dose-response function." | ( Vertical shifts in self-administration dose-response functions predict a drug-vulnerable phenotype predisposed to addiction. Deroche-Gamonent, V; Le Moal, M; Piazza, PV; Rouge-Pont, F, 2000) | 0.31 |
| " Pentobarbital had no statistically significant effect on the cocaine dose-response function." | ( Neuroactive steroids attenuate cocaine-induced sucrose intake in rats, but not cocaine-induced hyperactivity in mice. Carter, RB; Huber, M; Suruki, M; Vanover, KE; Wilent, WB, 2000) | 0.31 |
| " Cocaine shifted the dose-response curve of noradrenaline to the left and enhanced its maximal effects." | ( Post-junctional mechanisms involved in the potentiation of cardiac adrenergic responses by cocaine. Bechara, G; El-Bizri, NM; Khoury, HA; Sabra, R; Sharaf, LH, 2000) | 0.31 |
| " Chronic (daily) dosing with a dose that reduced, but did not eliminate, responding then occurred until response rates stabilized." | ( Effects of cocaine and morphine under mixed-ratio schedules of food delivery: support for a behavioral momentum analysis. Byrne, T; Christian, L; Lesage, MG; Poling, A, 2000) | 0.31 |
| " Cocaine concentration in hair (which was higher if urine tests were positive) had a dose-response relationship with birth weight: a 27-g decrease (95% CI: -51." | ( Cocaine use during pregnancy and intrauterine growth retardation: new insights based on maternal hair tests. Kline, J; Kuhn, L; Levin, B; Ng, S; Susser, M, 2000) | 0.31 |
| "25 mg/infusion) limb of the dose-response function." | ( N-[1-(2-benzo[b]thiophenyl)Cyclohexyl]- piperidine (BTCP) exerts cocaine-like actions on drug-maintained responding in rats. Martin-Fardon, R; Weiss, F, 2000) | 0.31 |
| "Several xenobiotics, including cocaine, are dosed by the nasal route for systemic effects." | ( Nasal mucosal versus gastrointestinal absorption of nasally administered cocaine. Benowitz, NL; Fattinger, K; Jones, RT; Verotta, D, 2000) | 0.31 |
| " The median systemic bioavailability after oral dosing was 33%." | ( Nasal mucosal versus gastrointestinal absorption of nasally administered cocaine. Benowitz, NL; Fattinger, K; Jones, RT; Verotta, D, 2000) | 0.31 |
| "Our data suggest that the main reason addicts prefer nasal to oral cocaine dosing is faster absorption, enhancing the subjective effects rather than higher bioavailability." | ( Nasal mucosal versus gastrointestinal absorption of nasally administered cocaine. Benowitz, NL; Fattinger, K; Jones, RT; Verotta, D, 2000) | 0.31 |
| "Prenatal cocaine exposure has been associated with alterations in neonatal behavior and more recently a dose-response relationship has been identified." | ( Teacher-assessed behavior of children prenatally exposed to cocaine. Ager, J; Covington, C; Czerwinski, RH; Delaney-Black, V; Leddick, L; Martier, S; Nordstrom-Klee, B; Sokol, RJ; Templin, T, 2000) | 0.31 |
| "To explore the effects of behavioral sensitization on the anatomy of the nucleus accumbens shell, we employed a typical cocaine dosing paradigm and assessed tyrosine hydroxylase immunoreactive varicosities in five different areas of the shell, as well as the core of the nucleus accumbens." | ( Assessment of tyrosine hydroxylase immunoreactive innervation in five subregions of the nucleus accumbens shell in rats treated with repeated cocaine. Stellar, JR; Todtenkopf, MS, 2000) | 0.31 |
| " Drug intake was decreased across several doses of cocaine, with the dose-response curve for cocaine self-administration shifted downward and flattened, suggesting that CP-154,526 decreased cocaine reinforcement." | ( Effects of the CRH receptor antagonist CP-154,526 on intravenous cocaine self-administration in rats. Goeders, NE; Guerin, GF, 2000) | 0.31 |
| " For patients with residual disability, the dosage was escalated during the first 10 weeks." | ( Pramipexole vs levodopa as initial treatment for Parkinson disease: A randomized controlled trial. Parkinson Study Group. , 2000) | 0.31 |
| " Plasma and saliva specimens were collected periodically during the dosing sessions and during the one-week withdrawal phase at the end of the study." | ( Elimination of cocaine and metabolites in plasma, saliva, and urine following repeated oral administration to human volunteers. Cone, EJ; Jufer, RA; Levine, BS; Walsh, SL; Wstadik, A, 2000) | 0.31 |
| " A significant dose-response relationship was observed for hair specimens." | ( The disposition of cocaine and opiate analytes in hair and fingernails of humans following cocaine and codeine administration. Cone, EJ; Goldberger, BA; Joseph, RE; Ropero-Miller, JD, 2000) | 0.31 |
| "Despite wide use of cumulative-dosing procedures to evaluate dose-response relations, limited attention has been paid to investigating drug concentration-effect relations." | ( Oral cocaine pharmacokinetics and pharmacodynamics in a cumulative-dose regimen: pharmacokinetic-pharmacodynamic modeling of concurrent operant and spontaneous behavior within an operant context. Falk, JL; Lau, CE; Simpao, A; Sun, L; Wang, Q, 2000) | 0.31 |
| "6 mg/kg) did not attenuate the discriminative-stimulus effects of the training dose of cocaine or methamphetamine and did not produce any shift in the cocaine and methamphetamine dose-response curves." | ( Failure of baclofen to modulate discriminative-stimulus effects of cocaine or methamphetamine in rats. Goldberg, SR; Kutkat, SW; Miller, CR; Munzar, P, 2000) | 0.31 |
| " This study demonstrates that the pigment-mediated differences in the incorporation of COC and its metabolites noted at 14 days after dosing are also evident a few hours after drug administration." | ( The incorporation of cocaine and metabolites into hair: effects of dose and hair pigmentation. Hubbard, DL; Rollins, DE; Wilkins, DG, 2000) | 0.31 |
| " Sixty female Long-Evans hooded rats were randomly assigned to one of three conditions (20 mg cocaine/kg/day, saline injected and uninjected), for dosing from postnatal day 21 (P21) through P60." | ( Adolescent cocaine and injection stress effects on the estrous cycle. Medici, CN; Morin, B; Raap, DK; Smith, RF, 2000) | 0.31 |
| " Self-administration of cocaine was readily initiated according to an inverted U-shaped unit dose-response curve." | ( Influence of buprenorphine, butorphanol and nalbuphine on the initiation of intravenous cocaine self-administration in drug naive mice. Gerrits, MA; Kuzmin, AV; van Ree, JM; Zvartau, EE, 2000) | 0.31 |
| " That dosage did not compromise mother or pup viability, weight, or gestation length." | ( The effects of prenatal cocaine exposure and genotype on the ultrasonic calls of infant mice. Benno, RH; Hahn, ME; Phadia, E; Schanz, N, 2000) | 0.31 |
| " The pigeons were then divided into six pairs, matched with respect to acute dose-response curves." | ( A comparison of fixed and variable doses of cocaine in producing and augmenting tolerance to its effects on schedule-controlled behavior. Branch, MN; Pinkston, JW; Wilhelm, MJ, 2000) | 0.31 |
| " Analysis by EIA and by gas chromatography-mass spectrometry (GC-MS) of oral fluids and urine specimens collected from current drug users in treatment programs and subjects participating in research studies involving controlled dosing of cocaine provided assessment of the clinical sensitivity and specificity of the STC Cocaine Metabolite EIA." | ( Immunoassay for detection of cocaine/metabolites in oral fluids. Cannon, A; Davis, A; Fries, T; Kardos, K; Niedbala, RS, ) | 0.13 |
| " The analytical performance of 12 commercially available ELISAs was determined in terms of binding characteristics, dose-response curves, limits of detection, sensitivity, intra- and interassay imprecision, and lot-to-lot reproducibility." | ( Comparison of ELISAs for opiates, methamphetamine, cocaine metabolite, benzodiazepines, phencyclidine, and cannabinoids in whole blood and urine. Kerrigan, S; Phillips, WH, 2001) | 0.31 |
| " When RTI 111 was given as a pretreatment to monkeys self-administering MA under a progressive-ratio schedule, the MA dose-response function shifted to the left and down." | ( Reinforcing and discriminative stimulus effects of RTI 111, a 3-phenyltropane analog, in rhesus monkeys: interaction with methamphetamine. Anderson, KG; Carroll, FI; Ranaldi, R; Woolverton, WL, 2000) | 0.31 |
| " The changes in effects across time (effect-time profiles) and dose-response curves (DRCs) were constructed to evaluate the duration of action and potency (ED50) of both drugs." | ( Contribution of the active metabolite, norcocaine, to cocaine's effects after intravenous and oral administration in rats: pharmacodynamics. Falk, JL; Lau, CE; Simpao, A; Sun, L; Wang, Q, 2001) | 0.31 |
| "The present study investigated the impact of dosing schedule on cocaine-induced receptor alterations." | ( The frequency of cocaine administration impacts cocaine-induced receptor alterations. Cuntapay, M; Kreek, MJ; Unterwald, EM, 2001) | 0.31 |
| "625-5 mg/kg) did not affect the dose-response curve for cocaine." | ( Effects of corticosterone and its synthesis blockade on the cocaine-induced discriminative stimulus effects in rats. Filip, M; Nowak, E; Przegaliński, E; Siwanowicz, J, ) | 0.13 |
| " Dose-response curves for morphine (1." | ( Repeated cocaine administration does not alter morphine-induced rotational behavior in nigrally denervated rats. Holtzman, SG; Kimmel, HL, 2001) | 0.31 |
| " This dosing regimen of MDMA is likely to release DA and to be neurotoxic to 5-HT neurons." | ( Pre-exposure to (+/-)3,4-methylenedioxy-methamphetamine (MDMA) facilitates acquisition of intravenous cocaine self-administration in rats. Fletcher, PJ; Robinson, SR; Slippoy, DL, 2001) | 0.31 |
| " We performed this study to determine whether repeated dosing with risperidone reduced the subjective effects of experimentally administered cocaine." | ( Risperidone pre-treatment reduces the euphoric effects of experimentally administered cocaine. Kalechstein, AD; Ling, W; Newton, TF; Tervo, K; Uslaner, J, 2001) | 0.31 |
| " Impairment on the DSST waned with repeated dosing suggesting the development of tolerance." | ( Repeated administration of the D1/5 antagonist ecopipam fails to attenuate the subjective effects of cocaine. Bigelow, GE; Donny, EC; Nann-Vernotica, E; Walsh, SL, 2001) | 0.31 |
| "Although the performance effects verify that these doses of ecopipam were behaviorally active, the absence of an attenuation of cocaine's effects of craving for cocaine in this chronic dosing paradigm suggests this compound is unlikely to be an effective pharmacotherapy for cocaine abuse." | ( Repeated administration of the D1/5 antagonist ecopipam fails to attenuate the subjective effects of cocaine. Bigelow, GE; Donny, EC; Nann-Vernotica, E; Walsh, SL, 2001) | 0.31 |
| " The article shows the usual dosage and "therapeutic", toxic and fatal concentrations." | ( [Pharmacokinetic and toxicokinetic parameters of some drugs of abuse]. Panas, M, 2001) | 0.31 |
| "5 mg/kg) produced a leftward shift in the cocaine dose-response curve; pretreatment with CP 94253 (5 mg/kg) prior to a dose of cocaine (2." | ( Role of 5-hydroxytryptamine1B receptors and 5-hydroxytryptamine uptake inhibition in the cocaine-evoked discriminative stimulus effects in rats. Filip, M; Nowak, E; Papla, I; Przegaliński, E, 2001) | 0.31 |
| "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 |
| " Although the current analysis did not rule out differences in pharmacological effects as a contributing factor, the results are consistent with an interpretation of a dose-response association between psychosocial/psychotherapeutic support and detoxification outcome." | ( Predictors for completing an inpatient detoxification program among intravenous heroin users, methadone substituted and codeine substituted patients. Backmund, M; Eichenlaub, D; Meyer, K; Schütz, CG, 2001) | 0.31 |
| "Initially, in phase 1, 30 experiments were performed to study the dose-response curve of both drugs." | ( Combined effects of cocaine and nicotine on cardiovascular performance in a canine model. Billie, MD; Jain, AC; Mehta, MC, 2001) | 0.31 |
| "Hemodynamic parameters observed were Phase I: Dose-response curve established the IV bolus dose of cocaine 2 mg/kg and nicotine 50 microg/kg." | ( Combined effects of cocaine and nicotine on cardiovascular performance in a canine model. Billie, MD; Jain, AC; Mehta, MC, 2001) | 0.31 |
| " These data suggest that these kappa-agonists may be safely administered in the presence of cocaine but do not produce significant attenuation of cocaine's direct effects or self-administration under these acute dosing conditions." | ( Enadoline and butorphanol: evaluation of kappa-agonists on cocaine pharmacodynamics and cocaine self-administration in humans. Bigelow, GE; Geter-Douglas, B; Strain, EC; Walsh, SL, 2001) | 0.31 |
| " In the multistage dosing design, subjects initially received placebo (PBO) or 15 to 30 mg of dextroamphetamine sulfate, sustained-release capsules." | ( Dextroamphetamine for cocaine-dependence treatment: a double-blind randomized clinical trial. Creson, D; Daruzska, LA; Grabowski, J; Moeller, FG; Rhoades, H; Schmitz, J; Stotts, A, 2001) | 0.31 |
| " When studied in combination with a range of cocaine doses, treatment with the agonists SKF 83959, SKF 77434, SKF 81297, and the antagonist SCH 39166 produced overall rightward and downward shifts in the dose-response function for cocaine self-administration." | ( Modulation of cocaine and food self-administration by low- and high-efficacy D1 agonists in squirrel monkeys. Platt, DM; Rowlett, JK; Spealman, RD, 2001) | 0.31 |
| " A bitonic dose-response function was obtained for response rates and the time with head in the food hopper, whereas dose-dependent decreases were observed in the mathematical index of curvature (Fry, Kelleher, & Cook, 1960)." | ( Tolerance to the effects of cocaine on performance under behavior-correlated reinforcement magnitude. Branch, MN; Brodkorb, GW; Miller, ML, 2001) | 0.31 |
| " When administered as a pretreatment, heroin shifted the dose-response function for cocaine to the left in the three monkeys for which heroin engendered cocaine-lever responding, but did not alter the DS effects of cocaine in the fourth monkey." | ( Similar enhancement of the discriminative stimulus effects of cocaine and GBR 12909 by heroin in squirrel monkeys. Platt, DM; Rowlett, JK; Spealman, RD, 2001) | 0.31 |
| " The purpose of the study was to investigate the nature of the shift of the dose-response curve and generalization to cocaine (COC) as a function of training dose." | ( Effects of training dose on amphetamine drug discrimination: dose-response functions and generalization to cocaine. Barrett, RJ; Caul, WF; Stadler, JR, ) | 0.13 |
| " After acquisition, a series of generalization/substitution tests were performed using a cumulative dosing procedure." | ( The effects of perinatal exposure to lead on the discriminative stimulus properties of cocaine and related drugs in rats. Bratton, GR; Miller, DK; Nation, JR, 2001) | 0.31 |
| " The nasal cavity of male Sprague-Dawley rats was isolated to prevent drainage of nasally applied dosing solution to non-nasal regions." | ( Direct nose-brain transport of benzoylecgonine following intranasal administration in rats. Anavy, N; Chow, HH; Villalobos, A, 2001) | 0.31 |
| " Sensitivity to low doses of cocaine falling on the ascending limb of the acquisition dose-response curve can be augmented by increasing circulating levels of corticosterone, but similar treatments do not affect responding maintained by higher doses." | ( The HPA axis and cocaine reinforcement. Goeders, NE, ) | 0.13 |
| " In rodent models, deficits in short-term memory have been noted in some, but not all, paradigms, although these studies also differ in routes of administration and dosing models." | ( Prenatal cocaine exposure disrupts non-spatial, short-term memory in adolescent and adult male rats. Elsworth, JD; Morrow, BA; Roth, RH, 2002) | 0.31 |
| "The results demonstrated that 7-NI reduced responses maintained by the cocaine training dose and produced a downward shift in the cocaine dose-response curve." | ( Neuronal nitric oxide synthase inhibition decreases cocaine self-administration behavior in rats. Collins, SL; Kantak, KM, 2002) | 0.31 |
| " The ability of (+/-)-1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane (DOI), a 5-HT(2A) receptor agonist, and ketanserin, a 5-HT(2A) receptor antagonist, to either substitute for or block the discriminative-stimulus effects of cocaine, or to shift the cocaine dose-response curve, was evaluated." | ( Differential involvement of 5-HT(2A) receptors in the discriminative-stimulus effects of cocaine and methamphetamine. Goldberg, SR; Justinova, Z; Kutkat, SW; Munzar, P, 2002) | 0.31 |
| " Both the values of clearance and terminal elimination rate constant for the self-administration paradigm were significantly greater than those after the bolus cocaine dosing series (0." | ( The pharmacokinetic determinants of the frequency and pattern of intravenous cocaine self-administration in rats by pharmacokinetic modeling. Lau, CE; Sun, L, 2002) | 0.31 |
| " We also analyze various biomarkers for cocaine detection in newborns and their mothers and, finally, we review pharmacogenetic and dose-response relation susceptibility factors." | ( [Cocaine toxicity in the newborn. Detection and prevalence]. García-Algar, O; López Segura, N; Mur Sierra, A, 2002) | 0.31 |
| " For patients with residual disability, the dosage was escalated during the first 10 weeks, and subsequently, open-label levodopa could be added." | ( Dopamine transporter brain imaging to assess the effects of pramipexole vs levodopa on Parkinson disease progression. , 2002) | 0.31 |
| "1 ml aliquots of 10% ethanol or 5% sucrose reinforcers were dosed once a week with cocaine (0, 5 and 15 mg/kg intraperitoneally) 30 min prior to their daily operant session using a Latin square design." | ( Effects of cocaine on responding for ethanol or sucrose under a progressive ratio schedule. Brown, G; Stephens, DN, 2002) | 0.31 |
| " Two advantages of this technique are: reduced variability in dose-response curves because the subject is his/her own control, and the (18)F label allows evaluation of longer-acting drugs." | ( Measurement of dopamine transporter occupancy for multiple injections of cocaine using a single injection of [F-18]FECNT. Goodman, MM; Hoffman, JM; Howell, LL; Kilts, CD; Lindsey, KP; Martarello, L; Votaw, JR, 2002) | 0.31 |
| "25-5 mg/kg) did not affect the cocaine dose-response curve or its ED50 values." | ( Does combined treatment with novel antidepressants and a dopamine D3 receptor agonist reproduce cocaine discrimination in rats? Filip, M; Papla, I, ) | 0.13 |
| " Attempts to estimate a dose-response relationship between solvent abuse and either neuropsychological tests or magnetic resonance imaging (MRI) abnormalities were also undertaken." | ( Neuropsychologic impairment and MRI abnormalities associated with chronic solvent abuse. Busenbark, D; Dreisbach, J; Grigsby, J; Grigsby, P; Rosenberg, NL, 2002) | 0.31 |
| " No clear dose-response relationship was seen between solvent abuse and abnormalities on neuropsychological tests, but a strong dose-response relationship was seen in the presence of MRI abnormalities." | ( Neuropsychologic impairment and MRI abnormalities associated with chronic solvent abuse. Busenbark, D; Dreisbach, J; Grigsby, J; Grigsby, P; Rosenberg, NL, 2002) | 0.31 |
| " These findings expand upon previous data regarding neurological abnormalities in solvent abusers, by demonstrating a dose-response relationship with MRI abnormalities." | ( Neuropsychologic impairment and MRI abnormalities associated with chronic solvent abuse. Busenbark, D; Dreisbach, J; Grigsby, J; Grigsby, P; Rosenberg, NL, 2002) | 0.31 |
| " In Experiment 2, a similar dose-response function was obtained with either the empty tube or a lever as the operant." | ( Cocaine-induced suppression of saccharin intake: a model of drug-induced devaluation of natural rewards. Grigson, PS; Twining, RC, 2002) | 0.31 |
| "Cocaine dosing regimens in animals are used to model behavioral and neurochemical changes in human cocaine abusers." | ( Behavioral sensitization is greater after repeated versus single chronic cocaine dosing regimens. Davidson, C; Ellinwood, EH; Lazarus, C; Lee, TH, 2002) | 0.31 |
| " When higher doses falling on the descending limb of the cocaine dose-response curve are self-administered, plasma corticosterone can still reach this reward threshold even when synthesis is inhibited and drug intake is not affected." | ( Stress and cocaine addiction. Goeders, NE, 2002) | 0.31 |
| " High grooming (HG) rats reached considerably higher breakpoints than low grooming (LG) rats but showed no differences in acquisition rate and dose-response relationships." | ( Enhanced motivation to self-administer cocaine is predicted by self-grooming behaviour and relates to dopamine release in the rat medial prefrontal cortex and amygdala. Binnekade, R; de Vries, TJ; Homberg, JR; Raasø, HS; Schoffelmeer, AN; van den Akker, M; Wardeh, G, 2002) | 0.31 |
| " Both compounds maintained self-administration with sigmoidal or biphasic dose-response functions." | ( Comparison of the reinforcing efficacy of two dopamine D2-like receptor agonists in rhesus monkeys using a progressive-ratio schedule of reinforcement. Ranaldi, R; Woolverton, WL, 2002) | 0.31 |
| " cocaine-induced activity in the mouse, which allows within-session determination of the dose-response function, and assessment of the development of behavioral sensitization and conditioned activity." | ( Intravenous cocaine-induced activity in A/J and C57BL/6J mice: behavioral sensitization and conditioned activity. Katz, JL; Mead, AN; Rocha, BA, 2002) | 0.31 |
| "Acute nicotine treatment produced an inverted U-shaped dose-response function with lower doses increasing and the highest dose decreasing the number of cocaine infusions obtained during a session." | ( Enhancement of cocaine-seeking behavior by repeated nicotine exposure in rats. Bechtholt, AJ; Mark, GP, 2002) | 0.31 |
| " Sustained exposure to high levels of cocaine produced a shift in the dose-response curve to the right indicating tolerance to the reinforcing effects." | ( Patterns of cocaine self-administration in rats produced by various access conditions under a discrete trials procedure. Brebner, K; Lynch, WJ; Roberts, DC; Vincler, M, 2002) | 0.31 |
| "5 mg/kg) produced a leftward shift in the cocaine dose-response curve and a decrease in its ED(50) value." | ( Effects of serotonin (5-HT)(1B) receptor ligands, microinjected into accumbens subregions, on cocaine discrimination in rats. Filip, M; Jungersmith, K; Nowak, E; Papla, I; Przegaliński, E, 2002) | 0.31 |
| "Initial studies established a dose-response curve using different concentrations of Form, and also determined that avoidance of Form was abolished by pretreatment with an anxiolytic dose of chlordiazepoxide." | ( Repeated cocaine decreases the avoidance response to a novel aversive stimulus in rats. Davidson, DL; Hochstatter, T; Sorg, BA; Sylvester, PW, 2002) | 0.31 |
| " Mice then received cocaine (3-25 mg/kg) intravenously according to a within-session cumulative dose-response design." | ( Intravenous cocaine induced-activity and behavioural sensitization in norepinephrine-, but not dopamine-transporter knockout mice. Donovan, DM; Katz, JL; Mead, AN; Rocha, BA, 2002) | 0.31 |
| " However, 24-h dosing of dopamine (DA) agonists may induce side effects of insomnia and psychosis, as well as anergia and anhedonia which may actually potentiate abuse." | ( Effect of daily dosing duration of direct and indirect dopamine receptor agonists: cocaine cross-tolerance following chronic regimens. Davidson, C; Ellinwood, EH; King, GR; Lee, TH; Yu, GZ, 2002) | 0.31 |
| " Both compounds maintained responding with sigmoidal or biphasic dose-response functions (0." | ( Reinforcing strength of a novel dopamine transporter ligand: pharmacodynamic and pharmacokinetic mechanisms. Kozikowski, A; Ordway, GA; Paul, IA; Petukhov, P; Ranaldi, R; Wang, Z; Woolverton, WL, 2002) | 0.31 |
| "A multiple schedule was used to evaluate the effects of changes in the magnitude of food reinforcement on the self-administration cocaine dose-response curve and on the behavioral potency of a dopamine receptor antagonist to decrease food- and cocaine-maintained responding." | ( Cocaine- and food-maintained responding under a multiple schedule in rhesus monkeys: environmental context and the effects of a dopamine antagonist. Mach, RH; Morgan, D; Nader, MA; Sinnott, RS, 2002) | 0.31 |
| " After completion of cocaine dose-response curves, the effects of the dopamine D(2)/D(3) receptor antagonist 2,3-dimethoxy-N-(9-p-fluorobenzyl)-azabicyclo[3." | ( Cocaine- and food-maintained responding under a multiple schedule in rhesus monkeys: environmental context and the effects of a dopamine antagonist. Mach, RH; Morgan, D; Nader, MA; Sinnott, RS, 2002) | 0.31 |
| ") either during the second dosing regimen (3." | ( Ondansetron given in the acute withdrawal from a repeated cocaine sensitization dosing regimen reverses the expression of sensitization and inhibits self-administration. Davidson, C; Ellinwood, EH; Lee, TH; Xiong, Z, 2002) | 0.31 |
| " This robust context-dependent sensitization was long lasting, and not abolished by a 5-day extinction procedure involving cumulative saline dosing in the locomotor activity chambers." | ( Cocaine sensitization in the mouse using a cumulative dosing regime. Elliot, EE, 2002) | 0.31 |
| " In particular, we have demonstrated that daily exposure to electric footshock stress or daily pretreatment with corticosterone shifts the ascending limb of the dose-response curve for the acquisition of cocaine self-administration upwards and to the left." | ( Pretreatment with corticosterone attenuates the nucleus accumbens dopamine response but not the stimulant response to cocaine in rats. Goeders, NE; Steketee, JD, 2002) | 0.31 |
| " In sensitized animals, there was a leftward shift in the dose-response curve for cocaine induction of Fos in the accumbens, but not in the caudate." | ( Locomotor sensitization to cocaine is associated with increased Fos expression in the accumbens, but not in the caudate. Crombag, HS; Hope, BT; Jedynak, JP; Redmond, K; Robinson, TE, 2002) | 0.31 |
| " Overexpression of 5-HT1B receptors also shifted the dose-response curve for cocaine-conditioned place preference to the left, indicating alterations in the rewarding effects of cocaine." | ( Elevated expression of 5-HT1B receptors in nucleus accumbens efferents sensitizes animals to cocaine. Arvanitogiannis, A; Carlezon, WA; Neumaier, JF; Vincow, ES; Wise, RA, 2002) | 0.31 |
| " Some studies have found a dose-response relationship, so that increasing levels of abuse are associated with greater risk of hemorrhage." | ( Cerebrovascular complications of alcohol and sympathomimetic drug abuse. Bruno, A, 2003) | 0.32 |
| " After responding diminished, the effects of the D1 antagonist on the dose-response functions of the D1 agonist for reinstatement of cocaine-seeking behavior by response-contingent cue presentations or cocaine priming were examined." | ( D1-receptor drugs and cocaine-seeking behavior: investigation of receptor mediation and behavioral disruption in rats. Alleweireldt, AT; Blake, CB; Kirschner, KF; Neisewander, JL, 2003) | 0.32 |
| "To date, the literature on the intravenous self-administration of cocaine by laboratory animals lacks a compelling demonstration of an ascending limb to the dose-response function." | ( The ascending limb of the cocaine dose-response curve for reinforcing effect in rhesus monkeys. Flory, GS; Woods, JH, 2003) | 0.32 |
| "0015(b) mg/kg per injection than at higher doses demonstrates that satiety was not the mechanism by which cocaine intake was regulated on the ascending limb of the dose-response curve." | ( The ascending limb of the cocaine dose-response curve for reinforcing effect in rhesus monkeys. Flory, GS; Woods, JH, 2003) | 0.32 |
| " These null findings were attributable to an absence of a dose-response effect for the group interventions in the day treatment condition." | ( Day treatment for cocaine dependence: incremental utility over outpatient counseling and voucher incentives. Festinger, DS; Kirby, KC; Marlowe, DB; Merikle, EP; Platt, JJ; Tran, GQ, 2003) | 0.32 |
| "This study investigated how D(1) receptor agonists and antagonists alter the shape and position of the dose-response function for reinstatement of drug seeking induced by a cocaine prime accompanied by restoration of the cocaine-paired stimulus." | ( Attenuation of relapse to cocaine seeking by dopamine D1 receptor agonists and antagonists in non-human primates. Khroyan, TV; Platt, DM; Rowlett, JK; Spealman, RD, 2003) | 0.32 |
| " When combined with cocaine, all D(1) receptor agonists and antagonists produced rightward and downward shifts in the cocaine dose-response function." | ( Attenuation of relapse to cocaine seeking by dopamine D1 receptor agonists and antagonists in non-human primates. Khroyan, TV; Platt, DM; Rowlett, JK; Spealman, RD, 2003) | 0.32 |
| "Within subjects, latencies were most consistent from infusion to infusion at unit doses on the descending limb of the dose-response curve." | ( Variability of drug self-administration in rats. Katz, JL; Panlilio, LV; Pickens, RW; Schindler, CW, 2003) | 0.32 |
| "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 |
| " HD-23 shifted the dose-response curve on the PR schedule to the left." | ( Effect of HD-23, a potent long acting cocaine-analog, on cocaine self-administration in rats. Davies, HM; Gregg, TM; Jungersmith, KR; Phelan, R; Roberts, DC, 2003) | 0.32 |
| " It is currently debated if the steep ascending part of the biphasic dose-response curve typically obtained in multiple-dosing lever-press-based operant conditioning procedures represents a satiety-driven, all-or-none response or if the response is gradual and tightly adjusted to the various doses of the reinforcer." | ( Opioids, cocaine, and food change runtime distribution in a rat runway procedure. Saria, A; Sturm, K; Wakonigg, G; Zernig, G, 2003) | 0.32 |
| " Questions about effectiveness of contingency management alone, role of coexisting psychiatric disorders on treatment outcome, and individualized treatment dosing are offered." | ( Day treatment with contingency management for cocaine abuse in homeless persons: 12-month follow-up. Frison, S; McNamara, C; Michael, M; Milby, JB; Schumacher, JE; Usdan, S; Wallace, D, 2003) | 0.32 |
| " In this study, we show that the selective inactivation of the GR gene in the brains of mice profoundly flattened the dose-response function for cocaine intravenous self-administration and suppressed sensitization, two experimental procedures considered relevant models of addiction." | ( The glucocorticoid receptor as a potential target to reduce cocaine abuse. Aouizerate, B; Deroche-Gamonet, V; Ghozland, S; Izawa, R; Jaber, M; Kellendonk, C; Le Moal, M; Piazza, PV; Schütz, G; Sillaber, I; Spanagel, R; Tronche, F, 2003) | 0.32 |
| " Functional reporter gene assays as well as 5-HT uptake and inhibitor binding measures revealed a genotype-dependent dose-response to glucocorticosteroid administration, which was antagonized by RU 38486, a non-specific glucocorticosteroid hormone antagonist." | ( Glucocorticoid-regulated human serotonin transporter (5-HTT) expression is modulated by the 5-HTT gene-promotor-linked polymorphic region. Glatz, K; Heils, A; Lesch, KP; Mössner, R, 2003) | 0.32 |
| " After responding stabilized, dose-response curves were determined for other drugs." | ( Retention of sequential drug discriminations under fixed-interval schedules for long time periods without training. Li, M; McMillan, DE, 2003) | 0.32 |
| " Thus, for example, NT69L after five daily injections at a fixed dosage was as effective at reversing cocaine-induced hyperactivity as after the first injection." | ( Selective tolerance to the hypothermic and anticataleptic effects of a neurotensin analog that crosses the blood-brain barrier. Boules, M; Fauq, A; McCormick, D; McMahon, B; Richelson, E; Stewart, J; Wang, R; Warrington, L; Yerbury, S, 2003) | 0.32 |
| " The A1 and A2A receptor antagonists (CPT and MSX-3) both produced high levels of drug-lever selection when substituted for either methamphetamine or cocaine and significantly shifted dose-response curves of both psychostimulants to the left." | ( Involvement of adenosine A1 and A2A receptors in the adenosinergic modulation of the discriminative-stimulus effects of cocaine and methamphetamine in rats. Antoniou, K; Ferre, S; Goldberg, SR; Highkin, JL; Hockemeyer, J; Justinova, Z; Munzar, P; Pappas, LA; Segal, PN; Solinas, M, 2003) | 0.32 |
| " The present study determined the effects of escalated cocaine self-administration in rats on the cocaine dose-response function under a progressive ratio schedule." | ( Increased motivation for self-administered cocaine after escalated cocaine intake. Markou, A; Paterson, NE, 2003) | 0.32 |
| ", dose-response curves for the drugs alone and in combination) and behavioral arrangements (e." | ( Behavioral and physiological effects of cocaine in humans following triazolam. Baker, RW; Haga, JL; Rush, CR, 2003) | 0.32 |
| " Additionally, 3-OH-pip-BTCP (10 mg/kg) shifted the cocaine dose-response to the left." | ( 3-OH-pip-BTCP, a metabolite of the potent DA uptake blocker BTCP, exerts cocaine-like action in rats. Kamenka, JM; Lorentz, CU; Martin-Fardon, R; Weiss, F, 2003) | 0.32 |
| " A potential issue with these studies is that the same challenge dose is used in sensitized and control conditions even though that dose may occupy different positions on the respective dose-response curves." | ( Ability of dopamine antagonists to inhibit the locomotor effects of cocaine in sensitized and non-sensitized C57BL/6 mice depends on the challenge dose. Colpaert, FC; Kleven, MS; Koek, W; Prinssen, EP, 2004) | 0.32 |
| " No compound showed death when dosed at 100 mg/kg; however, most compounds did show signs typical of dopamine activity." | ( Synthesis, monoamine transporter binding properties, and behavioral pharmacology of a series of 3beta-(substituted phenyl)-2beta-(3'-substituted isoxazol-5-yl)tropanes. Carroll, FI; Howard, JL; Kuhar, MJ; Pawlush, N; Pollard, GT, 2004) | 0.32 |
| "We performed dose-response analysis of cocaine conditioned place preference (CPP) and locomotor activity in periadolescent and adult C57Bl/6J mice." | ( Effects of periadolescent versus adult cocaine exposure on cocaine conditioned place preference and motor sensitization in mice. Pratt, AR; Schramm-Sapyta, NL; Winder, DG, 2004) | 0.32 |
| " (+)-HA-966 was evaluated as pretreatment on a complete dose-response for cocaine self-administration." | ( Effects on cocaine and food self-administration of (+)-HA-966, a partial agonist at the glycine/NMDA modulatory site, in rats. Carnovali, F; Cervo, L; Cocco, A, 2004) | 0.32 |
| ") or placebo conditions (N = 35; identical in appearance and dosage rate) using a 2-group, experimental, 16-week double-blind design featuring thrice-weekly cognitive-behavioral drug counseling groups." | ( Randomized placebo-controlled trial of baclofen for cocaine dependence: preliminary effects for individuals with chronic patterns of cocaine use. Charuvastra, VC; Hsieh, YC; Kintaudi, PC; Ling, W; Rotheram-Fuller, EJ; Shoptaw, S; Yang, X, 2003) | 0.32 |
| " While mu-opioid receptor knockout did not affect basal locomotion, locomotor stimulant effects of cocaine were enhanced in a within-subjects dose-response experiment." | ( mu-Opioid receptor knockout mice display reduced cocaine conditioned place preference but enhanced sensitization of cocaine-induced locomotion. Goeb, M; Hall, FS; Li, XF; Sora, I; Uhl, GR, 2004) | 0.32 |
| " Groups of rats were trained to self-administer cocaine, heroin, or cocaine/heroin combinations using a within session dosing procedure in which three doses were available each session." | ( Effects of 2beta-propanoyl-3beta-(4-tolyl)-tropane (PTT) on the self-administration of cocaine, heroin, and cocaine/heroin combinations in rats. Davies, HM; Martin, TJ; Sizemore, GM; Smith, JE, 2004) | 0.32 |
| " Further, a cocaine dose-response demonstrates that the increased lever presses in anti-beta-endorphin antibody-injected rats was still present after substitution with a lower dose of cocaine." | ( A critical role for beta-endorphin in cocaine-seeking behavior. Roth-Deri, I; Schindler, CJ; Yadid, G, 2004) | 0.32 |
| "37 mg/kg) dose-response curve was determined during four laboratory sessions: Two administrations of the same cocaine dose occurred each session at 40-min intervals." | ( Intranasal cocaine in humans: acute tolerance, cardiovascular and subjective effects. Foltin, RW; Haney, M, 2004) | 0.32 |
| " Subsequently, access conditions were made equal (3 h) across groups, and dose-response curves for cocaine were compared." | ( Sex differences in the escalation of intravenous cocaine intake following long- or short-access to cocaine self-administration. Carroll, ME; Roth, ME, 2004) | 0.32 |
| " This experiment was therefore designed to determine the effects of acute, repeated and chronic ketoconazole administration on corticotropin-releasing hormone (CRH) content in hypothalamic and extra-hypothalamic brain sites in rats following the same dosing regimen that we use in our behavioral studies." | ( Effects of acute and chronic ketoconazole administration on hypothalamo--pituitary--adrenal axis activity and brain corticotropin-releasing hormone. Goeders, NE; Smagin, GN, 2004) | 0.32 |
| "08) than did controls, and dose-response relationships were also found between external exposure (exposure category) or internal doses (urinary 1-hydroxypyrene) and DNA damage." | ( [Relationship of polycyclic aromatic hydrocarbon exposure with peripheral blood lymphocyte DNA damage in coke oven workers]. Dai, YF; Gu, YP; He, FS; Leng, SG; Li, T; Li, XH; Niu, Y; Pan, ZF; Wang, YW; Wang, ZX; Xiao, J; Zhang, WZ; Zheng, YX, 2004) | 0.32 |
| "There are dose-effect and dose-response relationships between PAHs exposure and lymphocyte DNA damage in coke oven workers." | ( [Relationship of polycyclic aromatic hydrocarbon exposure with peripheral blood lymphocyte DNA damage in coke oven workers]. Dai, YF; Gu, YP; He, FS; Leng, SG; Li, T; Li, XH; Niu, Y; Pan, ZF; Wang, YW; Wang, ZX; Xiao, J; Zhang, WZ; Zheng, YX, 2004) | 0.32 |
| " These findings, though tempered by design limitations, suggest a complex non-linear cortisol attention/recognition dose-response relationship and call for further research to elucidate cortisol's effects on cognition and their role in the pathophysiology of cocaine dependence." | ( Effects of acute cortisol and cocaine administration on attention, recall and recognition task performance in individuals with cocaine dependence. Adler, CM; Elman, I; Hopper, JW; Karlsgodt, KH; Lukas, SE; Macklin, EA, 2004) | 0.32 |
| " The present study sought to extend this work by using a dose-response design with an alternate strain of rat." | ( Prenatal intravenous cocaine and the heart rate-orienting response: a dose-response study. Booze, RM; Foltz, TL; Mactutus, CF; Snow, DM; Strupp, BJ, ) | 0.13 |
| " Following the acute dose-response curve, mice received saline followed by 5 days of 20." | ( Long-term, low-level adolescent nicotine exposure produces dose-dependent changes in cocaine sensitivity and reward in adult mice. Kelley, BM; Rowan, JD, ) | 0.13 |
| " Pigeons in the saline group were also exposed to a daily dosing regimen for 100 more sessions except that saline was substituted once every 5 days." | ( Tolerance to response-disruptive effects of cocaine is facilitated by opportunity to respond in the absence of drug. Branch, MN; Miller, ML, 2004) | 0.32 |
| " In phase I (30 experiments on 8 dogs), the doses were established by dose-response curve." | ( Effects of cocaine and caffeine alone and in combination on cardiovascular performance: an experimental hemodynamic and coronary flow reserve study in a canine model. Billie, M; Jain, AC; Mehta, MC, 2004) | 0.32 |
| " In rats dosed with this agent (2." | ( Gene transfer of cocaine hydrolase suppresses cardiovascular responses to cocaine in rats. Atanasova, E; Brimijoin, S; Gao, Y; Pancook, JD; Sui, N; Watkins, JD, 2005) | 0.33 |
| " The variation in behaviors of flies dosed with the airbrush was smaller than that of the smoke-dosed flies, indicating that the airbrush method gives better reproducibility." | ( A novel method of cocaine delivery to fruit flies using a graphic arts airbrush. Hirsh, J; Lease, KA, 2005) | 0.33 |
| "We compared two different methamphetamine dosing regimens and found distinct long-term behavioral and neurochemical changes." | ( Acute and chronic continuous methamphetamine have different long-term behavioral and neurochemical consequences. Davidson, C; Ellinwood, EH; Lee, TH, 2005) | 0.33 |
| " Initial studies examined the dose-response effects of injection of baclofen (0." | ( Injections of baclofen into the ventral medial prefrontal cortex block the initiation, but not the expression, of cocaine sensitization in rats. Beyer, CE; Steketee, JD, 2005) | 0.33 |
| ", number of responses and interinfusion intervals) indicated a significant main effect of cocaine dose, consistent with predicted dose-response relationships (i." | ( A paradigm to investigate the self-regulation of cocaine administration in humans. Berman, R; Coric, V; Gueorguieva, R; Jain, D; Jatlow, P; Lynch, WJ; Malison, RT; Self, D; Sughondhabirom, A, 2005) | 0.33 |
| " Prior nicotine treatment enhanced the dose-response to cocaine." | ( Periadolescent nicotine exposure causes heterologous sensitization to cocaine reinforcement. Davis, BJ; McMillen, BA; Soderstrom, K; Williams, HL, 2005) | 0.33 |
| " Moreover, the cocaine dose-response curve was flattened in the knockout group, suggesting that the differences observed between genotypes were related to changes in the reinforcing efficacy of the training dose of cocaine." | ( Lack of CB1 cannabinoid receptor impairs cocaine self-administration. Ledent, C; Maldonado, R; Mendizábal, V; Parmentier, M; Robledo, P; Soria, G; Touriño, C; Valverde, O, 2005) | 0.33 |
| " Dose-response curves obtained with different doses of cocaine used revealed a shift to the left in the locomotor activity curves of D rats compared to controls." | ( Pharmacological reactivity to cocaine in adult rats undernourished at perinatal age: behavioral and neurochemical correlates. Cuadra, GR; Isoardi, NA; Orsingher, OA; Valdomero, A, 2005) | 0.33 |
| " PET studies revealed that unlike more DAT selective analogues such as GBR 12 909 and 3-(4-chlorophenyl)tropane-2-carboxylic acid phenyl ester (RTI-113), 3b shows no detectible DAT occupancy when dosed at its ED(50) for reduction of cocaine self-administration." | ( Synthesis and monoamine transporter binding properties of 3beta-(3',4'-disubstituted phenyl)tropane-2beta-carboxylic acid methyl esters. Blough, BE; Carroll, FI; Howell, LL; Kuhar, MJ; Navarro, HA; Nie, Z, 2005) | 0.33 |
| "09 mg/kg/injection in a within-session dose-response curve (0." | ( Blunted response to cocaine in the Flinders hypercholinergic animal model of depression. Fagergren, P; Goiny, M; Hurd, YL; Overstreet, DH, 2005) | 0.33 |
| " Upon examining the effect of increasing concentrations of TB-1-099 on the apparent K(d) and B(max) of [(125)I]RTI-55 binding to hSERT, we found that TB-1-099 decreased the B(max) in a dose-dependent manner and affected the apparent K(d) in a manner well described by a sigmoid dose-response curve." | ( Studies of the biogenic amine transporters. XI. Identification of a 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine (GBR12909) analog that allosterically modulates the serotonin transporter. Boos, TL; Calhoun, WJ; Dersch, CM; Greiner, E; Jacobson, AE; Nightingale, B; Rice, KC; Rothman, RB, 2005) | 0.33 |
| " The dose-response curve for cocaine-induced convulsions was significantly shifted to the right in NET-KO mice, indicating higher seizure thresholds." | ( Genetic deletion of the norepinephrine transporter decreases vulnerability to seizures. Kaminski, RM; Rocha, BA; Shippenberg, TS; Witkin, JM, ) | 0.13 |
| " Here, we examined the pharmacokinetic profile of MDMA in squirrel monkeys after different routes of administration, and explored the relationship between acute plasma MDMA concentrations after repeated oral dosing and subsequent brain serotonin deficits." | ( Pharmacokinetic profile of single and repeated oral doses of MDMA in squirrel monkeys: relationship to lasting effects on brain serotonin neurons. Hatzidimitriou, G; Irvine, RJ; McCann, UD; Mechan, A; Ricaurte, GA; Yuan, J, 2006) | 0.33 |
| "0 mg/kg) dose-response break-point curve produced by 24 mg/kg SB-277011A is consistent with a reduction in cocaine's reinforcing efficacy." | ( Selective dopamine D3 receptor antagonism by SB-277011A attenuates cocaine reinforcement as assessed by progressive-ratio and variable-cost-variable-payoff fixed-ratio cocaine self-administration in rats. Ashby, CR; Gardner, EL; Gilbert, JG; Heidbreder, CA; Pak, AC; Xi, ZX, 2005) | 0.33 |
| " In addition, a vertical shift of the cocaine dose-response curve was observed in mice lacking A2A adenosine receptors in comparison with wild-type littermates." | ( The lack of A2A adenosine receptors diminishes the reinforcing efficacy of cocaine. Castañé, A; Ledent, C; Maldonado, R; Parmentier, M; Soria, G; Valverde, O, 2006) | 0.33 |
| " However, few studies have explored behavioral responses to the repeated dosing that is characteristic of human abuse of these substances." | ( Enhanced behavioral response to repeated-dose cocaine in adolescent rats. Caster, JM; Kuhn, CM; Walker, QD, 2005) | 0.33 |
| " Placebo, administered in the context of cocaine cues and dosing expectations, had no cocaine-like subjective or physiological effects." | ( Topographic imaging of quantitative EEG in response to smoked cocaine self-administration in humans. Flammino, F; Howard, B; Nilsen, D; Prichep, LS; Reid, MS, 2006) | 0.33 |
| "1 mg/(kg injection)) functioned as positive reinforcers with sigmoidal or biphasic dose-response functions, whereas DMI failed to do so." | ( Role of the increased noradrenergic neurotransmission in drug self-administration. He, R; Kozikowski, AP; Wang, Z; Wee, S; Woolverton, WL; Zhou, J, 2006) | 0.33 |
| "5-1 mg/kg) resulted in a rightward shift of the cocaine dose-response curve, while SDZ SER-082 (1 mg/kg) shifted the dose-response for cocaine to the left; SB 204741 (1-3 mg/kg) was inactive." | ( Contribution of serotonin (5-HT) 5-HT2 receptor subtypes to the discriminative stimulus effects of cocaine in rats. Bubar, MJ; Cunningham, KA; Filip, M, 2006) | 0.33 |
| " Adjusted mean height z scores demonstrated a dose-response with metahydroxybenzoylecgonine above a threshold of 100 ng/g of meconium and greater cocaine exposure predicted lower weight for height z score." | ( Dysmorphic and anthropometric outcomes in 6-year-old prenatally cocaine-exposed children. Alt, AA; Ellison, L; Kirchner, HL; Minnes, S; Robin, NH; Salbert, BA; Satayathum, S; Singer, LT, ) | 0.13 |
| " Similar infusions of CREB antisense in either core or shell produced a transient downward shift in cocaine self-administration dose-response curves on a fixed ratio 5 (five responses/injection) reinforcement schedule, indicating a reduction in cocaine reinforcement that fully recovered 3 days after treatment." | ( Antisense-induced reduction in nucleus accumbens cyclic AMP response element binding protein attenuates cocaine reinforcement. Choi, KH; Graham, DL; Self, DW; Whisler, K, 2006) | 0.33 |
| " We examined dose-response relationships to pressor and depressor agents to determine cardiovascular reactivity." | ( Contribution of baroreflex sensitivity and vascular reactivity to variable haemodynamic responses to cocaine in conscious rats. Aochi, T; Kawada, T; Knuepfer, MM; Shishido, T; Sunagawa, K; Traub, M, 2005) | 0.33 |
| " A smoked cocaine dose-response curve (0, 12, 25, 50 mg) was determined twice: on days 3-4 and days 6-7 of each baclofen maintenance condition." | ( Effects of baclofen on cocaine self-administration: opioid- and nonopioid-dependent volunteers. Foltin, RW; Haney, M; Hart, CL, 2006) | 0.33 |
| " Dosing order was determined by a within-subject Latin square design." | ( Different patterns of pharmacological reinstatement of cocaine-seeking behavior between Fischer 344 and Lewis rats. Kruzich, PJ; Xi, J, 2006) | 0.33 |
| " DHEA does not seem to decrease cocaine self-administration by increasing the reinforcing properties of the drug, as indicated by a cocaine dose-response determination." | ( DHEA, a neurosteroid, decreases cocaine self-administration and reinstatement of cocaine-seeking behavior in rats. Doron, R; Fridman, L; Gispan-Herman, I; Maayan, R; Weizman, A; Yadid, G, 2006) | 0.33 |
| " The aim of this study was to explore the dose-response relationship between COE exposure and COPD and to assess the interaction with cigarette smoking." | ( Increased risk of chronic obstructive pulmonary diseases in coke oven workers: interaction between occupational exposure and smoking. Chen, B; Hu, Y; Jia, L; Jin, T; Yin, Z; Zhou, Y, 2006) | 0.33 |
| " Using a population of 40 outbred Sprague-Dawley rats trained to self-administer cocaine for 3 weeks, we found that animals with higher preferred levels of cocaine intake exhibited a vertical and rightward shift in the self-administration dose-response function, and were more resistant to extinction from cocaine self-administration, similar to phenotypic changes reported in other models of cocaine addiction." | ( Addiction-related alterations in D1 and D2 dopamine receptor behavioral responses following chronic cocaine self-administration. Edwards, S; Fuller, DC; Orsulak, PJ; Self, DW; Whisler, KN, 2007) | 0.34 |
| " Throughout the dosing period, rats were evaluated on standard measures of sensory and motor development." | ( Postnatal manganese exposure attenuates cocaine-induced locomotor activity and reduces dopamine transporters in adult male rats. Crawford, CA; Farley, CM; McDougall, SA; Reichel, CM; Stanley, BJ; Wacan, JJ, ) | 0.13 |
| " Mice that acquired cocaine self-administration were subsequently tested in a between-session self-administration dose-response procedure." | ( Enhanced acquisition of cocaine self-administration by increasing percentages of C57BL/6J genes in mice with a nonpreferring outbred background. Hall, SK; Ruiz-Durántez, E; Self, DW; Steffen, C, 2006) | 0.33 |
| " In mice that acquired self-administration, only mice with 75% C57BL/6J genes showed a typical inverted U-shaped self-administration dose-response curve, whereas the curve was flat across doses for mice with < or = 50 and 100% C57BL/6J genes." | ( Enhanced acquisition of cocaine self-administration by increasing percentages of C57BL/6J genes in mice with a nonpreferring outbred background. Hall, SK; Ruiz-Durántez, E; Self, DW; Steffen, C, 2006) | 0.33 |
| "The PK parameters of AHN 1-055 were not changed, however, the effect on DA levels was affected when cocaine was administered with AHNDA profile is affected when dosed with cocaine." | ( Investigation of the potential pharmacokinetic and pharmaco-dynamic drug interaction between AHN 1-055, a potent benztropine analog used for cocaine abuse, and cocaine after dosing in rats using intracerebral microdialysis. Cao, J; Cornish, J; Eddington, ND; Katz, JL; Newman, AH; Raje, S, 2006) | 0.33 |
| " Dose-response functions were obtained by two methods and were similar for all groups." | ( Cocaine self-administration in rats with histories of cocaine exposure and discrimination. Childs, E; Shoaib, M; Stolerman, IP, 2006) | 0.33 |
| " A dose-response function for cocaine was assessed eight consecutive times during each of four phases of the experiment to assess the stability of effects of each dose." | ( Stability of cocaine dose-response functions at different inter-dose intervals. Branch, MN; Marusich, JA, 2006) | 0.33 |
| "This study examined dose-response effects of oral cocaine on the inhibitory control of behavior in adult cocaine users using two different behavioral models of inhibitory control." | ( Acute effects of cocaine in two models of inhibitory control: implications of non-linear dose effects. Fillmore, MT; Hays, L; Rush, CR, 2006) | 0.33 |
| "Although both tasks showed cocaine-induced facilitation of inhibitory control, dose-response functions differed depending on the measures." | ( Acute effects of cocaine in two models of inhibitory control: implications of non-linear dose effects. Fillmore, MT; Hays, L; Rush, CR, 2006) | 0.33 |
| "The evidence suggests a two-phasic dose-response in which facilitating effects of stimulant drugs on inhibitory control might be limited to a range of intermediate doses, above which improvement is no longer evident and impairing effects could possibly emerge." | ( Acute effects of cocaine in two models of inhibitory control: implications of non-linear dose effects. Fillmore, MT; Hays, L; Rush, CR, 2006) | 0.33 |
| "To explore the dose-response relationship between exposure to polycyclic aromatic hydrocarbons (PAHs) and the elevation of some serum liver enzymes in coke oven workers." | ( [Elevation of some serum liver enzymes in coke oven workers and the possible relationship with exposure to polycyclic aromatic hydrocarbons]. Chen, B; Pan, JS; Wang, XJ; Zheng, LX, 2006) | 0.33 |
| "The extraction methods in selected monographs of the European and the Swiss Pharmacopoeia were compared to pressurized liquid extraction (PLE) with respect to the yield of constituents to be dosed in the quantitative assay for the respective herbal drugs." | ( Are extraction methods in quantitative assays of pharmacopoeia monographs exhaustive? A comparison with pressurized liquid extraction. Basalo, C; Hamburger, M; Mohn, T, 2006) | 0.33 |
| " Upon observing stable levels of self-administration, METH was substituted for COC and a dose-response function for METH (0." | ( Reinforcing effects of smoked methamphetamine in rhesus monkeys. Carroll, ME; Newman, JL, 2006) | 0.33 |
| " The presented data demonstrate that there is no ascending limb of the dose-response curve and that the cocaine priming and satiety thresholds delineate the lower and upper limits, respectively, of a cocaine "compulsion zone"." | ( The compulsion zone: a pharmacological theory of acquired cocaine self-administration. Norman, AB; Tsibulsky, VL, 2006) | 0.33 |
| " Although repeated cocaine administration can result in drug accumulation and extended excretion time, there is a paucity of data from controlled dosing studies with repeated drug administration." | ( Effect of repeated cocaine administration on detection times in oral fluid and urine. Cone, EJ; Jufer, R; Sampson-Cone, A; Walsh, SL, 2006) | 0.33 |
| " Dose-response relationships were biphasic for MA and (+/-)-MDMA, and asymptotic for (+)-MDMA." | ( Estimating the relative reinforcing strength of (+/-)-3,4-methylenedioxymethamphetamine (MDMA) and its isomers in rhesus monkeys: comparison to (+)-methamphetamine. Wang, Z; Woolverton, WL, 2007) | 0.34 |
| "1-1 mg) 1 min before cocaine administration produced dose-dependent rightward shifts of the dose-response curve for cocaine toxicity." | ( Cocaine esterase: interactions with cocaine and immune responses in mice. Berlin, AA; Bowen, LD; Cooper, ZD; Ko, MC; Lukacs, NW; Narasimhan, D; Sunahara, RK; Woods, JH, 2007) | 0.34 |
| " Increasing cocaine use, based on self-reports and laboratory values, significantly exacerbates the immunopathology of HIV-1 in a dose-response manner, confirmed by a non-linear drop in CD4+ cell number for a given viral load in HIV+ AAW." | ( Crack cocaine: effect modifier of RNA viral load and CD4 count in HIV infected African American women. Chiappelli, F; Duncan, R; McCoy, CB; Messiah, SE; Page, JB; Shapshak, P, 2007) | 0.34 |
| " In ShA rats, the cocaine dose-response function was higher in rats at the two higher unit doses than at the lower doses." | ( Effects of dose and session duration on cocaine self-administration in rats. Koob, GF; Specio, SE; Wee, S, 2007) | 0.34 |
| " During each admission, an intranasal cocaine dose-response curve (0." | ( Intranasal cocaine in humans: effects of sex and menstrual cycle. Collins, SL; Evans, SM; Foltin, RW; Haney, M, 2007) | 0.34 |
| " Particular attention was paid to the effect of dosage and pH on the removal of chemical oxygen demand (COD) in the two processes." | ( Advanced treatment of coking wastewater by coagulation and zero-valent iron processes. Lai, P; Ni, JR; Wang, C; Zhao, HZ, 2007) | 0.34 |
| " When given in combination with cocaine, CJB 090 but not NGB 2904 attenuated the discriminative stimulus effects of cocaine, shifting the cocaine dose-response curve to the right." | ( Effects of two novel D3-selective compounds, NGB 2904 [N-(4-(4-(2,3-dichlorophenyl)piperazin-1-yl)butyl)-9H-fluorene-2-carboxamide] and CJB 090 [N-(4-(4-(2,3-dichlorophenyl)piperazin-1-yl)butyl)-4-(pyridin-2-yl)benzamide], on the reinforcing and discrimin Claytor, R; Martelle, JL; Nader, MA; Newman, AH; Reboussin, BA; Ross, JT, 2007) | 0.34 |
| " By measuring locomotor activity and using a range of doses of CART peptide and cocaine, both alone and together, with different dosing strategies, clear evidence of subadditivity was found." | ( Intra-VTA CART 55-102 reduces the locomotor effect of systemic cocaine in rats: an isobolographic analysis. Jaworski, JN; Kimmel, HL; Kuhar, MJ; Mitrano, DA; Tallarida, RJ, 2007) | 0.34 |
| "5 mg/kg amphetamine and to a cumulative dosing of amphetamine." | ( Social defeat stress, sensitization, and intravenous cocaine self-administration in mice. Miczek, KA; Yap, JJ, 2007) | 0.34 |
| " Presently, the dose-response characteristics between maternal cocaine use and fetal exposure and adverse effects are unknown." | ( Cocaine detection in maternal and neonatal hair: implications to fetal toxicology. Garcia-Bournissen, F; Karaskov, T; Koren, G; Rokach, B, 2007) | 0.34 |
| " drug injection, combining heroin with cocaine shifted the heroin dose-response function leftward, and isobolographic analysis indicated that the combined effects were dose-additive." | ( Modulation of heroin and cocaine self-administration by dopamine D1- and D2-like receptor agonists in rhesus monkeys. Platt, DM; Rowlett, JK; Spealman, RD; Yao, WD, 2007) | 0.34 |
| "l-THP produced a rightward and downward shift in the dose-response curve for cocaine SA and attenuated cocaine-induced reinstatement." | ( Levo-tetrahydropalmatine attenuates cocaine self-administration and cocaine-induced reinstatement in rats. Awad, S; Baker, DA; Katz, E; Li, SJ; Mantsch, JR; Risinger, R; Yang, Z, 2007) | 0.34 |
| " On the contrary, the ex-group-housed DBA mice showed an upward shift in the dose-response curve as compared to individually housed DBA." | ( Gene-environment interactions in vulnerability to cocaine intravenous self-administration: a brief social experience affects intake in DBA/2J but not in C57BL/6J mice. Deroche-Gamonet, V; Piazza, PV; van der Veen, R, 2007) | 0.34 |
| " Animals were then conditioned to associate place cues with the effects of either a low (5 mg/kg) or moderately high (20 mg/kg) dosage of cocaine immediately or 45 min after intraperitoneal cocaine administration." | ( 5-HT(1B) receptors in nucleus accumbens efferents enhance both rewarding and aversive effects of cocaine. Barot, SK; Ferguson, SM; Neumaier, JF, 2007) | 0.34 |
| "The purpose of the current study was to establish dose-response relationships for the effects of a number of commonly used illicit stimulants and investigate the behavioral response to increased core temperature." | ( Pharmacological and behavioral determinants of cocaine, methamphetamine, 3,4-methylenedioxymethamphetamine, and para-methoxyamphetamine-induced hyperthermia. Irvine, RJ; Jaehne, EJ; Salem, A, 2007) | 0.34 |
| " This differed to the slopes of the dose-response curves where MDMA and PMA showed the steepest slope for the doses used followed by methamphetamine then cocaine." | ( Pharmacological and behavioral determinants of cocaine, methamphetamine, 3,4-methylenedioxymethamphetamine, and para-methoxyamphetamine-induced hyperthermia. Irvine, RJ; Jaehne, EJ; Salem, A, 2007) | 0.34 |
| " Respondents were randomly assigned to a yes/no item or a dose-response scale to assess candy cigarette use." | ( History of childhood candy cigarette use is associated with tobacco smoking by adults. Klein, JD; Sutter, EJ; Thomas, RK, 2007) | 0.34 |
| " Dose-response functions for the immediate dose shifted to the left as delay increased." | ( Delay discounting of cocaine by rhesus monkeys. Green, L; Myerson, J; Woolverton, WL, 2007) | 0.34 |
| " All groups displayed an inverted-U shaped cocaine dose-response curve in both the sensitization and reinstatement tests." | ( Extended access to cocaine self-administration enhances drug-primed reinstatement but not behavioral sensitization. Kalivas, PW; Knackstedt, LA, 2007) | 0.34 |
| " Animals subjected to a binge mAMPH dosing regimen that damages brain dopamine and serotonin terminals show impairments in an object recognition (OR) task." | ( Methamphetamine influences on recognition memory: comparison of escalating and single-day dosing regimens. Belcher, AM; Feinstein, EM; Marshall, JF; O'Dell, SJ, 2008) | 0.35 |
| "25-10 mg/kg) dose-response curve in a drug discrimination procedure, while baclofen (1." | ( Effects of GABA(B) receptor antagonist, agonists and allosteric positive modulator on the cocaine-induced self-administration and drug discrimination. Filip, M; Frankowska, M; Przegaliński, E, 2007) | 0.34 |
| " Dose-response experiments revealed that a single dose of cocaine (5 mg/kg) is sufficient to upregulate BDNF mRNA levels selectively in rat prefrontal cortex 2 h after the injection, an effect that persists at least for 24 h and is paralleled by enhanced expression of mature (m)BDNF protein." | ( Repeated exposure to cocaine differently modulates BDNF mRNA and protein levels in rat striatum and prefrontal cortex. Caffino, L; Di Pasquale, L; Fumagalli, F; Racagni, G; Riva, MA, 2007) | 0.34 |
| " After extinction of responding with saline self-administration, dose-response studies showed that cocaine reliably and dose dependently maintained responding greater than saline in all wild-type mice but in none of the D1 receptor knock-out mice." | ( Lack of self-administration of cocaine in dopamine D1 receptor knock-out mice. Berkowitz, JS; Caine, SB; Gabriel, KI; Gold, LH; Koob, GF; Thomsen, M; Tonegawa, S; Xu, M; Zhang, J, 2007) | 0.34 |
| " Particular attention was paid on the effect of bottom ash particle size and dosage on the removal of chemical oxygen demand (COD)." | ( Adsorption of organic pollutants from coking and papermaking wastewaters by bottom ash. Ni, JR; Qu, YZ; Sun, WL; Yu, Q, 2008) | 0.35 |
| " These results suggest an inverted U-shaped dose-response curve for the effect of E on acquisition of cocaine self-administration." | ( Acquisition of cocaine self-administration in ovariectomized female rats: effect of estradiol dose or chronic estradiol administration. Becker, JB; Hu, M, 2008) | 0.35 |
| " Retention in treatment was increased by less-than-daily dosing of buprenorphine." | ( Multi-centre observational study of buprenorphine use in 32 Italian drug addiction centres. Fagetti, R; Hanna, N; Laurenzi, P; Leonardi, C, 2008) | 0.35 |
| " Psychosocial support and/or less-than-daily dosing also appeared to promote positive treatment outcomes." | ( Multi-centre observational study of buprenorphine use in 32 Italian drug addiction centres. Fagetti, R; Hanna, N; Laurenzi, P; Leonardi, C, 2008) | 0.35 |
| " The purpose of the present study was to examine the time course of effects of cocaine on operant behavior of pigeons, using a method that allowed comparison of dose-response functions, in individual subjects, within a session." | ( Differences in the behavioral time course of effects of rate-increasing and rate-decreasing doses of cocaine in pigeons. Branch, MN; Marusich, JA, 2008) | 0.35 |
| " Topiramate (1-60 mg/kg, intraperitoneal) did not produce any nicotine-like or cocaine-like discriminative effects by itself and did not produce any shift in the dose-response curves for nicotine or cocaine discrimination." | ( Topiramate does not alter nicotine or cocaine discrimination in rats. Barnes, C; Goldberg, SR; Justinova, Z; Le Foll, B; Wertheim, CE, 2008) | 0.35 |
| "A meta-analysis was conducted on data obtained from published articles which used in vivo microdialysis to assess dose-response curves of cocaine on dopamine (DA) overflow within the nucleus accumbens (NAC)." | ( Cocaine-induced dopamine overflow within the nucleus accumbens measured by in vivo microdialysis: a meta-analysis. Frank, ST; Krumm, B; Spanagel, R, 2008) | 0.35 |
| " Because fat oxidation measured by indirect calorimetry increased immediately after dosing in the postprandial state, the acute effect of rimonabant on lipolysis was investigated in postprandial male rats." | ( Increased energy expenditure contributes more to the body weight-reducing effect of rimonabant than reduced food intake in candy-fed wistar rats. Elvert, R; Haschke, G; Herling, AW; Kilp, S; Kramer, W, 2008) | 0.35 |
| "4 mg/kg, aripiprazole decreased rates of cocaine self-administration without shifting the peak of the dose-response function." | ( Aripiprazole blocks acute self-administration of cocaine and is not self-administered in mice. Brennum, LT; Fink-Jensen, A; Hee Bengtsen, C; Petersen, JH; Sager, TN; Sørensen, G; Thomsen, M; Thøgersen, P; Woldbye, DP; Wörtwein, G, 2008) | 0.35 |
| "Treatment with MPEP and dizocilpine significantly reduced cocaine self-administration, producing rightward and downward shifts in the ascending limb of the cocaine dose-response function." | ( Attenuation of cocaine self-administration in squirrel monkeys following repeated administration of the mGluR5 antagonist MPEP: comparison with dizocilpine. Platt, DM; Rowlett, JK; Spealman, RD, 2008) | 0.35 |
| " Significant differences of the total digital span, the forward digital span, backward digital span, digit symbol and Benton visual retentions existed in different urinary 1-hydroxypyrene concentration groups and showed a dose-response tendency." | ( [Characteristic of the neurobehavioral functional changes in coke oven workers]. Liu, HJ; Nie, JS; Niu, Q; Shi, YT; Song, J; Sun, JY; Wang, F; Wang, J; Wang, LP; Zeng, P; Zhang, HM, 2008) | 0.35 |
| " (+)-PD-128,907 also prevented the acquisition and expression of cocaine-kindled seizures engendered by repeated daily dosing with 60 mg/kg cocaine." | ( The dopamine D3/D2 agonist (+)-PD-128,907 [(R-(+)-trans-3,4a,10b-tetrahydro-4-propyl-2H,5H-[1]benzopyrano[4,3-b]-1,4-oxazin-9-ol)] protects against acute and cocaine-kindled seizures in mice: further evidence for the involvement of D3 receptors. Gasior, M; Kaminski, R; Levant, B; Witkin, JM; Zapata, A, 2008) | 0.35 |
| " Acute cocaine, through D(2) dopamine receptors, induced a dose-response increase in FADD protein in the cortex, with opposite effects over pFADD (Ser191/194), and no induction of apoptotic cell death (poly-(ADP-ribose) polymerase cleavage)." | ( Effect of cocaine on Fas-associated protein with death domain in the rat brain: individual differences in a model of differential vulnerability to drug abuse. Akil, H; Clinton, SM; García-Fuster, MJ; Watson, SJ, 2009) | 0.35 |
| " In addition, cocaine self-administration can be altered in an orderly fashion by presentation of an acute stressor, such as acting as an intruder into an unfamiliar social group, which can shift the cocaine dose-response curve to the left in subordinate monkeys and to the right in dominant animals, suggesting an interaction between social variables and acute stressors." | ( Review. Positron emission tomography imaging studies of dopamine receptors in primate models of addiction. Czoty, PW; Gould, RW; Nader, MA; Riddick, NV, 2008) | 0.35 |
| "Caffeine, CPT, and MSX-3 partially generalized to nicotine and shifted nicotine dose-response curves leftwards." | ( Effects of chronic caffeine exposure on adenosinergic modulation of the discriminative-stimulus effects of nicotine, methamphetamine, and cocaine in rats. Barnes, C; Ferré, S; Goldberg, SR; Justinova, Z; Le Foll, B; Pappas, LA; Wertheim, CE, 2009) | 0.35 |
| " Parametric manipulations, such as altering time-out (TO) values, can affect the shape of the cocaine dose-response curve." | ( Effect of time-out duration on the reinforcing strength of cocaine assessed under a progressive-ratio schedule in rhesus monkeys. Czoty, PW; Martelle, JL; Nader, MA, 2008) | 0.35 |
| "Both methamphetamine and cocaine increased locomotor activity in a dose-response fashion, but the magnitude of the increase was less in adolescents than adults." | ( Evaluation of a pharmacokinetic hypothesis for reduced locomotor stimulation from methamphetamine and cocaine in adolescent versus adult male C57BL/6J mice. Gupta, T; Rhodes, JS; Zombeck, JA, 2009) | 0.35 |
| "0 mg/kg was more effective at shifting to the right the pramipexole dose-response curve in pramipexole-trained rats, while 32 mg/kg of the selective D3 antagonist PG01037 had little effect." | ( The discriminative stimulus effects of dopamine D2- and D3-preferring agonists in rats. Greedy, B; Grundt, P; Husbands, SM; Koffarnus, MN; Newman, AH; Woods, JH, 2009) | 0.35 |
| " The dose-response relationship was improved when subjects with adduct levels above the 3rd tertile (>or=4." | ( Micronuclei related to anti-B[a]PDE-DNA adduct in peripheral blood lymphocytes of heavily polycyclic aromatic hydrocarbon-exposed nonsmoking coke-oven workers and controls. Bolognesi, C; Clonfero, E; Kapka, L; Mielzyñska, D; Pavanello, S; Siwinska, E, 2008) | 0.35 |
| " In mice self-administering cocaine, TrkB knockdown in the NAc produced a downward shift in the cocaine self-administration dose-response curve but had no effect on the acquisition of cocaine or sucrose self-administration." | ( Tropomyosin-related kinase B in the mesolimbic dopamine system: region-specific effects on cocaine reward. Bachtell, RK; Berton, O; Bolanos, CA; DiLeone, RJ; Edwards, S; Gent, LM; Graham, A; Graham, DL; Krishnan, V; Larson, EB; Nestler, EJ; Parada, LF; Self, DW; Simmons, D, 2009) | 0.35 |
| " The magnitude of the shift to the right in the cocaine dose-response function was directly related to PB dose." | ( Self-administration of cocaine-pentobarbital mixtures by rhesus monkeys. Wang, Z; Woolverton, WL, 2009) | 0.35 |
| " The BChE-/- mice demonstrated depressed respiration through 12 hr after dosing and abnormal respiratory patterns consisting of a pause at full inspiration (apneusis), whereas BChE+/+ mice had recovered normal respiration rates by 30 min." | ( Increased hepatotoxicity and cardiac fibrosis in cocaine-treated butyrylcholinesterase knockout mice. Carlson, M; Duysen, EG; Hinrichs, SH; Li, B; Li, YF; Lockridge, O; Wieseler, S, 2008) | 0.35 |
| "0 mg/kg) was coadministered with saline or different cocaine doses, we observed similar upward shifts in dose-response in both phenotypes." | ( Reduced sensitivity to the locomotor-stimulant effects of cocaine is associated with increased sensitivity to its discriminative stimulus properties. Gulley, JM; Klein, DA, 2009) | 0.35 |
| " Wild-type mice readily acquired cocaine self-administration and showed dose-response curves characteristic of the schedule of reinforcement that was used." | ( Dramatically decreased cocaine self-administration in dopamine but not serotonin transporter knock-out mice. Caine, SB; Hall, FS; Thomsen, M; Uhl, GR, 2009) | 0.35 |
| " MTEP also decreased cocaine self-administration without a clear graded dose-response profile and did not modify SCM-reinforced responding." | ( Dissociation of the effects of MTEP [3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]piperidine] on conditioned reinstatement and reinforcement: comparison between cocaine and a conventional reinforcer. Baptista, MA; Dayas, CV; Martin-Fardon, R; Weiss, F, 2009) | 0.35 |
| " This study was undertaken to examine effects of a long-term dosing regimen with selective MAOIs on cocaine and food reward." | ( Chronic treatment with monoamine oxidase-B inhibitors decreases cocaine reward in mice. Cherng, CG; Chiang, CY; Chuang, JY; Ho, MC; Kao, SF; Tsai, YP; Yu, L, 2009) | 0.35 |
| " In contrast, when doses along the ascending limb were available for self-administration, lidocaine inactivation of the lateral orbitofrontal cortex caused reductions in responding and cocaine intake, resulting in overall flattening of dose-response curves." | ( Role of the orbitofrontal cortex and dorsal striatum in regulating the dose-related effects of self-administered cocaine. Goodrich, CM; Janes, AC; Kantak, KM; Mashhoon, Y; Silverman, DN, 2009) | 0.35 |
| " However, when the cocaine dosage was increased, FSL rats demonstrated a similar cocaine-seeking behavior to that of controls." | ( Antidepressant treatment facilitates dopamine release and drug seeking behavior in a genetic animal model of depression. Abraham, L; Dikshtein, Y; Flaumenhaft, Y; Friedman, A; Lax, E; Roth-Deri, I; Yadid, G, 2009) | 0.35 |
| " Experiment 2: rats were trained to self-administer cocaine under a PR schedule and initial dose-response curves were determined before implantation of D-amphetamine mini-pumps." | ( Decreased reinforcing effects of cocaine following 2 weeks of continuous D-amphetamine treatment in rats. Chiodo, KA; Roberts, DC, 2009) | 0.35 |
| " The dosing regimen produced cocaine plasma concentrations (Cmax of 680 ng/mL) two to threefold higher than typically seen in acute dose studies." | ( Repeated dosing with oral cocaine in humans: assessment of direct effects, withdrawal, and pharmacokinetics. Bigelow, GE; Lin, SN; Moody, DE; Stoops, WW; Walsh, SL, 2009) | 0.35 |
| " Experiment 4 showed that tolerance from postsession cocaine administration could be observed even when daily dosing was discontinued during dose-response curve assessment." | ( Environmental and pharmacological factors in the development of noncontingent tolerance to cocaine in pigeons. Branch, MN; Marusich, JA, 2009) | 0.35 |
| " Furthermore, adding nicotine to cocaine shifted the cocaine dose-response function to the left in four of the five monkeys." | ( Self-administration of cocaine and nicotine mixtures by rhesus monkeys. Freeman, KB; Woolverton, WL, 2009) | 0.35 |
| " The purpose of the present study was to characterize the dose-response and time-course of mu receptor occupancy following systemic cocaine administration and to determine if release of endogenous opioids by cocaine is mediated by activation of D1 or D2 dopamine receptors." | ( Cocaine-induced mu opioid receptor occupancy within the striatum is mediated by dopamine D2 receptors. Soderman, AR; Unterwald, EM, 2009) | 0.35 |
| " We treated male Long-Evans rats with a regimen of four injections of 2 mg/kg mAMPH (or vehicle) within a single day, a dosing regimen shown earlier to produce object recognition impairments." | ( Reversal-specific learning impairments after a binge regimen of methamphetamine in rats: possible involvement of striatal dopamine. Belcher, AM; Cazares, VA; Chen, J; Izquierdo, A; Malvaez, M; Marshall, JF; O'Dell, SJ; Scott, L; Wu, T, 2010) | 0.36 |
| " However, cocaine was more potent in DBA mice than in C57 mice as revealed by a leftward shift in the cocaine dose-response curve." | ( Alcohol, cocaine, and brain stimulation-reward in C57Bl6/J and DBA2/J mice. Faccidomo, S; Fish, EW; Hodge, CW; Malanga, CJ; McGuigan, MM; Riday, TT, 2010) | 0.36 |
| "02 mg/kg, subcutaneous), on MDMA self-administration, effects of this dose range on the MA dose-response curve were determined." | ( Effect of D1-like and D2-like receptor antagonists on methamphetamine and 3,4-methylenedioxymethamphetamine self-administration in rats. Brennan, KA; Carati, C; Fitzmaurice, PS; Lea, RA; Schenk, S, 2009) | 0.35 |
| " In cocaine-trained monkeys, coadministration of cocaine and heroin produced leftward shifts in the cocaine dose-response function." | ( Asymmetric generalization and interaction profiles in rhesus monkeys discriminating intravenous cocaine or intravenous heroin from vehicle. Platt, DM; Rowlett, JK; Spealman, RD, 2010) | 0.36 |
| " Daily histone deacetylase (HDAC) inhibitor infusions in the shell of the nucleus accumbens (NAc) caused an upward shift in the dose-response curve under fixed-ratio schedule and increased the break point under progressive-ratio schedule, indicating enhanced motivation for self-administered drug." | ( Chronic cocaine-induced H3 acetylation and transcriptional activation of CaMKIIalpha in the nucleus accumbens is critical for motivation for drug reinforcement. Hu, Z; Hui, B; Lv, Z; Ma, L; Sheng, J; Sun, J; Wang, L, 2010) | 0.36 |
| " Compared with controls, maternally separated monkeys showed lower responding during the acquisition of self-administration and in the dose-response curves for both stimulants, and significantly lower response rates during maintenance of cocaine self-administration." | ( Impact of early life stress on the reinforcing and behavioral-stimulant effects of psychostimulants in rhesus monkeys. Ewing Corcoran, SB; Howell, LL, 2010) | 0.36 |
| " This effect was shown by the lower dosage of cocaine necessary to induce conditioning compared with rats receiving cocaine alone, as well as by the fewer number of sessions necessary to induce place preference." | ( GM1 ganglioside enhances the rewarding properties of cocaine in rats. Cuadra, GR; de Burgos, NG; Hansen, C; Orsingher, OA; Valdomero, A, 2010) | 0.36 |
| " However, a similar anisomycin dosing regimen failed to affect subsequent expression of cocaine-CPP when additional cocaine conditioning trial was used in the absence of additional saline trial." | ( Systemic treatment with protein synthesis inhibitors attenuates the expression of cocaine memory. Cheng, LY; Cherng, CG; Fan, HY; Lin, LC; Tsai, CJ; Yang, FY; Yu, L, 2010) | 0.36 |
| " Prior to these assessments, a fluoxetine dose-response function (3." | ( Preexposure to cocaine attenuates aversions induced by both cocaine and fluoxetine: Implications for the basis of cocaine-induced conditioned taste aversions. Riley, AL; Serafine, KM, 2010) | 0.36 |
| " Citalopram alone produced predominantly saline-appropriate responding, but when administered before cocaine, citalopram dose-dependently shifted the cocaine dose-response curve leftward." | ( Citalopram enhances cocaine's subjective effects in rats. Hiranita, T; Katz, JL; Soto, PL, 2009) | 0.35 |
| " Children were divided into two supplementation groups: daily dosage recommended by the Sociedade Brasileira de Pediatria (Brazilian Society of Pediatrics) (group 1, n=34) and weekly dosage recommended by the Brazilian Ministry of Health (group 2, n=69)." | ( Greater effectiveness of daily iron supplementation scheme in infants. Azeredo, CM; Cotta, RM; Franceschini, Sdo C; Lamounier, JA; Pedron, FA; Ribeiro, Rde C; Sant'Ana, LF, 2010) | 0.36 |
| "The daily dosage recommended by the Sociedade Brasileira de Pediatria was found to be more effective to prevent anemia in infants, when compared to the dosage used by the Ministry of Health." | ( Greater effectiveness of daily iron supplementation scheme in infants. Azeredo, CM; Cotta, RM; Franceschini, Sdo C; Lamounier, JA; Pedron, FA; Ribeiro, Rde C; Sant'Ana, LF, 2010) | 0.36 |
| " HaCaT cells treatment with a cocaine concentration of 2 mM for 24 h (as was chosen by dose-response experiments) markedly enhanced superoxide radicals and peroxides formation." | ( Cocaine induces oxidative damage to skin via xanthine oxidase and nitric oxide synthase. Kohen, R; Numa, R; Portugal-Cohen, M; Yaka, R, 2010) | 0.36 |
| " A dose-response test was then conducted, followed by extinction and cue- and nicotine-induced reinstatement." | ( The effects of response operandum and prior food training on intravenous nicotine self-administration in rats. Cador, M; Caillé, S; Clemens, KJ, 2010) | 0.36 |
| "The use of the NP operandum resulted in markedly higher levels of IVSA across acquisition and across dose-response testing compared with the LVR group." | ( The effects of response operandum and prior food training on intravenous nicotine self-administration in rats. Cador, M; Caillé, S; Clemens, KJ, 2010) | 0.36 |
| " After acquisition, rats were tested with a cumulative dose-response procedure (0-18 mg/kg) for 12 consecutive days." | ( The effects of home-cage access to a sweet solution on the discriminative stimulus effects of cocaine. Kohut, SJ; Riley, AL, 2010) | 0.36 |
| " Repeated dosing every six hours allowed both patients to restart oral nutrition without any reported side effects." | ( Topical cocaine for relief of mucosal pain. Coyne, P; Newport, K, 2010) | 0.36 |
| " A dose-response curve was followed by procedures of progressive ratio, extinction, cocaine- and cue-induced reinstatements." | ( A decrease in gamma-synuclein expression within the nucleus accumbens increases cocaine intravenous self-administration in the rat. Balado, E; Boyer, F; Deroche-Gamonet, V; Dreyer, JL; Piazza, PV, 2011) | 0.37 |
| " Examples of studies utilizing dose-response approaches and clinically relevant plasma drug curves are presented." | ( Translational issues for prenatal cocaine studies and the role of environment. Dow-Edwards, D, ) | 0.13 |
| "Acquisition, dose-response function, extinction, and cue-induced reinstatement of operant behavior were characterized." | ( Patterns of responding differentiate intravenous nicotine self-administration from responding for a visual stimulus in C57BL/6J mice. Contet, C; Jarrell, H; Kenny, PJ; Markou, A; Whisler, KN, 2010) | 0.36 |
| " Dependence was established using a noncontingent morphine dosing procedure that has been previously verified to maintain dependence while allowing for daily behavioral observation during a withdrawn state." | ( Reinforcer-dependent enhancement of operant responding in opioid-withdrawn rats. Cooper, ZD; Shi, YG; Woods, JH, 2010) | 0.36 |
| "Morphine withdrawal enhanced remifentanil self-administration, resulting in an upward and rightward shift of the descending limb of the dose-response curve, and increased operant responding for both food reinforcers." | ( Reinforcer-dependent enhancement of operant responding in opioid-withdrawn rats. Cooper, ZD; Shi, YG; Woods, JH, 2010) | 0.36 |
| "5mg/kg) produced a rightward shift in the dose-response curve for cocaine generalization." | ( Levo-tetrahydropalmatine attenuates cocaine self-administration under a progressive-ratio schedule and cocaine discrimination in rats. Baker, DA; Becker, A; Li, SJ; Mantsch, JR; Peters, C; Valentine, A; Vranjkovic, O; Wisniewski, S; Yang, Z, 2010) | 0.36 |
| "0 mg/kg, with dosing occurring every fifth day." | ( Response topography in behavioral tolerance to cocaine with rats. Branch, MN; Dallery, J; Weaver, MT, 2010) | 0.36 |
| " After determining a dose-response curve for cocaine (0." | ( Prolonged attenuation of the reinforcing strength of cocaine by chronic d-amphetamine in rhesus monkeys. Czoty, PW; Gould, RW; Martelle, JL; Nader, MA, 2011) | 0.37 |
| " A low dose of the selective adenosine A(2A) receptor antagonist MSX-3 (1 mg/kg) caused downward shifts of THC and anandamide dose-response curves." | ( Reinforcing and neurochemical effects of cannabinoid CB1 receptor agonists, but not cocaine, are altered by an adenosine A2A receptor antagonist. Ferré, S; Franco, R; Goldberg, SR; Justinová, Z; Mascia, P; Müller, CE; Quarta, D; Redhi, GH; Stroik, J; Yasar, S, 2011) | 0.37 |
| " A positive dose-response relationship was found between frequency of cocaine use and lack of consistent use of protective devices." | ( Association between cannabis and cocaine use, traffic injuries and use of protective devices. Barrio, G; Bravo, MJ; de la Fuente, L; Lardelli, P; Pulido, J; Regidor, E, 2011) | 0.37 |
| " Likewise, a similar dosing regimen of sarcosine or D-serine did not cause evident activity-impairing effect." | ( D-cycloserine, sarcosine and D-serine diminish the expression of cocaine-induced conditioned place preference. Chang, WT; Cheng, LY; Cherng, CG; Chuang, JY; Kao, GS; Lee, YS; Yang, FY; Yu, L, 2013) | 0.39 |
| " Using an unbiased, three-chamber conditioned place preference (CPP) paradigm the dose-response function for nicotine CPP was tested in GAL-/- and GAL+/+ mice." | ( Mice lacking the galanin gene show decreased sensitivity to nicotine conditioned place preference. Hales, CA; Henehan, RM; Neugebauer, NM; Picciotto, MR, 2011) | 0.37 |
| "Cocaine-treated rats displayed an enhanced locomotor response to cocaine, as well as a progressive and persistent leftward/upward shift of the ascending limb (72 h-42 day) and leftward shift of the descending limb (42 days) of the pramipexole-induced yawning dose-response curve." | ( Behavioral sensitization to cocaine in rats: evidence for temporal differences in dopamine D3 and D2 receptor sensitivity. Chen, J; Collins, GT; Levant, B; Truong, YN; Wang, S; Woods, JH, 2011) | 0.37 |
| " To assess this, we used electron microscopic immunolabeling in the VTA of adult male mice sacrificed at 30 min or 72 h after receiving the final of six (15 mg/kg) cocaine injections, a dosing paradigm that resulted in development of locomotor sensitization." | ( Differential glutamate AMPA-receptor plasticity in subpopulations of VTA neurons in the presence or absence of residual cocaine: implications for the development of addiction. Kreek, MJ; Lane, DA; Pickel, VM; Reed, B, 2011) | 0.37 |
| " Nevertheless, such a memantine dosing regimen did not affect dopamine metabolism in mPFC and Acb." | ( Memantine abolishes the formation of cocaine-induced conditioned place preference possibly via its IL-6-modulating effect in medial prefrontal cortex. Cherng, CG; Lin, KY; Lin, LC; Lu, RB; Yang, FR; Yu, L, 2011) | 0.37 |
| " A smoked cocaine dose-response curve (0, 12, 25, 50 mg) was determined twice under placebo and aripiprazole maintenance." | ( Aripiprazole maintenance increases smoked cocaine self-administration in humans. Foltin, RW; Haney, M; Rubin, E, 2011) | 0.37 |
| " Both treatments showed evidence of a dose-response effect, and no experiment found a statistically significant increase in risk of death." | ( Benzodiazepines and antipsychotic medications for treatment of acute cocaine toxicity in animal models--a systematic review and meta-analysis. Cleveland, NR; Heard, K; Krier, S, 2011) | 0.37 |
| " When it was administered with cocaine, AC927 shifted the cocaine dose-response curve to the left, suggesting an enhancement of the discriminative stimulus effects of cocaine." | ( Effects of the selective sigma receptor ligand, 1-(2-phenethyl)piperidine oxalate (AC927), on the behavioral and toxic effects of cocaine. Coop, A; Fantegrossi, WE; Katz, JL; Li, SM; Matsumoto, RR, 2011) | 0.37 |
| " Behavioral studies conducted in male, Swiss Webster mice, intraperitoneal or oral dosing with SN79 prior to a convulsive or locomotor stimulant dose of cocaine led to a significant attenuation of cocaine-induced convulsions and locomotor activity." | ( Synthesis and pharmacological evaluation of 6-acetyl-3-(4-(4-(4-fluorophenyl)piperazin-1-yl)butyl)benzo[d]oxazol-2(3H)-one (SN79), a cocaine antagonist, in rodents. Avery, BA; Kaushal, N; Matsumoto, RR; McCurdy, CR; Narayanan, S; Robson, MJ; Vinnakota, H, 2011) | 0.37 |
| " B6;129S F2 mice were conditioned by three dosing schedules of cocaine: (1) ascending, (2) fixed and (3) descending daily doses." | ( Changes in the magnitude of drug-unconditioned stimulus during conditioning modulate cocaine-induced place preference in mice. Anderson, KL; Itzhak, Y, 2012) | 0.38 |
| " One patient required a dosage reduction of ropinirole because of sleepiness and one patient assigned to aripiprazole who reported moderate akathysia had the dosage reduced to 5 mg/day." | ( Aripiprazole and ropinirole treatment for cocaine dependence: evidence from a pilot study. Ameglio, M; Biasci, L; Cecconi, D; Cellesi, V; Forgione, RN; Meini, M; Moncini, M; Pellegrini, M; Rucci, P; Simoni, G, 2011) | 0.37 |
| " D(2) and D(3) antagonists differentially affected pramipexole-induced PR responding, with L: -741,626 and PG01037 producing rightward, and downward shifts in the dose-response curve for CS-maintained responding, respectively." | ( Effects of pramipexole on the reinforcing effectiveness of stimuli that were previously paired with cocaine reinforcement in rats. Chen, J; Collins, GT; Cunningham, AR; Newman, AH; Wang, S; Woods, JH, 2012) | 0.38 |
| " The recovery period, which was needed for the DA system to return back to the basic level, was fairly long compared to the dosing period of the steroid." | ( Subchronic steroid administration induces long lasting changes in neurochemical and behavioral response to cocaine in rats. Kailanto, S; Kankaanpää, A; Seppälä, T, 2011) | 0.37 |
| "A novel behaviorally dependent dosing (BDD) schedule was used to examine the relationship between doses of cocaine self-administered by rats and brain drug levels within a session." | ( Brain-cocaine concentrations determine the dose self-administered by rats on a novel behaviorally dependent dosing schedule. Dobrin, CV; Roberts, DC; Zimmer, BA, 2011) | 0.37 |
| " Then the dose-response effects of a selective mGluR2/3 agonist LY 379268 microinjected into the VTA on cocaine-induced reinstatement of cocaine-seeking behavior were assessed." | ( Regulation of cocaine-induced reinstatement by group II metabotropic glutamate receptors in the ventral tegmental area. Lu, L; Rebec, GV; Steketee, JD; Sun, W; Xue, Y, 2012) | 0.38 |
| " Intra-DLS infusion of the dopamine receptor antagonist α-flupenthixol did not affect the acquisition of cocaine self-administration, increased cocaine self-administration under a fixed ratio-1 (FR-1) schedule of reinforcement, caused a rightward and downward shift of the dose-response curve of cocaine under an FR-1 schedule of reinforcement and decreased responding for cocaine under a progressive ratio (PR) schedule of reinforcement." | ( Distinct contributions of dopamine in the dorsolateral striatum and nucleus accumbens shell to the reinforcing properties of cocaine. Broekhoven, MH; Damsteegt, R; Vanderschuren, LJ; Veeneman, MM, 2012) | 0.38 |
| " Particular attention was paid to the effect of initial pH, dosage of H(2)O(2) and to improvement in biodegradation." | ( Treatment of coking wastewater by an advanced Fenton oxidation process using iron powder and hydrogen peroxide. Chu, L; Dong, J; Liu, H; Sun, X; Wang, J, 2012) | 0.38 |
| " Increasing CREB expression in NAc shell markedly enhanced cocaine reinforcement of self-administration behavior, as indicated by leftward (long-term) and upward (short-term) shifts in fixed ratio dose-response curves." | ( Overexpression of CREB in the nucleus accumbens shell increases cocaine reinforcement in self-administering rats. Arzaga, RR; Bass, CE; Buzin, N; Graham, DL; Green, TA; Larson, EB; Nestler, EJ; Neve, RL; Self, DW; Terwilliger, EF; Webb, J, 2011) | 0.37 |
| " Dose-response curves were assessed before, during and after chronic (daily) administration of cocaine." | ( Tolerance to cocaine's effects on schedule-controlled behavior: role of delay between pause-ending responses and reinforcement. Branch, MN; Macaskill, AC, 2012) | 0.38 |
| "Placing treats in the home cage shifted the cocaine dose-response curve to the left in five monkeys tested and to the right in 4 of 12 animals." | ( Individual differences in the effects of environmental stimuli on cocaine choice in socially housed male cynomolgus monkeys. Czoty, PW; Nader, MA, 2012) | 0.38 |
| " Dose-response curves were assessed with increasing doses of cocaine (0." | ( Cocaine self-administration in Warsaw alcohol high-preferring (WHP) and Warsaw alcohol low-preferring (WLP) rats. Acewicz, A; Bienkowski, P; Dyr, W; Jastrzebska, A; Korkosz, I; Kostowski, W; Mierzejewski, P; Nauman, P; Samochowiec, J; Wyszogrodzka, E, 2012) | 0.38 |
| " Whereas ketamine produced progressive increases in activity with repeated administration in rats of both ages, MDMA increased, and then decreased, activity in the chronic dosing regimen in female adolescents only." | ( Locomotor activity changes in female adolescent and adult rats during repeated treatment with a cannabinoid or club drug. Evans, RL; Grainger, DB; Nicholson, KL; Wiley, JL, 2011) | 0.37 |
| " Results from the post-LgA dose-response ShA condition indicated that both LoS and HiS vehicle-treated and progesterone-treated rats earned more infusions than pre-LgA, but mainly at low doses." | ( Effects of progesterone on escalation of intravenous cocaine self-administration in rats selectively bred for high or low saccharin intake. Anker, JJ; Carroll, ME; Holtz, NA, 2012) | 0.38 |
| "In self-administration, L-152,804 prominently decreased nose-poking for the peak dose of cocaine and shifted the dose-response curve for cocaine downward." | ( Neuropeptide Y Y5 receptor antagonism attenuates cocaine-induced effects in mice. Bengtsen, CH; Christiansen, SH; Dencker, D; Fink-Jensen, A; Jensen, M; Loland, CJ; Petersen, JH; Sørensen, G; Weikop, P; Woldbye, DP; Wörtwein, G, 2012) | 0.38 |
| " A redetermination of the dose-response function following chronic exposure revealed reduced potency (i." | ( Effects of acute and chronic cocaine administration on titrating-delay matching-to-sample performance. Branch, MN; Kangas, BD, 2012) | 0.38 |
| " Local application of Arg or actin polymerization inhibitors exaggerated cocaine sensitization, as did reduced gene dosage of the Arg substrate, p190RhoGAP." | ( Arg kinase regulates prefrontal dendritic spine refinement and cocaine-induced plasticity. Gourley, SL; Koleske, AJ; Olevska, A; Taylor, JR; Warren, MS, 2012) | 0.38 |
| " Rhesus macaques self-administering cocaine underwent a 6-week dosing regimen with fluoxetine designed to approximate serum concentrations observed in humans." | ( Neurobiological changes mediating the effects of chronic fluoxetine on cocaine use. Goodman, MM; Howell, LL; Kimmel, HL; Mun, J; Nye, JA; Rice, KC; Sawyer, EK; Stehouwer, JS; Voll, RJ, 2012) | 0.38 |
| " Rats exposed to both repeated and variable stress displayed shifts in the cocaine dose-response curve but with different patterns of responding." | ( Differential modulation of cocaine's discriminative cue by repeated and variable stress exposure: relation to monoamine transporter levels. Baumann, MH; Decicco-Skinner, KL; Hurwitz, ZE; Johari, S; Kohut, SJ; Riley, AL, 2012) | 0.38 |
| " This study was aimed at characterizing the immunologic responses to repeated dosing with DM CocE and determining whether the development of anti-CocE antibodies altered the capacity of DM CocE to reduce plasma cocaine levels and ameliorate the cardiovascular effects of cocaine in rhesus monkeys." | ( Repeated administration of a mutant cocaine esterase: effects on plasma cocaine levels, cocaine-induced cardiovascular activity, and immune responses in rhesus monkeys. Brim, RL; Collins, GT; Ko, MC; Lukacs, NW; Narasimhan, D; Noon, KR; Sunahara, RK; Woods, JH, 2012) | 0.38 |
| " Testing began with acquisition of sucrose pellet self-administration, implantation of intravenous catheter, acquisition of cocaine self-administration, and dose-response testing (fixed ratio or progressive ratio)." | ( Cocaine self-administration behaviors in ClockΔ19 mice. Larson, EB; McClung, CA; Ozburn, AR; Self, DW, 2012) | 0.38 |
| " Using fixed ratio and progressive ratio schedules of reinforcement dose-response paradigms, we found that cocaine is a more efficacious reinforcer in ClockΔ19 mice than in WT mice." | ( Cocaine self-administration behaviors in ClockΔ19 mice. Larson, EB; McClung, CA; Ozburn, AR; Self, DW, 2012) | 0.38 |
| "5-HT(1B)R receptor gene transfer during maintenance shifted the dose-response curve for cocaine self-administration upward and to the left and increased breakpoints and cocaine intake on a progressive ratio schedule, consistent with enhanced reinforcing effects of cocaine." | ( Protracted withdrawal from cocaine self-administration flips the switch on 5-HT(1B) receptor modulation of cocaine abuse-related behaviors. Adams, MD; Cheung, TH; Neisewander, JL; Neumaier, JF; Pentkowski, NS; Toy, WA, 2012) | 0.38 |
| "56 mg/kg) significantly reduced drug-reinforced responding, resulting in a downward displacement of dose-response functions." | ( Antagonism of metabotropic glutamate 1 receptors attenuates behavioral effects of cocaine and methamphetamine in squirrel monkeys. Achat-Mendes, C; Platt, DM; Spealman, RD, 2012) | 0.38 |
| " The results suggest that the combination of buprenorphine and naltrexone at an appropriate dosage decreases compulsive cocaine self-administration with minimal liability to produce opioid dependence and may be useful as a treatment for cocaine addiction." | ( A combination of buprenorphine and naltrexone blocks compulsive cocaine intake in rodents without producing dependence. Koob, GF; Misra, KK; Schlosburg, JE; Vendruscolo, LF; Wee, S, 2012) | 0.38 |
| " As repeated drug dosing can have differential effects and is more clinically relevant than acute dosing, in the current study we examined the effects of repeated SB-334867 on cocaine self-administration, extinction, and reinstatement to cocaine seeking in Sprague-Dawley rats." | ( Repeated orexin 1 receptor antagonism effects on cocaine seeking in rats. Aston-Jones, G; Do, PH; See, RE; Smith, RJ; Zhou, L, 2012) | 0.38 |
| "0 mg/kg/infusion) and a dose-response curve was generated (0." | ( Effects of adolescent nicotine exposure and withdrawal on intravenous cocaine self-administration during adulthood in male C57BL/6J mice. Blaha, CD; Dickson, PE; Miller, MM; Mittleman, G; Rogers, TD, 2014) | 0.4 |
| "Rats self-administered cocaine using a behaviorally dependent dosing schedule of reinforcement, under which the size of each dose was determined by the length of time the lever was held down." | ( Examination of behavioral strategies regulating cocaine intake in rats. Dobrin, CV; Roberts, DC; Zimmer, BA, 2013) | 0.39 |
| "Occupational exposure to COEs is associated with a dose-response decrease in HRV." | ( The dose-response decrease in heart rate variability: any association with the metabolites of polycyclic aromatic hydrocarbons in coke oven workers? Dai, X; Deng, H; Deng, Q; Feng, Y; Guo, H; He, M; He, Y; Huang, K; Huang, S; Kuang, D; Li, X; Lin, D; Wu, T; Xin, L; Zhang, W; Zhang, X, 2012) | 0.38 |
| " Our results suggest that the use of weight-based medication doses would produce more reliable effects, consistent with weight-based dosing used in pediatrics and in preclinical research." | ( The impact of disulfiram treatment on the reinforcing effects of cocaine: a randomized clinical trial. De La Garza, R; Haile, CN; Kosten, TR; Mahoney, JJ; Newton, TF; Nielsen, DA, 2012) | 0.38 |
| "03 mm; initial dosage of zeolite powder, 50." | ( Adsorption characteristics of ammonium exchange by zeolite and the optimal application in the tertiary treatment of coking wastewater using response surface methodology. Tang, X; Wen, D; Zhang, J; Zhao, C; Zheng, Z, 2013) | 0.39 |
| "We sought to examine the impact of differing cocaine administration schedules and dosing on the magnitude of cocaine conditioned place preference (CPP), extinction, and stress- and cocaine-induced reinstatement of CPP." | ( Assessment of the impact of pattern of cocaine dosing schedule during conditioning and reconditioning on magnitude of cocaine CPP, extinction, and reinstatement. Conrad, KL; Louderback, KM; Milano, EJ; Winder, DG, 2013) | 0.39 |
| "5 mg/kg; total of 30 mg/kg), a fixed-high dose (FH; 16 mg/kg; total of 64 mg/kg), or an ascending dosing schedule (Asc; 2, 4, 8, and 16 mg/kg; total of 30 mg/kg)." | ( Assessment of the impact of pattern of cocaine dosing schedule during conditioning and reconditioning on magnitude of cocaine CPP, extinction, and reinstatement. Conrad, KL; Louderback, KM; Milano, EJ; Winder, DG, 2013) | 0.39 |
| "0 g/kg alcohol, attenuated the development of locomotor sensitization to alcohol with repeated exposure, and produced a shift in the dose-response curve for alcohol on BSR threshold without affecting maximum operant response rate (MAX)." | ( Levetiracetam has opposite effects on alcohol- and cocaine-related behaviors in C57BL/6J mice. Chen, M; Faccidomo, S; Fish, EW; Hodge, CW; Howard, EC; Krouse, MC; Malanga, CJ; Robinson, JE; Stamatakis, AM, 2013) | 0.39 |
| ") dose-response curves were determined, self-administration sessions were suspended and MPD (0." | ( Effects of chronic methylphenidate on cocaine self-administration under a progressive-ratio schedule of reinforcement in rhesus monkeys. Czoty, PW; Gould, RW; Martelle, SE; Nader, MA, 2013) | 0.39 |
| " In contrast, elevating the relative expression of Homer2b versus Homer1 within mPFC, by overexpressing Homer2b or knocking down Homer1c, shifted the dose-response function for cocaine-conditioned reward to the left, without affecting cocaine locomotion or sensitization." | ( Imbalances in prefrontal cortex CC-Homer1 versus CC-Homer2 expression promote cocaine preference. Ary, AW; Ben-Shahar, O; Campbell, RR; Klugmann, M; Lominac, KD; Szumlinski, KK; von Jonquieres, G; Williams, AR; Wroten, MG, 2013) | 0.39 |
| " The system operation was tested with the extraction, separation and detection of propranolol and associated metabolites from drug dosed tissues, caffeine from a coffee bean, cocaine from paper currency, and proteins from dried sheep blood spots on paper." | ( Continuous-flow liquid microjunction surface sampling probe connected on-line with high-performance liquid chromatography/mass spectrometry for spatially resolved analysis of small molecules and proteins. Kertesz, V; Van Berkel, GJ, 2013) | 0.39 |
| " A 5-point (1-5 mM) dose-response curve of NAC clearly indicated no adverse effect on astroglial cell viability." | ( Attenuating effect of N-acetyl-L-cysteine against acute cocaine toxicity in rat C6 astroglial cells. Badisa, RB; Fitch-Pye, CA; Goodman, CB, 2013) | 0.39 |
| "Polycyclic aromatic hydrocarbons (PAHs) are known to induce reactive oxygen species and oxidative stress, but the dose-response relationships between exposure to PAHs and oxidative stress levels have not been established." | ( Dose-response relationships of polycyclic aromatic hydrocarbons exposure and oxidative damage to DNA and lipid in coke oven workers. Deng, Q; Guan, L; Guo, H; Hu, D; Huang, K; Kuang, D; Wu, T; Zhang, W; Zhang, X, 2013) | 0.39 |
| " Further, subtle alterations of ligand structure and the specific dosage levels employed influence the behavioral effects observed, with a 3-methoxy substituent apparently conferring the ability of a ligand to enhance cocaine's locomotor stimulatory effects." | ( Effects of N-phenylpropyl-N'-substituted piperazine sigma receptor ligands on cocaine-induced hyperactivity in mice. Davis, DC; Fan, KH; Lever, JR; Lever, SZ; Miller, DK; Nahas, RI; Oelrichs, CE; Sage, AS, 2013) | 0.39 |
| " A distinct dose-response effects of these peptides on cocaine locomotion probably arise from differential functional activation (targeting) of the DOR and MOR by both deltorphins analogs." | ( Involvement of delta and mu opioid receptors in the acute and sensitized locomotor action of cocaine in mice. Gibula-Bruzda, E; Izdebski, J; Kotlinska, JH; Witkowska, E, 2013) | 0.39 |
| " Further, MFZ 10-7 appeared to be more potent than MTEP in inducing downward shifts in the cocaine dose-response curve, but less effective than MTEP in attenuating sucrose-induced reinstatement of sucrose-seeking behavior." | ( A novel mGluR5 antagonist, MFZ 10-7, inhibits cocaine-taking and cocaine-seeking behavior in rats. Bi, GH; Gardner, EL; Keck, TM; Newman, AH; Srivastava, R; Wang, XF; Xi, ZX; Yang, HJ; Zhang, HY; Zou, MF, 2014) | 0.4 |
| " Additionally, we evaluated the effect of OS-3-106 (10 mg/kg) on the dose-response function of cocaine self-administration and the effect of WW-III-55 (0-5." | ( Reduction of cocaine self-administration and D3 receptor-mediated behavior by two novel dopamine D3 receptor-selective partial agonists, OS-3-106 and WW-III-55. Chandler, KN; Cheung, TH; Lenz, JD; Loriaux, AL; Luedtke, RR; Mach, RH; Neisewander, JL; Schaan, RF; Weber, SM, 2013) | 0.39 |
| " However, in combination studies, pretreatment with either disulfiram or nepicastat produced leftward shifts in the cocaine dose-response function and also conferred cocaine-like stimulus effects to the selective NE transporter inhibitor, reboxetine (0." | ( Dopamine β-hydroxylase inhibitors enhance the discriminative stimulus effects of cocaine in rats. DePoy, LM; Manvich, DF; Weinshenker, D, 2013) | 0.39 |
| "083 mg/infusion) of cocaine, but the sensitivity to cocaine reinforcement, assessed using a dose-response analysis, was not altered in isolated rats." | ( Disrupted social development enhances the motivation for cocaine in rats. Baarendse, PJ; Limpens, JH; Vanderschuren, LJ, 2014) | 0.4 |
| " This may result in sub-therapeutic dosing creating withdrawal symptoms leading to additional substance use." | ( Rates of fetal polydrug exposures in methadone-maintained pregnancies from a high-risk population. Delano, K; Gareri, J; Koren, G, 2013) | 0.39 |
| " There was indirect evidence of facilitated learning in extinction and set shift tests, but the effective dosage was different (2." | ( Drugs of abuse as memory modulators: a study of cocaine in rats. Cloke, JM; Gallagher, N; Leri, F; Rkieh, N; Winters, BD, 2014) | 0.4 |
| " In Experiment 2, histamine decreased cocaine's potency and effectiveness as a reinforcer in a dose-dependent manner as indicated by rightward and downward shifts, respectively, in the dose-response functions." | ( Assessment of the effects of contingent histamine injections on the reinforcing effectiveness of cocaine using behavioral economic and progressive-ratio designs. Freeman, KB; McMaster, BC; Roma, PG; Woolverton, WL, 2014) | 0.4 |
| "This study sought to answer the question "Does prenatal exposure to cocaine, in a dose-response fashion, alter the rewarding effects of cocaine using a conditioned place preference (CPP) procedure during adolescence in the rat?" Further, we wanted to assess the possible sex differences and the role of being raised in an enriched versus impoverished environment." | ( The effects of prenatal cocaine, post-weaning housing and sex on conditioned place preference in adolescent rats. Dow-Edwards, D; Iijima, M; Jackson, A; Stephenson, S; Weedon, J, 2014) | 0.4 |
| "Virgin female Sprague-Dawley rats were dosed daily with cocaine at 30 mg/kg (C30), 60 mg/kg (C60), or vehicle intragastrically prior to mating and throughout gestation." | ( The effects of prenatal cocaine, post-weaning housing and sex on conditioned place preference in adolescent rats. Dow-Edwards, D; Iijima, M; Jackson, A; Stephenson, S; Weedon, J, 2014) | 0.4 |
| ", self-administration) sessions and 1 dose-response session, were conducted (once during the lead-in and twice after randomization)." | ( Aripiprazole effects on self-administration and pharmacodynamics of intravenous cocaine and cigarette smoking in humans. Campbell, C; Lofwall, MR; Nuzzo, PA; Walsh, SL, 2014) | 0.4 |
| " The second experiment examined effects of repeated dosing with ketamine (3." | ( Dissociable effects of the noncompetitive NMDA receptor antagonists ketamine and MK-801 on intracranial self-stimulation in rats. Hillhouse, TM; Negus, SS; Porter, JH, 2014) | 0.4 |
| " Repeated dosing with ketamine produced dose-dependent tolerance to the rate-decreasing effects of ketamine (10." | ( Dissociable effects of the noncompetitive NMDA receptor antagonists ketamine and MK-801 on intracranial self-stimulation in rats. Hillhouse, TM; Negus, SS; Porter, JH, 2014) | 0.4 |
| " These miRNAs were associated with a dose-response increase in 8-OH-dG (β > 0), and with a dose-response decrease in 8-iso-PGF2α (β < 0), especially in workers with lower PAHs exposure levels, in nonsmokers, and in nondrinkers." | ( Polycyclic aromatic hydrocarbons-associated microRNAs and their interactions with the environment: influences on oxidative DNA damage and lipid peroxidation in coke oven workers. Dai, X; Deng, H; Deng, Q; Feng, J; Guo, H; Hu, D; Huang, K; Huang, S; Kuang, D; Wang, T; Wu, T; Zhang, W; Zhang, X, 2014) | 0.4 |
| " However, acute EB treatment resulted in a rightward shift in the cocaine dose-response curve; rats demonstrated a significant preference at only the moderate and high conditioning doses of cocaine (10 and 15mg/kg)." | ( Acute estradiol treatment affects the expression of cocaine-induced conditioned place preference in ovariectomized female rats. Bobzean, SA; Dennis, TS; Perrotti, LI, 2014) | 0.4 |
| "In coke oven workers, increased IL-6 was associated with a dose-response decreased HRV in the high-PAHs metabolites groups, whereas increase of Hsp70 can result in significant dose-related increase in HRV in the low-PAHs metabolites groups." | ( Association of plasma IL-6 and Hsp70 with HRV at different levels of PAHs metabolites. Deng, Q; Feng, Y; He, X; Wu, T; Yang, L; Ye, J; Zhang, X; Zhu, R; Zhu, X, 2014) | 0.4 |
| " Combined subthreshold dosing of VTA ghrelin with a subthreshold dose of cocaine also evoked reliable increases in intake compared to vehicle." | ( Ghrelin alters the stimulatory effect of cocaine on ethanol intake following mesolimbic or systemic administration. Cepko, LC; Currie, PJ; Fimmel, AI; Goldberg, SA; Merfeld, EB; Selva, JA, 2014) | 0.4 |
| "4 mg/kg) produced a downward shift in the cocaine dose-response curve under a fixed ratio schedule of reinforcement and decreased the cocaine breaking point." | ( On the role of adenosine (A)₂A receptors in cocaine-induced reward: a pharmacological and neurochemical analysis in rats. Filip, M; Fuxe, K; Gołembiowska, K; Kamińska, K; Suder, A; Wydra, K, 2015) | 0.42 |
| " We found that α6 KO mice exhibited a rightward shift in the nicotine dose-response curve compared with WT littermates but that α4 KO failed to show nicotine preference, suggesting that α6α4β2*-nAChRs are involved." | ( Differential roles of α6β2* and α4β2* neuronal nicotinic receptors in nicotine- and cocaine-conditioned reward in mice. Bowers, MS; Brunzell, DH; Damaj, MI; Maldoon, PP; Marks, MJ; Maskos, U; McIntosh, JM; Sanjakdar, SS, 2015) | 0.42 |
| "0, the dosage of Fe 73." | ( Denitrification of coking wastewater with micro-electrolysis. Lv, Y; Shan, M; Shen, X; Su, Y; Wang, Y, 2011) | 0.37 |
| " Breath was collected from 10 healthy adult cocaine users by asking them to breathe into a SensAbues device for 3 min before and up to 22 h following 25 mg intravenous (IV) cocaine dosing on days 1, 5, and 10, and assayed with a validated liquid chromatography-high-resolution mass spectrometry (LC-HRMS) method to quantify breath cocaine, benzoylecgonine (BE), ecgonine methyl ester (EME), and norcocaine." | ( Quantification of cocaine and metabolites in exhaled breath by liquid chromatography-high-resolution mass spectrometry following controlled administration of intravenous cocaine. Beck, O; Concheiro, M; Ellefsen, KN; Gorelick, DA; Huestis, MA; Pirard, S, 2014) | 0.4 |
| "Conventional dosage forms such as tablets, capsules and syrups are prescribed in the normal course of practice." | ( Confectionery-based dose forms. Boyd, BJ; Ho, QP; Tangso, KJ, 2015) | 0.42 |
| "Urinary 1-hydroxyphenanthrene is associated with a dose-response increase in serum uric acid levels in coke oven workers, and exposure to phenanthrene in PAHs may be a risk factor for hyperuricemia." | ( [Association between urinary polycyclic aromatic hydrocarbon metabolites and elevated serum uric acid levels in coke oven workers]. Deng, Q; Deng, S; Guo, H; Hu, D; Li, J; Wu, T; Zhu, X, 2014) | 0.4 |
| " For cocaine dosing over extended periods, cocaine was provided in drinking water using continuous and scheduled regimens." | ( Chronic cocaine causes long-term alterations in circadian period and photic entrainment in the mouse. Amicarelli, MJ; Glass, JD; Prosser, RA; Stowie, AC, 2015) | 0.42 |
| "3 mg/kg/injection cocaine or MA) choice paradigm in which complete SA dose-response curves were determined each session (N = 3/group)." | ( Effects of buspirone and the dopamine D3 receptor compound PG619 on cocaine and methamphetamine self-administration in rhesus monkeys using a food-drug choice paradigm. Banala, AK; John, WS; Nader, MA; Newman, AH, 2015) | 0.42 |
| " We previously described that exogenous GM1 ganglioside pretreatment enhances the rewarding properties of cocaine, evidenced by a lower number of sessions and/or dosage necessary to induce conditioned place preference (CPP)." | ( Exogenous GM1 ganglioside increases accumbal BDNF levels in rats. Cuadra, GR; Orsingher, OA; Perondi, MC; Valdomero, A, 2015) | 0.42 |
| "5, 1, 2, and 24 hours after dosing in subjects with confirmed cocaine use and abstinence." | ( The impact of recent cocaine use on plasma levels of methadone and buprenorphine in patients with and without HIV-infection. DInh, AT; Fiellin, DA; Fiellin, LE; Lruie, BS; McCance-Katz, EF; Moody, DE; Tetrault, JM, 2015) | 0.42 |
| " In the conditioned place-preference assay, DMAA produced an inverted-U-shaped dose-response curve, with intermediate doses producing significant place preference." | ( Abuse liability of the dietary supplement dimethylamylamine. Dolan, SB; Gatch, MB, 2015) | 0.42 |
| " Eight male rhesus monkeys (n=4/group) served as subjects in which complete cocaine and MA dose-response curves were determined daily in each session." | ( Differential effects of the dopamine D3 receptor antagonist PG01037 on cocaine and methamphetamine self-administration in rhesus monkeys. John, WS; Nader, MA; Newman, AH, 2015) | 0.42 |
| " The present study compared the dose-response functions for intravenous self-administration of cocaine and heroin between male HIV-1 transgenic (HIV-1 Tg) and Fischer 344 rats." | ( Increased Sensitivity to Cocaine Self-Administration in HIV-1 Transgenic Rats is Associated with Changes in Striatal Dopamine Transporter Binding. Childers, SR; Hemby, SE; McIntosh, S; Pattison, LP; Sexton, T, 2015) | 0.42 |
| "Male BALB/C mice were given several cocaine dosage and treatment regimens, and the free and acid-labile H2S tissue concentrations were determined with a modified spectrophotometric method of Siegel." | ( Cocaine exposure alters H2S tissue concentrations in peripheral mouse organs. Filip, M; Frankowska, M; Opoka, W; Piotrowska, J; Somogyi, E; Wiliński, B, 2015) | 0.42 |
| " Here, in order to shed light on the influence of TAAR1 on cocaine's reward and reinforcement, we studied the effects of partial and full activation of TAAR1on (1) the dose-response curve for cocaine self-administration and (2) cocaine-induced changes in intracranial self-stimulation (ICSS)." | ( Selective activation of the trace amine-associated receptor 1 decreases cocaine's reinforcing efficacy and prevents cocaine-induced changes in brain reward thresholds. Canales, JJ; Hoener, MC; Mortas, P; Pei, Y, 2015) | 0.42 |
| " In monkeys discriminating cocaine from saline, lorcaserin alone did not occasion cocaine-appropriate responding but shifted the cocaine dose-response curve to the right and down in two of three monkeys." | ( Lorcaserin Reduces the Discriminative Stimulus and Reinforcing Effects of Cocaine in Rhesus Monkeys. Collins, GT; France, CP; Gerak, LR; Javors, MA, 2016) | 0.43 |
| " Mice from 29 BXD strains completed a full dose-response curve (0." | ( Systems genetics of intravenous cocaine self-administration in the BXD recombinant inbred mouse panel. Bubier, JA; Calton, MA; Chesler, EJ; Cook, MN; Dickson, PE; Goldowitz, D; Miller, MM; Mittleman, G, 2016) | 0.43 |
| " Next, monkeys were treated with quetiapine (25 mg, by mouth, twice a day) for approximately 30 days, and then the quetiapine self-administration dose-response curve was redetermined." | ( Evaluation of the Reinforcing Effect of Quetiapine, Alone and in Combination with Cocaine, in Rhesus Monkeys. Brutcher, RE; Nader, MA; Nader, SH, 2016) | 0.43 |
| " Given the general observation that the biological half-life of a protein drug is significantly longer in humans than in rodents, the CocH-Fc reported in this study could allow dosing once every 2-4 wk, or longer, for treatment of cocaine addiction in humans." | ( Long-acting cocaine hydrolase for addiction therapy. Chen, X; Hou, S; Jin, Z; Xue, L; Zhan, CG; Zhang, T; Zheng, F, 2016) | 0.43 |
| "32 mg/kg/h, IV) dose-dependently decreased cocaine-maintained responding; the highest dosage reduced cocaine intake to levels of saline self-administration without appreciable effects on food-maintained responding." | ( Effects of L-methamphetamine treatment on cocaine- and food-maintained behavior in rhesus monkeys. Bergman, J; Blough, BE; Kohut, SJ, 2016) | 0.43 |
| " Dose-response relationship resembled a sigmoidal curve, with low doses not reaching statistical significance and high doses reliably inhibiting self-administration of drugs of abuse." | ( Negative Allosteric Modulators of Metabotropic Glutamate Receptors Subtype 5 in Addiction: a Therapeutic Window. Hasler, G; Mihov, Y, 2016) | 0.43 |
| " Dose-response curves had inverted U shapes, with peak response rates occurring at a dose of 10 μg/kg/injection." | ( Self-administration of the anandamide transport inhibitor AM404 by squirrel monkeys. Goldberg, SR; Justinova, Z; Makriyannis, A; Redhi, GH; Scherma, M; Schindler, CW; Vadivel, SK, 2016) | 0.43 |
| " Facial emotion recognition was measured twice during target LCE dosing and twice on placebo: once without cocaine and once after repeated cocaine doses." | ( Effects of levodopa-carbidopa-entacapone and smoked cocaine on facial affect recognition in cocaine smokers. Bedi, G; Bisaga, A; Foltin, RW; Nunes, EV; Shiffrin, L; Vadhan, NP, 2016) | 0.43 |
| " Therefore, it is important to assess whether chronic dosing of mirtazapine alters locomotor effects of cocaine as well as induction and expression of cocaine sensitization." | ( Mirtazapine prevents induction and expression of cocaine-induced behavioral sensitization in rats. Antón, B; Barbosa-Méndez, S; Hernández-Miramontes, R; Jurado, N; Leff, P; Salazar-Juárez, A, 2016) | 0.43 |
| " After completing a cocaine self-administration dose-response curve, sessions were suspended and PDM was administered (1." | ( Attenuation of cocaine self-administration by chronic oral phendimetrazine in rhesus monkeys. Blough, BE; Czoty, PW; Fennell, TR; Nader, MA; Snyder, RW, 2016) | 0.43 |
| " The effect of temperature, initial chemical oxygen demand (COD) and AC dosage on COD removal efficiency was investigated." | ( Treatment of soil eluate containing nitro aromatic compounds by adsorption on activated coke (AC). Gao, X; Jiang, Z; Su, H; Ye, Z; Zhang, Y; Zhang, Z; Zhao, Q, 2016) | 0.43 |
| "5mg/kg), assessing their dose-response and extinction." | ( Unaltered cocaine self-administration in the prenatal LPS rat model of schizophrenia. Ambrosio, E; Borcel, É; Capellán, R; Higuera-Matas, A; Orihuel, J; Roura-Martínez, D; Santos-Toscano, R; Ucha, M, 2016) | 0.43 |
| " The sucrose-experienced (sucrose) group exhibited higher lever press, cocaine infusion and break point, as well as upshift of cocaine dose-response curve in cocaine self-administration test, as compared with the control (chow) group." | ( [Sucrose reward promotes rats' motivation for cocaine]. LE, QM; Li, YQ; Ma, L; Wang, FF; Yu, XC, 2016) | 0.43 |
| " As a result of this increased intake, the cocaine self-administration dose-response curve was shifted upward indicating an increase in cocaine reinforcement." | ( Nicotine produces long-term increases in cocaine reinforcement in adolescent but not adult rats. Izenwasser, S; Reed, SC, 2017) | 0.46 |
| " In sub-analysis, consistent dose-response patterns were observed between levels of alcohol use and unprotected sex, homelessness, and daily heroin injection." | ( Unsafe sexual behaviour associated with hazardous alcohol use among street-involved youth. DeBeck, K; Dong, H; Fairbairn, N; Kerr, T; Wood, E, 2017) | 0.46 |
| " Corticosterone failed to re-establish extinguished preference alone but produced a leftward shift in the dose-response curve for cocaine-primed reinstatement." | ( Corticosterone Potentiation of Cocaine-Induced Reinstatement of Conditioned Place Preference in Mice is Mediated by Blockade of the Organic Cation Transporter 3. Ambrosius, T; Baker, DA; Derricks, O; Gasser, PJ; Kurtoglu, B; Mantsch, JR; McReynolds, JR; Nino, B; Taylor, A; Vranjkovic, O; Wheeler, RA, 2017) | 0.46 |
| "0 mg/kg/infusion) followed by a dose-response curve after acquisition of cocaine self-administration." | ( Prior Exposure to Alcohol Has No Effect on Cocaine Self-Administration and Relapse in Rats: Evidence from a Rat Model that Does Not Support the Gateway Hypothesis. Adhikary, S; Bonci, A; Bossert, JM; Fredriksson, I; Shaham, Y; Steensland, P; Vendruscolo, LF, 2017) | 0.46 |
| " The present study compared the rewarding and reinforcing properties of MDPV and cocaine using systemic injection dose-response and self-administration models." | ( Comparing rewarding and reinforcing properties between 'bath salt' 3,4-methylenedioxypyrovalerone (MDPV) and cocaine using ultrasonic vocalizations in rats. Barker, DJ; Gentile, TA; Gregg, RA; Mo, L; Muschamp, JW; Rawls, SM; Simmons, SJ; Tran, FH; von Weltin, E; Watterson, LR, 2018) | 0.48 |
| "Primary outcome measures were (i) the percentage of samples purchased on-line and (ii) the chemical purity of powders (or dosage per tablet); adulteration; and the price per gram, blotter or tablet of drugs bought on-line compared with drugs bought off-line." | ( Purity, adulteration and price of drugs bought on-line versus off-line in the Netherlands. Brunt, TM; van der Gouwe, D; van der Pol, P; van Laar, M, 2017) | 0.46 |
| "All rats acquired cocaine self-administration and generated "inverted-U" dose-response functions." | ( Comparison of cocaine reinforcement in lean and obese Zucker rats: Relative potency and reinstatement of extinguished operant responding. Freeman, KB; Townsend, EA, 2017) | 0.46 |
| "The aim of this study is to analyse cardiac specimens from human cocaine-related overdose, to verify the hypothesis that cardiac toxicity by acute exposure to high dosage of cocaine could be mediated by unbalanced myocardial oxidative stress, and to evaluate the apoptotic response." | ( Myocardial oxidative damage is induced by cardiac Fas-dependent and mitochondria-dependent apoptotic pathways in human cocaine-related overdose. Cantatore, S; Cerretani, D; Cipolloni, L; Di Paolo, M; Fiaschi, AI; Fineschi, V; Frati, P; Micheli, L; Neri, M; Pinchi, E; Riezzo, I; Santurro, A; Turillazzi, E; Vullo, A, 2017) | 0.46 |
| " Moreover, the mirtazapine dosed for 30 days during extinction produced sustained attenuation of lever-press responses during re-acquisition of cocaine self-administration, without changing food-seeking behavior." | ( Mirtazapine attenuates cocaine seeking in rats. Arías-Caballero, A; Barbosa-Méndez, S; Heinze, G; Hernández-Miramontes, R; Leff, P; Salazar-Juárez, A, 2017) | 0.46 |
| " This study focused on exploring whether different mirtazapine dosing regimens could optimize and/or improve the effect of 30mg/kg mirtazapine administered for 30 days on cocaine-induced locomotor activity during the expression phase of behavioral sensitization." | ( Dose- and time-dependent effects of mirtazapine on the expression of cocaine-induced behavioral sensitization in rats. Barbosa-Méndez, S; Flores-Zamora, A; Jurado, N; Matus-Ortega, M; Salazar-Juárez, A, 2017) | 0.46 |
| " During dose-response determinations (when dose on the variable and fixed options were not equal), making the schedule, dose, or both variable generally did not alter cocaine's potency as a reinforcer." | ( Choice between variable and fixed cocaine injections in male rhesus monkeys. Freeman, KB; Huskinson, SL; Petry, NM; Rowlett, JK, 2017) | 0.46 |
| " In most monkeys, social reorganization shifted the cocaine dose-response curve to the right, also consistent with environmental enrichment." | ( Effects of social reorganization on dopamine D2/D3 receptor availability and cocaine self-administration in male cynomolgus monkeys. Czoty, PW; Gage, HD; Gould, RW; Nader, MA, 2017) | 0.46 |
| " We observed a dose-response relationship between the number of traumas and drug use in adolescence [marijuana, adjusted odds ratio (aOR) one trauma versus none = 1." | ( Childhood traumatic experiences and the association with marijuana and cocaine use in adolescence through adulthood. Beharie, NN; Cottler, LB; Frueh, BC; Khan, MR; McGorray, SP; Quinn, K; Scheidell, JD, 2018) | 0.48 |
| " Hence, the successful development of future TRIs for depression will demand strong translational evidence, an optimal dosing regimen, and better tolerability." | ( Triple Reuptake Inhibitors as Potential Therapeutics for Depression and Other Disorders: Design Paradigm and Developmental Challenges. Subbaiah, MAM, 2018) | 0.48 |
| " Toxicology stated the dosage of cocaine intoxication as lethal." | ( Death by "Snow"! A Fatal Forensic Case of Cocaine Leakage in a "Drug Mule" on Postmortem Computed and Magnetic Resonance Tomography Compared With Autopsy. Ebert, LC; Fader, R; Flach, PM; Gascho, D; Martinez, R; Thali, MJ, 2017) | 0.46 |
| " We found that chronic treatment with the mirtazapine-prazosin combination significantly improved the effect of single mirtazapine dosing on cocaine-induced locomotor activity and on the induction and expression of cocaine sensitization." | ( Synergistic interactions between mirtazapine and prazosin prevent the induction and expression of behavioral sensitization to cocaine in rats. Barbosa-Méndez, S; Matus-Ortega, M; Salazar-Juárez, A, 2017) | 0.46 |
| "Locally-acting lozenges are among the most common types of solid dosage forms applied in the oral cavity." | ( Bioequivalence of locally acting lozenges: Evaluation of critical in vivo parameters and first steps towards a bio-predictive in vitro test method. Gutknecht, SI; Klein, S; Tietz, K, 2018) | 0.48 |
| " This unexpected finding suggests that chronic effects of cocaine on inflammation may be different from acute effects or that higher dosing may have differential effects as compared to lower dose used here." | ( Intravenous Cocaine Results in an Acute Decrease in Levels of Biomarkers of Vascular Inflammation in Humans. Dawn, B; Dileepan, KN; Grasing, K; Gupta, K; He, J; Masoomi, R; Sharma, R; Singh, V; Smith, DD, 2018) | 0.48 |
| " Here, we compared the effect of decreased mRNA level of Drd2 in each region on cocaine self-administration in a dose-response function." | ( High and low doses of cocaine intake are differentially regulated by dopamine D2 receptors in the ventral tegmental area and the nucleus accumbens. Chen, R; Childers, SR; Hemby, SE; Martin, TJ; McIntosh, S; Sexton, T; Sun, H, 2018) | 0.48 |
| " Fourteen healthy inpatient participants (six males) with current histories of cocaine use were administered two oral doses (100 and 200 mg) and one intravenous (IV) dose (40 mg) of cocaine during three separate dosing sessions." | ( Bioavailability and Pharmacokinetics of Oral Cocaine in Humans. Coe, MA; Cone, EJ; Jufer Phipps, RA; Walsh, SL, 2018) | 0.48 |
| "We used Wistar rats which were dosed with cocaine, nicotine or cocaine and nicotine combination and recorded their locomotor activity in different phases of the experiment." | ( Cocaine + nicotine mixture enhances induction and expression of behavioral sensitization in rats. Barbosa-Méndez, S; Salazar-Juárez, A, 2018) | 0.48 |
| " The amendments tested included fine and coarse coal-based activated carbons (AC), an enhanced pinewood derived biochar (EPB), organoclay, and coke dosed at 5% of sediment dry weight." | ( Enhanced biochars can match activated carbon performance in sediments with high native bioavailability and low final porewater PCB concentrations. Ghosh, U; Gomez-Eyles, JL, 2018) | 0.48 |
| "6 mg/kg) produced a significant downward shift in the d-methamphetamine dose-response function; surprisingly, lower and higher pretreatment doses (3." | ( Limited modulation of the abuse-related behavioral effects of d-methamphetamine by disulfiram. Bergman, J; de Moura, FB; Kohut, SJ, 2018) | 0.48 |
| " We found that the urinary level of 1-hydroxypyrene (1-OHP) had significant dose-response relationships with increased TL decline [β(95%CI) = 0." | ( The interaction effects of polycyclic aromatic hydrocarbons exposure and TERT- CLPTM1L variants on longitudinal telomere length shortening: A prospective cohort study. Bai, Y; Chen, W; Chen, Z; Fu, W; Guo, H; He, M; Li, G; Li, X; Wang, G; Wang, S; Wu, T; Wu, X; Zhang, X, 2018) | 0.48 |
| " Here, we investigated sensitivity to cocaine self-administration (SA) through a dose-response protocol in RHAs and RLAs, and reinstatement of drug-seeking behavior at 15 days and 5 weeks following withdrawal." | ( Differential involvement of D2 and D3 receptors during reinstatement of cocaine-seeking behavior in the Roman high- and low-avoidance rats. Bellés Añó, L; Dimiziani, A; Ginovart, N; Herrmann, F; Millet, P; Tsartsalis, S, 2019) | 0.51 |
| " These changes include a leftward shift in the dose-response to a D1-like agonist that indicates a behavioral D1R hypersensitivity, a shift from PKA to ERK intracellular signaling cascades upon D1R activation, and a reduction in the density of bridging collaterals from D1R-expressing neurons to pallidal areas." | ( D1 receptor hypersensitivity in mice with low striatal D2 receptors facilitates select cocaine behaviors. Alvarez, VA; Bocarsly, ME; Bock, R; Dobbs, LK; Eberhart, L; Kaplan, AR; Phamluong, K; Ron, D; Shin, JH, 2019) | 0.51 |
| " Batch desorption assays were run on particulate matter dosed with 4-nonylphenol." | ( Environmental conditions affecting re-release from particulate matter of 4-Nonylphenol into an aqueous medium. Bowyer, C; Lyons, R; Togashi, T, 2019) | 0.51 |
| "Baseline data were analyzed from the STimulant Reduction Intervention using Dosed Exercise trial, a multisite randomized clinical trial that evaluated exercise versus health education on drug use outcomes in individuals with stimulant use disorders." | ( The Stimulant Selective Severity Assessment: A replication and exploratory extension of the Cocaine Selective Severity Assessment. Bernstein, I; Greer, TL; Northrup, TF; Tillitski, J; Trivedi, MH; Walker, R, 2019) | 0.51 |
| "3 and 1 mg/kg) reduced cocaine-primed reinstatement of drug-seeking behavior and caused significant downward shift of the dose-response curve in cocaine self-administration tests (0." | ( MP1104, a mixed kappa-delta opioid receptor agonist has anti-cocaine properties with reduced side-effects in rats. Atigari, DV; Kivell, BM; Majumdar, S; Pasternak, GW; Uprety, R, 2019) | 0.51 |
| " dosing schedule with the conditioned place preference (CPP) model we investigated the persisting effects of cocaine conditioning on long-term potentiation (LTP) in the CA1 region of the ventral hippocampus (vH), and spatial working memory in a radial arm maze (RAM) task." | ( Cocaine conditioning induces persisting changes in ventral hippocampus synaptic transmission, long-term potentiation, and radial arm maze performance in the mouse. Brown, KA; Preston, CJ; Wagner, JJ, 2019) | 0.51 |
| "This study sought to determine whether chronic dosing of mirtazapine during cocaine withdrawal reduced depression- and anxiety-like behaviors that characterize cocaine withdrawal in animals." | ( Mirtazapine attenuates anxiety- and depression-like behaviors in rats during cocaine withdrawal. Barbosa Méndez, S; Salazar-Juárez, A, 2019) | 0.51 |
| "We found that chronic dosing with different doses of mirtazapine (30 and 60 mg/kg) decreased depression- and anxiety-like behaviors induced by different doses of cocaine (10, 20 and 40 mg/kg) during the 60-day cocaine withdrawal." | ( Mirtazapine attenuates anxiety- and depression-like behaviors in rats during cocaine withdrawal. Barbosa Méndez, S; Salazar-Juárez, A, 2019) | 0.51 |
| " Designing the preparation procedures and selecting the age-appropriate dosage form should be based on a benefit-risk approach, taking into account safety, efficacy, ease of use and accessibility to the patient." | ( Modern pediatric formulations of the soft candies in the form of a jelly: determination of metoclopramide content and dissolution. Karaiskou, SG; Kouskoura, MG; Markopoulou, CK, 2020) | 0.56 |
| " This study measured differences in cognitive behavior performance on the object recognition test (ORT) and social recognition test (SRT) and serum levels of corticosterone (CORT) between C57BL/6J and BALB/cJ mice after 14-day chronic exposure to either cocaine (5 mg/kg) or morphine (3 mg/kg) at a dosage of 10 ml/kg/day." | ( Differences in cocaine- and morphine-induced cognitive impairments and serum corticosterone between C57BL/6J and BALB/cJ mice. Chao, R; Chen, L; Gong, D; Liang, Y; Yang, S; Yu, P; Zhao, H, 2019) | 0.51 |
| " In this study, we evaluated the motivation for drug seeking in cocaine self-administering rats exposed to an escalated dosing regimen that endeavored to mimic the characteristic of escalating drug intake in human addicts." | ( Tropisetron Facilitates Footshock Suppression of Compulsive Cocaine Seeking. Shen, HW; Shi, J; Yu, ZP; Zhang, LY; Zhang, XQ; Zhou, YQ, 2019) | 0.51 |
| " In addition, FLT1 hypermethylation and gene suppression appeared in primary human lymphocytes in a dose-response manner following COEs treatment." | ( FLT1 hypermethylation is involved in polycyclic aromatic hydrocarbons-induced cell transformation. Chen, L; Chen, S; Chen, W; Dong, G; Duan, H; He, Z; Li, D; Li, H; Li, Q; Niu, Y; Wang, Q; Wang, Z; Xiao, Y; Xing, X; Ye, L; Yu, D; Zhang, R; Zheng, Y, 2019) | 0.51 |
| " The current study examines the impact of non-contingent acute, repeated, and withdrawal-inducing morphine dosing regimens on glutamate transmission in D1- or D2-MSNs in the nucleus accumbens shell (NAcSh) and core (NAcC) sub-regions in hopes of identifying excitatory plasticity that may contribute to unique facets of opioid addiction-related behavior." | ( Cell-type and region-specific nucleus accumbens AMPAR plasticity associated with morphine reward, reinstatement, and spontaneous withdrawal. Anderson, EM; Gomez, D; Hearing, MC; Ingebretson, AE; Madayag, AC; Thomas, MJ, 2019) | 0.51 |
| " Drug concentrations for amphetamines, cannabis, cocaine, opioids, and benzodiazepines are reviewed in the context of the dosing condition and the collection method." | ( Oral Fluid Drug Testing: Analytical Approaches, Issues and Interpretation of Results. Desrosiers, NA; Huestis, MA, 2019) | 0.51 |
| " There were significantly dose-response relationships between COEs exposure and telomere damage with telomere length as a biomarker." | ( Benchmark dose assessment for coke oven emissions-induced telomere length effects in occupationally exposed workers in China. Duan, X; Feng, F; Feng, X; Li, G; Li, L; Wang, P; Wang, S; Wang, T; Wang, W; Wang, Y; Yan, Z; Yang, Y; Yao, W; Zhang, Y; Zhao, J; Zhou, X, 2019) | 0.51 |
| " Our behavioral data showed that a lack of Rhes in knockout animals caused profound alterations in motor stimulation following cocaine exposure, eliciting a significant leftward shift in the dose-response curve and triggering a dramatic hyperactivity." | ( The striatal-enriched protein Rhes is a critical modulator of cocaine-induced molecular and behavioral responses. Avallone, L; Biagini, T; Chambery, A; De Rosa, A; Di Maio, A; Federici, M; Garofalo, M; Ledonne, A; Mazza, T; Mercuri, NB; Migliarini, S; Napolitano, F; Nuzzo, T; Pasqualetti, M; Rizzo, FR; Russo, R; Usiello, A, 2019) | 0.51 |
| " However, following normal saline-extinction, wild type (WT) mice show a classic inverted-U dose-response function, while Arc/Arg3." | ( The activity-regulated cytoskeleton-associated protein, Arc/Arg3.1, influences mouse cocaine self-administration. Cowan, CW; Guo, Y; Penrod, RD; Smith, LN; Taniguchi, M; Thomsen, M, 2020) | 0.56 |
| " The effective dosage of bupropion increased responding for cocaine alone, nicotine alone, and for saline injections and significantly increased measures of daily activity." | ( Effects of chronic treatment with bupropion on self-administration of nicotine + cocaine mixtures in nonhuman primates. Barkin, CE; Blough, BE; Carroll, FI; de Moura, FB; Kohut, SJ; Mello, NK, 2020) | 0.56 |
| "037) had significant dose-response relationships with increased PR of MetS." | ( The interaction effects of smoking and polycyclic aromatic hydrocarbons exposure on the prevalence of metabolic syndrome in coke oven workers. Dong, J; Fu, Y; Li, Q; Li, X; Nie, J; Pan, B; Yang, A; Yang, J; Zhang, B; Zhao, X, 2020) | 0.56 |
| "We combed and analyzed the research situation of health food dosage forms and effects,the functional factors of TCM functional soft candy,gelatin,sweetener,production process,and quality evaluation,etc." | ( [Research progress on functional soft candy of traditional Chinese medicine]. Chen, DZ; Fan, J; Li, HJ; Luan, N; Sheng, K; Wang, YH, 2019) | 0.51 |
| "5 mg/kg) under fixed and progressive ratio schedules, dose-response testing, extinction and cue-induced drug-seeking." | ( Maternal immune activation is associated with a lower number of dopamine receptor 3-expressing granulocytes with no alterations in cocaine reward, resistance to extinction or cue-induced reinstatement. Ambrosio, E; Borcel, É; Higuera-Matas, A; Santos-Toscano, R; Ucha, M, 2020) | 0.56 |
| ") did not induce significant hyperactivity itself, but significantly potentiated cocaine-induced hyperactivity on Days 4 to 7 after the repeated daily dosing of the drug." | ( Effects of Cebranopadol on Cocaine-induced Hyperactivity and Cocaine Pharmacokinetics in Rats. Shang, L; Wei, H; Zhan, CG; Zheng, F, 2020) | 0.56 |
| " The objective of this study was to evaluate the efficacy of daily dosing of mirtazapine on cocaine-induced locomotor activity and sensitization in naive female rats compared to male rats." | ( Mirtazapine reduces the expression of cocaine-induced locomotor sensitization in male and female Wistar rats. Barbosa-Méndez, S; Osorio-Santiago, KL; Salazar-Juárez, A, 2020) | 0.56 |
| "Male and female Wistar rats were daily dosed with 10 mg/kg of cocaine." | ( Mirtazapine reduces the expression of cocaine-induced locomotor sensitization in male and female Wistar rats. Barbosa-Méndez, S; Osorio-Santiago, KL; Salazar-Juárez, A, 2020) | 0.56 |
| "We aimed to investigate the dose-response relationship between various PAH metabolites and workers' neurobehavioral changes and to explore whether mitochondrial DNA copy number (mtDNAcn) can be used as a potential biomarker to reflect changes in neurobehavioral behavior." | ( Urinary polycyclic aromatic hydrocarbon metabolites, peripheral blood mitochondrial DNA copy number, and neurobehavioral function in coke oven workers. Cao, X; Du, J; Li, J; Nie, J; Pan, B; Yang, J, 2020) | 0.56 |
| " The dose-response relationships were evaluated using restricted cubic spline models." | ( Urinary polycyclic aromatic hydrocarbon metabolites, peripheral blood mitochondrial DNA copy number, and neurobehavioral function in coke oven workers. Cao, X; Du, J; Li, J; Nie, J; Pan, B; Yang, J, 2020) | 0.56 |
| "We found dose-response relationships between urinary 2-hydroxynaphthalene (2-OH Nap), sum of PAH metabolites (Ʃ -OH PAHs) and total digit span (DSP), backward digit span (DSPB), forward digit span (DSPF) and mtDNAcn." | ( Urinary polycyclic aromatic hydrocarbon metabolites, peripheral blood mitochondrial DNA copy number, and neurobehavioral function in coke oven workers. Cao, X; Du, J; Li, J; Nie, J; Pan, B; Yang, J, 2020) | 0.56 |
| " Some studies report that dosing of melatonin decreases cocaine-induced locomotor activity and cocaine self-administration and that luzindole, an MT1, and MT2 melatonin receptor antagonist, blocks the melatonin-dependent decrease in cocaine-induced locomotor activity." | ( Melatonin decreases cocaine-induced locomotor sensitization and cocaine-conditioned place preference in rats. Barbosa-Méndez, S; Becerril-Villanueva, E; Pérez-Sánchez, G; Salazar-Juárez, A, 2021) | 0.62 |
| " Cannabis use-MH data are consistent with causal relationships in the forward direction and include dose-response and temporal-sequential relationships." | ( Co-occurrence across time and space of drug- and cannabinoid- exposure and adverse mental health outcomes in the National Survey of Drug Use and Health: combined geotemporospatial and causal inference analysis. Hulse, GK; Reece, AS, 2020) | 0.56 |
| " Dose-response curves for MDPV were generated under FR5 and progressive ratio (PR) schedules of reinforcement." | ( MDPV self-administration in female rats: influence of reinforcement history. Collins, GT; Doyle, MR; Rice, KC; Sulima, A, 2021) | 0.62 |
| " These data indicate that functional connectivity between regions involved in motor, reward, and cognitive processing differed between subjects with recent histories of cocaine self-administration and controls; in dACC, connectivity appears to be related to cumulative cocaine dosage during chronic exposure." | ( Effects of long-term cocaine self-administration on brain resting-state functional connectivity in nonhuman primates. Bergman, J; Brown, K; Gillis, TE; Kangas, BD; Kaufman, MJ; Kohut, SJ; Mintzopoulos, D; Rohan, ML; Shields, H, 2020) | 0.56 |
| ") using a cumulative dosing procedure." | ( Intermittent dietary supplementation with fish oil prevents high fat diet-induced enhanced sensitivity to dopaminergic drugs. Beltran, NM; Cruz, B; Echeverri Alegre, JI; Galindo, KI; Hernandez-Casner, C; Ramos, J; Serafine, KM, 2021) | 0.62 |
| ", MDPV, αPVP, MCAT, and methylone) with a range of pharmacological effects at dopamine and serotonin transporters were compared to cocaine and MDMA using dose-response analysis under a simple FR schedule and behavioral economic procedures that generated demand curves for two doses of each drug." | ( Reinforcing effects of synthetic cathinones in rhesus monkeys: Dose-response and behavioral economic analyses. Bergman, J; de Moura, FB; Kohut, SJ; Paronis, CA; Prisinzano, TE; Sherwood, A, 2021) | 0.62 |
| " The results of these models consistently suggested the negative dose-response relationships of urinary 1-hydroxynaphthalene (1-OHNa), antimony (Sb), and molybdenum (Mo) with mLRR-Y." | ( Effects of polycyclic aromatic hydrocarbons and multiple metals co-exposure on the mosaic loss of chromosome Y in peripheral blood. Bai, Y; Feng, Y; Fu, M; Guan, X; Guo, H; He, M; Jie, J; Li, G; Li, H; Li, M; Meng, H; Wang, C; Wei, W; Zhang, X, 2021) | 0.62 |
| "The aim was to explore the dose-response relationship between occupational polycyclic aromatic hydrocarbons (PAHs) exposure and mitochondrial damage in coke oven plants workers." | ( Benchmark dose analysis for PAHs hydroxyl metabolites in urine based on mitochondrial damage of peripheral blood leucocytes in coke oven workers in China. Cheng, S; Duan, X; Shi, L; Wang, P; Wang, S; Wang, W; Yang, Y; Zhang, H; Zou, K, 2021) | 0.62 |
| " There is a dose-response relationship between 1-hydroxypyrene, 3-hydroxyphenanthrene and mitochondrial DNA damage." | ( Benchmark dose analysis for PAHs hydroxyl metabolites in urine based on mitochondrial damage of peripheral blood leucocytes in coke oven workers in China. Cheng, S; Duan, X; Shi, L; Wang, P; Wang, S; Wang, W; Yang, Y; Zhang, H; Zou, K, 2021) | 0.62 |
| " After determining a cocaine dose-response curve (0." | ( Chronic levetiracetam (Keppra®) treatment increases the reinforcing strength of cocaine in rhesus monkeys. Czoty, PW; Gould, RW; Nader, MA; O'Donovan, CA, 2021) | 0.62 |
| " Utilizing a cocaine intravenous self-administration (IVSA) assay in Fmr1 knockout (KO) and wild-type (WT) littermate mice, we find that, despite normal acquisition and extinction learning, Fmr1 KO mice fail to make a normal upward shift in responding during dose-response testing." | ( The fragile X mental retardation protein promotes adjustments in cocaine self-administration that preserve reinforcement level. Davis, MC; Guo, Y; Huebschman, JL; Smith, LN; Tovar Pensa, C, 2021) | 0.62 |
| " Herein, we examined the capacity of single oral dosing with everolimus, an FDA-approved inhibitor of the PI3K/Akt effector mTOR, to reduce incubated cocaine-craving and reverse incubation-associated changes in vmPFC kinase activity and mGlu expression." | ( Preclinical evidence to support repurposing everolimus for craving reduction during protracted drug withdrawal. Barger, BD; Chiu, AS; Elias, KN; Fabella, AM; Holder, KN; Huerta Sanchez, LL; Jimenez Chavez, CL; Kang, MC; Kippin, TE; Shin, CB; Szumlinski, KK, 2021) | 0.62 |
| " Thus, the objective of this study was to determine if dosing of mirtazapine in an enriched housing environment enhanced the mirtazapine-induced decrease on the induction and expression of cocaine-induced locomotor sensitization." | ( Mirtazapine-induced decrease in cocaine sensitization is enhanced by environmental enrichment in rats. Barbosa-Méndez, S; López-Morado, C; Salazar-Juárez, A, 2021) | 0.62 |
| " Both Sch 23390 and haloperidol attenuated the discrimination of low MDPV doses and essentially shifted the dose-response curve to the right but failed to block discrimination of the training dose." | ( Characterization of 3,4-methylenedioxypyrovalerone discrimination in female Sprague-Dawley rats. Baker, LE; Cargile, KJ; Lunn, JA; Thomas, AM, 2021) | 0.62 |
| " Here we show that systemic administration of ibudilast dose-dependently reduced cocaine self-administration under fixed- and progressive-ratio reinforcement schedules in rats and shifted cocaine dose-response curves downward." | ( Ibudilast attenuates cocaine self-administration and prime- and cue-induced reinstatement of cocaine seeking in rats. Friedman, V; Hu, M; Kelly, TJ; Liu, QS; Liu, X; Mu, L; Yu, H; Zhao, L, 2021) | 0.62 |
| " Color removal efficiency of 80-90% along with COD removal efficiency of 40-50% was observed within 30 min by 120 g/L dosage of the adsorbent." | ( Application of coke breeze for removal of colour from coke plant wastewater. Banerjee, SK; Bhunia, P; Biswas, P; Ghosh, R; Ghosh, TK; Kadukar, S; Sarkar, S, 2022) | 0.72 |
| " Here, we investigated the effects of an escalating cocaine dosing schedule on vH CA1 excitatory transmission by measuring place preference and recording excitatory postsynaptic currents (EPSCs) at three different withdrawal time points: withdrawal day (WD) 2, 9 or 28." | ( Withdrawal from cocaine conditioning progressively alters AMPA receptor-mediated transmission in the ventral hippocampus. Preston, CJ; Wagner, JJ, 2022) | 0.72 |
| " We also found correlations between significant ROI and impulsivity, onset age of cocaine use and weekly dosage with Viso-NODDI." | ( Neurite orientation dispersion and density imaging in cocaine use disorder. Garza-Villarreal, EA; Ingalhalikar, M; Rasgado-Toledo, J; Shah, A, 2022) | 0.72 |
| "Our study is a cross-sectional dose-response study." | ( Dose-response relationship between urinary PAH metabolites and blood viscosity among coke oven workers: a cross-sectional study. Liu, C; Nie, J; Wang, H; Wu, M; Yang, J, 2021) | 0.62 |
| " Microinjections of TFB-TBOA into the NAc, but not the ventral tegmental area (VTA), or dorsal striatum (DS), dose-dependently inhibited cocaine self-administration under fixed-ratio and progressive-ratio (PR) reinforcement schedules, shifted the cocaine dose-response curve downward, and inhibited intracranial BSR." | ( Elevation of Extracellular Glutamate by Blockade of Astrocyte Glutamate Transporters Inhibits Cocaine Reinforcement in Rats via a NMDA-GluN2B Receptor Mechanism. Bi, GH; Gardner, EL; He, Y; Hempel, BJ; Xi, ZX; Yang, HJ; Zhang, HY, 2022) | 0.72 |
| "To explore sex differences and dose-response relationships between nine urinary polycyclic aromatic hydrocarbon (PAH) metabolites and neutrophil-lymphocyte ratio (NLR), platelet-lymphocyte ratio (PLR) and complete blood counts among coke oven workers." | ( Dose-response relationships between polycyclic aromatic hydrocarbon exposure and blood cell counts among coke oven workers: a sex-stratified analysis. Fu, M; Liu, C; Nie, J; Wang, H; Wu, M, 2021) | 0.62 |
| "General linear models, p values for trend tests and natural cubic spline models were used to explore the dose-response relationships between nine urinary PAH metabolites and NLR, PLR and complete blood counts." | ( Dose-response relationships between polycyclic aromatic hydrocarbon exposure and blood cell counts among coke oven workers: a sex-stratified analysis. Fu, M; Liu, C; Nie, J; Wang, H; Wu, M, 2021) | 0.62 |
| " The ability of acute versus chronic drug treatment to differentially affect human cocaine self-administration was not determined because buprenorphine was the only pretreatment drug that was assessed under both acute and chronic dosing regimens." | ( Clinical neuropharmacology of cocaine reinforcement: A narrative review of human laboratory self-administration studies. Lile, JA; Regnier, SD; Rush, CR; Stoops, WW, 2022) | 0.72 |
| " Furthermore, the dose-response relationship analysis revealed a nonlinear U-shape curve of TRIM36 or RASSF1a methylation in combined population, which led to determination of the threshold of health risk." | ( CpG site-specific methylation as epi-biomarkers for the prediction of health risk in PAHs-exposed populations. Aschner, M; Chen, L; Chen, S; Chen, W; Dong, G; Duan, H; Guo, P; He, Z; Li, D; Ma, L; Niu, Y; Wang, Q; Xiao, Y; Xing, X; Ye, L; Yu, D; Zeng, X; Zheng, Y, 2022) | 0.72 |
| " Additional factors associated with decreased drug taking include intermittent dosing for dopamine antagonists and use of progressive-ratio schedules for lorcaserin." | ( Biphasic reward effects are characteristic of both lorcaserin and drugs of abuse: implications for treatment of substance use disorders. Burnell, K; De, A; Grasing, KW, 2022) | 0.72 |
| "32 mg/kg/inf cocaine, after which full dose-response curves for MDPV (0." | ( Interactions between impulsivity and MDPV self-administration in rats. Abbott, MS; Collins, GT; Doyle, MR; Maguire, DR; Rice, KC; Seaman, RW, 2022) | 0.72 |
| " We found that systemic administration of PIMSR dose-dependently inhibited cocaine self-administration under fixed-ratio (FR5), but not FR1, reinforcement, shifted the cocaine self-administration dose-response curve downward, decreased incentive motivation to seek cocaine under progressive-ratio reinforcement, and reduced cue-induced reinstatement of cocaine seeking." | ( Therapeutic potential of PIMSR, a novel CB1 receptor neutral antagonist, for cocaine use disorder: evidence from preclinical research. Bi, GH; Galaj, E; Gardner, EL; Hempel, B; Klein, B; Moore, A; Seltzman, HH; Xi, ZX, 2022) | 0.72 |
| " The dose-response relationships were evaluated using restricted cubic spline models." | ( Urinary polycyclic aromatic hydrocarbon metabolites, plasma p-tau231 and mild cognitive impairment in coke oven workers. Bai, Q; Du, J; Fu, M; Nie, J; Niu, Q; Wang, H, 2022) | 0.72 |
| " We recently reported a series of preclinical studies that showed that dosing of mirtazapine, a noradrenergic and serotonergic antidepressant, in male and female Wistar rats decreased cocaine-induced locomotor activity and attenuated the induction and expression of cocaine-induced locomotor sensitization." | ( Mirtazapine attenuates the cocaine-induced locomotor sensitization in male and female C57BL/6J and BALBA/cJ mouse. Méndez, SB; Salazar-Juárez, A, 2023) | 0.91 |
| "Male and female BALB/cJ and C57BL/6J inbred mice (20-25 g) were daily dosed with 10 mg/kg of cocaine during the induction and expression of locomotor sensitization." | ( Mirtazapine attenuates the cocaine-induced locomotor sensitization in male and female C57BL/6J and BALBA/cJ mouse. Méndez, SB; Salazar-Juárez, A, 2023) | 0.91 |
| " The average concentration of cocaine detected in cardiac cases (900 ng/mL) was considerably lower than that detected in cases where acute (19,100 ng/mL) or chronic/binge (6,200 ng/mL) dosing was evident." | ( From Bumps to Binges: Overview of Deaths Associated with Cocaine in England, Wales and Northern Ireland (2000-2019). Copeland, C; Rock, K; Rooney, B; Sobiecka, P, 2023) | 0.91 |
| " Cocaine was noted as accumulating in zebrafish eyes, possibly due to melanin binding, and causing dose-response cardiac effects in both embryos and adults." | ( Zebrafish (Danio rerio) as a model to assess the effects of cocaine as a drug of abuse and its environmental implications. Correia, FV; de Farias Araujo, G; Maciel-Magalhães, M; Medeiros, RJ; Saggioro, EM, 2023) | 0.91 |
| "We identified three themes related to patients' internal relationships to methadone: patients (1) viewed methadone as a bridge to opioid-free recovery, (2) believed that long-term methadone damages the body, and (3) felt that methadone increases craving for cocaine; and three themes related to their external relationships with opioid treatment programs and society at large: patients (4) viewed daily dosing as burdensome, (5) feared methadone inaccessibility could trigger relapse, and (6) experienced stigma from friends, family, and peers." | ( Transitioning off methadone: A qualitative study exploring why patients discontinue methadone treatment for opioid use disorder. Chander, G; Pytell, JD; Stoller, KB; Thakrar, AP; Walters, V; Weiss, RD, 2023) | 0.91 |
| " Depleting the microbiome by antibiotic treatment in males revealed increased infusions for CC04 during a cocaine intravenous self-administration dose-response curve." | ( The microbial community dynamics of cocaine sensitization in two behaviorally divergent strains of collaborative cross mice. Bubier, JA; Chesler, EJ; Monroy Hernandez, C; Nguyen, H; Tarantino, LM; Tran, TDB; Weinstock, GM; Wright, S; Zhou, Y, 2023) | 0.91 |
| " Primary outcomes were retention in treatment at 1, 3, 6, 12, and 24 months, treatment adherence (measured through doses taken as prescribed, dosing visits attended, and biological measures), or extra-medical opioid use (measured by urinalysis and self-report)." | ( Buprenorphine versus methadone for the treatment of opioid dependence: a systematic review and meta-analysis of randomised and observational studies. Clark, B; Degenhardt, L; Farrell, M; Hickman, M; Kimber, J; Larance, B; Leppan, O; Macpherson, G; Martino-Burke, D; Nielsen, S; Zahra, E, 2023) | 0.91 |
| "When treating opioid users with polydrug drug use, special attention should be paid to dosing when in opioid agonist methadone/buprenorphine treatment and to the presence of physical pain." | ( Predictors and motives of polydrug use in opioid users. A narrative review. Pierce, M; van Amsterdam, J; van den Brink, W, 2023) | 0.91 |
| " After adjusting for age, sex, smoking, drinking and BMI, generalised linear model revealed dose-response associations between COEs and T-AOC, RTL and mtDNAcn, respectively." | ( Chain-mediating effect of interaction between telomeres and mitochondria under oxidative stress in coke oven workers. Duan, X; Fan, Y; Gu, Z; Niu, Z; Sun, J; Wang, W; Yan, Z; Yang, Y; Yao, W; Zhao, X, 2023) | 0.91 |
| " For experiments, 1-3, female rats were daily dosed with 10 mg/kg of cocaine during the 10 days of induction and expression of locomotor sensitization." | ( Estradiol enhances the mirtazapine effects on the expression of cocaine-induced locomotor sensitization in female rats. Barbosa-Méndez, S; Salazar-Juárez, A, 2023) | 0.91 |
| "1mg/kg/injection) dose-response curves were determined." | ( A comparison of the reinforcing strength of cocaethylene and cocaine in monkeys responding under progressive-ratio and concurrent choice schedules of reinforcement. Allen, MI; Johnson, BN; Nader, MA, 2023) | 0.91 |
| "The cocaine unit dose-response function is an inverted U with the ascending and descending limbs representing the positive and rate limiting cocaine effects, respectively." | ( The ascending limb of the cocaine unit dose-response function in rats as an experimental artifact. Desai, JN; Norman, AB; Tron Esqueda, LE, 2023) | 0.91 |
| " The screening and the subsequent dosage revealed the following substances: cocaine (86 ng/mL), benzoylecgonine (383 ng/mL), cocaethylene (17 ng/mL), ecgonine methyl ester (130 ng/mL), caffeine, cuscohygrine, cinnamoylcocaine and synephrine." | ( Mariani wine: What's really in it? Analysis of the most popular tonic drink of the 19th century after 100 years of storage. Arbouche, N; de Lestrange, A; Kintz, P; Raul, JS, 2024) | 1.44 |
| " We explore dosing regimens of dopamine or cocaine to simulate acute or chronic exposure." | ( Reactive Oxygen Species Mediate Transcriptional Responses to Dopamine and Cocaine in Human Cerebral Organoids. Keung, AJ; Rudibaugh, TT; Stuppy, SR, 2023) | 0.91 |
| Item | Process | Frequency |
|---|---|---|
| Biscuits | core-ingredient | 1 |
| Biscuits and cakes | core-ingredient | 1 |
| Sweet snacks | core-ingredient | 1 |
| Snacks | core-ingredient | 1 |
| Role | Description |
|---|---|
| local anaesthetic | Any member of a group of drugs that reversibly inhibit the propagation of signals along nerves. Wide variations in potency, stability, toxicity, water-solubility and duration of action determine the route used for administration, e.g. topical, intravenous, epidural or spinal block. |
| central nervous system stimulant | Any drug that enhances the activity of the central nervous system. |
| sodium channel blocker | An agent that inhibits sodium influx through cell membranes. |
| adrenergic uptake inhibitor | Adrenergic uptake inhibitors are drugs that block the transport of adrenergic transmitters into axon terminals or into storage vesicles within terminals. The tricyclic antidepressants and amphetamines are among the therapeutically important drugs that may act via inhibition of adrenergic transport. Many of these drugs also block transport of serotonin. |
| dopamine uptake inhibitor | A dopaminergic agent that blocks the transport of dopamine into axon terminals or into storage vesicles within terminals. Most of the adrenergic uptake inhibitors also inhibit dopamine uptake. |
| serotonin uptake inhibitor | A compound that specifically inhibits the reuptake of serotonin in the brain. This increases the serotonin concentration in the synaptic cleft which then activates serotonin receptors to a greater extent. |
| sympathomimetic agent | A drug that mimics the effects of stimulating postganglionic adrenergic sympathetic nerves. Included in this class are drugs that directly stimulate adrenergic receptors and drugs that act indirectly by provoking the release of adrenergic transmitters. |
| vasoconstrictor agent | Drug used to cause constriction of the blood vessels. |
| xenobiotic | A xenobiotic (Greek, xenos "foreign"; bios "life") is a compound that is foreign to a living organism. Principal xenobiotics include: drugs, carcinogens and various compounds that have been introduced into the environment by artificial means. |
| environmental contaminant | Any minor or unwanted substance introduced into the environment that can have undesired effects. |
| plant metabolite | Any eukaryotic metabolite produced during a metabolic reaction in plants, the kingdom that include flowering plants, conifers and other gymnosperms. |
| mouse metabolite | Any mammalian metabolite produced during a metabolic reaction in a mouse (Mus musculus). |
| [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 |
|---|---|
| tropane alkaloid | |
| methyl ester | Any carboxylic ester resulting from the formal condensation of a carboxy group with methanol. |
| benzoate ester | Esters of benzoic acid or substituted benzoic acids. |
| tertiary amino compound | A compound formally derived from ammonia by replacing three hydrogen atoms by organyl groups. |
| [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 |
|---|---|---|
| Metabolism | 1496 | 1108 |
| Biological oxidations | 150 | 276 |
| Phase I - Functionalization of compounds | 69 | 175 |
| Cocaine Action Pathway | 31 | 11 |
| Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| ATAD5 protein, partial | Homo sapiens (human) | Potency | 23.0999 | 0.0041 | 10.8903 | 31.5287 | AID504467 |
| Microtubule-associated protein tau | Homo sapiens (human) | Potency | 8.9125 | 0.1800 | 13.5574 | 39.8107 | AID1468 |
| geminin | Homo sapiens (human) | Potency | 0.2909 | 0.0046 | 11.3741 | 33.4983 | AID624296 |
| ATP-dependent phosphofructokinase | Trypanosoma brucei brucei TREU927 | Potency | 12.5893 | 0.0601 | 10.7453 | 37.9330 | AID492961 |
| [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) |
|---|---|---|---|---|---|---|---|
| Chain A, CHIMERA OF IG KAPPA CHAIN: HUMAN CONSTANT REGION AND MOUSE VARIABLE REGION | synthetic construct | Kd | 0.4000 | 0.4000 | 0.4000 | 0.4000 | AID977611 |
| Chain B, CHIMERA OF IG GAMMA-1 CHAIN: HUMAN CONSTANT REGION AND MOUSE VARIABLE REGION | synthetic construct | Kd | 0.4000 | 0.4000 | 0.4000 | 0.4000 | AID977611 |
| Chain H, Fab M82G2, Heavy chain | Mus musculus (house mouse) | Kd | 0.1400 | 0.1400 | 0.1400 | 0.1400 | AID977611 |
| Chain L, Fab M82G2, Light chain | Mus musculus (house mouse) | Kd | 0.1400 | 0.1400 | 0.1400 | 0.1400 | AID977611 |
| Chain H, Fab M82g2, Heavy Chain | Mus musculus (house mouse) | Kd | 0.1400 | 0.1400 | 0.1400 | 0.1400 | AID977611 |
| Chain L, Fab M82g2, Light Chain | Mus musculus (house mouse) | Kd | 0.1400 | 0.1400 | 0.1400 | 0.1400 | AID977611 |
| [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) |
|---|---|---|---|---|---|---|---|
| Sodium-dependent serotonin transporter | Rattus norvegicus (Norway rat) | Km | 0.2000 | 0.2000 | 0.2000 | 0.2000 | AID386308 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID504749 | qHTS profiling for inhibitors of Plasmodium falciparum proliferation | 2011 | Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043 | Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets. |
| AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
| AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5 | Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
| AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
| AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
| AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5 | Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
| AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
| AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
| AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5 | Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
| AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
| AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | |||
| AID504812 | Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7 | A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
| AID504810 | Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7 | A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
| AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
| AID576612 | Inhibition of human ERG | 2011 | European journal of medicinal chemistry, Feb, Volume: 46, Issue:2 | Predicting hERG activities of compounds from their 3D structures: development and evaluation of a global descriptors based QSAR model. |
| AID493017 | Wombat Data for BeliefDocking | 1991 | Journal of medicinal chemistry, Mar, Volume: 34, Issue:3 | Synthesis and ligand binding of cocaine isomers at the cocaine receptor. |
| AID386308 | Inhibition of [3H]5HT transport at rat SERT expressed in pig LLC-PK1 cells at 5 uM | 2007 | The Journal of biological chemistry, Oct-05, Volume: 282, Issue:40 | Ibogaine, a noncompetitive inhibitor of serotonin transport, acts by stabilizing the cytoplasm-facing state of the transporter. |
| AID540218 | Clearance in monkey after iv administration | 2005 | Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7 | Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure. |
| AID232435 | Ratio of inhibition of reuptake of norepinephrine to 5-hydroxytryptamine | 2000 | Journal of medicinal chemistry, May-18, Volume: 43, Issue:10 | Novel conformationally constrained tropane analogues by 6-endo-trig radical cyclization and stille coupling - switch of activity toward the serotonin and/or norepinephrine transporter. |
| AID192998 | Number of animals(n) completing 20 responses on either lever out of the number of animals tested (N) at dose 5 mg/kg evaluated by dose-response tests in trained rats; n/N=7/7 | 1992 | Journal of medicinal chemistry, Dec-11, Volume: 35, Issue:25 | Structure-activity relationship studies of cocaine: replacement of the C-2 ester group by vinyl argues against H-bonding and provides an esterase-resistant, high-affinity cocaine analogue. |
| AID196434 | Inhibitory concentration for [3H]-dopamine uptake by striatal membrane preparations in presence of 50 nM compound 43 | 2001 | Bioorganic & medicinal chemistry letters, Feb-26, Volume: 11, Issue:4 | Pharmacophore-based discovery, synthesis, and biological evaluation of 4-phenyl-1-arylalkyl piperidines as dopamine transporter inhibitors. |
| AID444520 | Inhibition of [3H]dopamine reuptake at human DAT expressed in HEK293 cells | 2009 | Journal of medicinal chemistry, Nov-12, Volume: 52, Issue:21 | Synthesis and biological evaluation of bupropion analogues as potential pharmacotherapies for cocaine addiction. |
| AID174372 | The compound was evaluated for its behavioral activity i.e., locomotor arousal in rat for a dose of 3 mg/kg in time interval of 2 hours | 1994 | Journal of medicinal chemistry, May-27, Volume: 37, Issue:11 | N-omega-fluoroalkyl analogs of (1R)-2 beta-carbomethoxy-3 beta-(4-iodophenyl)-tropane (beta-CIT): radiotracers for positron emission tomography and single photon emission computed tomography imaging of dopamine transporters. |
| AID360439 | Displacement of [3H]CFT from human DAT expressed in HEK293 cells | 2007 | The Journal of biological chemistry, Mar-23, Volume: 282, Issue:12 | Localization of cocaine analog [125I]RTI 82 irreversible binding to transmembrane domain 6 of the dopamine transporter. |
| AID204693 | Inhibition of reuptake of [3H]5-HT at serotonin transporter | 2000 | Journal of medicinal chemistry, May-18, Volume: 43, Issue:10 | Novel conformationally constrained tropane analogues by 6-endo-trig radical cyclization and stille coupling - switch of activity toward the serotonin and/or norepinephrine transporter. |
| AID147757 | Compound was tested for inhibition of [3H]NE binding to norepinephrine transporter HEK cells | 2003 | Bioorganic & medicinal chemistry letters, Jul-07, Volume: 13, Issue:13 | Bivalent biogenic amine reuptake inhibitors. |
| AID242175 | Inhibition of [3H]paroxetine binding to rat cortex serotonin transporter | 2005 | Journal of medicinal chemistry, Jun-02, Volume: 48, Issue:11 | Synthesis and monoamine transporter binding properties of 3alpha-(substituted phenyl)nortropane-2beta-carboxylic acid methyl esters. Norepinephrine transporter selective compounds. |
| AID64995 | Inhibition of binding of [3H]WIN-35 428 to (DAT) dopamine transporter in rat striatum | 2003 | Bioorganic & medicinal chemistry letters, May-05, Volume: 13, Issue:9 | Design, synthesis, and activity of novel cis- and trans-3,6-disubstituted pyran biomimetics of 3,6-disubstituted piperidine as potential ligands for the dopamine transporter. |
| AID275443 | Displacement of [125I]RTI-55 from human SERT expressing HEK293 cells | 2007 | Journal of medicinal chemistry, Jan-25, Volume: 50, Issue:2 | Slow-onset, long-duration, alkyl analogues of methylphenidate with enhanced selectivity for the dopamine transporter. |
| AID7946 | Percentage of tracer or metabolite (unchanged) in baboon plasma at 5 min after injection of the compound | 1992 | Journal of medicinal chemistry, Jun-12, Volume: 35, Issue:12 | Synthesis of carbon-11 labeled iodinated cocaine derivatives and their distribution in baboon brain measured using positron emission tomography. |
| AID232635 | Inhibition of reuptake of norepinephrine compared to dopamine. | 2003 | Bioorganic & medicinal chemistry letters, Oct-20, Volume: 13, Issue:20 | Synthesis and pharmacological evaluation of (Z)-9-(heteroarylmethylene)-7-azatricyclo[4.3.1.0(3,7)]decanes: thiophene analogues as potent norepinephrine transporter inhibitors. |
| AID184425 | To inhibit high affinity uptake of [3H]5-HT into nerve endings (synaptosomes) prepared from various regions of the rat brain. | 2000 | Journal of medicinal chemistry, Aug-24, Volume: 43, Issue:17 | Chemical synthesis and pharmacology of 6- and 7-hydroxylated 2-carbomethoxy-3-(p-tolyl)tropanes: antagonism of cocaine's locomotor stimulant effects. |
| AID111612 | Percent change from vehicle in locomotor activity in mice at 5.6 mg/kg (ip) in 4 h | 2004 | Journal of medicinal chemistry, Jan-15, Volume: 47, Issue:2 | Synthesis, monoamine transporter binding properties, and behavioral pharmacology of a series of 3beta-(substituted phenyl)-2beta-(3'-substituted isoxazol-5-yl)tropanes. |
| AID229277 | Ratio of IC50 of 5-HT (serotonin transporter)to IC50 of DA(dopamine transporter) | 1999 | Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23 | Synthesis and pharmacology of site-specific cocaine abuse treatment agents: 2-substituted-6-amino-5-phenylbicyclo[2.2.2]octanes. |
| AID220760 | Percentage unmetabolized in baboon plasma at 30 min after administration. | 1992 | Journal of medicinal chemistry, Jun-12, Volume: 35, Issue:12 | Synthesis of carbon-11 labeled iodinated cocaine derivatives and their distribution in baboon brain measured using positron emission tomography. |
| AID65637 | Binding affinity Sprague-Dawley rats using [3H]WIN-35428 ligand | 1999 | Journal of medicinal chemistry, Oct-21, Volume: 42, Issue:21 | Structure-activity relationships at the monoamine transporters and sigma receptors for a novel series of 9-[3-(cis-3, 5-dimethyl-1-piperazinyl)propyl]carbazole (rimcazole) analogues. |
| AID204370 | Inhibition of 0.2 nM [3H]paroxetine binding to Serotonin transporter | 2000 | Bioorganic & medicinal chemistry letters, Nov-06, Volume: 10, Issue:21 | 3alpha-(4-Substituted phenyl)nortropane-2beta-carboxylic acid methyl esters show selective binding at the norepinephrine transporter. |
| AID195345 | Mean responses per minute at dose 10 mg/kg evaluated by temporal tests in trained rats(post injection interval 5 min) | 1992 | Journal of medicinal chemistry, Dec-11, Volume: 35, Issue:25 | Structure-activity relationship studies of cocaine: replacement of the C-2 ester group by vinyl argues against H-bonding and provides an esterase-resistant, high-affinity cocaine analogue. |
| AID174459 | Percent response at dose 10 mg/kg evaluated by temporal tests in trained rats(post injection interval 120 min) | 1992 | Journal of medicinal chemistry, Dec-11, Volume: 35, Issue:25 | Structure-activity relationship studies of cocaine: replacement of the C-2 ester group by vinyl argues against H-bonding and provides an esterase-resistant, high-affinity cocaine analogue. |
| AID65506 | ability to displace [3H]- Mazindol binding to cocaine binding sites on Dopamine transporter of rat striatal membranes | 2000 | Bioorganic & medicinal chemistry letters, Jul-03, Volume: 10, Issue:13 | An enantioselective synthesis and biobehavioral evaluation of 7-fluoro-3-(p-fluorophenyl)-2-propyltropanes. |
| AID64690 | Binding affinity for compound at site labeled by [3H]BTCP (1-[1-(2-benxo[b]thienyl)cyclohexyl]piperidine) in rat forebrain. | 1993 | Journal of medicinal chemistry, Apr-30, Volume: 36, Issue:9 | Synthesis and biological evaluation of 1-[1-(2-benzo[b]thienyl)cyclohexyl]piperidine homologues at dopamine-uptake and phencyclidine- and sigma-binding sites. |
| AID64857 | Displacement of 0.5 nM [3H]WIN-35248 from Dopamine transporter | 2000 | Bioorganic & medicinal chemistry letters, Nov-06, Volume: 10, Issue:21 | 3alpha-(4-Substituted phenyl)nortropane-2beta-carboxylic acid methyl esters show selective binding at the norepinephrine transporter. |
| AID204378 | Inhibitory activity against Serotonin transporter using 0.2 nM [3H]paroxetine as radioligand | 1997 | Journal of medicinal chemistry, Apr-11, Volume: 40, Issue:8 | Synthesis and transporter binding properties of 2,3-diphenyltropane stereoisomers. Comparison to 3beta-phenyltropane-2beta-carboxylic acid esters. |
| AID204866 | Ratio of IC50(5-HT) to the IC50(DA) | 1992 | Journal of medicinal chemistry, Jun-26, Volume: 35, Issue:13 | Isopropyl and phenyl esters of 3 beta-(4-substituted phenyl)tropan-2 beta-carboxylic acids. Potent and selective compounds for the dopamine transporter. |
| AID204233 | Binding affinity was evaluated by measuring inhibiting the binding of [3H]citalopram to Serotonin transporter in rat brain tissue | 2001 | Bioorganic & medicinal chemistry letters, Sep-03, Volume: 11, Issue:17 | Rational design and synthesis of novel 2,5-disubstituted cis- and trans-piperidine derivatives exhibiting differential activity for the dopamine transporter. |
| AID425652 | Total body clearance in human | 2009 | Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15 | Physicochemical determinants of human renal clearance. |
| AID65353 | Displacement of [3H]WIN-35428 from dopamine transporter (DAT) in Rat Caudate Putamen | 1997 | Journal of medicinal chemistry, Mar-14, Volume: 40, Issue:6 | Synthesis, dopamine transporter affinity, dopamine uptake inhibition, and locomotor stimulant activity of 2-substituted 3 beta-phenyltropane derivatives. |
| AID111611 | Percent change from vehicle in locomotor activity in mice at 5.6 mg/kg (ip) in 3 h | 2004 | Journal of medicinal chemistry, Jan-15, Volume: 47, Issue:2 | Synthesis, monoamine transporter binding properties, and behavioral pharmacology of a series of 3beta-(substituted phenyl)-2beta-(3'-substituted isoxazol-5-yl)tropanes. |
| AID64364 | Inhibition of [3H]dopamine reuptake in HEK293 cells expressing human dopamine transporter | 2000 | Journal of medicinal chemistry, Jan-27, Volume: 43, Issue:2 | Novel 3-aminomethyl- and 4-aminopiperidine analogues of 1-[2-(diphenylmethoxy)ethyl]-4-(3-phenylpropyl)piperazines: synthesis and evaluation as dopamine transporter ligands. |
| AID552081 | Displacement of [3H]citalopram from human SERT expressed in HEK293 cell membrane | 2011 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1 | The synthesis and biological evaluation of 2-(3-methyl or 3-phenylisoxazol-5-yl)-3-aryl-8-thiabicyclo[3.2.1]octanes. |
| AID204371 | In vitro inhibitory activity against radioligand [3H]paroxetine binding to serotonin transporter (5-HTT) in rat midbrain tissue | 1997 | Journal of medicinal chemistry, Nov-21, Volume: 40, Issue:24 | 3 Beta-(4-ethyl-3-iodophenyl)nortropane-2 beta-carboxylic acid methyl ester as a high-affinity selective ligand for the serotonin transporter. |
| AID65184 | Ability to inhibit high affinity uptake of [3H]DA at Dopamine transporter (DAT) using rat brain striatum | 2004 | Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12 | Synthesis, molecular modeling, and biological studies of novel piperidine-based analogues of cocaine: evidence of unfavorable interactions proximal to the 3alpha-position of the piperidine ring. |
| AID111609 | Percent change from vehicle in locomotor activity in mice at 5.6 mg/kg (ip) in 1 h | 2004 | Journal of medicinal chemistry, Jan-15, Volume: 47, Issue:2 | Synthesis, monoamine transporter binding properties, and behavioral pharmacology of a series of 3beta-(substituted phenyl)-2beta-(3'-substituted isoxazol-5-yl)tropanes. |
| AID226487 | Hill coefficient was determined | 1998 | Journal of medicinal chemistry, May-21, Volume: 41, Issue:11 | Chemistry and pharmacology of the piperidine-based analogues of cocaine. Identification of potent DAT inhibitors lacking the tropane skeleton. |
| AID61818 | Compound was evaluated for binding affinity to dopamine transporter using [125I]RTI-55 as a radioligand in HEK cells expressing human transporters. | 2000 | Journal of medicinal chemistry, May-18, Volume: 43, Issue:10 | Novel conformationally constrained tropane analogues by 6-endo-trig radical cyclization and stille coupling - switch of activity toward the serotonin and/or norepinephrine transporter. |
| AID266636 | Displacement of [3H]WIN-35428 from human DAT | 2006 | Journal of medicinal chemistry, Jul-27, Volume: 49, Issue:15 | Synthesis and monoamine transporter binding properties of 2,3-cyclo analogues of 3beta-(4'-aminophenyl)-2beta-tropanemethanol. |
| AID64341 | Compound was evaluated for inhibition of specifically bound [3H]- cocaine (2.7 nM) against Dopamine transporter in cynomolgus monkeys | 1991 | Journal of medicinal chemistry, May, Volume: 34, Issue:5 | Synthesis and receptor binding of N-substituted tropane derivatives. High-affinity ligands for the cocaine receptor. |
| AID1705907 | Toxicity in Swiss Webster mouse assessed as stimulation of ambulatory activity by measuring total distance travelled at 30 mg/kg, ip measured every 5 mins for 2 hrs | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | Structure-activity relationships for a series of (Bis(4-fluorophenyl)methyl)sulfinylethyl-aminopiperidines and -piperidine amines at the dopamine transporter: Bioisosteric replacement of the piperazine improves metabolic stability. |
| AID1443759 | Inhibition of [3H]mazindol binding to recombinant human NET expressed in HEK293 cell membranes preincubated for 10 mins followed by radioligand addition measured after 90 mins by micro beta scintillation counting analysis | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | Scaffold Repurposing of Nucleosides (Adenosine Receptor Agonists): Enhanced Activity at the Human Dopamine and Norepinephrine Sodium Symporters. |
| AID570372 | Displacement of [3H]citalopram from SERT in Sprague-Dawley rat brain membranes | 2010 | ACS medicinal chemistry letters, Oct-10, Volume: 2, Issue:1 | Structure-Activity Relationships at the Monoamine Transporters for a Novel Series of Modafinil (2-[(diphenylmethyl)sulfinyl]acetamide) Analogues. |
| AID204236 | Binding affinity towards serotonin transporter in rat striatum using [3H]citalopram as radioligand | 2003 | Journal of medicinal chemistry, Mar-27, Volume: 46, Issue:7 | High affinity hydroxypiperidine analogues of 4-(2-benzhydryloxyethyl)-1-(4-fluorobenzyl)piperidine for the dopamine transporter: stereospecific interactions in vitro and in vivo. |
| AID111736 | Percent change from vehicle in locomotor activity in mice at 56 mg/kg (ip) in 4 h | 2004 | Journal of medicinal chemistry, Jan-15, Volume: 47, Issue:2 | Synthesis, monoamine transporter binding properties, and behavioral pharmacology of a series of 3beta-(substituted phenyl)-2beta-(3'-substituted isoxazol-5-yl)tropanes. |
| AID261029 | Inhibition of [3H] norepinephrine uptake into human NET expressed in HEK293 cells | 2006 | Journal of medicinal chemistry, Feb-23, Volume: 49, Issue:4 | 1-(4-Methylphenyl)-2-pyrrolidin-1-yl-pentan-1-one (Pyrovalerone) analogues: a promising class of monoamine uptake inhibitors. |
| AID311935 | Partition coefficient, log P of the compound | 2008 | Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2 | Identification of new functional inhibitors of acid sphingomyelinase using a structure-property-activity relation model. |
| AID393256 | Inhibition of [3H]dopamine reuptake at human DAT expressed in HEK cells | 2009 | Bioorganic & medicinal chemistry, Mar-01, Volume: 17, Issue:5 | 2,5-Disubstituted tetrahydrofurans as selective serotonin re-uptake inhibitors. |
| AID275442 | Inhibition of [3H]DA uptake at human DAT expressing HEK293 cells | 2007 | Journal of medicinal chemistry, Jan-25, Volume: 50, Issue:2 | Slow-onset, long-duration, alkyl analogues of methylphenidate with enhanced selectivity for the dopamine transporter. |
| AID64865 | Inhibition of [3H]DA binding to DAT in rat striatal synaptosomes. | 2003 | Journal of medicinal chemistry, Apr-10, Volume: 46, Issue:8 | Synthesis and pharmacology of site specific cocaine abuse treatment agents: 8-substituted isotropane (3-azabicyclo[3.2.1]octane) dopamine uptake inhibitors. |
| AID444518 | Displacement of [125I]RTI55 from cloned human SERT expressed in HEK293 cells | 2009 | Journal of medicinal chemistry, Nov-12, Volume: 52, Issue:21 | Synthesis and biological evaluation of bupropion analogues as potential pharmacotherapies for cocaine addiction. |
| AID65031 | Tested for radioligand [3H]cocaine displacement from dopamine transporter in rat forebrain | 1993 | Journal of medicinal chemistry, Dec-10, Volume: 36, Issue:25 | Further studies of the structure-activity relationships of 1-[1-(2-benzo[b]thienyl)cyclohexyl]piperidine. Synthesis and evaluation of 1-(2-benzo[b]thienyl)-N,N-dialkylcyclohexylamines at dopamine uptake and phencyclidine binding sites. |
| AID228127 | In vitro Ki against [3H]mazindol binding. | 2001 | Bioorganic & medicinal chemistry letters, May-07, Volume: 11, Issue:9 | Pharmacophore-based discovery of 3,4-disubstituted pyrrolidines as a novel class of monoamine transporter inhibitors. |
| AID393257 | Displacement of [125I]RTI55 from human DAT expressed in HEK cells | 2009 | Bioorganic & medicinal chemistry, Mar-01, Volume: 17, Issue:5 | 2,5-Disubstituted tetrahydrofurans as selective serotonin re-uptake inhibitors. |
| AID174368 | The compound was evaluated for its behavioral activity i.e., locomotor arousal in rat for a dose of 1 mg/kg in time interval of 2 hours | 1994 | Journal of medicinal chemistry, May-27, Volume: 37, Issue:11 | N-omega-fluoroalkyl analogs of (1R)-2 beta-carbomethoxy-3 beta-(4-iodophenyl)-tropane (beta-CIT): radiotracers for positron emission tomography and single photon emission computed tomography imaging of dopamine transporters. |
| AID52202 | Inhibition of [3H]cocaine binding to Cocaine receptor in rat striatal membranes | 1998 | Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6 | (-)-3 beta-Substituted ecgonine methyl esters as inhibitors for cocaine binding and dopamine uptake. |
| AID145703 | Binding affinity was evaluated by measuring inhibiting the binding of [3H]nisoxetine to Norepinephrine transporter in rat brain tissue | 2001 | Bioorganic & medicinal chemistry letters, Sep-03, Volume: 11, Issue:17 | Rational design and synthesis of novel 2,5-disubstituted cis- and trans-piperidine derivatives exhibiting differential activity for the dopamine transporter. |
| AID540215 | Volume of distribution at steady state in rat after iv administration | 2005 | Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7 | Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure. |
| AID65480 | In vitro dopamine transporter binding affinity using [3H]WIN-35428 as radioligand was determined | 2003 | Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14 | Structure-activity relationship comparison of (S)-2beta-substituted 3alpha-(bis[4-fluorophenyl]methoxy)tropanes and (R)-2beta-substituted 3beta-(3,4-dichlorophenyl)tropanes at the dopamine transporter. |
| AID226639 | The compound Hill coefficient value determined for WIN-Binding | 1996 | Journal of medicinal chemistry, Mar-15, Volume: 39, Issue:6 | Synthesis and pharmacology of potential cocaine antagonists. 2. Structure-activity relationship studies of aromatic ring-substituted methylphenidate analogs. |
| AID384547 | Binding affinity at SERT | 2008 | Journal of medicinal chemistry, May-08, Volume: 51, Issue:9 | Design and synthesis of 2- and 3-substituted-3-phenylpropyl analogs of 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine and 1-[2-(diphenylmethoxy)ethyl]-4-(3-phenylpropyl)piperazine: role of amino, fluoro, hydroxyl, methoxyl, methyl, m |
| AID266638 | Displacement of [3H]paroxetine from human 5HTT | 2006 | Journal of medicinal chemistry, Jul-27, Volume: 49, Issue:15 | Synthesis and monoamine transporter binding properties of 2,3-cyclo analogues of 3beta-(4'-aminophenyl)-2beta-tropanemethanol. |
| AID232403 | Ratio of Ki at 5-HT transporter and Ki at dopamine transporter. | 2002 | Journal of medicinal chemistry, Jul-18, Volume: 45, Issue:15 | SAR studies of piperidine-based analogues of cocaine. 4. Effect of N-modification and ester replacement. |
| AID145560 | The compound was tested for inhibition of [3H]norepinephrine uptake in HEK cells by expressing cDNA for human norepinephrine transporter | 2000 | Bioorganic & medicinal chemistry letters, Feb-07, Volume: 10, Issue:3 | Design, synthesis and biological evaluation of 7-azatricyclodecanes: analogues of cocaine. |
| AID275447 | Selectivity for human DAT over human NET in radio ligand binding assay | 2007 | Journal of medicinal chemistry, Jan-25, Volume: 50, Issue:2 | Slow-onset, long-duration, alkyl analogues of methylphenidate with enhanced selectivity for the dopamine transporter. |
| AID181696 | Compound was evaluated for its ability to inhibit high-affinity uptake of [3H]dopamine into striatal nerve endings of rat | 1992 | Journal of medicinal chemistry, Dec-11, Volume: 35, Issue:25 | Structure-activity relationship studies of cocaine: replacement of the C-2 ester group by vinyl argues against H-bonding and provides an esterase-resistant, high-affinity cocaine analogue. |
| AID65155 | Inhibition of dopamine uptake into rat striatal tissue, using [3H]- dopamine as the radioligand. | 1999 | Journal of medicinal chemistry, Mar-11, Volume: 42, Issue:5 | Synthesis and pharmacology of site-specific cocaine abuse treatment agents: 2-(aminomethyl)-3-phenylbicyclo[2.2.2]- and -[2.2.1]alkane dopamine uptake inhibitors. |
| AID64698 | Binding affinity towards dopamine transporter was determined using DA[3H]WIN-35428 as radioligand | 1995 | Journal of medicinal chemistry, Sep-01, Volume: 38, Issue:18 | Synthesis and ligand binding study of 3 beta-(4'-substituted phenyl)-2 beta-(heterocyclic)tropanes. |
| AID192995 | Number of animals(n) completing 20 responses on either lever out of the number of animals tested (N) at dose 10 mg/kg evaluated by temporal tests in trained rats(post injection interval 5 min); n/N=7/7 | 1992 | Journal of medicinal chemistry, Dec-11, Volume: 35, Issue:25 | Structure-activity relationship studies of cocaine: replacement of the C-2 ester group by vinyl argues against H-bonding and provides an esterase-resistant, high-affinity cocaine analogue. |
| AID204692 | Displacement of [3H]-citalopram from serotonin transporter of rat brain membrane | 2004 | Bioorganic & medicinal chemistry letters, Jun-21, Volume: 14, Issue:12 | The effect of 6-substituted-4',4"-difluorobenztropines on monoamine transporters and the muscarinic M1 receptor. |
| AID65029 | Tested for its ability to inhibit high affinity uptake of [3H]dopamine into rat caudate-putamen tissue | 1994 | Journal of medicinal chemistry, Nov-11, Volume: 37, Issue:23 | Synthesis, cocaine receptor affinity, and dopamine uptake inhibition of several new 2 beta-substituted 3 beta-phenyltropanes. |
| AID64704 | Inhibition of [3H]WIN-35428l binding to Dopamine transporter | 1992 | Journal of medicinal chemistry, Jun-26, Volume: 35, Issue:13 | Isopropyl and phenyl esters of 3 beta-(4-substituted phenyl)tropan-2 beta-carboxylic acids. Potent and selective compounds for the dopamine transporter. |
| AID64863 | Inhibitory concentration required to inhibit dopamine transporter DAT was determined by using [3H]WIN-35428 radioligand | 2004 | Journal of medicinal chemistry, Jan-15, Volume: 47, Issue:2 | Synthesis, monoamine transporter binding properties, and behavioral pharmacology of a series of 3beta-(substituted phenyl)-2beta-(3'-substituted isoxazol-5-yl)tropanes. |
| AID241426 | Inhibition of [3H]WIN-35428 binding to dopamine transporter (DAT) | 2004 | Bioorganic & medicinal chemistry letters, Dec-20, Volume: 14, Issue:24 | Synthesis of 8-thiabicyclo[3.2.1]oct-2-enes and their binding affinity for the dopamine and serotonin transporters. |
| AID64214 | Inhibition of [3H]WIN-35428 binding to dopamine transporter (DAT) of cynomolgus monkey caudate-putamen | 1999 | Bioorganic & medicinal chemistry letters, Mar-22, Volume: 9, Issue:6 | Bicyclo[3.2.1]octanes: synthesis and inhibition of binding at the dopamine and serotonin transporters. |
| AID226637 | Hill coefficient value of the compound | 1991 | Journal of medicinal chemistry, Mar, Volume: 34, Issue:3 | Synthesis and ligand binding of cocaine isomers at the cocaine receptor. |
| AID145382 | Inhibition of [3H]mazindol binding to Norepinephrine transporter | 1992 | Journal of medicinal chemistry, Jun-26, Volume: 35, Issue:13 | Isopropyl and phenyl esters of 3 beta-(4-substituted phenyl)tropan-2 beta-carboxylic acids. Potent and selective compounds for the dopamine transporter. |
| AID261028 | Displacement of [125I]RTI-55 from human NET expressed in HEK293 cells | 2006 | Journal of medicinal chemistry, Feb-23, Volume: 49, Issue:4 | 1-(4-Methylphenyl)-2-pyrrolidin-1-yl-pentan-1-one (Pyrovalerone) analogues: a promising class of monoamine uptake inhibitors. |
| AID281808 | Locomotor activity in ip dosed CD1 mouse in peak hour | 2004 | Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25 | Monoamine transporter binding, locomotor activity, and drug discrimination properties of 3-(4-substituted-phenyl)tropane-2-carboxylic acid methyl ester isomers. |
| AID64846 | Binding affinity at the dopamine transporter in rast striatum by [3H]WIN-35428 displacement. | 2003 | Journal of medicinal chemistry, May-22, Volume: 46, Issue:11 | Interaction of cis-(6-benzhydrylpiperidin-3-yl)benzylamine analogues with monoamine transporters: structure-activity relationship study of structurally constrained 3,6-disubstituted piperidine analogues of (2,2-diphenylethyl)-[1-(4-fluorobenzyl)piperidin- |
| AID360441 | Inhibition of [3H]dopamine uptake at human DAT M272L/R344M mutant expressed in HEK293 cells | 2007 | The Journal of biological chemistry, Mar-23, Volume: 282, Issue:12 | Localization of cocaine analog [125I]RTI 82 irreversible binding to transmembrane domain 6 of the dopamine transporter. |
| AID63033 | Inhibition of [3H]dopamine uptake in HEK cells expressing human DAT | 2003 | Bioorganic & medicinal chemistry letters, Nov-17, Volume: 13, Issue:22 | Synthesis and biological activity of 2-carbomethoxy-3-catechol-8-azabicyclo[3.2.1]octanes. |
| AID195347 | Mean responses per minute at dose 2.5 mg/kg evaluated by dose-response tests in trained rats(post injection interval 15 min) | 1992 | Journal of medicinal chemistry, Dec-11, Volume: 35, Issue:25 | Structure-activity relationship studies of cocaine: replacement of the C-2 ester group by vinyl argues against H-bonding and provides an esterase-resistant, high-affinity cocaine analogue. |
| AID204708 | Compound was tested for its ability to inhibit high affinity uptake of [3H]5-HT into mid brain nerve endings (synaptosomes) in rat | 2000 | Bioorganic & medicinal chemistry letters, Jul-03, Volume: 10, Issue:13 | An enantioselective synthesis and biobehavioral evaluation of 7-fluoro-3-(p-fluorophenyl)-2-propyltropanes. |
| AID7738 | Baboon plasma free fraction. | 1992 | Journal of medicinal chemistry, Jun-12, Volume: 35, Issue:12 | Synthesis of carbon-11 labeled iodinated cocaine derivatives and their distribution in baboon brain measured using positron emission tomography. |
| AID145387 | Inhibition of binding of [3H]- nisoxatine to Norepinephrine transporter (NET) of rat cerebral cortex. | 2002 | Journal of medicinal chemistry, Jan-31, Volume: 45, Issue:3 | Expansion of structure-activity studies of piperidine analogues of 1-[2-(diphenylmethoxy)ethyl]-4-(3-phenylpropyl)piperazine (GBR 12935) compounds by altering substitutions in the N-benzyl moiety and behavioral pharmacology of selected molecules. |
| AID281866 | Activity in CD1 mouse assessed as hyperactivity at 100 mg/kg, ip after 4 hrs | 2004 | Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25 | Monoamine transporter binding, locomotor activity, and drug discrimination properties of 3-(4-substituted-phenyl)tropane-2-carboxylic acid methyl ester isomers. |
| AID64542 | Binding affinity towards dopamine transporter using [3H]WIN-35428 as radioligand from rat caudate putamen tissue (low affinity) | 1996 | Journal of medicinal chemistry, Mar-29, Volume: 39, Issue:7 | Synthesis and ligand binding of eta(6)-(2beta-carbomethoxy-3beta-phenyltropane) transition metal complexes. |
| AID174463 | Percent response at dose 10 mg/kg evaluated by temporal tests in trained rats(post injection interval 60 min) | 1992 | Journal of medicinal chemistry, Dec-11, Volume: 35, Issue:25 | Structure-activity relationship studies of cocaine: replacement of the C-2 ester group by vinyl argues against H-bonding and provides an esterase-resistant, high-affinity cocaine analogue. |
| AID234769 | Selectivity for Dopamine and Norepinephrine transporters | 1996 | Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2 | N-substituted analogs of 2 beta-carbomethoxy-3 beta- (4'-iodophenyl)tropane (beta-CIT) with selective affinity to dopamine or serotonin transporters in rat forebrain. |
| AID242495 | Inhibition of [3H]dopamine uptake in HEK293 cells expressing human dopamine transporter | 2005 | Journal of medicinal chemistry, Apr-21, Volume: 48, Issue:8 | Synthesis and pharmacology of ethylphenidate enantiomers: the human transesterification metabolite of methylphenidate and ethanol. |
| AID235525 | Selectivity for Norepinephrine and Dopamine Transporters was evaluated | 1998 | Journal of medicinal chemistry, Jun-18, Volume: 41, Issue:13 | 2beta-Substituted analogues of 4'-iodococaine: synthesis and dopamine transporter binding potencies. |
| AID204524 | Inhibition of high affinity serotonin uptake into rat synaptosomes using [3H]5-HT | 2001 | Journal of medicinal chemistry, May-10, Volume: 44, Issue:10 | Pharmacological and behavioral analysis of the effects of some bivalent ligand-based monoamine reuptake inhibitors. |
| AID296175 | Inhibition of [3H]DA uptake in human NET expressed in COS1 cell membrane | 2007 | Bioorganic & medicinal chemistry, Jun-15, Volume: 15, Issue:12 | Synthesis, inhibition and binding of simple non-nitrogen inhibitors of monoamine transporters. |
| AID1324603 | Displacement of [3H]WIN35,428 from wild type human DAT expressed in COS7 cell membranes incubated for >90 mins by radioligand binding assay | 2016 | Journal of medicinal chemistry, 12-08, Volume: 59, Issue:23 | Novel and High Affinity 2-[(Diphenylmethyl)sulfinyl]acetamide (Modafinil) Analogues as Atypical Dopamine Transporter Inhibitors. |
| AID64687 | Binding affinity at the Dopamine transporter in rat striata by inhibition of 0.5 nM [3H]WIN-35428 binding | 1995 | Journal of medicinal chemistry, Jan-20, Volume: 38, Issue:2 | Cocaine and 3 beta-(4'-substituted phenyl)tropane-2 beta-carboxylic acid ester and amide analogues. New high-affinity and selective compounds for the dopamine transporter. |
| AID552080 | Displacement of [3H]WIN35428 from human DAT transfected cell membrane | 2011 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1 | The synthesis and biological evaluation of 2-(3-methyl or 3-phenylisoxazol-5-yl)-3-aryl-8-thiabicyclo[3.2.1]octanes. |
| AID200914 | Inhibition of reuptake of [3H]5-HT (20 nM) by serotonin transporter | 2000 | Journal of medicinal chemistry, Dec-28, Volume: 43, Issue:26 | Slow-onset, long-duration 3-(3',4'-dichlorophenyl)-1-indanamine monoamine reuptake blockers as potential medications to treat cocaine abuse. |
| AID360442 | Inhibition of [3H]dopamine uptake at human DAT R344M mutant expressed in HEK293 cells | 2007 | The Journal of biological chemistry, Mar-23, Volume: 282, Issue:12 | Localization of cocaine analog [125I]RTI 82 irreversible binding to transmembrane domain 6 of the dopamine transporter. |
| AID281848 | Drug discrimination effect in CD Albino rat assessed as percent of rat choosing cocaine lever at 5.6 mg/kg, ip | 2004 | Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25 | Monoamine transporter binding, locomotor activity, and drug discrimination properties of 3-(4-substituted-phenyl)tropane-2-carboxylic acid methyl ester isomers. |
| AID1443747 | Inhibition of recombinant human NET expressed in HEK293 cell membranes assessed as reduction in [3H]-norepinephrine uptake incubated for 22 mins by micro beta scintillation counting analysis | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | Scaffold Repurposing of Nucleosides (Adenosine Receptor Agonists): Enhanced Activity at the Human Dopamine and Norepinephrine Sodium Symporters. |
| AID42235 | Binding constant towards Beta-cyclodextrin at pH 7.4 in unbuffered water at 25 C in a one-to-one complex | 2000 | Bioorganic & medicinal chemistry letters, Sep-04, Volume: 10, Issue:17 | The binding of cocaine to cyclodextrins. |
| AID234941 | Selectivity in uptake of NE to that of DA | 2001 | Bioorganic & medicinal chemistry letters, Aug-20, Volume: 11, Issue:16 | Sar studies of piperidine-based analogues of cocaine. Part 3: oxadiazoles. |
| AID204870 | Binding affinity against Serotonin transporter in male Sprague-Dawley rats using [3H]paroxetine ligand | 1999 | Journal of medicinal chemistry, Oct-21, Volume: 42, Issue:21 | Structure-activity relationships at the monoamine transporters and sigma receptors for a novel series of 9-[3-(cis-3, 5-dimethyl-1-piperazinyl)propyl]carbazole (rimcazole) analogues. |
| AID65320 | Displacement of [125I]RTI-55 from Dopamine transporter of rat caudate membranes | 2002 | Bioorganic & medicinal chemistry letters, Aug-19, Volume: 12, Issue:16 | Identification of a novel partial inhibitor of dopamine transporter among 4-substituted 2-phenylquinazolines. |
| AID384548 | Inhibition of [3H]DA uptake in DAT | 2008 | Journal of medicinal chemistry, May-08, Volume: 51, Issue:9 | Design and synthesis of 2- and 3-substituted-3-phenylpropyl analogs of 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine and 1-[2-(diphenylmethoxy)ethyl]-4-(3-phenylpropyl)piperazine: role of amino, fluoro, hydroxyl, methoxyl, methyl, m |
| AID64342 | Compound was tested for binding affinity to dopamine reuptake sites in the tissue homogenates prepared from primate rat striatum using [3H]CFT as radioligand | 1991 | Journal of medicinal chemistry, Oct, Volume: 34, Issue:10 | [123I]-2 beta-carbomethoxy-3 beta-(4-iodophenyl)tropane: high-affinity SPECT radiotracer of monoamine reuptake sites in brain. |
| AID221395 | Tested for rate of horizontal activity during a 30-min period after administration of compound at a concentration of 30 mg/kg | 2001 | Bioorganic & medicinal chemistry letters, Dec-17, Volume: 11, Issue:24 | [3-cis-3,5-Dimethyl-(1-piperazinyl)alkyl]-bis-(4'-fluorophenyl)amine analogues as novel probes for the dopamine transporter. |
| AID145877 | In vitro binding affinity towards Norepinephrine transporter rat cerebral cortical homogenates by [3H]nisoxetine displacement. | 1996 | Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2 | N-substituted analogs of 2 beta-carbomethoxy-3 beta- (4'-iodophenyl)tropane (beta-CIT) with selective affinity to dopamine or serotonin transporters in rat forebrain. |
| AID7942 | Percentage of tracer or metabolite (acid metabolites) in baboon plasma at 5 min after injection of the compound | 1992 | Journal of medicinal chemistry, Jun-12, Volume: 35, Issue:12 | Synthesis of carbon-11 labeled iodinated cocaine derivatives and their distribution in baboon brain measured using positron emission tomography. |
| AID230942 | Relative affinity for serotonin and dopamine transporters | 2000 | Bioorganic & medicinal chemistry letters, Aug-07, Volume: 10, Issue:15 | Synthesis and biological evaluation of 1-azabicyclo-[3.2.1]octanes: new dopamine transporter inhibitors. |
| AID395334 | Displacement of [125I]RTI-55 from human recombinant SERT expressed in HEK293 cells by scintillation counting | 2009 | Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6 | Dual inhibitors of phosphodiesterase-4 and serotonin reuptake. |
| AID204712 | Displacement of [3H]5-HT from serotonin transporter of rat brain | 2001 | Bioorganic & medicinal chemistry letters, Aug-20, Volume: 11, Issue:16 | Sar studies of piperidine-based analogues of cocaine. Part 3: oxadiazoles. |
| AID65179 | Ability to inhibit [3H]DA reuptake at dopamine transporter from rat brain | 2003 | Journal of medicinal chemistry, May-08, Volume: 46, Issue:10 | Biaryl analogues of conformationally constrained tricyclic tropanes as potent and selective norepinephrine reuptake inhibitors: synthesis and evaluation of their uptake inhibition at monoamine transporter sites. |
| AID65651 | Inhibition of [3H]dopamine uptake at the dopamine transporter. | 1992 | Journal of medicinal chemistry, Mar-20, Volume: 35, Issue:6 | Cocaine receptor: biochemical characterization and structure-activity relationships of cocaine analogues at the dopamine transporter. |
| 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. |
| AID204379 | Inhibitory activity against Serotonin transporter was determined for [3H]5-HT (serotonin) uptake by striated synaptosomes | 1998 | Journal of medicinal chemistry, Dec-03, Volume: 41, Issue:25 | Synthesis and biological properties of new 2beta-alkyl- and 2beta-aryl-3-(substituted phenyl)tropane derivatives: stereochemical effect of C-3 on affinity and selectivity for neuronal dopamine and serotonin transporters. |
| AID281824 | Locomotor activity in CD1 mouse assessed as stimulation at 100 mg/kg, ip after 4 hrs relative to control | 2004 | Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25 | Monoamine transporter binding, locomotor activity, and drug discrimination properties of 3-(4-substituted-phenyl)tropane-2-carboxylic acid methyl ester isomers. |
| AID235524 | Selectivity for Norepinephrine and Dopamine Transporters was evaluated | 1998 | Journal of medicinal chemistry, Jun-18, Volume: 41, Issue:13 | 2beta-Substituted analogues of 4'-iodococaine: synthesis and dopamine transporter binding potencies. |
| AID145884 | Inhibition of [3H]NE binding to norepinephrine transporter of rat brain synaptosomes | 2000 | Bioorganic & medicinal chemistry letters, Aug-07, Volume: 10, Issue:15 | Synthesis and biological evaluation of 1-azabicyclo-[3.2.1]octanes: new dopamine transporter inhibitors. |
| AID65343 | Compound was evaluated for its ability to displace [3H]WIN-35428 binding in rat caudate-putamen | 1994 | Journal of medicinal chemistry, Jul-22, Volume: 37, Issue:15 | Novel 3 alpha-(diphenylmethoxy)tropane analogs: potent dopamine uptake inhibitors without cocaine-like behavioral profiles. |
| AID1388096 | Half life in human brain | 2018 | Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6 | Triple Reuptake Inhibitors as Potential Therapeutics for Depression and Other Disorders: Design Paradigm and Developmental Challenges. |
| AID147736 | Inhibition of [3H]nisoxetine binding at norepinephrine transporter was determined | 2003 | Journal of medicinal chemistry, May-08, Volume: 46, Issue:10 | 2002 Medicinal Chemistry Division Award address: monoamine transporters and opioid receptors. Targets for addiction therapy. |
| AID296173 | Inhibition of [3H]DA uptake in human DAT expressed in COS1 cell membrane | 2007 | Bioorganic & medicinal chemistry, Jun-15, Volume: 15, Issue:12 | Synthesis, inhibition and binding of simple non-nitrogen inhibitors of monoamine transporters. |
| AID65484 | Inhibition of [3H]DA Uptake was measured by liquid scintillation spectrometry | 2000 | Journal of medicinal chemistry, Feb-10, Volume: 43, Issue:3 | Discovery of a novel dopamine transporter inhibitor, 4-hydroxy-1-methyl-4-(4-methylphenyl)-3-piperidyl 4-methylphenyl ketone, as a potential cocaine antagonist through 3D-database pharmacophore searching. Molecular modeling, structure-activity relationshi |
| AID127359 | Dissociation Constant for human monoclonal antibody 2E2 with [3H]cocaine | 2004 | Journal of medicinal chemistry, Jan-01, Volume: 47, Issue:1 | Three-dimensional quantitative structure-activity relationship modeling of cocaine binding by a novel human monoclonal antibody. |
| AID64695 | Binding affinity was evaluated by measuring the inhibition of [3H]WIN-35428 binding to Dopamine transporter in rat brain tissue | 2001 | Bioorganic & medicinal chemistry letters, Sep-03, Volume: 11, Issue:17 | Rational design and synthesis of novel 2,5-disubstituted cis- and trans-piperidine derivatives exhibiting differential activity for the dopamine transporter. |
| AID238628 | Inhibition of [3H]WIN-35428 binding to rat dopamine transporter | 2005 | Journal of medicinal chemistry, Mar-10, Volume: 48, Issue:5 | Synthesis and biological evaluation of meperidine analogues at monoamine transporters. |
| AID64860 | In vitro inhibitory activity against radioligand [3H]-WN 35,428 binding to dopamine transporter (DAT) in rat striatal tissue | 1997 | Journal of medicinal chemistry, Nov-21, Volume: 40, Issue:24 | 3 Beta-(4-ethyl-3-iodophenyl)nortropane-2 beta-carboxylic acid methyl ester as a high-affinity selective ligand for the serotonin transporter. |
| AID1443758 | Inhibition of [125I]RTI-55 binding to recombinant human NET expressed in HEK293 cell membranes preincubated for 10 mins followed by radioligand addition measured after 90 mins by micro beta scintillation counting analysis | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | Scaffold Repurposing of Nucleosides (Adenosine Receptor Agonists): Enhanced Activity at the Human Dopamine and Norepinephrine Sodium Symporters. |
| AID65794 | Affinity to inhibit [3H]DA uptake | 2003 | Bioorganic & medicinal chemistry letters, Feb-10, Volume: 13, Issue:3 | Pharmacophore-based discovery of substituted pyridines as novel dopamine transporter inhibitors. |
| AID65003 | Inhibitory activity determined for [3H]DA (Dopamine transporter) uptake by striated synaptosomes | 1998 | Journal of medicinal chemistry, Dec-03, Volume: 41, Issue:25 | Synthesis and biological properties of new 2beta-alkyl- and 2beta-aryl-3-(substituted phenyl)tropane derivatives: stereochemical effect of C-3 on affinity and selectivity for neuronal dopamine and serotonin transporters. |
| AID52203 | In vitro inhibitory activity towards [3H]cocaine binding to rat striatal tissue | 1991 | Journal of medicinal chemistry, Feb, Volume: 34, Issue:2 | Synthesis of 3-carbamoylecgonine methyl ester analogues as inhibitors of cocaine binding and dopamine uptake. |
| AID64711 | Binding against Dopamine transporter using radioligand as [3H]GBR 12935 | 1996 | Journal of medicinal chemistry, Nov-22, Volume: 39, Issue:24 | Development of novel, potent, and selective dopamine reuptake inhibitors through alteration of the piperazine ring of 1-[2-(diphenylmethoxy)ethyl]-and 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazines (GBR 12935 and GBR 12909). |
| AID15715 | Calculated partition coefficient (clogP) | 2004 | Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12 | Synthesis, molecular modeling, and biological studies of novel piperidine-based analogues of cocaine: evidence of unfavorable interactions proximal to the 3alpha-position of the piperidine ring. |
| AID64833 | Compound was tested for binding against Dopamine transporter using radioligand as [3H]-RTI 55 | 1996 | Journal of medicinal chemistry, Nov-22, Volume: 39, Issue:24 | Development of novel, potent, and selective dopamine reuptake inhibitors through alteration of the piperazine ring of 1-[2-(diphenylmethoxy)ethyl]-and 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazines (GBR 12935 and GBR 12909). |
| AID174295 | Drug discrimination effect of compound in rats, expressed as percent of rats choosing the cocaine lever at dose 5.6 mg/kg (ip) | 2004 | Journal of medicinal chemistry, Jan-15, Volume: 47, Issue:2 | Synthesis, monoamine transporter binding properties, and behavioral pharmacology of a series of 3beta-(substituted phenyl)-2beta-(3'-substituted isoxazol-5-yl)tropanes. |
| AID65182 | Inhibition of high affinity uptake of [3H]dopamine into striatal nerve endings (synaptosomes) | 1999 | Bioorganic & medicinal chemistry letters, Jul-05, Volume: 9, Issue:13 | Synthesis of 8-Oxa analogues of norcocaine endowed with interesting cocaine-like activity. |
| AID1443761 | Inhibition of [3H]mazindol binding to recombinant human SERT expressed in HEK293 cell membranes preincubated for 10 mins followed by radioligand addition measured after 90 mins by micro beta scintillation counting analysis | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | Scaffold Repurposing of Nucleosides (Adenosine Receptor Agonists): Enhanced Activity at the Human Dopamine and Norepinephrine Sodium Symporters. |
| AID204853 | Ratio of Ki value towards Serotonin transporter to that of dopamine transporter | 1995 | Journal of medicinal chemistry, Jan-20, Volume: 38, Issue:2 | Cocaine and 3 beta-(4'-substituted phenyl)tropane-2 beta-carboxylic acid ester and amide analogues. New high-affinity and selective compounds for the dopamine transporter. |
| AID187150 | Binding affinity against [3H]mazindol | 1993 | Journal of medicinal chemistry, Nov-26, Volume: 36, Issue:24 | Methoxylation of cocaine reduces binding affinity and produces compounds of differential binding and dopamine uptake inhibitory activity: discovery of a weak cocaine "antagonist". |
| AID204850 | Inhibition of [3H]5-HT uptake at striatal nerve endings by serotonin transporter | 1999 | Bioorganic & medicinal chemistry letters, Dec-06, Volume: 9, Issue:23 | N-phenylalkyl-substituted tropane analogs of boat conformation with high selectivity for the dopamine versus serotonin transporter. |
| AID393260 | Inhibition of [3H]serotonin reuptake at human SERT expressed in HEK cells | 2009 | Bioorganic & medicinal chemistry, Mar-01, Volume: 17, Issue:5 | 2,5-Disubstituted tetrahydrofurans as selective serotonin re-uptake inhibitors. |
| AID752492 | Inhibition of [3H]norepinephrine uptake at human NET expressed in HEK293 cells preincubated for 10 mins prior to substrate addition measured after 4 mins by FLIPR assay | 2013 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11 | An analysis of the synthetic tryptamines AMT and 5-MeO-DALT: emerging 'Novel Psychoactive Drugs'. |
| AID234157 | Ratio of norepinephrine uptake to norepinephrine binding | 2000 | Journal of medicinal chemistry, Dec-28, Volume: 43, Issue:26 | Slow-onset, long-duration 3-(3',4'-dichlorophenyl)-1-indanamine monoamine reuptake blockers as potential medications to treat cocaine abuse. |
| AID283004 | Displacement of [3H]paroxetine from 5HTT | 2005 | Journal of medicinal chemistry, Nov-17, Volume: 48, Issue:23 | Synthesis and monoamine transporter binding properties of 2,3-diaryltropanes. |
| AID360438 | Displacement of [3H]CFT from human DAT R344M mutant expressed in HEK293 cells | 2007 | The Journal of biological chemistry, Mar-23, Volume: 282, Issue:12 | Localization of cocaine analog [125I]RTI 82 irreversible binding to transmembrane domain 6 of the dopamine transporter. |
| AID451840 | Inhibition of [3H]DA reuptake at human DAT expressed in HEK293 cells | 2009 | Bioorganic & medicinal chemistry, Oct-01, Volume: 17, Issue:19 | Inhibition of serotonin and norepinephrine reuptake and inhibition of phosphodiesterase by multi-target inhibitors as potential agents for depression. |
| AID233814 | Ratio of uptake inhibition from dopamine transporter to that of binding affinity towards dopamine transporter | 2003 | Journal of medicinal chemistry, Mar-27, Volume: 46, Issue:7 | High affinity hydroxypiperidine analogues of 4-(2-benzhydryloxyethyl)-1-(4-fluorobenzyl)piperidine for the dopamine transporter: stereospecific interactions in vitro and in vivo. |
| AID28233 | Fraction ionized (pH 7.4) | 2002 | Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13 | Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data. |
| AID261024 | Displacement of [125I]RTI-55 from human DAT expressed in HEK293 cells | 2006 | Journal of medicinal chemistry, Feb-23, Volume: 49, Issue:4 | 1-(4-Methylphenyl)-2-pyrrolidin-1-yl-pentan-1-one (Pyrovalerone) analogues: a promising class of monoamine uptake inhibitors. |
| AID7932 | Percentage of tracer or metabolite (CO2) in baboon plasma at 1 min after injection of the compound | 1992 | Journal of medicinal chemistry, Jun-12, Volume: 35, Issue:12 | Synthesis of carbon-11 labeled iodinated cocaine derivatives and their distribution in baboon brain measured using positron emission tomography. |
| AID281807 | Displacement of [3H]paroxetine from 5HTT | 2004 | Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25 | Monoamine transporter binding, locomotor activity, and drug discrimination properties of 3-(4-substituted-phenyl)tropane-2-carboxylic acid methyl ester isomers. |
| AID64362 | Compound was tested for inhibition of [3H]DA binding to Dopamine transporter in HEK cells | 2003 | Bioorganic & medicinal chemistry letters, Jul-07, Volume: 13, Issue:13 | Bivalent biogenic amine reuptake inhibitors. |
| AID204716 | In vitro binding affinity towards serotonin transporter in rat cerebral cortical homogenates by [3H]paroxetine displacement. | 1996 | Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2 | N-substituted analogs of 2 beta-carbomethoxy-3 beta- (4'-iodophenyl)tropane (beta-CIT) with selective affinity to dopamine or serotonin transporters in rat forebrain. |
| AID281847 | Drug discrimination effect in CD Albino rat assessed as percent of rat choosing cocaine lever at 3 mg/kg, ip | 2004 | Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25 | Monoamine transporter binding, locomotor activity, and drug discrimination properties of 3-(4-substituted-phenyl)tropane-2-carboxylic acid methyl ester isomers. |
| AID195336 | Mean responses per minute at dose 0.62 mg/kg evaluated by dose-response tests in trained rats(post injection interval 15 min) | 1992 | Journal of medicinal chemistry, Dec-11, Volume: 35, Issue:25 | Structure-activity relationship studies of cocaine: replacement of the C-2 ester group by vinyl argues against H-bonding and provides an esterase-resistant, high-affinity cocaine analogue. |
| AID266637 | Displacement of [3H]nisoxetine from human NET | 2006 | Journal of medicinal chemistry, Jul-27, Volume: 49, Issue:15 | Synthesis and monoamine transporter binding properties of 2,3-cyclo analogues of 3beta-(4'-aminophenyl)-2beta-tropanemethanol. |
| AID419688 | Antagonist activity at muscarinic receptor | 2009 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 19, Issue:11 | 3D-QSAR study of 8-azabicyclo[3.2.1] octane analogs antagonists of cholinergic receptor. |
| AID65485 | Inhibition of [3H]DA uptake at Dopamine transporter in rat cortex. | 2001 | Bioorganic & medicinal chemistry letters, May-07, Volume: 11, Issue:9 | Pharmacophore-based discovery of 3,4-disubstituted pyrrolidines as a novel class of monoamine transporter inhibitors. |
| AID181697 | Compound was evaluated for its ability to inhibit the uptake of dopamine(DA) into nerve ending using [3H]DA on synaptosomes obtained from dissected rat striata. | 2000 | Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6 | Further SAR studies of piperidine-based analogues of cocaine. 2. Potent dopamine and serotonin reuptake inhibitors. |
| AID1142752 | Vascular activity in receptor-independent rat mesenteric resistance artery assessed as inhibition of KCl-induced contraction at 3 x 10'-6 M after 5 mins | 2014 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 24, Issue:11 | Vascular effects of diphenylmethoxypiperidine-derived dopamine uptake inhibitors. |
| AID257284 | Displacement of [3H]WIN-from DAT in rat brain membrane | 2005 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 15, Issue:24 | N-8-Substituted benztropinamine analogs as selective dopamine transporter ligands. |
| AID222148 | K+ channel blocking activity in human embryonic kidney cells expressing HERG Kv11.1 | 2002 | Journal of medicinal chemistry, Aug-29, Volume: 45, Issue:18 | Toward a pharmacophore for drugs inducing the long QT syndrome: insights from a CoMFA study of HERG K(+) channel blockers. |
| AID64841 | Inhibition of dopamine DA reuptake | 1996 | Journal of medicinal chemistry, Nov-22, Volume: 39, Issue:24 | Development of novel, potent, and selective dopamine reuptake inhibitors through alteration of the piperazine ring of 1-[2-(diphenylmethoxy)ethyl]-and 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazines (GBR 12935 and GBR 12909). |
| AID248219 | Inhibition of [3H]dopamine uptake into rat striatal synaptosomes | 2005 | Journal of medicinal chemistry, May-05, Volume: 48, Issue:9 | Synthesis and pharmacology of 6-substituted benztropines: discovery of novel dopamine uptake inhibitors possessing low binding affinity to the dopamine transporter. |
| AID570370 | Displacement of [3H]WIN35428 from DAT in Sprague-Dawley rat brain membranes | 2010 | ACS medicinal chemistry letters, Oct-10, Volume: 2, Issue:1 | Structure-Activity Relationships at the Monoamine Transporters for a Novel Series of Modafinil (2-[(diphenylmethyl)sulfinyl]acetamide) Analogues. |
| AID16309 | Partition coefficient (logD) | 2004 | Journal of medicinal chemistry, Jun-17, Volume: 47, Issue:13 | Structure-activity relationships at monoamine transporters for a series of N-substituted 3alpha-(bis[4-fluorophenyl]methoxy)tropanes: comparative molecular field analysis, synthesis, and pharmacological evaluation. |
| AID65634 | In vitro ability to inhibit the [3H]WIN-35428 binding to cocaine binding site on dopamine transporter in rat striatal membranes irreversibly after two washes. | 1992 | Journal of medicinal chemistry, May-15, Volume: 35, Issue:10 | Probes for the cocaine receptor. Potentially irreversible ligands for the dopamine transporter. |
| AID360437 | Displacement of [3H]CFT from human DAT M272L/R344M mutant expressed in HEK293 cells | 2007 | The Journal of biological chemistry, Mar-23, Volume: 282, Issue:12 | Localization of cocaine analog [125I]RTI 82 irreversible binding to transmembrane domain 6 of the dopamine transporter. |
| AID145710 | Inhibition of 0.5 nM [3H]nisoxetine binding toNorepinephrine transporter | 2000 | Bioorganic & medicinal chemistry letters, Nov-06, Volume: 10, Issue:21 | 3alpha-(4-Substituted phenyl)nortropane-2beta-carboxylic acid methyl esters show selective binding at the norepinephrine transporter. |
| AID242167 | Displacement of [125I]RTI-55 from human Serotonin transporter expressed in HEK293 cells | 2005 | Journal of medicinal chemistry, Apr-21, Volume: 48, Issue:8 | Synthesis and pharmacology of ethylphenidate enantiomers: the human transesterification metabolite of methylphenidate and ethanol. |
| AID65494 | Inhibitory constant towards reuptake of [125I]-12 from dopamine transporter in rat striatal membranes | 1994 | Journal of medicinal chemistry, May-13, Volume: 37, Issue:10 | Synthesis and characterization of radioiodinated N-(3-iodopropen-1-yl)-2 beta-carbomethoxy-3 beta-(4-chlorophenyl)tropanes: potential dopamine reuptake site imaging agents. |
| AID1443757 | Inhibition of [3H]mazindol binding to recombinant human DAT expressed in HEK293 cell membranes preincubated for 10 mins followed by radioligand addition measured after 90 mins by micro beta scintillation counting analysis | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | Scaffold Repurposing of Nucleosides (Adenosine Receptor Agonists): Enhanced Activity at the Human Dopamine and Norepinephrine Sodium Symporters. |
| AID145722 | Selectivity for the norepinephrine transporter using [3H]nisoxetine binding assay | 1999 | Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23 | Synthesis and pharmacology of site-specific cocaine abuse treatment agents: 2-substituted-6-amino-5-phenylbicyclo[2.2.2]octanes. |
| AID145705 | Binding potency for Norepinephrine transporter using [3H]NE | 1996 | Journal of medicinal chemistry, Oct-11, Volume: 39, Issue:21 | 3 alpha-(4'-substituted phenyl)tropane-2 beta-carboxylic acid methyl esters: novel ligands with high affinity and selectivity at the dopamine transporter. |
| AID145550 | Compound was evaluated for binding affinity using [125I]RTI-55 as a radioligand in HEK-hNET cells expressing human norepinephrine transporter | 2000 | Journal of medicinal chemistry, May-18, Volume: 43, Issue:10 | Novel conformationally constrained tropane analogues by 6-endo-trig radical cyclization and stille coupling - switch of activity toward the serotonin and/or norepinephrine transporter. |
| AID19262 | Aqueous solubility | 2000 | Bioorganic & medicinal chemistry letters, Jun-05, Volume: 10, Issue:11 | Prediction of drug solubility from Monte Carlo simulations. |
| AID64356 | Inhibition of dopamine uptake in HEK cells expressing human dopamine transporter (hDAT) | 2002 | Journal of medicinal chemistry, Sep-12, Volume: 45, Issue:19 | Mazindol analogues as potential inhibitors of the cocaine binding site at the dopamine transporter. |
| AID232638 | Inhibition of reuptake of norepinephrine compared to serotonin. | 2003 | Bioorganic & medicinal chemistry letters, Oct-20, Volume: 13, Issue:20 | Synthesis and pharmacological evaluation of (Z)-9-(heteroarylmethylene)-7-azatricyclo[4.3.1.0(3,7)]decanes: thiophene analogues as potent norepinephrine transporter inhibitors. |
| AID181076 | Values for substitution for Cocaine in rats Trained to discriminate Cocaine from saline | 1997 | Journal of medicinal chemistry, Mar-14, Volume: 40, Issue:6 | Synthesis, dopamine transporter affinity, dopamine uptake inhibition, and locomotor stimulant activity of 2-substituted 3 beta-phenyltropane derivatives. |
| AID145701 | Binding affinity at the Norepinephrine transporter in rat frontal cortex by inhibition of 0.5 nM [3H]nisoxetine binding | 1995 | Journal of medicinal chemistry, Jan-20, Volume: 38, Issue:2 | Cocaine and 3 beta-(4'-substituted phenyl)tropane-2 beta-carboxylic acid ester and amide analogues. New high-affinity and selective compounds for the dopamine transporter. |
| AID360444 | Displacement of [3H]RTI82 from DAT in rat striatal membrane | 2007 | The Journal of biological chemistry, Mar-23, Volume: 282, Issue:12 | Localization of cocaine analog [125I]RTI 82 irreversible binding to transmembrane domain 6 of the dopamine transporter. |
| AID204523 | Ability to inhibit [3H]5-HT reuptake at serotonin transporter from rat brain | 2003 | Journal of medicinal chemistry, May-08, Volume: 46, Issue:10 | Biaryl analogues of conformationally constrained tricyclic tropanes as potent and selective norepinephrine reuptake inhibitors: synthesis and evaluation of their uptake inhibition at monoamine transporter sites. |
| AID6428 | Inhibition of [3H]5-HT uptake in HEK cells expressing human SERT | 2003 | Bioorganic & medicinal chemistry letters, Nov-17, Volume: 13, Issue:22 | Synthesis and biological activity of 2-carbomethoxy-3-catechol-8-azabicyclo[3.2.1]octanes. |
| AID230708 | Ratio of affinity for Norepinephrine transporter to that of Serotonin transporter | 2004 | Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12 | Synthesis, molecular modeling, and biological studies of novel piperidine-based analogues of cocaine: evidence of unfavorable interactions proximal to the 3alpha-position of the piperidine ring. |
| AID36995 | Binding constant towards alpha-cyclodextrin | 2000 | Bioorganic & medicinal chemistry letters, Sep-04, Volume: 10, Issue:17 | The binding of cocaine to cyclodextrins. |
| AID232486 | Selectivity ratio is IC50 value of 5-HTT to that of DAT | 1997 | Journal of medicinal chemistry, Nov-21, Volume: 40, Issue:24 | 3 Beta-(4-ethyl-3-iodophenyl)nortropane-2 beta-carboxylic acid methyl ester as a high-affinity selective ligand for the serotonin transporter. |
| AID204373 | Inhibition of [3H]citalopram binding to Serotonin transporter (5-HTT) in rat cortical tissue. | 2003 | Journal of medicinal chemistry, Apr-10, Volume: 46, Issue:8 | Synthesis and pharmacology of site specific cocaine abuse treatment agents: 8-substituted isotropane (3-azabicyclo[3.2.1]octane) dopamine uptake inhibitors. |
| AID204537 | Binding affinity for Serotonin transporter was determined by [3H]5-HT (serotonin) uptake by striated synaptosomes | 1998 | Journal of medicinal chemistry, Dec-03, Volume: 41, Issue:25 | Synthesis and biological properties of new 2beta-alkyl- and 2beta-aryl-3-(substituted phenyl)tropane derivatives: stereochemical effect of C-3 on affinity and selectivity for neuronal dopamine and serotonin transporters. |
| AID233626 | Ratio of binding affinity towards serotonin transporter to that of dopamine transporter | 2003 | Journal of medicinal chemistry, Mar-27, Volume: 46, Issue:7 | High affinity hydroxypiperidine analogues of 4-(2-benzhydryloxyethyl)-1-(4-fluorobenzyl)piperidine for the dopamine transporter: stereospecific interactions in vitro and in vivo. |
| AID127477 | Relative binding affinity for human monoclonal antibody (mAb) 2E2 | 2004 | Journal of medicinal chemistry, Jan-01, Volume: 47, Issue:1 | Three-dimensional quantitative structure-activity relationship modeling of cocaine binding by a novel human monoclonal antibody. |
| AID64682 | In vitro binding affinity at dopamine transporter in rat striatum by [3H]WIN-35428 displacement. | 2001 | Journal of medicinal chemistry, Mar-15, Volume: 44, Issue:6 | Structure-activity relationship studies of 4-[2-(diphenylmethoxy)ethyl]-1-benzylpiperidine derivatives and their N-analogues: evaluation of O-and N-analogues and their binding to monoamine transporters. |
| AID181688 | Compound was evaluated for its ability to antagonizing norepinephrine (NE), high affinity uptake was determined using [3H]NE on synaptosomes prepared from rat occipital cortices. | 2000 | Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6 | Further SAR studies of piperidine-based analogues of cocaine. 2. Potent dopamine and serotonin reuptake inhibitors. |
| AID145714 | Inhibition of [3H]nisoxetine binding to norepinephrine (NE) transporter | 1994 | Journal of medicinal chemistry, Apr-15, Volume: 37, Issue:8 | Secondary amine analogues of 3 beta-(4'-substituted phenyl)tropane-2 beta-carboxylic acid esters and N-norcocaine exhibit enhanced affinity for serotonin and norepinephrine transporters. |
| AID145396 | Inhibition of [3H]NE uptake by Norepinephrine transporter of rat occipital cortex synaptosomes | 2000 | Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6 | Further SAR studies of piperidine-based analogues of cocaine. 2. Potent dopamine and serotonin reuptake inhibitors. |
| AID1443742 | Enhancing of [125I]RTI-55 binding to recombinant human DAT expressed in HEK293 cell membranes preincubated for 10 mins followed by radioligand addition measured after 90 mins by micro beta scintillation counting analysis | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | Scaffold Repurposing of Nucleosides (Adenosine Receptor Agonists): Enhanced Activity at the Human Dopamine and Norepinephrine Sodium Symporters. |
| AID111841 | Ability to reverse electroconvulsive shock induced amnesia in mice, after administering intraperitoneally at a dose of 5 mg/kg | 1984 | Journal of medicinal chemistry, May, Volume: 27, Issue:5 | Amnesia-reversal activity of a series of N-[(disubstituted-amino)alkyl] -2-oxo-1-pyrrolidineacetamides, including pramiracetam. |
| AID281806 | Displacement of [3H]nisoxetine from NET | 2004 | Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25 | Monoamine transporter binding, locomotor activity, and drug discrimination properties of 3-(4-substituted-phenyl)tropane-2-carboxylic acid methyl ester isomers. |
| AID64683 | Affinity for dopamine transporter was assessed by the ability to displace [3H]WIN-35428 from rat caudate-putamen tissue | 2002 | Journal of medicinal chemistry, Mar-14, Volume: 45, Issue:6 | Synthesis and biological evaluation of 2-substituted 3beta-tolyltropane derivatives at dopamine, serotonin, and norepinephrine transporters. |
| AID179055 | Compound was evaluated in vitro, for the ability to inhibit [3H]- dopamine uptake into synaptosomes (prepared from rat striatal tissues). | 1991 | Journal of medicinal chemistry, Feb, Volume: 34, Issue:2 | Synthesis of 3-carbamoylecgonine methyl ester analogues as inhibitors of cocaine binding and dopamine uptake. |
| AID65334 | Binding affinity was tested by measuring its ability to displace [3H]mazindol binding against dopamine transporter (DAT) of rat striatal membranes | 1994 | Journal of medicinal chemistry, Sep-30, Volume: 37, Issue:20 | Structure-activity relationship studies of N-sulfonyl analogs of cocaine: role of ionic interaction in cocaine binding. |
| AID127361 | Binding affinity towards human monoclonal antibody 2E2 using [3H]cocaine | 2004 | Journal of medicinal chemistry, Jan-01, Volume: 47, Issue:1 | Three-dimensional quantitative structure-activity relationship modeling of cocaine binding by a novel human monoclonal antibody. |
| AID241708 | Displacement of [3H]WIN-35428 from Dopamine transporter of rat caudate putamen | 2005 | Journal of medicinal chemistry, May-05, Volume: 48, Issue:9 | Synthesis and pharmacology of 6-substituted benztropines: discovery of novel dopamine uptake inhibitors possessing low binding affinity to the dopamine transporter. |
| AID65156 | Inhibitory binding activity against rat striatal tissue using [3H]WIN-35248 as the radioligand. | 1999 | Journal of medicinal chemistry, Mar-11, Volume: 42, Issue:5 | Synthesis and pharmacology of site-specific cocaine abuse treatment agents: 2-(aminomethyl)-3-phenylbicyclo[2.2.2]- and -[2.2.1]alkane dopamine uptake inhibitors. |
| AID174293 | Drug discrimination effect of compound in rats, expressed as percent of rats choosing the cocaine lever at dose 3 mg/kg (ip) | 2004 | Journal of medicinal chemistry, Jan-15, Volume: 47, Issue:2 | Synthesis, monoamine transporter binding properties, and behavioral pharmacology of a series of 3beta-(substituted phenyl)-2beta-(3'-substituted isoxazol-5-yl)tropanes. |
| AID174458 | Percent response at dose 10 mg/kg evaluated by dose-response tests in trained rats(post injection interval 15 min) | 1992 | Journal of medicinal chemistry, Dec-11, Volume: 35, Issue:25 | Structure-activity relationship studies of cocaine: replacement of the C-2 ester group by vinyl argues against H-bonding and provides an esterase-resistant, high-affinity cocaine analogue. |
| AID268240 | Inhibition of [3H]WIN-35428 binding to rat DAT expressed in D8 cells | 2006 | Journal of medicinal chemistry, Jul-13, Volume: 49, Issue:14 | Development of peptidic dopamine transporter inhibitors via aromatic modification-mediated conformational restriction. |
| AID231930 | Selectivity for serotonin transporter compared to dopamine transporter. | 2001 | Journal of medicinal chemistry, Mar-15, Volume: 44, Issue:6 | Structure-activity relationship studies of 4-[2-(diphenylmethoxy)ethyl]-1-benzylpiperidine derivatives and their N-analogues: evaluation of O-and N-analogues and their binding to monoamine transporters. |
| AID7933 | Percentage of tracer or metabolite (CO2) in baboon plasma at 30 min after injection of the compound | 1992 | Journal of medicinal chemistry, Jun-12, Volume: 35, Issue:12 | Synthesis of carbon-11 labeled iodinated cocaine derivatives and their distribution in baboon brain measured using positron emission tomography. |
| AID64679 | Ability to displace [3H]WIN-35428 from Dopamine Transporter of rat striatal membrane | 2002 | Journal of medicinal chemistry, Sep-12, Volume: 45, Issue:19 | Mazindol analogues as potential inhibitors of the cocaine binding site at the dopamine transporter. |
| AID7934 | Percentage of tracer or metabolite (CO2) in baboon plasma at 5 min after injection of the compound | 1992 | Journal of medicinal chemistry, Jun-12, Volume: 35, Issue:12 | Synthesis of carbon-11 labeled iodinated cocaine derivatives and their distribution in baboon brain measured using positron emission tomography. |
| AID242257 | Inhibition of [3H]nisoxetine binding to rat cerebral cortex norepinephrine transporter | 2005 | Journal of medicinal chemistry, Jun-02, Volume: 48, Issue:11 | Synthesis and monoamine transporter binding properties of 3alpha-(substituted phenyl)nortropane-2beta-carboxylic acid methyl esters. Norepinephrine transporter selective compounds. |
| AID111598 | Percent change from vehicle in locomotor activity in mice at 17 mg/kg (ip) in 2 h | 2004 | Journal of medicinal chemistry, Jan-15, Volume: 47, Issue:2 | Synthesis, monoamine transporter binding properties, and behavioral pharmacology of a series of 3beta-(substituted phenyl)-2beta-(3'-substituted isoxazol-5-yl)tropanes. |
| AID65348 | Compound was tested for its ability to inhibit high affinity uptake of [3H]DA into rat striatal membrane | 2000 | Bioorganic & medicinal chemistry letters, Jul-03, Volume: 10, Issue:13 | An enantioselective synthesis and biobehavioral evaluation of 7-fluoro-3-(p-fluorophenyl)-2-propyltropanes. |
| AID436599 | Displacement of [3H]WIN-35428 from DAT | 2009 | Bioorganic & medicinal chemistry, Jul-15, Volume: 17, Issue:14 | Synthesis and structure-activity relationship of 3beta-(4-alkylthio, -methylsulfinyl, and -methylsulfonylphenyl)tropane and 3beta-(4-alkylthiophenyl)nortropane derivatives for monoamine transporters. |
| 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. |
| AID234191 | Ratio of inhibition of serotonin uptake to inhibition of dopamine uptake | 2000 | Journal of medicinal chemistry, Dec-28, Volume: 43, Issue:26 | Slow-onset, long-duration 3-(3',4'-dichlorophenyl)-1-indanamine monoamine reuptake blockers as potential medications to treat cocaine abuse. |
| AID234451 | Uptake ratio at norepinephrine to dopamine transporters from rat brain | 2003 | Journal of medicinal chemistry, May-08, Volume: 46, Issue:10 | Biaryl analogues of conformationally constrained tricyclic tropanes as potent and selective norepinephrine reuptake inhibitors: synthesis and evaluation of their uptake inhibition at monoamine transporter sites. |
| AID65333 | Binding affinity towards dopamine transporter using [3H]- mazindol as radioligand in rat striatal membranes | 1999 | Bioorganic & medicinal chemistry letters, Jul-05, Volume: 9, Issue:13 | Synthesis of 8-Oxa analogues of norcocaine endowed with interesting cocaine-like activity. |
| AID193342 | Degradation rate constant for dopamine transporter in nucleus accumbens was determined | 2003 | Journal of medicinal chemistry, May-08, Volume: 46, Issue:10 | 2002 Medicinal Chemistry Division Award address: monoamine transporters and opioid receptors. Targets for addiction therapy. |
| AID1146628 | Hypoglycemic activity in Sprague-Dawley rat assessed as reduction of blood glucose level at 88 mg/kg, po by glucagon-impaired glucose disposal test relative to control | 1978 | Journal of medicinal chemistry, Dec, Volume: 21, Issue:12 | (exo, exo)-2-Aryltropane-3-carboxylic esters, hypoglycemic agents with accompanying analgesic activity. |
| AID232487 | Selectivity ratio is IC50 value of NET to that of DAT | 1997 | Journal of medicinal chemistry, Nov-21, Volume: 40, Issue:24 | 3 Beta-(4-ethyl-3-iodophenyl)nortropane-2 beta-carboxylic acid methyl ester as a high-affinity selective ligand for the serotonin transporter. |
| AID281846 | Drug discrimination effect in CD Albino rat assessed as percent of rat choosing cocaine lever at 1.7 mg/kg, ip | 2004 | Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25 | Monoamine transporter binding, locomotor activity, and drug discrimination properties of 3-(4-substituted-phenyl)tropane-2-carboxylic acid methyl ester isomers. |
| AID204356 | Inhibition of [3H]paroxetine binding to Serotonin transporter | 1992 | Journal of medicinal chemistry, Jun-26, Volume: 35, Issue:13 | Isopropyl and phenyl esters of 3 beta-(4-substituted phenyl)tropan-2 beta-carboxylic acids. Potent and selective compounds for the dopamine transporter. |
| AID145392 | Ability to inhibit high affinity reuptake of [3H]-NE (Norepinephrine transporter) into nerve ending synaptosomes prepared from brain regions | 2002 | Journal of medicinal chemistry, Apr-25, Volume: 45, Issue:9 | Further studies on conformationally constrained tricyclic tropane analogues and their uptake inhibition at monoamine transporter sites: synthesis of (Z)-9-(substituted arylmethylene)-7-azatricyclo[4.3.1.0(3,7)]decanes as a novel class of serotonin transpo |
| AID111610 | Percent change from vehicle in locomotor activity in mice at 5.6 mg/kg (ip) in 2 h | 2004 | Journal of medicinal chemistry, Jan-15, Volume: 47, Issue:2 | Synthesis, monoamine transporter binding properties, and behavioral pharmacology of a series of 3beta-(substituted phenyl)-2beta-(3'-substituted isoxazol-5-yl)tropanes. |
| AID65186 | Affinity for dopamine transporter was assessed by the ability to displace [3H]WIN-35428 from rat caudate-putamen tissue | 2002 | Journal of medicinal chemistry, Mar-14, Volume: 45, Issue:6 | Synthesis and biological evaluation of 2-substituted 3beta-tolyltropane derivatives at dopamine, serotonin, and norepinephrine transporters. |
| AID65513 | Potency for inhibition of [3H]WIN-35428 binding to rat striatal membrane dopamine transporter | 1991 | Journal of medicinal chemistry, Mar, Volume: 34, Issue:3 | Synthesis and ligand binding of cocaine isomers at the cocaine receptor. |
| AID275448 | Selectivity for human DAT over human NET in radio ligand uptake assay | 2007 | Journal of medicinal chemistry, Jan-25, Volume: 50, Issue:2 | Slow-onset, long-duration, alkyl analogues of methylphenidate with enhanced selectivity for the dopamine transporter. |
| AID1653639 | Displacement of [3H]WIN 35428 from human DAT transiently expressed in COS7 cells | |||
| AID1324602 | Displacement of [3H]WIN35,428 from human DAT Y156F mutant expressed in COS7 cell membranes incubated for >90 mins by radioligand binding assay | 2016 | Journal of medicinal chemistry, 12-08, Volume: 59, Issue:23 | Novel and High Affinity 2-[(Diphenylmethyl)sulfinyl]acetamide (Modafinil) Analogues as Atypical Dopamine Transporter Inhibitors. |
| AID204067 | Compound was tested for inhibition of [3H]5-HT binding to Serotonin transporter in HEK cells | 2003 | Bioorganic & medicinal chemistry letters, Jul-07, Volume: 13, Issue:13 | Bivalent biogenic amine reuptake inhibitors. |
| AID7547 | Clearance from plasma(with matabolite-corrected plasma radioactivity-time integral) at 30 min after administration. | 1992 | Journal of medicinal chemistry, Jun-12, Volume: 35, Issue:12 | Synthesis of carbon-11 labeled iodinated cocaine derivatives and their distribution in baboon brain measured using positron emission tomography. |
| AID360436 | Displacement of [3H]CFT from human DAT M272L/1291M/R344M mutant expressed in HEK293 cells | 2007 | The Journal of biological chemistry, Mar-23, Volume: 282, Issue:12 | Localization of cocaine analog [125I]RTI 82 irreversible binding to transmembrane domain 6 of the dopamine transporter. |
| AID204089 | Binding affinity for serotonin transporter using [125I]RTI-55 | 2000 | Journal of medicinal chemistry, Jan-27, Volume: 43, Issue:2 | Novel 3-aminomethyl- and 4-aminopiperidine analogues of 1-[2-(diphenylmethoxy)ethyl]-4-(3-phenylpropyl)piperazines: synthesis and evaluation as dopamine transporter ligands. |
| AID52195 | Binding affinity was determined against cocaine receptor by measuring the ability of compound to displace bound [3H]-3 from rat caudate-putamen tissue | 1994 | Journal of medicinal chemistry, Nov-11, Volume: 37, Issue:23 | Synthesis, cocaine receptor affinity, and dopamine uptake inhibition of several new 2 beta-substituted 3 beta-phenyltropanes. |
| 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. |
| AID230710 | Ratio of affinity for Norepinephrine transporter to that of dopamine transporter | 2004 | Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12 | Synthesis, molecular modeling, and biological studies of novel piperidine-based analogues of cocaine: evidence of unfavorable interactions proximal to the 3alpha-position of the piperidine ring. |
| AID127135 | Peak striatal uptake in baboon expressed as percentage of injected dose per mL of tissue. | 1992 | Journal of medicinal chemistry, Jun-12, Volume: 35, Issue:12 | Synthesis of carbon-11 labeled iodinated cocaine derivatives and their distribution in baboon brain measured using positron emission tomography. |
| AID204358 | Inhibition of [3H]5-HT reuptake at rat serotonin transporter | 1996 | Journal of medicinal chemistry, Nov-22, Volume: 39, Issue:24 | Development of novel, potent, and selective dopamine reuptake inhibitors through alteration of the piperazine ring of 1-[2-(diphenylmethoxy)ethyl]-and 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazines (GBR 12935 and GBR 12909). |
| AID1443745 | Inhibition of recombinant human DAT expressed in HEK293 cell membranes assessed as reduction in [3H]-DA uptake incubated for 22 mins by micro beta scintillation counting analysis | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | Scaffold Repurposing of Nucleosides (Adenosine Receptor Agonists): Enhanced Activity at the Human Dopamine and Norepinephrine Sodium Symporters. |
| AID147731 | Binding affinity towards norepinephrine transporter in rat striatum using [3H]nisoxetine as radioligand | 2003 | Journal of medicinal chemistry, Mar-27, Volume: 46, Issue:7 | High affinity hydroxypiperidine analogues of 4-(2-benzhydryloxyethyl)-1-(4-fluorobenzyl)piperidine for the dopamine transporter: stereospecific interactions in vitro and in vivo. |
| AID234452 | Uptake ratio at norepinephrine to serotonin transporters from rat brain | 2003 | Journal of medicinal chemistry, May-08, Volume: 46, Issue:10 | Biaryl analogues of conformationally constrained tricyclic tropanes as potent and selective norepinephrine reuptake inhibitors: synthesis and evaluation of their uptake inhibition at monoamine transporter sites. |
| AID145692 | Inhibition of [125I]RTI-55 binding to norepinephrine transporter (NET) expressed in HEK cells | 1999 | Journal of medicinal chemistry, Sep-09, Volume: 42, Issue:18 | Design, synthesis, and biological evaluation of novel non-piperazine analogues of 1-[2-(diphenylmethoxy)ethyl]- and 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazines as dopamine transporter inhibitors. |
| AID393261 | Inhibition of [3H]norepinephrine reuptake at human NET expressed in HEK cells | 2009 | Bioorganic & medicinal chemistry, Mar-01, Volume: 17, Issue:5 | 2,5-Disubstituted tetrahydrofurans as selective serotonin re-uptake inhibitors. |
| AID221398 | Tested for rate of horizontal activity during a 30-min period after administration of compound at a concentration of 5 mg/kg | 2001 | Bioorganic & medicinal chemistry letters, Dec-17, Volume: 11, Issue:24 | [3-cis-3,5-Dimethyl-(1-piperazinyl)alkyl]-bis-(4'-fluorophenyl)amine analogues as novel probes for the dopamine transporter. |
| AID275444 | Inhibition of [3H]5-HT uptake into human SERT expressing HEK293 cells | 2007 | Journal of medicinal chemistry, Jan-25, Volume: 50, Issue:2 | Slow-onset, long-duration, alkyl analogues of methylphenidate with enhanced selectivity for the dopamine transporter. |
| AID420669 | Lipophilicity, log D at pH 7.0 | 2009 | European journal of medicinal chemistry, May, Volume: 44, Issue:5 | GRIND-based 3D-QSAR and CoMFA to investigate topics dominated by hydrophobic interactions: the case of hERG K+ channel blockers. |
| AID205267 | Inhibition of binding of Batrachotoxinin [3H]BTX-B to high affinity sites on voltage dependent sodium channels in a vesicular preparation from guinea pig cerebral cortex | 1985 | Journal of medicinal chemistry, Mar, Volume: 28, Issue:3 | [3H]Batrachotoxinin A 20 alpha-benzoate binding to voltage-sensitive sodium channels: a rapid and quantitative assay for local anesthetic activity in a variety of drugs. |
| AID239218 | Displacement of [3H]nisoxetine from norepinephrine transporter of rat cerebral cortex | 2005 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 15, Issue:4 | Synthesis and monoamine transporter affinity of new 2beta-carbomethoxy-3beta-[4-(substituted thiophenyl)]phenyltropanes: discovery of a selective SERT antagonist with picomolar potency. |
| AID450269 | Displacement of [3H]-BTX-B from neuronal voltage-gated sodium channel in rat cerebral cortex synaptoneurosomes | 2009 | Bioorganic & medicinal chemistry, Oct-01, Volume: 17, Issue:19 | Ligand-based design and synthesis of novel sodium channel blockers from a combined phenytoin-lidocaine pharmacophore. |
| AID65178 | Displacement of [3H]mazindol binding to dopamine transporter (DAT) in rat synaptosomes | 2001 | Journal of medicinal chemistry, May-10, Volume: 44, Issue:10 | Pharmacological and behavioral analysis of the effects of some bivalent ligand-based monoamine reuptake inhibitors. |
| AID65327 | Binding affinity at dopamine transporter in rat brain by [3H]WIN-35428 displacement. | 2004 | Journal of medicinal chemistry, Jun-17, Volume: 47, Issue:13 | Structure-activity relationships at monoamine transporters for a series of N-substituted 3alpha-(bis[4-fluorophenyl]methoxy)tropanes: comparative molecular field analysis, synthesis, and pharmacological evaluation. |
| AID145542 | Inhibition of reuptake of [3H]-NE (20 nM) by norepinephrine transporter | 2000 | Journal of medicinal chemistry, Dec-28, Volume: 43, Issue:26 | Slow-onset, long-duration 3-(3',4'-dichlorophenyl)-1-indanamine monoamine reuptake blockers as potential medications to treat cocaine abuse. |
| AID145400 | Ability to inhibit reuptake of norepinephrine ([3H]NE) at norepinephrine transporter of rat parietal/occipital region | 2003 | Bioorganic & medicinal chemistry letters, Oct-20, Volume: 13, Issue:20 | Synthesis and pharmacological evaluation of (Z)-9-(heteroarylmethylene)-7-azatricyclo[4.3.1.0(3,7)]decanes: thiophene analogues as potent norepinephrine transporter inhibitors. |
| AID242266 | Inhibition of [3H]5-HT uptake in HEK293 cells expressing human serotonin transporter | 2005 | Journal of medicinal chemistry, Apr-21, Volume: 48, Issue:8 | Synthesis and pharmacology of ethylphenidate enantiomers: the human transesterification metabolite of methylphenidate and ethanol. |
| AID261025 | Inhibition of [3H] dopamine uptake into human DAT expressed in HEK293 cells | 2006 | Journal of medicinal chemistry, Feb-23, Volume: 49, Issue:4 | 1-(4-Methylphenyl)-2-pyrrolidin-1-yl-pentan-1-one (Pyrovalerone) analogues: a promising class of monoamine uptake inhibitors. |
| AID233749 | Discrimination ratio against DAT as ratio of IC50 to that of Ki uptake to DAT. | 2002 | Journal of medicinal chemistry, Sep-12, Volume: 45, Issue:19 | Mazindol analogues as potential inhibitors of the cocaine binding site at the dopamine transporter. |
| AID65013 | Inhibitory potency against dopamine (DA) transporter using [3H]WIN-35428 (WIN-) binding assay. | 1999 | Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23 | Synthesis and pharmacology of site-specific cocaine abuse treatment agents: 2-substituted-6-amino-5-phenylbicyclo[2.2.2]octanes. |
| AID205269 | Inhibition of binding of Batrachotoxinin [3H]BTX-B to high-affinity sites on voltage-dependent sodium channels in a vesicular preparation from guinea pig cerebral cortex at 100 uM | 1985 | Journal of medicinal chemistry, Mar, Volume: 28, Issue:3 | [3H]Batrachotoxinin A 20 alpha-benzoate binding to voltage-sensitive sodium channels: a rapid and quantitative assay for local anesthetic activity in a variety of drugs. |
| AID65354 | Inhibition of high affinity uptake of [3H]DA using rat nerve endings obtained from brain regions enriched in DAT. | 2001 | Bioorganic & medicinal chemistry letters, Aug-20, Volume: 11, Issue:16 | Sar studies of piperidine-based analogues of cocaine. Part 3: oxadiazoles. |
| AID1443744 | Enhancing of [125I]RTI-55 binding to recombinant human NET expressed in HEK293 cell membranes preincubated for 10 mins followed by radioligand addition measured after 90 mins by micro beta scintillation counting analysis | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | Scaffold Repurposing of Nucleosides (Adenosine Receptor Agonists): Enhanced Activity at the Human Dopamine and Norepinephrine Sodium Symporters. |
| AID395501 | Displacement of [125I]RTI-55 from human recombinant NET expressed in HEK293 cells by scintillation counting | 2009 | Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6 | Dual inhibitors of phosphodiesterase-4 and serotonin reuptake. |
| AID425653 | Renal clearance in human | 2009 | Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15 | Physicochemical determinants of human renal clearance. |
| AID408566 | Displacement of [3H]paroxetine from serotonin transporter | 2008 | Bioorganic & medicinal chemistry, May-15, Volume: 16, Issue:10 | Synthesis and receptor binding properties of 2beta-alkynyl and 2beta-(1,2,3-triazol)substituted 3beta-(substituted phenyl)tropane derivatives. |
| AID7940 | Percentage of tracer or metabolite (acid metabolites) in baboon plasma at 1 min after injection of the compound | 1992 | Journal of medicinal chemistry, Jun-12, Volume: 35, Issue:12 | Synthesis of carbon-11 labeled iodinated cocaine derivatives and their distribution in baboon brain measured using positron emission tomography. |
| AID232641 | Inhibition of reuptake of serotonin compared to dopamine. | 2003 | Bioorganic & medicinal chemistry letters, Oct-20, Volume: 13, Issue:20 | Synthesis and pharmacological evaluation of (Z)-9-(heteroarylmethylene)-7-azatricyclo[4.3.1.0(3,7)]decanes: thiophene analogues as potent norepinephrine transporter inhibitors. |
| AID204212 | Ratio of uptake inhibition to binding affinity to human Serotonin transporter (IC50/Ki) | 2003 | Bioorganic & medicinal chemistry letters, Jul-07, Volume: 13, Issue:13 | Bivalent biogenic amine reuptake inhibitors. |
| AID540220 | Clearance in human after iv administration | 2005 | Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7 | Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure. |
| AID65174 | Displacement of [3H]mazindol from cocaine binding site on Dopamine transporter (DAT) | 1999 | Bioorganic & medicinal chemistry letters, Dec-06, Volume: 9, Issue:23 | N-phenylalkyl-substituted tropane analogs of boat conformation with high selectivity for the dopamine versus serotonin transporter. |
| AID29925 | Volume of distribution in man (IV dose) | 2002 | Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13 | Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data. |
| AID204383 | Inhibitory activity against radioligand [3H]paroxetine binding at the serotonin transporter | 1998 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 8, Issue:24 | Synthesis and transporter binding properties of (R)-2 beta, 3 beta- and (R)-2 alpha, 3 alpha-diaryltropanes. |
| AID145557 | Inhibition of [3H]norepinephrine uptake in HEK cells expressing human NET | 2003 | Bioorganic & medicinal chemistry letters, Nov-17, Volume: 13, Issue:22 | Synthesis and biological activity of 2-carbomethoxy-3-catechol-8-azabicyclo[3.2.1]octanes. |
| AID65502 | Inhibition of [3H]DA binding to dopamine transporter of rat brain synaptosomes | 2000 | Bioorganic & medicinal chemistry letters, Aug-07, Volume: 10, Issue:15 | Synthesis and biological evaluation of 1-azabicyclo-[3.2.1]octanes: new dopamine transporter inhibitors. |
| AID233045 | Relative affinity for dopamine and norepinephrine transporters | 2004 | Journal of medicinal chemistry, Jun-17, Volume: 47, Issue:13 | Structure-activity relationships at monoamine transporters for a series of N-substituted 3alpha-(bis[4-fluorophenyl]methoxy)tropanes: comparative molecular field analysis, synthesis, and pharmacological evaluation. |
| AID64997 | Inhibition of high-affinity uptake of [3H]dopamine at dopamine transporter into rat striatal nerve endings (synaptosomes) | 1998 | Journal of medicinal chemistry, May-21, Volume: 41, Issue:11 | Chemistry and pharmacology of the piperidine-based analogues of cocaine. Identification of potent DAT inhibitors lacking the tropane skeleton. |
| AID450273 | Lipophilicity, log P of the compound | 2009 | Bioorganic & medicinal chemistry, Oct-01, Volume: 17, Issue:19 | Ligand-based design and synthesis of novel sodium channel blockers from a combined phenytoin-lidocaine pharmacophore. |
| AID242441 | Inhibition of [3H]norepinephrine uptake in HEK293 cells expressing human norepinephrine transporter | 2005 | Journal of medicinal chemistry, Apr-21, Volume: 48, Issue:8 | Synthesis and pharmacology of ethylphenidate enantiomers: the human transesterification metabolite of methylphenidate and ethanol. |
| AID235145 | Selectivity was measured as NET/DAT | 2001 | Bioorganic & medicinal chemistry letters, Sep-03, Volume: 11, Issue:17 | Rational design and synthesis of novel 2,5-disubstituted cis- and trans-piperidine derivatives exhibiting differential activity for the dopamine transporter. |
| AID64867 | Inhibition of [3H]WIN-35428 binding at dopamine transporter was determined | 2003 | Journal of medicinal chemistry, May-08, Volume: 46, Issue:10 | 2002 Medicinal Chemistry Division Award address: monoamine transporters and opioid receptors. Targets for addiction therapy. |
| AID229299 | Ratio of IC50 of NE(norepinephrine transporter) to IC50 of DA(dopamine transporter) | 1999 | Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23 | Synthesis and pharmacology of site-specific cocaine abuse treatment agents: 2-substituted-6-amino-5-phenylbicyclo[2.2.2]octanes. |
| AID229303 | Ratio of IC50 of [3H]-BTCP to that of [3H]DA uptake | 1993 | Journal of medicinal chemistry, Dec-10, Volume: 36, Issue:25 | Further studies of the structure-activity relationships of 1-[1-(2-benzo[b]thienyl)cyclohexyl]piperidine. Synthesis and evaluation of 1-(2-benzo[b]thienyl)-N,N-dialkylcyclohexylamines at dopamine uptake and phencyclidine binding sites. |
| AID1324604 | Inhibition of DAT (unknown origin) expressed in COS7 cells assessed as reduction in [3H]DA uptake incubated for 5 mins by beta-scintillation counting method | 2016 | Journal of medicinal chemistry, 12-08, Volume: 59, Issue:23 | Novel and High Affinity 2-[(Diphenylmethyl)sulfinyl]acetamide (Modafinil) Analogues as Atypical Dopamine Transporter Inhibitors. |
| AID65171 | Ability to inhibit high affinity reuptake of [3H]DA from dopamine transporter into nerve endings synaptosomes | 2002 | Journal of medicinal chemistry, Apr-25, Volume: 45, Issue:9 | Further studies on conformationally constrained tricyclic tropane analogues and their uptake inhibition at monoamine transporter sites: synthesis of (Z)-9-(substituted arylmethylene)-7-azatricyclo[4.3.1.0(3,7)]decanes as a novel class of serotonin transpo |
| AID233919 | Selectivity ratio for DAT binding compared to 5-HTT binding. | 2003 | Journal of medicinal chemistry, Apr-10, Volume: 46, Issue:8 | Synthesis and pharmacology of site specific cocaine abuse treatment agents: 8-substituted isotropane (3-azabicyclo[3.2.1]octane) dopamine uptake inhibitors. |
| AID281849 | Drug discrimination effect in CD Albino rat assessed as percent of rat choosing cocaine lever at 10 mg/kg, ip | 2004 | Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25 | Monoamine transporter binding, locomotor activity, and drug discrimination properties of 3-(4-substituted-phenyl)tropane-2-carboxylic acid methyl ester isomers. |
| AID281822 | Locomotor activity in CD1 mouse assessed as stimulation at 100 mg/kg, ip after 2 hrs relative to control | 2004 | Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25 | Monoamine transporter binding, locomotor activity, and drug discrimination properties of 3-(4-substituted-phenyl)tropane-2-carboxylic acid methyl ester isomers. |
| AID64996 | Inhibition of [3H]WIN-35428 binding to dopamine transporter in rat striatal membranes. | 1993 | Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23 | Analysis of cocaine receptor site ligand binding by three-dimensional Voronoi site modeling approach. |
| AID196432 | Inhibitory concentration for [3H]dopamine uptake by striatal membrane preparations in presence of 20 nM compound 43 | 2001 | Bioorganic & medicinal chemistry letters, Feb-26, Volume: 11, Issue:4 | Pharmacophore-based discovery, synthesis, and biological evaluation of 4-phenyl-1-arylalkyl piperidines as dopamine transporter inhibitors. |
| AID436602 | Selectivity ratio of Ki for NET to IC50 for DAT | 2009 | Bioorganic & medicinal chemistry, Jul-15, Volume: 17, Issue:14 | Synthesis and structure-activity relationship of 3beta-(4-alkylthio, -methylsulfinyl, and -methylsulfonylphenyl)tropane and 3beta-(4-alkylthiophenyl)nortropane derivatives for monoamine transporters. |
| AID65650 | Inhibition of [3H]cocaine binding to the dopamine transporter. | 1992 | Journal of medicinal chemistry, Mar-20, Volume: 35, Issue:6 | Cocaine receptor: biochemical characterization and structure-activity relationships of cocaine analogues at the dopamine transporter. |
| AID232820 | Ratio of Ki value for 5-HT to that of DA. | 1998 | Journal of medicinal chemistry, Dec-03, Volume: 41, Issue:25 | Synthesis and biological properties of new 2beta-alkyl- and 2beta-aryl-3-(substituted phenyl)tropane derivatives: stereochemical effect of C-3 on affinity and selectivity for neuronal dopamine and serotonin transporters. |
| AID234384 | Selectivity ratio as ratio of IC50 value against NET to that of DAT | 2002 | Journal of medicinal chemistry, Sep-12, Volume: 45, Issue:19 | Mazindol analogues as potential inhibitors of the cocaine binding site at the dopamine transporter. |
| AID451837 | Displacement of [125I]RTI-55 from human recombinant DAT expressed in HEK293 cells | 2009 | Bioorganic & medicinal chemistry, Oct-01, Volume: 17, Issue:19 | Inhibition of serotonin and norepinephrine reuptake and inhibition of phosphodiesterase by multi-target inhibitors as potential agents for depression. |
| 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. |
| AID125065 | Concentration inhibiting [3H]cocaine binding to rat striatal membranes. | 1992 | Journal of medicinal chemistry, Jun-12, Volume: 35, Issue:12 | Synthesis of carbon-11 labeled iodinated cocaine derivatives and their distribution in baboon brain measured using positron emission tomography. |
| AID64678 | Ability to displace [3H]WIN-35428 binding to dopamine transporter from rat striatal membranes | 1998 | Journal of medicinal chemistry, May-21, Volume: 41, Issue:11 | Chemistry and pharmacology of the piperidine-based analogues of cocaine. Identification of potent DAT inhibitors lacking the tropane skeleton. |
| AID234158 | Ratio of norepinephrine uptake to that of dopamine | 2000 | Journal of medicinal chemistry, Dec-28, Volume: 43, Issue:26 | Slow-onset, long-duration 3-(3',4'-dichlorophenyl)-1-indanamine monoamine reuptake blockers as potential medications to treat cocaine abuse. |
| AID1442399 | Induction of stimulus generalization in Sprague-Dawley rat trained to discriminate S(-)MCAT assessed as appropriate responding level to training drug by two lever method | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | The 2014 Philip S. Portoghese Medicinal Chemistry Lectureship: The "Phenylalkylaminome" with a Focus on Selected Drugs of Abuse. |
| AID64506 | Binding affinity against cloned human dopamine transporter using 40-80 pM [125I]RTI. | 2000 | Journal of medicinal chemistry, Dec-28, Volume: 43, Issue:26 | Slow-onset, long-duration 3-(3',4'-dichlorophenyl)-1-indanamine monoamine reuptake blockers as potential medications to treat cocaine abuse. |
| AID268243 | Effect on place preference in BALB/c mouse at 10 mg/kg measured as pre and procondition time difference | 2006 | Journal of medicinal chemistry, Jul-13, Volume: 49, Issue:14 | Development of peptidic dopamine transporter inhibitors via aromatic modification-mediated conformational restriction. |
| AID232157 | Ratio of 5-hydroxy tryptamine and norepinephrine transporter inhibition | 2000 | Bioorganic & medicinal chemistry letters, Feb-07, Volume: 10, Issue:3 | Design, synthesis and biological evaluation of 7-azatricyclodecanes: analogues of cocaine. |
| AID145704 | Binding affinity towards Norepinephrine transporter was determined using NE[3H]Nisoxetine as radioligand | 1995 | Journal of medicinal chemistry, Sep-01, Volume: 38, Issue:18 | Synthesis and ligand binding study of 3 beta-(4'-substituted phenyl)-2 beta-(heterocyclic)tropanes. |
| AID273270 | Displacement of [3H]nisoxetine from NET in Sprague-Dawley rat brain | 2006 | Journal of medicinal chemistry, Oct-19, Volume: 49, Issue:21 | Structure-activity relationship studies on a novel series of (S)-2beta-substituted 3alpha-[bis(4-fluoro- or 4-chlorophenyl)methoxy]tropane analogues for in vivo investigation. |
| AID275445 | Displacement of [125I]RTI-55 from human NET expressing HEK293 cells | 2007 | Journal of medicinal chemistry, Jan-25, Volume: 50, Issue:2 | Slow-onset, long-duration, alkyl analogues of methylphenidate with enhanced selectivity for the dopamine transporter. |
| AID147746 | Displacement of [3H]NE from Norepinephrine transporter of rat brain | 2001 | Bioorganic & medicinal chemistry letters, Aug-20, Volume: 11, Issue:16 | Sar studies of piperidine-based analogues of cocaine. Part 3: oxadiazoles. |
| AID1443748 | Enhancing of [125I]RTI-55 binding to recombinant human SERT expressed in HEK293 cell membranes preincubated for 10 mins followed by radioligand addition measured after 90 mins by micro beta scintillation counting analysis | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | Scaffold Repurposing of Nucleosides (Adenosine Receptor Agonists): Enhanced Activity at the Human Dopamine and Norepinephrine Sodium Symporters. |
| AID1443743 | Enhancing of [3H]mazindol binding to recombinant human DAT expressed in HEK293 cell membranes preincubated for 10 mins followed by radioligand addition measured after 90 mins by micro beta scintillation counting analysis | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | Scaffold Repurposing of Nucleosides (Adenosine Receptor Agonists): Enhanced Activity at the Human Dopamine and Norepinephrine Sodium Symporters. |
| AID1061889 | Displacement of [3H]BTX-B from neuronal voltage-gated sodium channel in rat cerebral cortex synaptoneurosomes after 60 mins by scintillation counting | 2014 | Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1 | A highly predictive 3D-QSAR model for binding to the voltage-gated sodium channel: design of potent new ligands. |
| AID752493 | Inhibition of [3H]dopamine uptake at human DAT expressed in HEK293 cells preincubated for 10 mins prior to substrate addition measured after 4 mins by FLIPR assay | 2013 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11 | An analysis of the synthetic tryptamines AMT and 5-MeO-DALT: emerging 'Novel Psychoactive Drugs'. |
| AID65349 | Ability to inhibit reuptake of dopamine ([3H]DA) at dopamine transporter of rat striatum | 2003 | Bioorganic & medicinal chemistry letters, Oct-20, Volume: 13, Issue:20 | Synthesis and pharmacological evaluation of (Z)-9-(heteroarylmethylene)-7-azatricyclo[4.3.1.0(3,7)]decanes: thiophene analogues as potent norepinephrine transporter inhibitors. |
| AID174461 | Percent response at dose 10 mg/kg evaluated by temporal tests in trained rats(post injection interval 30 min) | 1992 | Journal of medicinal chemistry, Dec-11, Volume: 35, Issue:25 | Structure-activity relationship studies of cocaine: replacement of the C-2 ester group by vinyl argues against H-bonding and provides an esterase-resistant, high-affinity cocaine analogue. |
| AID281817 | Locomotor activity in CD1 mouse assessed as stimulation at 30 mg/kg, ip after 1 hr relative to control | 2004 | Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25 | Monoamine transporter binding, locomotor activity, and drug discrimination properties of 3-(4-substituted-phenyl)tropane-2-carboxylic acid methyl ester isomers. |
| AID65339 | Affinity for rat dopamine transporter using [3H]WIN-35428 displacement. | 1995 | Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20 | Novel 4'-substituted and 4',4"-disubstituted 3 alpha-(diphenylmethoxy)tropane analogs as potent and selective dopamine uptake inhibitors. |
| AID444362 | Selectivity ratio of Ki for rat NET to Ki for DAT | 2009 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 19, Issue:24 | Synthesis and monoamine transporter affinity of 3alpha-arylmethoxy-3beta-arylnortropanes. |
| AID147743 | Inhibition of [3H]-NE reuptake at Norepinephrine transporter in rat parietal/occipital cortex | 2002 | Bioorganic & medicinal chemistry letters, Apr-08, Volume: 12, Issue:7 | Thiophene derivatives: a new series of potent norepinephrine and serotonin reuptake inhibitors. |
| AID65633 | In vitro ability to inhibit the [3H]WIN-35428 binding to cocaine binding site on dopamine transporter in rat striatal membranes irreversibly after three washes. | 1992 | Journal of medicinal chemistry, May-15, Volume: 35, Issue:10 | Probes for the cocaine receptor. Potentially irreversible ligands for the dopamine transporter. |
| AID179067 | Inhibition [3H]DA uptake in rat striatal synaptosomes. | 1998 | Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6 | (-)-3 beta-Substituted ecgonine methyl esters as inhibitors for cocaine binding and dopamine uptake. |
| AID63021 | Inhibition of [3H]-DA binding to Dopamine receptor in rat brain | 1998 | Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6 | (-)-3 beta-Substituted ecgonine methyl esters as inhibitors for cocaine binding and dopamine uptake. |
| AID436600 | Displacement of [3H]paroxetine from 5-HTT | 2009 | Bioorganic & medicinal chemistry, Jul-15, Volume: 17, Issue:14 | Synthesis and structure-activity relationship of 3beta-(4-alkylthio, -methylsulfinyl, and -methylsulfonylphenyl)tropane and 3beta-(4-alkylthiophenyl)nortropane derivatives for monoamine transporters. |
| AID1135266 | Inhibition of norepinephrine release in sc dosed mouse heart administered 60 mins before [3H]-norepinephrine challenge | 1977 | Journal of medicinal chemistry, May, Volume: 20, Issue:5 | N-(2,4,5-Trihydroxyphenehtyl)normetazocine, a potential irreversible inhibitor of the narcotic receptor. |
| AID1653654 | Effect on locomotor activity in mouse assessed as increase in total ambulations at 3 to 30 mg/kg, ip measured during 30 mins of 2 hrs test by open field test | |||
| AID29337 | Ionisation constant (pKa) | 2002 | Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13 | Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data. |
| AID114665 | Stimulation of locomotor activity of mice | 1997 | Journal of medicinal chemistry, Mar-14, Volume: 40, Issue:6 | Synthesis, dopamine transporter affinity, dopamine uptake inhibition, and locomotor stimulant activity of 2-substituted 3 beta-phenyltropane derivatives. |
| AID204072 | Inhibition of [3H]5-HT reuptake in HEK293 cells expressing human serotonin transporter | 2000 | Journal of medicinal chemistry, Jan-27, Volume: 43, Issue:2 | Novel 3-aminomethyl- and 4-aminopiperidine analogues of 1-[2-(diphenylmethoxy)ethyl]-4-(3-phenylpropyl)piperazines: synthesis and evaluation as dopamine transporter ligands. |
| AID239191 | Displacement of [3H]paroxetine from serotonin transporter (5-HT) of rat cerebral cortex | 2005 | Journal of medicinal chemistry, Jun-02, Volume: 48, Issue:11 | Synthesis and monoamine transporter binding properties of 3alpha-(substituted phenyl)nortropane-2beta-carboxylic acid methyl esters. Norepinephrine transporter selective compounds. |
| AID64862 | In vitro potency for inhibiting [3H]- dopamine uptake was determined | 2003 | Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14 | Structure-activity relationship comparison of (S)-2beta-substituted 3alpha-(bis[4-fluorophenyl]methoxy)tropanes and (R)-2beta-substituted 3beta-(3,4-dichlorophenyl)tropanes at the dopamine transporter. |
| AID204719 | Inhibition of 0.2 nM [3H]paroxetine binding to Serotonin transporter | 2000 | Bioorganic & medicinal chemistry letters, Nov-06, Volume: 10, Issue:21 | 3alpha-(4-Substituted phenyl)nortropane-2beta-carboxylic acid methyl esters show selective binding at the norepinephrine transporter. |
| AID273274 | Selectivity for Sprague-Dawley rat DAT over rat M1 receptor | 2006 | Journal of medicinal chemistry, Oct-19, Volume: 49, Issue:21 | Structure-activity relationship studies on a novel series of (S)-2beta-substituted 3alpha-[bis(4-fluoro- or 4-chlorophenyl)methoxy]tropane analogues for in vivo investigation. |
| AID281857 | Activity in CD1 mouse assessed as hyperactivity at 10 mg/kg, ip after 4 hrs | 2004 | Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25 | Monoamine transporter binding, locomotor activity, and drug discrimination properties of 3-(4-substituted-phenyl)tropane-2-carboxylic acid methyl ester isomers. |
| AID261027 | Inhibition of [3H] serotonin uptake into human SERT expressed in HEK293 cells | 2006 | Journal of medicinal chemistry, Feb-23, Volume: 49, Issue:4 | 1-(4-Methylphenyl)-2-pyrrolidin-1-yl-pentan-1-one (Pyrovalerone) analogues: a promising class of monoamine uptake inhibitors. |
| AID408340 | Inhibition of human ERG expressed in CHO cells by whole cell patch clamp technique | 2008 | Bioorganic & medicinal chemistry, Jun-01, Volume: 16, Issue:11 | Support vector machines classification of hERG liabilities based on atom types. |
| AID195343 | Mean responses per minute at dose 10 mg/kg evaluated by temporal tests in trained rats(post injection interval 15 min) | 1992 | Journal of medicinal chemistry, Dec-11, Volume: 35, Issue:25 | Structure-activity relationship studies of cocaine: replacement of the C-2 ester group by vinyl argues against H-bonding and provides an esterase-resistant, high-affinity cocaine analogue. |
| AID229546 | Relative affinity for norepinephrine and dopamine transporters | 1994 | Journal of medicinal chemistry, Apr-15, Volume: 37, Issue:8 | Secondary amine analogues of 3 beta-(4'-substituted phenyl)tropane-2 beta-carboxylic acid esters and N-norcocaine exhibit enhanced affinity for serotonin and norepinephrine transporters. |
| AID193343 | Degradation rate constant for dopamine transporter in striatum was determined | 2003 | Journal of medicinal chemistry, May-08, Volume: 46, Issue:10 | 2002 Medicinal Chemistry Division Award address: monoamine transporters and opioid receptors. Targets for addiction therapy. |
| AID65030 | Tested for radioligand [3H]BTCP displacement from dopamine transporter in rat forebrain | 1993 | Journal of medicinal chemistry, Dec-10, Volume: 36, Issue:25 | Further studies of the structure-activity relationships of 1-[1-(2-benzo[b]thienyl)cyclohexyl]piperidine. Synthesis and evaluation of 1-(2-benzo[b]thienyl)-N,N-dialkylcyclohexylamines at dopamine uptake and phencyclidine binding sites. |
| AID234448 | Uptake ratio Ki of dopamine relative to serotonin (5-HT) at monoamine transporter | 2002 | Journal of medicinal chemistry, Apr-25, Volume: 45, Issue:9 | Further studies on conformationally constrained tricyclic tropane analogues and their uptake inhibition at monoamine transporter sites: synthesis of (Z)-9-(substituted arylmethylene)-7-azatricyclo[4.3.1.0(3,7)]decanes as a novel class of serotonin transpo |
| AID145873 | Compound was tested for its ability to inhibit high-affinity uptake of [3H]NE into parietal and occipital cortex in rat | 2000 | Bioorganic & medicinal chemistry letters, Jul-03, Volume: 10, Issue:13 | An enantioselective synthesis and biobehavioral evaluation of 7-fluoro-3-(p-fluorophenyl)-2-propyltropanes. |
| AID283003 | Displacement of [3H]nisoxetine from NET | 2005 | Journal of medicinal chemistry, Nov-17, Volume: 48, Issue:23 | Synthesis and monoamine transporter binding properties of 2,3-diaryltropanes. |
| AID145719 | Inhibitory activity against radioligand [3H]nisoxetine binding at the norepinephrine transporter | 1998 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 8, Issue:24 | Synthesis and transporter binding properties of (R)-2 beta, 3 beta- and (R)-2 alpha, 3 alpha-diaryltropanes. |
| AID7944 | Percentage of tracer or metabolite (unchanged) in baboon plasma at 1 min after injection of the compound | 1992 | Journal of medicinal chemistry, Jun-12, Volume: 35, Issue:12 | Synthesis of carbon-11 labeled iodinated cocaine derivatives and their distribution in baboon brain measured using positron emission tomography. |
| AID229509 | Ratio of IC50 value against 5-HT to that of DA transporters | 1995 | Journal of medicinal chemistry, Jan-20, Volume: 38, Issue:2 | Cocaine and 3 beta-(4'-substituted phenyl)tropane-2 beta-carboxylic acid ester and amide analogues. New high-affinity and selective compounds for the dopamine transporter. |
| AID124565 | Stimulation of locomotor activity of mice | 1997 | Journal of medicinal chemistry, Mar-14, Volume: 40, Issue:6 | Synthesis, dopamine transporter affinity, dopamine uptake inhibition, and locomotor stimulant activity of 2-substituted 3 beta-phenyltropane derivatives. |
| AID64539 | Inhibitory activity against [3H]-Dopamine uptake from Dopamine transporter in rat caudate putamen tissue | 1996 | Journal of medicinal chemistry, Mar-29, Volume: 39, Issue:7 | Synthesis and ligand binding of eta(6)-(2beta-carbomethoxy-3beta-phenyltropane) transition metal complexes. |
| AID180282 | Inhibitory activity against [3H]dopamine uptake in rat striatal tissue | 1996 | Journal of medicinal chemistry, Mar-15, Volume: 39, Issue:6 | Synthesis and pharmacology of potential cocaine antagonists. 2. Structure-activity relationship studies of aromatic ring-substituted methylphenidate analogs. |
| AID234449 | Uptake ratio Ki of norepinephrine relative to dopamine at monoamine transporter | 2002 | Journal of medicinal chemistry, Apr-25, Volume: 45, Issue:9 | Further studies on conformationally constrained tricyclic tropane analogues and their uptake inhibition at monoamine transporter sites: synthesis of (Z)-9-(substituted arylmethylene)-7-azatricyclo[4.3.1.0(3,7)]decanes as a novel class of serotonin transpo |
| AID65318 | Binding affinity of compound on dopamine transporters of rat striated membranes using [3H]- mazindol. | 1998 | Journal of medicinal chemistry, Dec-03, Volume: 41, Issue:25 | Synthesis and biological properties of new 2beta-alkyl- and 2beta-aryl-3-(substituted phenyl)tropane derivatives: stereochemical effect of C-3 on affinity and selectivity for neuronal dopamine and serotonin transporters. |
| AID64703 | Compound was evaluated for its ability to displace [3H]WIN-35428 from dopamine transporter in rat caudate putamen tissue | 1997 | Journal of medicinal chemistry, Dec-19, Volume: 40, Issue:26 | Synthesis, structure, dopamine transporter affinity, and dopamine uptake inhibition of 6-alkyl-3-benzyl-2-[(methoxycarbonyl)methyl]tropane derivatives. |
| AID395503 | Displacement of [3H]serotonin from human recombinant SERT expressed in HEK293 cells by scintillation counting | 2009 | Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6 | Dual inhibitors of phosphodiesterase-4 and serotonin reuptake. |
| AID412236 | Lipophilicity, log P of the compound | 2009 | Bioorganic & medicinal chemistry, Jan-01, Volume: 17, Issue:1 | Comparison of benzil and trifluoromethyl ketone (TFK)-mediated carboxylesterase inhibition using classical and 3D-quantitative structure-activity relationship analysis. |
| AID7943 | Percentage of tracer or metabolite (unchanged) in baboon plasma at 10 min after injection of the compound | 1992 | Journal of medicinal chemistry, Jun-12, Volume: 35, Issue:12 | Synthesis of carbon-11 labeled iodinated cocaine derivatives and their distribution in baboon brain measured using positron emission tomography. |
| AID351888 | Inhibition of [3H]dopamine uptake at human DAT expressed in HEK293 cells | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11 | Design, synthesis, and evaluation of 10-N-substituted acridones as novel chemosensitizers in Plasmodium falciparum. |
| AID281841 | Cocaine discrimination in ip dosed CD Albino rat | 2004 | Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25 | Monoamine transporter binding, locomotor activity, and drug discrimination properties of 3-(4-substituted-phenyl)tropane-2-carboxylic acid methyl ester isomers. |
| AID229513 | Ratio of IC50 value against NE to that of DA transporters | 1995 | Journal of medicinal chemistry, Jan-20, Volume: 38, Issue:2 | Cocaine and 3 beta-(4'-substituted phenyl)tropane-2 beta-carboxylic acid ester and amide analogues. New high-affinity and selective compounds for the dopamine transporter. |
| AID65640 | Inhibition of [3H]WIN-35428 binding to dopamine transporter in rat striatal tissue | 1996 | Journal of medicinal chemistry, Mar-15, Volume: 39, Issue:6 | Synthesis and pharmacology of potential cocaine antagonists. 2. Structure-activity relationship studies of aromatic ring-substituted methylphenidate analogs. |
| AID229540 | Relative affinity for serotonin and dopamine transporters | 1994 | Journal of medicinal chemistry, Apr-15, Volume: 37, Issue:8 | Secondary amine analogues of 3 beta-(4'-substituted phenyl)tropane-2 beta-carboxylic acid esters and N-norcocaine exhibit enhanced affinity for serotonin and norepinephrine transporters. |
| AID42236 | Binding constant towards Beta-cyclodextrin at pH 7.4 in unbuffered water at 25 C in a one-to-one complex | 2000 | Bioorganic & medicinal chemistry letters, Sep-04, Volume: 10, Issue:17 | The binding of cocaine to cyclodextrins. |
| AID65028 | Tested for inhibition of radioligand [3H]dopamine (DA) uptake in rat synaptosomes | 1993 | Journal of medicinal chemistry, Dec-10, Volume: 36, Issue:25 | Further studies of the structure-activity relationships of 1-[1-(2-benzo[b]thienyl)cyclohexyl]piperidine. Synthesis and evaluation of 1-(2-benzo[b]thienyl)-N,N-dialkylcyclohexylamines at dopamine uptake and phencyclidine binding sites. |
| AID311934 | Dissociation constant, pKa of the compound | 2008 | Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2 | Identification of new functional inhibitors of acid sphingomyelinase using a structure-property-activity relation model. |
| AID147748 | Inhibition of [3H]nisoxetine binding at norepinephrine transporter was determined | 2003 | Journal of medicinal chemistry, May-08, Volume: 46, Issue:10 | 2002 Medicinal Chemistry Division Award address: monoamine transporters and opioid receptors. Targets for addiction therapy. |
| AID111614 | Percent change from vehicle in locomotor activity in mice at 56 mg/kg (ip) in 2 h | 2004 | Journal of medicinal chemistry, Jan-15, Volume: 47, Issue:2 | Synthesis, monoamine transporter binding properties, and behavioral pharmacology of a series of 3beta-(substituted phenyl)-2beta-(3'-substituted isoxazol-5-yl)tropanes. |
| AID273271 | Displacement of [3H]pirenzepine from M1 receptor in Sprague-Dawley rat brain | 2006 | Journal of medicinal chemistry, Oct-19, Volume: 49, Issue:21 | Structure-activity relationship studies on a novel series of (S)-2beta-substituted 3alpha-[bis(4-fluoro- or 4-chlorophenyl)methoxy]tropane analogues for in vivo investigation. |
| AID195341 | Mean responses per minute at dose 10 mg/kg evaluated by dose-response tests in trained rats(post injection interval 15 min) | 1992 | Journal of medicinal chemistry, Dec-11, Volume: 35, Issue:25 | Structure-activity relationship studies of cocaine: replacement of the C-2 ester group by vinyl argues against H-bonding and provides an esterase-resistant, high-affinity cocaine analogue. |
| AID233974 | Ratio of dopamine uptake to dopamine binding | 2000 | Journal of medicinal chemistry, Dec-28, Volume: 43, Issue:26 | Slow-onset, long-duration 3-(3',4'-dichlorophenyl)-1-indanamine monoamine reuptake blockers as potential medications to treat cocaine abuse. |
| AID233283 | Selectivity ratio is IC 50 value of dopamine receptor to that of serotonin 5-HT | 1993 | Journal of medicinal chemistry, Apr-02, Volume: 36, Issue:7 | Substituted 3-phenyltropane analogs of cocaine: synthesis, inhibition of binding at cocaine recognition sites, and positron emission tomography imaging. |
| AID235146 | Selectivity was measured as SERT/DAT | 2001 | Bioorganic & medicinal chemistry letters, Sep-03, Volume: 11, Issue:17 | Rational design and synthesis of novel 2,5-disubstituted cis- and trans-piperidine derivatives exhibiting differential activity for the dopamine transporter. |
| AID145712 | Inhibition of norepinephrine transporter (NET) determined using [3H]nisoxetine radioligand. | 2004 | Journal of medicinal chemistry, Jan-15, Volume: 47, Issue:2 | Synthesis, monoamine transporter binding properties, and behavioral pharmacology of a series of 3beta-(substituted phenyl)-2beta-(3'-substituted isoxazol-5-yl)tropanes. |
| AID181504 | Ability to inhibit high-affinity uptake of [3H]DA into striatal nerve endings (synaptosomes) | 2001 | Bioorganic & medicinal chemistry letters, Mar-26, Volume: 11, Issue:6 | Effects of two-carbon bridge region methoxylation of benztropine: discovery of novel chiral ligands for the dopamine transporter. |
| AID204849 | Inhibition of [3H]5-HT uptake at Serotonin transporter in rat mid brain | 2001 | Bioorganic & medicinal chemistry letters, May-07, Volume: 11, Issue:9 | Pharmacophore-based discovery of 3,4-disubstituted pyrrolidines as a novel class of monoamine transporter inhibitors. |
| AID200773 | Inhibition of high affinity re-uptake of [3H]5-HT (serotonin) into nerve ending synaptosomes | 2002 | Journal of medicinal chemistry, Apr-25, Volume: 45, Issue:9 | Further studies on conformationally constrained tricyclic tropane analogues and their uptake inhibition at monoamine transporter sites: synthesis of (Z)-9-(substituted arylmethylene)-7-azatricyclo[4.3.1.0(3,7)]decanes as a novel class of serotonin transpo |
| AID184428 | Inhibition of high affinity uptake of [3H]dopamine into nerve endings (synaptosomes) prepared from various regions of the rat brain. | 2000 | Journal of medicinal chemistry, Aug-24, Volume: 43, Issue:17 | Chemical synthesis and pharmacology of 6- and 7-hydroxylated 2-carbomethoxy-3-(p-tolyl)tropanes: antagonism of cocaine's locomotor stimulant effects. |
| AID196431 | Inhibitory concentration for [3H]-dopamine uptake by striatal membrane preparations in presence of 1000 nM compound 5 | 2001 | Bioorganic & medicinal chemistry letters, Feb-26, Volume: 11, Issue:4 | Pharmacophore-based discovery, synthesis, and biological evaluation of 4-phenyl-1-arylalkyl piperidines as dopamine transporter inhibitors. |
| AID143647 | Inhibition of [3H]NE Uptake in rat parietal/occipital cortex | 2000 | Journal of medicinal chemistry, Feb-10, Volume: 43, Issue:3 | Discovery of a novel dopamine transporter inhibitor, 4-hydroxy-1-methyl-4-(4-methylphenyl)-3-piperidyl 4-methylphenyl ketone, as a potential cocaine antagonist through 3D-database pharmacophore searching. Molecular modeling, structure-activity relationshi |
| AID281820 | Locomotor activity in CD1 mouse assessed as stimulation at 30 mg/kg, ip after 4 hrs relative to control | 2004 | Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25 | Monoamine transporter binding, locomotor activity, and drug discrimination properties of 3-(4-substituted-phenyl)tropane-2-carboxylic acid methyl ester isomers. |
| AID65008 | Inhibitory activity on dopamine transporters of rat striated membranes using [3H]- mazindol. | 1998 | Journal of medicinal chemistry, Dec-03, Volume: 41, Issue:25 | Synthesis and biological properties of new 2beta-alkyl- and 2beta-aryl-3-(substituted phenyl)tropane derivatives: stereochemical effect of C-3 on affinity and selectivity for neuronal dopamine and serotonin transporters. |
| AID174460 | Percent response at dose 10 mg/kg evaluated by temporal tests in trained rats(post injection interval 15 min) | 1992 | Journal of medicinal chemistry, Dec-11, Volume: 35, Issue:25 | Structure-activity relationship studies of cocaine: replacement of the C-2 ester group by vinyl argues against H-bonding and provides an esterase-resistant, high-affinity cocaine analogue. |
| AID412743 | Inhibition of [3H]NE from human recombinant NET expressed in HEK293 cells | 2009 | Bioorganic & medicinal chemistry, Jan-01, Volume: 17, Issue:1 | Stereoselective inhibition of serotonin re-uptake and phosphodiesterase by dual inhibitors as potential agents for depression. |
| AID204057 | Inhibition of [3H]citalopram binding to serotonin transporter (SERT) of cynomolgus monkey caudate-putamen | 1999 | Bioorganic & medicinal chemistry letters, Mar-22, Volume: 9, Issue:6 | Bicyclo[3.2.1]octanes: synthesis and inhibition of binding at the dopamine and serotonin transporters. |
| AID296171 | Displacement of [125I]RTI55 from human SERT expressed in COS1 cell membrane | 2007 | Bioorganic & medicinal chemistry, Jun-15, Volume: 15, Issue:12 | Synthesis, inhibition and binding of simple non-nitrogen inhibitors of monoamine transporters. |
| AID64853 | Inhibition of [3H]3-beta-(p-fluorophenyl)tropane-2beta-carboxylic acid methyl ester binding to Dopamine transporter in rat striatal membranes. | 1992 | Journal of medicinal chemistry, Jan, Volume: 35, Issue:1 | 2 beta-substituted analogues of cocaine. Synthesis and inhibition of binding to the cocaine receptor. |
| AID204525 | Inhibition of high affinity uptake of [3H]5-HT by serotonin transporter in nerve endings obtained from rat brain. | 2002 | Journal of medicinal chemistry, Jul-18, Volume: 45, Issue:15 | SAR studies of piperidine-based analogues of cocaine. 4. Effect of N-modification and ester replacement. |
| AID143641 | Binding affinity at the norepinephrine transporter was measured using [125I]RTI-55 as a radioligand | 2000 | Journal of medicinal chemistry, Jan-27, Volume: 43, Issue:2 | Novel 3-aminomethyl- and 4-aminopiperidine analogues of 1-[2-(diphenylmethoxy)ethyl]-4-(3-phenylpropyl)piperazines: synthesis and evaluation as dopamine transporter ligands. |
| AID64692 | Binding affinity of compound at site labeled by [3H]-cocaine in rat forebrain. | 1993 | Journal of medicinal chemistry, Apr-30, Volume: 36, Issue:9 | Synthesis and biological evaluation of 1-[1-(2-benzo[b]thienyl)cyclohexyl]piperidine homologues at dopamine-uptake and phencyclidine- and sigma-binding sites. |
| AID200913 | Binding affinity against cloned serotonin human transporter using 40-80 PM [125I]RTI | 2000 | Journal of medicinal chemistry, Dec-28, Volume: 43, Issue:26 | Slow-onset, long-duration 3-(3',4'-dichlorophenyl)-1-indanamine monoamine reuptake blockers as potential medications to treat cocaine abuse. |
| AID195342 | Mean responses per minute at dose 10 mg/kg evaluated by temporal tests in trained rats(post injection interval 120 min) | 1992 | Journal of medicinal chemistry, Dec-11, Volume: 35, Issue:25 | Structure-activity relationship studies of cocaine: replacement of the C-2 ester group by vinyl argues against H-bonding and provides an esterase-resistant, high-affinity cocaine analogue. |
| AID65337 | Displacement of [3H]WIN-35428 from dopamine transporter of rat brain membrane | 2004 | Bioorganic & medicinal chemistry letters, Jun-21, Volume: 14, Issue:12 | The effect of 6-substituted-4',4"-difluorobenztropines on monoamine transporters and the muscarinic M1 receptor. |
| AID281812 | Locomotor activity in CD1 mouse assessed as stimulation at 3 mg/kg, ip after 4 hrs relative to control | 2004 | Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25 | Monoamine transporter binding, locomotor activity, and drug discrimination properties of 3-(4-substituted-phenyl)tropane-2-carboxylic acid methyl ester isomers. |
| AID147751 | Relative reuptake inhibition at norepinephrine and serotonin transporters | 2002 | Bioorganic & medicinal chemistry letters, Apr-08, Volume: 12, Issue:7 | Thiophene derivatives: a new series of potent norepinephrine and serotonin reuptake inhibitors. |
| AID238905 | Binding affinity towards norepinephrine transporter determined using [3H]nisoxetine as radioligand | 2005 | Journal of medicinal chemistry, Apr-21, Volume: 48, Issue:8 | Synthesis and monoamine transporter binding properties of 3beta-(3',4'-disubstituted phenyl)tropane-2beta-carboxylic acid methyl esters. |
| 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. |
| AID451838 | Displacement of [125I]RTI-55 from human recombinant SERT expressed in HEK293 cells | 2009 | Bioorganic & medicinal chemistry, Oct-01, Volume: 17, Issue:19 | Inhibition of serotonin and norepinephrine reuptake and inhibition of phosphodiesterase by multi-target inhibitors as potential agents for depression. |
| AID232306 | Discrimination ratio as ratio of dopamine uptake compared to WIN-35428 binding to dopamine transporter | 1996 | Journal of medicinal chemistry, Mar-15, Volume: 39, Issue:6 | Synthesis and pharmacology of potential cocaine antagonists. 2. Structure-activity relationship studies of aromatic ring-substituted methylphenidate analogs. |
| AID393259 | Displacement of [125I]RTI55 from human NET expressed in HEK cells | 2009 | Bioorganic & medicinal chemistry, Mar-01, Volume: 17, Issue:5 | 2,5-Disubstituted tetrahydrofurans as selective serotonin re-uptake inhibitors. |
| AID145370 | Compound was tested for inhibition of [125I]-RTI-55 binding to norepinephrine transporter HEK cells | 2003 | Bioorganic & medicinal chemistry letters, Jul-07, Volume: 13, Issue:13 | Bivalent biogenic amine reuptake inhibitors. |
| AID65501 | Inhibition of [3H]- Mazindol binding to dopamine transporter of rat striatal membrane. | 2000 | Bioorganic & medicinal chemistry letters, Aug-07, Volume: 10, Issue:15 | Synthesis and biological evaluation of 1-azabicyclo-[3.2.1]octanes: new dopamine transporter inhibitors. |
| AID174289 | Drug discrimination effect of compound in rats, expressed as percent of rats choosing the cocaine lever at dose 1 mg/kg (ip) | 2004 | Journal of medicinal chemistry, Jan-15, Volume: 47, Issue:2 | Synthesis, monoamine transporter binding properties, and behavioral pharmacology of a series of 3beta-(substituted phenyl)-2beta-(3'-substituted isoxazol-5-yl)tropanes. |
| AID281845 | Drug discrimination effect in CD Albino rat assessed as percent of rat choosing cocaine lever at 1 mg/kg, ip | 2004 | Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25 | Monoamine transporter binding, locomotor activity, and drug discrimination properties of 3-(4-substituted-phenyl)tropane-2-carboxylic acid methyl ester isomers. |
| AID456232 | Activity at human recombinant CES1 expressed in baculovirus-infected Spodoptera frugiperda Sf21 cells assessed as substrate hydrolysis by fluorescence assay | 2010 | Bioorganic & medicinal chemistry, Jan-01, Volume: 18, Issue:1 | In silico prediction of human carboxylesterase-1 (hCES1) metabolism combining docking analyses and MD simulations. |
| AID281811 | Locomotor activity in CD1 mouse assessed as stimulation at 3 mg/kg, ip after 3 hrs relative to control | 2004 | Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25 | Monoamine transporter binding, locomotor activity, and drug discrimination properties of 3-(4-substituted-phenyl)tropane-2-carboxylic acid methyl ester isomers. |
| AID65340 | Inhibition of reuptake of [3H]DA at Dopamine transporter (DAT) | 2000 | Journal of medicinal chemistry, May-18, Volume: 43, Issue:10 | Novel conformationally constrained tropane analogues by 6-endo-trig radical cyclization and stille coupling - switch of activity toward the serotonin and/or norepinephrine transporter. |
| AID65644 | Inhibition of [125I]RTI-55 cocaine binding to the dopamine transporter. | 1992 | Journal of medicinal chemistry, Mar-20, Volume: 35, Issue:6 | Cocaine receptor: biochemical characterization and structure-activity relationships of cocaine analogues at the dopamine transporter. |
| AID204363 | Inhibition of serotonin Transporter Affinity against rat whole brain using [3H]paroxetine as radioligand | 1998 | Journal of medicinal chemistry, Jun-18, Volume: 41, Issue:13 | 2beta-Substituted analogues of 4'-iodococaine: synthesis and dopamine transporter binding potencies. |
| AID178197 | Effective dose in blocking conditioned avoidance responding (CAR) in the rat when administered intraperitoneally | 1989 | Journal of medicinal chemistry, May, Volume: 32, Issue:5 | Activity of aromatic substituted phenylpiperazines lacking affinity for dopamine binding sites in a preclinical test of antipsychotic efficacy. |
| AID111597 | Percent change from vehicle in locomotor activity in mice at 17 mg/kg (ip) in 1 h | 2004 | Journal of medicinal chemistry, Jan-15, Volume: 47, Issue:2 | Synthesis, monoamine transporter binding properties, and behavioral pharmacology of a series of 3beta-(substituted phenyl)-2beta-(3'-substituted isoxazol-5-yl)tropanes. |
| AID203920 | Compound was evaluated for binding affinity using [125I]RTI-55 as a radioligand in HEK-hSERT cells expressing human serotonin transporter | 2000 | Journal of medicinal chemistry, May-18, Volume: 43, Issue:10 | Novel conformationally constrained tropane analogues by 6-endo-trig radical cyclization and stille coupling - switch of activity toward the serotonin and/or norepinephrine transporter. |
| AID204526 | Ability to inhibit high affinity uptake of [3H]-5-HT at Serotonin transporter (SERT) using rat midbrain | 2004 | Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12 | Synthesis, molecular modeling, and biological studies of novel piperidine-based analogues of cocaine: evidence of unfavorable interactions proximal to the 3alpha-position of the piperidine ring. |
| AID204699 | Inhibition of [3H]5-HT reuptake at serotonin transporter in rat mid brain | 2002 | Bioorganic & medicinal chemistry letters, Apr-08, Volume: 12, Issue:7 | Thiophene derivatives: a new series of potent norepinephrine and serotonin reuptake inhibitors. |
| AID64526 | Inhibition of reuptake of [3H]DA (20 nM) by dopamine transporter | 2000 | Journal of medicinal chemistry, Dec-28, Volume: 43, Issue:26 | Slow-onset, long-duration 3-(3',4'-dichlorophenyl)-1-indanamine monoamine reuptake blockers as potential medications to treat cocaine abuse. |
| AID204094 | Compound was tested for inhibition of [125I]RTI-55 binding to Serotonin transporter in HEK cells | 2003 | Bioorganic & medicinal chemistry letters, Jul-07, Volume: 13, Issue:13 | Bivalent biogenic amine reuptake inhibitors. |
| AID64872 | Inhibition of [3H]WIN-35428 binding to dopamine (DA) transporter | 1994 | Journal of medicinal chemistry, Apr-15, Volume: 37, Issue:8 | Secondary amine analogues of 3 beta-(4'-substituted phenyl)tropane-2 beta-carboxylic acid esters and N-norcocaine exhibit enhanced affinity for serotonin and norepinephrine transporters. |
| AID540221 | Volume of distribution at steady state in human after iv administration | 2005 | Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7 | Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure. |
| AID190639 | Time during which activity returned to baseline level in rat by intraperitoneal administration | 2003 | Journal of medicinal chemistry, May-08, Volume: 46, Issue:10 | 2002 Medicinal Chemistry Division Award address: monoamine transporters and opioid receptors. Targets for addiction therapy. |
| AID28235 | Unbound fraction (plasma) | 2002 | Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13 | Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data. |
| AID147756 | Inhibition of NE uptake in HEK cells expressing human noradrenaline transporter (hNET) | 2002 | Journal of medicinal chemistry, Sep-12, Volume: 45, Issue:19 | Mazindol analogues as potential inhibitors of the cocaine binding site at the dopamine transporter. |
| AID145871 | Displacement of [3H]-nisoxatine from norepinephrine transporter of rat brain membrane | 2004 | Bioorganic & medicinal chemistry letters, Jun-21, Volume: 14, Issue:12 | The effect of 6-substituted-4',4"-difluorobenztropines on monoamine transporters and the muscarinic M1 receptor. |
| AID145728 | Ability to inhibit high affinity uptake of norepinephrine transporter into the nerve endings of rat synaptosomes using [3H]NE as a radioligand | 2001 | Journal of medicinal chemistry, May-10, Volume: 44, Issue:10 | Pharmacological and behavioral analysis of the effects of some bivalent ligand-based monoamine reuptake inhibitors. |
| AID221394 | Tested for rate of horizontal activity during a 30-min period after administration of compound at a concentration of 10 mg/kg | 2001 | Bioorganic & medicinal chemistry letters, Dec-17, Volume: 11, Issue:24 | [3-cis-3,5-Dimethyl-(1-piperazinyl)alkyl]-bis-(4'-fluorophenyl)amine analogues as novel probes for the dopamine transporter. |
| 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. |
| AID65341 | Displacement of [3H]WIN-35428 from dopamine transporter in rat caudate putamen tissue | 1997 | Journal of medicinal chemistry, Dec-19, Volume: 40, Issue:26 | Synthesis, structure, dopamine transporter affinity, and dopamine uptake inhibition of 6-alkyl-3-benzyl-2-[(methoxycarbonyl)methyl]tropane derivatives. |
| AID156830 | Tested for affinity by radioligand [3H]-TCP displacement from phencyclidine binding site (PCP) in rat homogenates | 1993 | Journal of medicinal chemistry, Dec-10, Volume: 36, Issue:25 | Further studies of the structure-activity relationships of 1-[1-(2-benzo[b]thienyl)cyclohexyl]piperidine. Synthesis and evaluation of 1-(2-benzo[b]thienyl)-N,N-dialkylcyclohexylamines at dopamine uptake and phencyclidine binding sites. |
| AID145395 | Inhibition of reuptake of [3H]-NE at Norepinephrine transporter | 2000 | Journal of medicinal chemistry, May-18, Volume: 43, Issue:10 | Novel conformationally constrained tropane analogues by 6-endo-trig radical cyclization and stille coupling - switch of activity toward the serotonin and/or norepinephrine transporter. |
| AID234450 | Uptake ratio Ki of norepinephrine relative to serotonin (5-HT) at monoamine transporter | 2002 | Journal of medicinal chemistry, Apr-25, Volume: 45, Issue:9 | Further studies on conformationally constrained tricyclic tropane analogues and their uptake inhibition at monoamine transporter sites: synthesis of (Z)-9-(substituted arylmethylene)-7-azatricyclo[4.3.1.0(3,7)]decanes as a novel class of serotonin transpo |
| AID229304 | Ratio of IC50 of [3H]cocaine to that of [3H]-DA uptake | 1993 | Journal of medicinal chemistry, Dec-10, Volume: 36, Issue:25 | Further studies of the structure-activity relationships of 1-[1-(2-benzo[b]thienyl)cyclohexyl]piperidine. Synthesis and evaluation of 1-(2-benzo[b]thienyl)-N,N-dialkylcyclohexylamines at dopamine uptake and phencyclidine binding sites. |
| AID451839 | Displacement of [125I]RTI-55 from human recombinant NET expressed in HEK293 cells by scintillation counting | 2009 | Bioorganic & medicinal chemistry, Oct-01, Volume: 17, Issue:19 | Inhibition of serotonin and norepinephrine reuptake and inhibition of phosphodiesterase by multi-target inhibitors as potential agents for depression. |
| AID111826 | Ability to reverse electroconvulsive shock induced amnesia in mice, after administering intraperitoneally at a dose of 1.25 mg/kg | 1984 | Journal of medicinal chemistry, May, Volume: 27, Issue:5 | Amnesia-reversal activity of a series of N-[(disubstituted-amino)alkyl] -2-oxo-1-pyrrolidineacetamides, including pramiracetam. |
| AID451841 | Inhibition of [3H]5HT reuptake at human SERT expressed in HEK293 cells | 2009 | Bioorganic & medicinal chemistry, Oct-01, Volume: 17, Issue:19 | Inhibition of serotonin and norepinephrine reuptake and inhibition of phosphodiesterase by multi-target inhibitors as potential agents for depression. |
| AID64503 | Displacement of [125I]RT155 binding in HEK cells expressing human DAT | 2003 | Bioorganic & medicinal chemistry letters, Nov-17, Volume: 13, Issue:22 | Synthesis and biological activity of 2-carbomethoxy-3-catechol-8-azabicyclo[3.2.1]octanes. |
| AID204867 | Relative reuptake inhibition at serotonin and dopamine transporters | 2002 | Bioorganic & medicinal chemistry letters, Apr-08, Volume: 12, Issue:7 | Thiophene derivatives: a new series of potent norepinephrine and serotonin reuptake inhibitors. |
| AID444363 | Selectivity ratio of Ki for rat NET to Ki for SERT | 2009 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 19, Issue:24 | Synthesis and monoamine transporter affinity of 3alpha-arylmethoxy-3beta-arylnortropanes. |
| AID111825 | Ability to reverse electroconvulsive shock (ECS) induced amnesia in mice, after administering intraperitoneally, at a dose of 0.63 mg/kg | 1984 | Journal of medicinal chemistry, May, Volume: 27, Issue:5 | Amnesia-reversal activity of a series of N-[(disubstituted-amino)alkyl] -2-oxo-1-pyrrolidineacetamides, including pramiracetam. |
| AID65344 | Inhibition of [3H]DA reuptake at dopamine transporter in rat striatum | 2002 | Bioorganic & medicinal chemistry letters, Apr-08, Volume: 12, Issue:7 | Thiophene derivatives: a new series of potent norepinephrine and serotonin reuptake inhibitors. |
| AID23920 | Partition coefficient value was determined from the ratio of ACD/LogD | 2003 | Journal of medicinal chemistry, Jun-19, Volume: 46, Issue:13 | Dual probes for the dopamine transporter and sigma1 receptors: novel piperazinyl alkyl-bis(4'-fluorophenyl)amine analogues as potential cocaine-abuse therapeutic agents. |
| AID1443756 | Inhibition of [125I]RTI-55 binding to recombinant human DAT expressed in HEK293 cell membranes preincubated for 10 mins followed by radioligand addition measured after 90 mins by micro beta scintillation counting analysis | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | Scaffold Repurposing of Nucleosides (Adenosine Receptor Agonists): Enhanced Activity at the Human Dopamine and Norepinephrine Sodium Symporters. |
| AID145708 | Inhibition of norepinephrine Transporter Affinity against rat whole brain using [3H]nisoxetine radioligand | 1998 | Journal of medicinal chemistry, Jun-18, Volume: 41, Issue:13 | 2beta-Substituted analogues of 4'-iodococaine: synthesis and dopamine transporter binding potencies. |
| AID204698 | Inhibition of [3H]5-HT uptake by Serotonin transporter of rat midbrain or parietal synaptosomes | 2000 | Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6 | Further SAR studies of piperidine-based analogues of cocaine. 2. Potent dopamine and serotonin reuptake inhibitors. |
| AID275446 | Inhibition of [3H]NE uptake into human NET expressing HEK293 cells | 2007 | Journal of medicinal chemistry, Jan-25, Volume: 50, Issue:2 | Slow-onset, long-duration, alkyl analogues of methylphenidate with enhanced selectivity for the dopamine transporter. |
| AID230004 | Relative binding affinity for dopamine and norepinephrine receptors | 1995 | Journal of medicinal chemistry, Jan-20, Volume: 38, Issue:2 | Cocaine and 3 beta-(4'-substituted phenyl)tropane-2 beta-carboxylic acid ester and amide analogues. New high-affinity and selective compounds for the dopamine transporter. |
| AID228689 | Discrimination ratio of compound is the ratio of inhibitory activity against [3H]dopamine uptake over [3H]WIN-35248 binding | 1999 | Journal of medicinal chemistry, Mar-11, Volume: 42, Issue:5 | Synthesis and pharmacology of site-specific cocaine abuse treatment agents: 2-(aminomethyl)-3-phenylbicyclo[2.2.2]- and -[2.2.1]alkane dopamine uptake inhibitors. |
| AID196433 | Inhibitory concentration for [3H]dopamine uptake by striatal membrane preparations in presence of 500 nM compound 5 | 2001 | Bioorganic & medicinal chemistry letters, Feb-26, Volume: 11, Issue:4 | Pharmacophore-based discovery, synthesis, and biological evaluation of 4-phenyl-1-arylalkyl piperidines as dopamine transporter inhibitors. |
| AID189631 | Time taken to produce maximal locomotor activity at 30 min period in rat by intraperitoneal administration | 2003 | Journal of medicinal chemistry, May-08, Volume: 46, Issue:10 | 2002 Medicinal Chemistry Division Award address: monoamine transporters and opioid receptors. Targets for addiction therapy. |
| AID386310 | Inhibition of 2-(aminoethyl)methanethiosulphonate hydrobromide-induced inactivation of rat SERT S277 mutant assessed as drug level causing half maximal protection from inactivation | 2007 | The Journal of biological chemistry, Oct-05, Volume: 282, Issue:40 | Ibogaine, a noncompetitive inhibitor of serotonin transport, acts by stabilizing the cytoplasm-facing state of the transporter. |
| AID64849 | Inhibition of dopamine Transporter Affinity against rat whole brain using [3H]WIN-35428 as radioligand | 1998 | Journal of medicinal chemistry, Jun-18, Volume: 41, Issue:13 | 2beta-Substituted analogues of 4'-iodococaine: synthesis and dopamine transporter binding potencies. |
| AID281819 | Locomotor activity in CD1 mouse assessed as stimulation at 30 mg/kg, ip after 3 hrs relative to control | 2004 | Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25 | Monoamine transporter binding, locomotor activity, and drug discrimination properties of 3-(4-substituted-phenyl)tropane-2-carboxylic acid methyl ester isomers. |
| AID64701 | Inhibition of [3H]WIN-35428 binding to Dopamine transporter | 1996 | Journal of medicinal chemistry, Oct-11, Volume: 39, Issue:21 | 3 alpha-(4'-substituted phenyl)tropane-2 beta-carboxylic acid methyl esters: novel ligands with high affinity and selectivity at the dopamine transporter. |
| AID114687 | Effective dose for locomotor activity in mice in the peak hour. | 2004 | Journal of medicinal chemistry, Jan-15, Volume: 47, Issue:2 | Synthesis, monoamine transporter binding properties, and behavioral pharmacology of a series of 3beta-(substituted phenyl)-2beta-(3'-substituted isoxazol-5-yl)tropanes. |
| AID196214 | Compound was evaluated for inhibition of [3H]- dopamine uptake in rat caudate - putamen tissue. | 1997 | Journal of medicinal chemistry, Mar-14, Volume: 40, Issue:6 | Synthesis, dopamine transporter affinity, dopamine uptake inhibition, and locomotor stimulant activity of 2-substituted 3 beta-phenyltropane derivatives. |
| AID196430 | Inhibitory concentration for [3H]dopamine uptake by striatal membrane preparations | 2001 | Bioorganic & medicinal chemistry letters, Feb-26, Volume: 11, Issue:4 | Pharmacophore-based discovery, synthesis, and biological evaluation of 4-phenyl-1-arylalkyl piperidines as dopamine transporter inhibitors. |
| AID65154 | Inhibition of Dopamine uptake in male Sprague-Dawley rats using [3H]DA ligand | 1999 | Journal of medicinal chemistry, Oct-21, Volume: 42, Issue:21 | Structure-activity relationships at the monoamine transporters and sigma receptors for a novel series of 9-[3-(cis-3, 5-dimethyl-1-piperazinyl)propyl]carbazole (rimcazole) analogues. |
| AID65500 | Binding affinity for dopamine transporters in rat brain tissue. | 1994 | Journal of medicinal chemistry, May-27, Volume: 37, Issue:11 | N-omega-fluoroalkyl analogs of (1R)-2 beta-carbomethoxy-3 beta-(4-iodophenyl)-tropane (beta-CIT): radiotracers for positron emission tomography and single photon emission computed tomography imaging of dopamine transporters. |
| AID238826 | Binding affinity towards serotonin transporter determined using [3H]paroxetine as radioligand | 2005 | Journal of medicinal chemistry, Apr-21, Volume: 48, Issue:8 | Synthesis and monoamine transporter binding properties of 3beta-(3',4'-disubstituted phenyl)tropane-2beta-carboxylic acid methyl esters. |
| AID395333 | Displacement of [125I]RTI-55 from human recombinant DAT expressed in HEK293 cells by scintillation counting | 2009 | Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6 | Dual inhibitors of phosphodiesterase-4 and serotonin reuptake. |
| AID65475 | Displacement of [3H]WIN-35428 from dopamine transporter of rat caudate putamen tissue | 2002 | Bioorganic & medicinal chemistry letters, Sep-02, Volume: 12, Issue:17 | Synthesis and dopamine transporter binding affinities of 3alpha-benzyl-8-(diarylmethoxyethyl)-8-azabicyclo[3.2.1]octanes. |
| AID232406 | Ratio of Ki at norepinephrine transporter and Ki at 5-HT transporter. | 2002 | Journal of medicinal chemistry, Jul-18, Volume: 45, Issue:15 | SAR studies of piperidine-based analogues of cocaine. 4. Effect of N-modification and ester replacement. |
| AID204852 | Inhibition of [3H]paroxetine binding at serotonin transporter was determined | 2003 | Journal of medicinal chemistry, May-08, Volume: 46, Issue:10 | 2002 Medicinal Chemistry Division Award address: monoamine transporters and opioid receptors. Targets for addiction therapy. |
| AID147750 | Relative reuptake inhibition at norepinephrine and dopamine transporters | 2002 | Bioorganic & medicinal chemistry letters, Apr-08, Volume: 12, Issue:7 | Thiophene derivatives: a new series of potent norepinephrine and serotonin reuptake inhibitors. |
| AID1443760 | Inhibition of [125I]RTI-55 binding to recombinant human SERT expressed in HEK293 cell membranes preincubated for 10 mins followed by radioligand addition measured after 90 mins by micro beta scintillation counting analysis | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | Scaffold Repurposing of Nucleosides (Adenosine Receptor Agonists): Enhanced Activity at the Human Dopamine and Norepinephrine Sodium Symporters. |
| AID1130115 | Inhibition of [3H]norepinephrine reuptake at norepinephrine transporter in CD Charles River albino rat brain synaptosomes after 5 mins by scintillation counting analysis | 1979 | Journal of medicinal chemistry, Jul, Volume: 22, Issue:7 | Synthesis and biological activity of cocaine analogues. 2. 6H-[2]Benzopyrano[4,3-c]pyridin-6-ones. |
| AID223443 | Effective dose on 8 hr locomotor assay in mice (value is standard error of the population of 72 independent determinations) | 2000 | Journal of medicinal chemistry, Dec-28, Volume: 43, Issue:26 | Slow-onset, long-duration 3-(3',4'-dichlorophenyl)-1-indanamine monoamine reuptake blockers as potential medications to treat cocaine abuse. |
| AID261026 | Displacement of [125I]RTI-55 from human SERT expressed in HEK293 cells | 2006 | Journal of medicinal chemistry, Feb-23, Volume: 49, Issue:4 | 1-(4-Methylphenyl)-2-pyrrolidin-1-yl-pentan-1-one (Pyrovalerone) analogues: a promising class of monoamine uptake inhibitors. |
| AID233047 | Binding affinity at DAT compared to at 5-HTT. | 2004 | Journal of medicinal chemistry, Jun-17, Volume: 47, Issue:13 | Structure-activity relationships at monoamine transporters for a series of N-substituted 3alpha-(bis[4-fluorophenyl]methoxy)tropanes: comparative molecular field analysis, synthesis, and pharmacological evaluation. |
| AID65795 | Binding Affinity to Dopamine transporter in caudate nuclei which was homogenized and incubated with [3H]mazindol. | 2000 | Journal of medicinal chemistry, Feb-10, Volume: 43, Issue:3 | Discovery of a novel dopamine transporter inhibitor, 4-hydroxy-1-methyl-4-(4-methylphenyl)-3-piperidyl 4-methylphenyl ketone, as a potential cocaine antagonist through 3D-database pharmacophore searching. Molecular modeling, structure-activity relationshi |
| AID7936 | Percentage of tracer or metabolite(EME) in baboon plasma at 1 min after injection of the compound | 1992 | Journal of medicinal chemistry, Jun-12, Volume: 35, Issue:12 | Synthesis of carbon-11 labeled iodinated cocaine derivatives and their distribution in baboon brain measured using positron emission tomography. |
| AID1142753 | Vascular activity in receptor-dependent rat mesenteric resistance artery assessed as inhibition of noradrenaline-induced contraction at 3 x 10'-6 M after 5 mins | 2014 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 24, Issue:11 | Vascular effects of diphenylmethoxypiperidine-derived dopamine uptake inhibitors. |
| AID243077 | Selectivity for inhibition of serotonin and norepinephrine transporters | 2005 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 15, Issue:4 | Synthesis and monoamine transporter affinity of new 2beta-carbomethoxy-3beta-[4-(substituted thiophenyl)]phenyltropanes: discovery of a selective SERT antagonist with picomolar potency. |
| AID234770 | Selectivity for Dopamine and Serotonin transporters | 1996 | Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2 | N-substituted analogs of 2 beta-carbomethoxy-3 beta- (4'-iodophenyl)tropane (beta-CIT) with selective affinity to dopamine or serotonin transporters in rat forebrain. |
| AID174462 | Percent response at dose 10 mg/kg evaluated by temporal tests in trained rats(post injection interval 5 min) | 1992 | Journal of medicinal chemistry, Dec-11, Volume: 35, Issue:25 | Structure-activity relationship studies of cocaine: replacement of the C-2 ester group by vinyl argues against H-bonding and provides an esterase-resistant, high-affinity cocaine analogue. |
| AID7937 | Percentage of tracer or metabolite(EME) in baboon plasma at 30 min after injection of the compound | 1992 | Journal of medicinal chemistry, Jun-12, Volume: 35, Issue:12 | Synthesis of carbon-11 labeled iodinated cocaine derivatives and their distribution in baboon brain measured using positron emission tomography. |
| AID232433 | Ratio of inhibition of reuptake of 5-hydroxytryptamine to Dopamine | 2000 | Journal of medicinal chemistry, May-18, Volume: 43, Issue:10 | Novel conformationally constrained tropane analogues by 6-endo-trig radical cyclization and stille coupling - switch of activity toward the serotonin and/or norepinephrine transporter. |
| AID145861 | Ability to inhibit high affinity uptake of [3H]NE at Norepinephrine transporter (NET) using rat brain parietal/occipital cortex | 2004 | Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12 | Synthesis, molecular modeling, and biological studies of novel piperidine-based analogues of cocaine: evidence of unfavorable interactions proximal to the 3alpha-position of the piperidine ring. |
| AID351894 | Inhibition of [3H]norepinephrine uptake at human NET expressed in HEK293 cells | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11 | Design, synthesis, and evaluation of 10-N-substituted acridones as novel chemosensitizers in Plasmodium falciparum. |
| AID281815 | Locomotor activity in CD1 mouse assessed as stimulation at 10 mg/kg, ip after 3 hrs relative to control | 2004 | Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25 | Monoamine transporter binding, locomotor activity, and drug discrimination properties of 3-(4-substituted-phenyl)tropane-2-carboxylic acid methyl ester isomers. |
| AID145717 | Inhibition of [3H]nisoxetine binding to the norepinephrine transporter in rat midbrain. | 1996 | Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20 | Synthesis and transporter binding properties of 3 beta-(4'-alkyl-, 4'-alkenyl-, and 4'-alkynylphenyl)nortropane-2 beta-carboxylic acid methyl esters: serotonin transporter selective analogs. |
| AID273273 | Selectivity for Sprague-Dawley rat DAT over NET | 2006 | Journal of medicinal chemistry, Oct-19, Volume: 49, Issue:21 | Structure-activity relationship studies on a novel series of (S)-2beta-substituted 3alpha-[bis(4-fluoro- or 4-chlorophenyl)methoxy]tropane analogues for in vivo investigation. |
| AID204377 | Inhibition of binding of [3H]citalopram to (SERT) serotonin transporter in rat striatum | 2003 | Bioorganic & medicinal chemistry letters, May-05, Volume: 13, Issue:9 | Design, synthesis, and activity of novel cis- and trans-3,6-disubstituted pyran biomimetics of 3,6-disubstituted piperidine as potential ligands for the dopamine transporter. |
| AID204375 | Inhibition of [3H]paroxetine binding to serotonin transporter in rat frontal cortex | 1996 | Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20 | Synthesis and transporter binding properties of 3 beta-(4'-alkyl-, 4'-alkenyl-, and 4'-alkynylphenyl)nortropane-2 beta-carboxylic acid methyl esters: serotonin transporter selective analogs. |
| AID273268 | Inhibition of [3H]dopamine uptake at DAT in Sprague-Dawley rat brain | 2006 | Journal of medicinal chemistry, Oct-19, Volume: 49, Issue:21 | Structure-activity relationship studies on a novel series of (S)-2beta-substituted 3alpha-[bis(4-fluoro- or 4-chlorophenyl)methoxy]tropane analogues for in vivo investigation. |
| AID204230 | Binding affinity at the Serotonin transporter in rat midbrain by inhibition of 0.5 nM [3H]-paroxetine binding | 1995 | Journal of medicinal chemistry, Jan-20, Volume: 38, Issue:2 | Cocaine and 3 beta-(4'-substituted phenyl)tropane-2 beta-carboxylic acid ester and amide analogues. New high-affinity and selective compounds for the dopamine transporter. |
| AID1442398 | Induction of stimulus generalization in Sprague-Dawley rat trained to discriminate S(+)AMPH assessed as appropriate responding level to training drug by two lever method | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | The 2014 Philip S. Portoghese Medicinal Chemistry Lectureship: The "Phenylalkylaminome" with a Focus on Selected Drugs of Abuse. |
| AID241997 | Inhibition of [3H]nisoxetine binding to norepinephrine transporter of rat cerebral cortex | 2004 | Journal of medicinal chemistry, Oct-07, Volume: 47, Issue:21 | Further structurally constrained analogues of cis-(6-benzhydrylpiperidin-3-yl)benzylamine with elucidation of bioactive conformation: discovery of 1,4-diazabicyclo[3.3.1]nonane derivatives and evaluation of their biological properties for the monoamine tr |
| AID241855 | Inhibition of [3H]citalopram binding to serotonin transporter of rat cerebral cortex | 2004 | Journal of medicinal chemistry, Oct-07, Volume: 47, Issue:21 | Further structurally constrained analogues of cis-(6-benzhydrylpiperidin-3-yl)benzylamine with elucidation of bioactive conformation: discovery of 1,4-diazabicyclo[3.3.1]nonane derivatives and evaluation of their biological properties for the monoamine tr |
| AID192875 | Number of animals(n) completing 20 responses on either lever out of the number of animals tested (N) at dose 0.62 mg/kg evaluated by dose-response tests in trained rats(post injection interval 15 min); n/N=7/7 | 1992 | Journal of medicinal chemistry, Dec-11, Volume: 35, Issue:25 | Structure-activity relationship studies of cocaine: replacement of the C-2 ester group by vinyl argues against H-bonding and provides an esterase-resistant, high-affinity cocaine analogue. |
| AID204238 | Binding potency for Serotonin transporter using [3H]- paroxetine | 1996 | Journal of medicinal chemistry, Oct-11, Volume: 39, Issue:21 | 3 alpha-(4'-substituted phenyl)tropane-2 beta-carboxylic acid methyl esters: novel ligands with high affinity and selectivity at the dopamine transporter. |
| AID221397 | Tested for rate of horizontal activity during a 30-min period after administration of compound at a concentration of 50 mg/kg | 2001 | Bioorganic & medicinal chemistry letters, Dec-17, Volume: 11, Issue:24 | [3-cis-3,5-Dimethyl-(1-piperazinyl)alkyl]-bis-(4'-fluorophenyl)amine analogues as novel probes for the dopamine transporter. |
| AID65477 | In vitro binding affinity towards dopamine transporter in rat striatal membranes by [3H]GBR-12395 displacement. | 1996 | Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2 | N-substituted analogs of 2 beta-carbomethoxy-3 beta- (4'-iodophenyl)tropane (beta-CIT) with selective affinity to dopamine or serotonin transporters in rat forebrain. |
| AID145393 | Inhibition of high affinity uptake of [3H]NE by norepinephrine transporter in nerve endings obtained from rat brain. | 2002 | Journal of medicinal chemistry, Jul-18, Volume: 45, Issue:15 | SAR studies of piperidine-based analogues of cocaine. 4. Effect of N-modification and ester replacement. |
| AID444519 | Displacement of [125I]RTI55 from cloned human NET expressed in HEK293 cells | 2009 | Journal of medicinal chemistry, Nov-12, Volume: 52, Issue:21 | Synthesis and biological evaluation of bupropion analogues as potential pharmacotherapies for cocaine addiction. |
| AID436603 | Selectivity ratio of Ki for NET to Ki for 5-HTT | 2009 | Bioorganic & medicinal chemistry, Jul-15, Volume: 17, Issue:14 | Synthesis and structure-activity relationship of 3beta-(4-alkylthio, -methylsulfinyl, and -methylsulfonylphenyl)tropane and 3beta-(4-alkylthiophenyl)nortropane derivatives for monoamine transporters. |
| AID239085 | Displacement of [3H]GBR-12935 from dopamine transporter of rat caudate-putamen | 2005 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 15, Issue:4 | Synthesis and monoamine transporter affinity of new 2beta-carbomethoxy-3beta-[4-(substituted thiophenyl)]phenyltropanes: discovery of a selective SERT antagonist with picomolar potency. |
| AID64852 | Inhibition of [3H]WIN-35248 binding to the dopamine transporter in rat striatal membranes. | 1992 | Journal of medicinal chemistry, May-15, Volume: 35, Issue:10 | Probes for the cocaine receptor. Potentially irreversible ligands for the dopamine transporter. |
| AID145537 | Inhibition of [3H]-NE uptake evaluated at the monoamine transporter (NET) | 2003 | Bioorganic & medicinal chemistry letters, Feb-10, Volume: 13, Issue:3 | Pharmacophore-based discovery of substituted pyridines as novel dopamine transporter inhibitors. |
| AID65631 | In vitro ability to inhibit the [3H]WIN-35428 binding to cocaine binding site on dopamine transporter in rat striatal membranes irreversibly after no wash. | 1992 | Journal of medicinal chemistry, May-15, Volume: 35, Issue:10 | Probes for the cocaine receptor. Potentially irreversible ligands for the dopamine transporter. |
| AID351887 | Inhibition of [3H]5HT uptake at human SERT expressed in HEK293 cells | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11 | Design, synthesis, and evaluation of 10-N-substituted acridones as novel chemosensitizers in Plasmodium falciparum. |
| AID52197 | Competitive inhibition against [3H]cocaine binding to cocaine receptor in bovine striatal tissue | 1990 | Journal of medicinal chemistry, Jul, Volume: 33, Issue:7 | Synthesis of 3-arylecgonine analogues as inhibitors of cocaine binding and dopamine uptake. |
| AID204550 | Binding affinity at serotonin transporter in rat brain by [3H]-citalopram displacement. | 2004 | Journal of medicinal chemistry, Jun-17, Volume: 47, Issue:13 | Structure-activity relationships at monoamine transporters for a series of N-substituted 3alpha-(bis[4-fluorophenyl]methoxy)tropanes: comparative molecular field analysis, synthesis, and pharmacological evaluation. |
| AID65505 | Inhibition of [3H]mazindol binding to dopamine transporter of rat striatal membranes. | 2000 | Journal of medicinal chemistry, Aug-24, Volume: 43, Issue:17 | Chemical synthesis and pharmacology of 6- and 7-hydroxylated 2-carbomethoxy-3-(p-tolyl)tropanes: antagonism of cocaine's locomotor stimulant effects. |
| AID64541 | Binding affinity towards dopamine transporter using [3H]WIN-35428 as radioligand from rat caudate putamen tissue (high affinity) | 1996 | Journal of medicinal chemistry, Mar-29, Volume: 39, Issue:7 | Synthesis and ligand binding of eta(6)-(2beta-carbomethoxy-3beta-phenyltropane) transition metal complexes. |
| AID7939 | Percentage of tracer or metabolite (acid metabolites) in baboon plasma at 10 min after injection of the compound | 1992 | Journal of medicinal chemistry, Jun-12, Volume: 35, Issue:12 | Synthesis of carbon-11 labeled iodinated cocaine derivatives and their distribution in baboon brain measured using positron emission tomography. |
| AID178035 | Effective dose for drug discrimination effect in rat (ip) | 2004 | Journal of medicinal chemistry, Jan-15, Volume: 47, Issue:2 | Synthesis, monoamine transporter binding properties, and behavioral pharmacology of a series of 3beta-(substituted phenyl)-2beta-(3'-substituted isoxazol-5-yl)tropanes. |
| AID71577 | Binding constant towards gamma-cyclodextrin | 2000 | Bioorganic & medicinal chemistry letters, Sep-04, Volume: 10, Issue:17 | The binding of cocaine to cyclodextrins. |
| AID241549 | Inhibition of [3H]WIN-35428 binding to dopamine transporter of rat striatum | 2004 | Journal of medicinal chemistry, Oct-07, Volume: 47, Issue:21 | Further structurally constrained analogues of cis-(6-benzhydrylpiperidin-3-yl)benzylamine with elucidation of bioactive conformation: discovery of 1,4-diazabicyclo[3.3.1]nonane derivatives and evaluation of their biological properties for the monoamine tr |
| AID1142754 | Vascular activity in receptor-dependent rat mesenteric resistance artery assessed as inhibition of noradrenaline-induced contraction at 3 x 10'-6 M after 5 mins relative to maximal response to KCl | 2014 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 24, Issue:11 | Vascular effects of diphenylmethoxypiperidine-derived dopamine uptake inhibitors. |
| AID384549 | Inhibition of [3H]5HT uptake in SERT | 2008 | Journal of medicinal chemistry, May-08, Volume: 51, Issue:9 | Design and synthesis of 2- and 3-substituted-3-phenylpropyl analogs of 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine and 1-[2-(diphenylmethoxy)ethyl]-4-(3-phenylpropyl)piperazine: role of amino, fluoro, hydroxyl, methoxyl, methyl, m |
| AID234385 | Selectivity ratio as ratio of IC50 value against SERT to that of DAT | 2002 | Journal of medicinal chemistry, Sep-12, Volume: 45, Issue:19 | Mazindol analogues as potential inhibitors of the cocaine binding site at the dopamine transporter. |
| AID243189 | Inhibition of partially open human voltage-gated potassium channel subunit Kv11.1 (ERG K+ channel) | 2005 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 15, Issue:6 | A two-state homology model of the hERG K+ channel: application to ligand binding. |
| AID65647 | Inhibition of [3H]WIN-35065-2 binding to the dopamine transporter. | 1992 | Journal of medicinal chemistry, Mar-20, Volume: 35, Issue:6 | Cocaine receptor: biochemical characterization and structure-activity relationships of cocaine analogues at the dopamine transporter. |
| AID145559 | Inhibition of [3H]- NE uptake in HEK cells expressing norepinephrine transporter | 1999 | Journal of medicinal chemistry, Sep-09, Volume: 42, Issue:18 | Design, synthesis, and biological evaluation of novel non-piperazine analogues of 1-[2-(diphenylmethoxy)ethyl]- and 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazines as dopamine transporter inhibitors. |
| AID145868 | Binding affinity towards norepinephrine transporter was determined using [3H]nisoxetine radioligand. | 2004 | Journal of medicinal chemistry, Jan-15, Volume: 47, Issue:2 | Synthesis, monoamine transporter binding properties, and behavioral pharmacology of a series of 3beta-(substituted phenyl)-2beta-(3'-substituted isoxazol-5-yl)tropanes. |
| 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. |
| AID174371 | The compound was evaluated for its behavioral activity i.e., locomotor arousal in rat for a dose of 3 mg/kg in time interval of 1 hour | 1994 | Journal of medicinal chemistry, May-27, Volume: 37, Issue:11 | N-omega-fluoroalkyl analogs of (1R)-2 beta-carbomethoxy-3 beta-(4-iodophenyl)-tropane (beta-CIT): radiotracers for positron emission tomography and single photon emission computed tomography imaging of dopamine transporters. |
| AID145699 | Affinity at norepinephrine transporter (NET) in rat striatum, using [3H]- nisoxatine as radioligand | 2001 | Journal of medicinal chemistry, Mar-15, Volume: 44, Issue:6 | Structure-activity relationship studies of 4-[2-(diphenylmethoxy)ethyl]-1-benzylpiperidine derivatives and their N-analogues: evaluation of O-and N-analogues and their binding to monoamine transporters. |
| AID203921 | Compound was evaluated for inhibition of [3H]5-HT uptake in HEK-hSERT cells expressing Human serotonin transporter | 2000 | Journal of medicinal chemistry, May-18, Volume: 43, Issue:10 | Novel conformationally constrained tropane analogues by 6-endo-trig radical cyclization and stille coupling - switch of activity toward the serotonin and/or norepinephrine transporter. |
| AID174453 | Percent response at dose 0.62 mg/kg evaluated by dose-response tests in trained rats(post injection interval 15 min) | 1992 | Journal of medicinal chemistry, Dec-11, Volume: 35, Issue:25 | Structure-activity relationship studies of cocaine: replacement of the C-2 ester group by vinyl argues against H-bonding and provides an esterase-resistant, high-affinity cocaine analogue. |
| AID204083 | Displacement of [125I]- RTI-55 from Serotonin transporter expressed in HEK cells | 2002 | Journal of medicinal chemistry, Sep-12, Volume: 45, Issue:19 | Mazindol analogues as potential inhibitors of the cocaine binding site at the dopamine transporter. |
| AID242144 | Displacement of [125I]-RTI-55 from Dopamine transporter expressed in HEK293 cells | 2005 | Journal of medicinal chemistry, Apr-21, Volume: 48, Issue:8 | Synthesis and pharmacology of ethylphenidate enantiomers: the human transesterification metabolite of methylphenidate and ethanol. |
| AID192994 | Number of animals(n) completing 20 responses on either lever out of the number of animals tested (N) at dose 10 mg/kg evaluated by temporal tests in trained rats(post injection interval 30 min); n/N=7/7 | 1992 | Journal of medicinal chemistry, Dec-11, Volume: 35, Issue:25 | Structure-activity relationship studies of cocaine: replacement of the C-2 ester group by vinyl argues against H-bonding and provides an esterase-resistant, high-affinity cocaine analogue. |
| AID360440 | Inhibition of [3H]dopamine uptake at human DAT M272L/1291M/R344M mutant expressed in HEK293 cells | 2007 | The Journal of biological chemistry, Mar-23, Volume: 282, Issue:12 | Localization of cocaine analog [125I]RTI 82 irreversible binding to transmembrane domain 6 of the dopamine transporter. |
| AID1324611 | Induction of locomotor activity in C57BL/6J mouse assessed as increase in traveled distance every 10 mins at 3 and 10 mg/kg, ip | 2016 | Journal of medicinal chemistry, 12-08, Volume: 59, Issue:23 | Novel and High Affinity 2-[(Diphenylmethyl)sulfinyl]acetamide (Modafinil) Analogues as Atypical Dopamine Transporter Inhibitors. |
| 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. |
| AID65328 | Binding affinity towards dopamine transporter using [3H]WIN-35428 as radioligand in rat caudate-putamen tissue | 1998 | Journal of medicinal chemistry, Jun-18, Volume: 41, Issue:13 | Synthesis and dopamine transporter affinity of the four stereoisomers of (+/-)-2-(methoxycarbonyl)-7-methyl-3-phenyl-7-azabicyclo[2.2.1]heptane. |
| AID444525 | Antidepressant activity in ip dosed mouse assessed as time to reach peak stimulation of locomotor activity | 2009 | Journal of medicinal chemistry, Nov-12, Volume: 52, Issue:21 | Synthesis and biological evaluation of bupropion analogues as potential pharmacotherapies for cocaine addiction. |
| AID64847 | Inhibition of [3H]3-beta-(p-fluorophenyl)tropane-2beta-carboxylic acid methyl ester [3H]7a binding to Dopamine transporter of rat striatal membranes | 1992 | Journal of medicinal chemistry, Jan, Volume: 35, Issue:1 | N-modified analogues of cocaine: synthesis and inhibition of binding to the cocaine receptor. |
| AID64513 | Inhibition of [125I]RTI-55 binding at Dopamine transporter (DAT) expressed in HEK cells | 1999 | Journal of medicinal chemistry, Sep-09, Volume: 42, Issue:18 | Design, synthesis, and biological evaluation of novel non-piperazine analogues of 1-[2-(diphenylmethoxy)ethyl]- and 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazines as dopamine transporter inhibitors. |
| AID234453 | Uptake ratio at serotonin to dopamine transporters from rat brain | 2003 | Journal of medicinal chemistry, May-08, Volume: 46, Issue:10 | Biaryl analogues of conformationally constrained tricyclic tropanes as potent and selective norepinephrine reuptake inhibitors: synthesis and evaluation of their uptake inhibition at monoamine transporter sites. |
| AID7941 | Percentage of tracer or metabolite (acid metabolites) in baboon plasma at 30 min after injection of the compound | 1992 | Journal of medicinal chemistry, Jun-12, Volume: 35, Issue:12 | Synthesis of carbon-11 labeled iodinated cocaine derivatives and their distribution in baboon brain measured using positron emission tomography. |
| AID181698 | Compound was evaluated for its ability to inhibit uptake of [3H]-dopamine into rat caudate putamen tissue | 1997 | Journal of medicinal chemistry, Dec-19, Volume: 40, Issue:26 | Synthesis, structure, dopamine transporter affinity, and dopamine uptake inhibition of 6-alkyl-3-benzyl-2-[(methoxycarbonyl)methyl]tropane derivatives. |
| AID241849 | Binding affinity of compound towards dopamine transporter determined using [3H]WIN-35 428 as radioligand | 2005 | Journal of medicinal chemistry, Apr-21, Volume: 48, Issue:8 | Synthesis and monoamine transporter binding properties of 3beta-(3',4'-disubstituted phenyl)tropane-2beta-carboxylic acid methyl esters. |
| AID196928 | Compound was tested for inhibition of [3H]dopamine uptake (DAUI) in rat synaptosomes | 2004 | Journal of medicinal chemistry, Jun-17, Volume: 47, Issue:13 | Structure-activity relationships at monoamine transporters for a series of N-substituted 3alpha-(bis[4-fluorophenyl]methoxy)tropanes: comparative molecular field analysis, synthesis, and pharmacological evaluation. |
| AID204234 | Binding affinity towards Serotonin transporter was determined using 5-HT [3H]paroxetine as radioligand | 1995 | Journal of medicinal chemistry, Sep-01, Volume: 38, Issue:18 | Synthesis and ligand binding study of 3 beta-(4'-substituted phenyl)-2 beta-(heterocyclic)tropanes. |
| AID408564 | Displacement of [3H]WIN-35428 from dopamine transporter | 2008 | Bioorganic & medicinal chemistry, May-15, Volume: 16, Issue:10 | Synthesis and receptor binding properties of 2beta-alkynyl and 2beta-(1,2,3-triazol)substituted 3beta-(substituted phenyl)tropane derivatives. |
| AID7938 | Percentage of tracer or metabolite(EME) in baboon plasma at 5 min after injection of the compound | 1992 | Journal of medicinal chemistry, Jun-12, Volume: 35, Issue:12 | Synthesis of carbon-11 labeled iodinated cocaine derivatives and their distribution in baboon brain measured using positron emission tomography. |
| AID752491 | Inhibition of [3H]5-HT uptake at human SERT expressed in HEK293 cells preincubated for 10 mins prior to substrate addition measured after 4 mins by FLIPR assay | 2013 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11 | An analysis of the synthetic tryptamines AMT and 5-MeO-DALT: emerging 'Novel Psychoactive Drugs'. |
| AID64367 | Inhibition of [3H]dopamine uptake in HEK cells expressing human Dopamine transporter | 2000 | Bioorganic & medicinal chemistry letters, Feb-07, Volume: 10, Issue:3 | Design, synthesis and biological evaluation of 7-azatricyclodecanes: analogues of cocaine. |
| AID52204 | Binding inhibition of [3H]-cocaine to cocaine receptor in rat brain | 1998 | Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6 | (-)-3 beta-Substituted ecgonine methyl esters as inhibitors for cocaine binding and dopamine uptake. |
| AID233751 | Discrimination ratio against SERT as ratio of IC50 to that of Ki uptake to SERT. | 2002 | Journal of medicinal chemistry, Sep-12, Volume: 45, Issue:19 | Mazindol analogues as potential inhibitors of the cocaine binding site at the dopamine transporter. |
| AID233044 | Binding affinity at DAT compared to at M1 receptor. | 2004 | Journal of medicinal chemistry, Jun-17, Volume: 47, Issue:13 | Structure-activity relationships at monoamine transporters for a series of N-substituted 3alpha-(bis[4-fluorophenyl]methoxy)tropanes: comparative molecular field analysis, synthesis, and pharmacological evaluation. |
| AID239454 | Displacement of [3H]nisoxetine from norepinephrine transporter (NET) of rat cerebral cortex | 2005 | Journal of medicinal chemistry, Jun-02, Volume: 48, Issue:11 | Synthesis and monoamine transporter binding properties of 3alpha-(substituted phenyl)nortropane-2beta-carboxylic acid methyl esters. Norepinephrine transporter selective compounds. |
| AID268232 | Inhibition of rat SERT-mediated serotonin uptake in CHO cells | 2006 | Journal of medicinal chemistry, Jul-13, Volume: 49, Issue:14 | Development of peptidic dopamine transporter inhibitors via aromatic modification-mediated conformational restriction. |
| AID204372 | Inhibitory concentration required to inhibit serotonin transporter 5-HTT was determined by using [3H]paroxetine radioligand | 2004 | Journal of medicinal chemistry, Jan-15, Volume: 47, Issue:2 | Synthesis, monoamine transporter binding properties, and behavioral pharmacology of a series of 3beta-(substituted phenyl)-2beta-(3'-substituted isoxazol-5-yl)tropanes. |
| AID412738 | Displacement of [125I]RTI55 from human recombinant DAT expressed in HEK293 cells | 2009 | Bioorganic & medicinal chemistry, Jan-01, Volume: 17, Issue:1 | Stereoselective inhibition of serotonin re-uptake and phosphodiesterase by dual inhibitors as potential agents for depression. |
| AID281805 | Displacement of [3H]WIN-35428 from DAT | 2004 | Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25 | Monoamine transporter binding, locomotor activity, and drug discrimination properties of 3-(4-substituted-phenyl)tropane-2-carboxylic acid methyl ester isomers. |
| AID64530 | Ratio of uptake inhibition to binding affinity to human Dopamine transporter (IC50/Ki) | 2003 | Bioorganic & medicinal chemistry letters, Jul-07, Volume: 13, Issue:13 | Bivalent biogenic amine reuptake inhibitors. |
| AID193667 | Half life of recovery for dopamine transporter in striatum was determined | 2003 | Journal of medicinal chemistry, May-08, Volume: 46, Issue:10 | 2002 Medicinal Chemistry Division Award address: monoamine transporters and opioid receptors. Targets for addiction therapy. |
| AID255050 | Displacement of [125I]RTI-55 dopamine transporter binding in rat striatal membrane | 2005 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 15, Issue:22 | The synthesis and biological evaluation of dopamine transporter inhibiting activity of substituted diphenylmethoxypiperidines. |
| AID595990 | Displacement of [3H]-(+)-pentazocine from sigma 1 receptor in guinea pig brain membranes after 150 mins in presence of 1 mM to 250 uM of phenytoin | 2011 | Journal of medicinal chemistry, May-26, Volume: 54, Issue:10 | Novel potent and selective σ ligands: evaluation of their agonist and antagonist properties. |
| AID196581 | Compound was tested to inhibit high affinity uptake of [3H]- -Dopamine into striatal nerve endings (synaptosomes) | 1994 | Journal of medicinal chemistry, Sep-30, Volume: 37, Issue:20 | Structure-activity relationship studies of N-sulfonyl analogs of cocaine: role of ionic interaction in cocaine binding. |
| AID52199 | Inhibitory effect of [3H]cocaine binding when pre incubation was conducted under ultraviolet light | 1994 | Journal of medicinal chemistry, Jul-08, Volume: 37, Issue:14 | Synthesis of substituted 3-carbamoylecgonine methyl ester analogues: irreversible and photoaffinity ligands for the cocaine receptor/dopamine transporter. |
| AID395502 | Displacement of [3H]dopamine from human recombinant DAT expressed in HEK293 cells by scintillation counting | 2009 | Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6 | Dual inhibitors of phosphodiesterase-4 and serotonin reuptake. |
| AID232104 | Ratio of binding affinities for dopamine transporter over sigma-1 receptor | 2003 | Journal of medicinal chemistry, Jun-19, Volume: 46, Issue:13 | Dual probes for the dopamine transporter and sigma1 receptors: novel piperazinyl alkyl-bis(4'-fluorophenyl)amine analogues as potential cocaine-abuse therapeutic agents. |
| AID19424 | Partition coefficient (logD7.4) | 2001 | Journal of medicinal chemistry, Jul-19, Volume: 44, Issue:15 | ElogD(oct): a tool for lipophilicity determination in drug discovery. 2. Basic and neutral compounds. |
| AID145866 | Displacement of [3H]nisoxetine from norepinephrine transporter (NET) of rat brain | 2004 | Journal of medicinal chemistry, Jun-17, Volume: 47, Issue:13 | Structure-activity relationships at monoamine transporters for a series of N-substituted 3alpha-(bis[4-fluorophenyl]methoxy)tropanes: comparative molecular field analysis, synthesis, and pharmacological evaluation. |
| AID192996 | Number of animals(n) completing 20 responses on either lever out of the number of animals tested (N) at dose 10 mg/kg evaluated by temporal tests in trained rats(post injection interval 60 min); n/N=7/7 | 1992 | Journal of medicinal chemistry, Dec-11, Volume: 35, Issue:25 | Structure-activity relationship studies of cocaine: replacement of the C-2 ester group by vinyl argues against H-bonding and provides an esterase-resistant, high-affinity cocaine analogue. |
| AID195348 | Mean responses per minute at dose 5 mg/kg evaluated by dose-response tests in trained rats(post injection interval 15 min) | 1992 | Journal of medicinal chemistry, Dec-11, Volume: 35, Issue:25 | Structure-activity relationship studies of cocaine: replacement of the C-2 ester group by vinyl argues against H-bonding and provides an esterase-resistant, high-affinity cocaine analogue. |
| AID273267 | Displacement of [3H]WIN-35428 from DAT in Sprague-Dawley rat brain | 2006 | Journal of medicinal chemistry, Oct-19, Volume: 49, Issue:21 | Structure-activity relationship studies on a novel series of (S)-2beta-substituted 3alpha-[bis(4-fluoro- or 4-chlorophenyl)methoxy]tropane analogues for in vivo investigation. |
| AID147733 | Binding affinity at the norepinephrine transporter in rat striatum by [3H]nisoxetine displacement. | 2003 | Journal of medicinal chemistry, May-22, Volume: 46, Issue:11 | Interaction of cis-(6-benzhydrylpiperidin-3-yl)benzylamine analogues with monoamine transporters: structure-activity relationship study of structurally constrained 3,6-disubstituted piperidine analogues of (2,2-diphenylethyl)-[1-(4-fluorobenzyl)piperidin- |
| AID233750 | Discrimination ratio against NET as ratio of IC50 to that of Ki uptake to NET. | 2002 | Journal of medicinal chemistry, Sep-12, Volume: 45, Issue:19 | Mazindol analogues as potential inhibitors of the cocaine binding site at the dopamine transporter. |
| AID7935 | Percentage of tracer or metabolite(EME) in baboon plasma at 10 min after injection of the compound | 1992 | Journal of medicinal chemistry, Jun-12, Volume: 35, Issue:12 | Synthesis of carbon-11 labeled iodinated cocaine derivatives and their distribution in baboon brain measured using positron emission tomography. |
| AID65824 | Inhibition of high affinity DA uptake into rat synaptosomes using [3H]DA | 2001 | Journal of medicinal chemistry, May-10, Volume: 44, Issue:10 | Pharmacological and behavioral analysis of the effects of some bivalent ligand-based monoamine reuptake inhibitors. |
| AID177070 | Compound was evaluated for dose-response in trained rats and expressed as effective dose(post injection interval 15 min) | 1992 | Journal of medicinal chemistry, Dec-11, Volume: 35, Issue:25 | Structure-activity relationship studies of cocaine: replacement of the C-2 ester group by vinyl argues against H-bonding and provides an esterase-resistant, high-affinity cocaine analogue. |
| AID242265 | Displacement of [125I]RTI-55 from human Norepinephrine transporter expressed in HEK293 cells | 2005 | Journal of medicinal chemistry, Apr-21, Volume: 48, Issue:8 | Synthesis and pharmacology of ethylphenidate enantiomers: the human transesterification metabolite of methylphenidate and ethanol. |
| AID268233 | Inhibition of mouse GAT1-mediated gamma-aminobutyric acid uptake in CHO cells | 2006 | Journal of medicinal chemistry, Jul-13, Volume: 49, Issue:14 | Development of peptidic dopamine transporter inhibitors via aromatic modification-mediated conformational restriction. |
| AID681641 | TP_TRANSPORTER: inhibition of Dopamine uptake (Dopamine: 0.1 uM, Cocaine: 1 uM) in OCT2-expressing HEK293 cells | 1998 | The Journal of biological chemistry, Nov-20, Volume: 273, Issue:47 | Transport of monoamine transmitters by the organic cation transporter type 2, OCT2. |
| AID412741 | Inhibition of [3H]DA from human recombinant DAT expressed in HEK293 cells | 2009 | Bioorganic & medicinal chemistry, Jan-01, Volume: 17, Issue:1 | Stereoselective inhibition of serotonin re-uptake and phosphodiesterase by dual inhibitors as potential agents for depression. |
| AID540219 | Volume of distribution at steady state in monkey after iv administration | 2005 | Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7 | Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure. |
| AID239125 | Displacement of [3H]paroxetine from serotonin transporter of rat cerebral cortex | 2005 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 15, Issue:4 | Synthesis and monoamine transporter affinity of new 2beta-carbomethoxy-3beta-[4-(substituted thiophenyl)]phenyltropanes: discovery of a selective SERT antagonist with picomolar potency. |
| AID204084 | Displacement of [125I]RT155 binding in HEK cells expressing human SERT | 2003 | Bioorganic & medicinal chemistry letters, Nov-17, Volume: 13, Issue:22 | Synthesis and biological activity of 2-carbomethoxy-3-catechol-8-azabicyclo[3.2.1]octanes. |
| AID540214 | Clearance in rat after iv administration | 2005 | Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7 | Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure. |
| AID174457 | Percent response at dose 1.25 mg/kg evaluated by dose-response tests in trained rats(post injection interval 15 min) | 1992 | Journal of medicinal chemistry, Dec-11, Volume: 35, Issue:25 | Structure-activity relationship studies of cocaine: replacement of the C-2 ester group by vinyl argues against H-bonding and provides an esterase-resistant, high-affinity cocaine analogue. |
| AID235154 | Selectivity of uptake of 5-HT to DA | 1999 | Bioorganic & medicinal chemistry letters, Dec-06, Volume: 9, Issue:23 | N-phenylalkyl-substituted tropane analogs of boat conformation with high selectivity for the dopamine versus serotonin transporter. |
| AID229006 | Ability to inhibit [3H]citalopram binding to serotonin transporter in cynomolgus monkey striatum | 1993 | Journal of medicinal chemistry, Apr-02, Volume: 36, Issue:7 | Substituted 3-phenyltropane analogs of cocaine: synthesis, inhibition of binding at cocaine recognition sites, and positron emission tomography imaging. |
| AID275441 | Displacement of [125I]RTI-55 from human DAT expressing HEK293 cells | 2007 | Journal of medicinal chemistry, Jan-25, Volume: 50, Issue:2 | Slow-onset, long-duration, alkyl analogues of methylphenidate with enhanced selectivity for the dopamine transporter. |
| AID187153 | Compound tested for inhibitory activity against [3H]dopamine uptake in synaptosomes from rat caudate nucleus | 1993 | Journal of medicinal chemistry, Nov-26, Volume: 36, Issue:24 | Methoxylation of cocaine reduces binding affinity and produces compounds of differential binding and dopamine uptake inhibitory activity: discovery of a weak cocaine "antagonist". |
| AID393258 | Displacement of [125I]RTI55 from human SERT expressed in HEK cells | 2009 | Bioorganic & medicinal chemistry, Mar-01, Volume: 17, Issue:5 | 2,5-Disubstituted tetrahydrofurans as selective serotonin re-uptake inhibitors. |
| AID239641 | Inhibition of high affinity uptake by the serotonin transporter (5-HT) from rat synaptosomal nerve endings by using [3H]5-HT as radioligand | 2004 | Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24 | Piperidine-based nocaine/modafinil hybrid ligands as highly potent monoamine transporter inhibitors: efficient drug discovery by rational lead hybridization. |
| AID28236 | Unbound fraction (tissues) | 2002 | Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13 | Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data. |
| AID540217 | Volume of distribution at steady state in dog after iv administration | 2005 | Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7 | Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure. |
| AID204882 | Inhibition of [3H]-5-HT uptake evaluated at the Serotonin transporter | 2003 | Bioorganic & medicinal chemistry letters, Feb-10, Volume: 13, Issue:3 | Pharmacophore-based discovery of substituted pyridines as novel dopamine transporter inhibitors. |
| AID229306 | Ratio of IC50 of [3H]cocaine to that of dopamine | 1993 | Journal of medicinal chemistry, Apr-30, Volume: 36, Issue:9 | Synthesis and biological evaluation of 1-[1-(2-benzo[b]thienyl)cyclohexyl]piperidine homologues at dopamine-uptake and phencyclidine- and sigma-binding sites. |
| AID64868 | Inhibition of [3H]WIN-35428 binding to Dopamine transporter in rat striatal synaptic membranes | 2001 | Bioorganic & medicinal chemistry letters, Dec-03, Volume: 11, Issue:23 | Synthesis and binding affinities of 2 beta-(3-iodoallyloxycarbonyl)-3 beta-(4-substituted-aryl)tropane analogues as ligands for the dopamine transporter studies. |
| AID281809 | Locomotor activity in CD1 mouse assessed as stimulation at 3 mg/kg, ip after 1 hr relative to control | 2004 | Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25 | Monoamine transporter binding, locomotor activity, and drug discrimination properties of 3-(4-substituted-phenyl)tropane-2-carboxylic acid methyl ester isomers. |
| AID256094 | Locomotor activity in mice after intraperitoneal administration at 17.8 lmol/kg | 2005 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 15, Issue:22 | The synthesis and biological evaluation of dopamine transporter inhibiting activity of substituted diphenylmethoxypiperidines. |
| AID233343 | Value is difference between the cocaine binding and DA uptake | 1998 | Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6 | (-)-3 beta-Substituted ecgonine methyl esters as inhibitors for cocaine binding and dopamine uptake. |
| AID111599 | Percent change from vehicle in locomotor activity in mice at 17 mg/kg (ip) in 3 h | 2004 | Journal of medicinal chemistry, Jan-15, Volume: 47, Issue:2 | Synthesis, monoamine transporter binding properties, and behavioral pharmacology of a series of 3beta-(substituted phenyl)-2beta-(3'-substituted isoxazol-5-yl)tropanes. |
| AID281874 | Activity in CD1 mouse assessed as convulsions at 100 mg/kg, ip after 4 hrs | 2004 | Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25 | Monoamine transporter binding, locomotor activity, and drug discrimination properties of 3-(4-substituted-phenyl)tropane-2-carboxylic acid methyl ester isomers. |
| AID195344 | Mean responses per minute at dose 10 mg/kg evaluated by temporal tests in trained rats(post injection interval 30 min) | 1992 | Journal of medicinal chemistry, Dec-11, Volume: 35, Issue:25 | Structure-activity relationship studies of cocaine: replacement of the C-2 ester group by vinyl argues against H-bonding and provides an esterase-resistant, high-affinity cocaine analogue. |
| AID72313 | Affinity against recombinant Gamma-aminobutyric acid A (GABA-A) receptor | 2000 | Journal of medicinal chemistry, Apr-20, Volume: 43, Issue:8 | GABA-Activated ligand gated ion channels: medicinal chemistry and molecular biology. |
| AID65509 | Binding affinity against dopamine transporter in rat caudate putamen tissue using [3H]WIN-35428 radioligand. (from other reference) | 1996 | Journal of medicinal chemistry, Nov-22, Volume: 39, Issue:24 | Synthesis and dopamine transporter affinity of 2-(methoxycarbonyl)-9-methyl-3-phenyl-9-azabicyclo[3.3.1]nonane derivatives. |
| AID218789 | Inhibition of [3H]DA uptake by dopamine transporter of rat striata synaptosomes | 2000 | Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6 | Further SAR studies of piperidine-based analogues of cocaine. 2. Potent dopamine and serotonin reuptake inhibitors. |
| AID195340 | Mean responses per minute at dose 1.25 mg/kg evaluated by dose-response tests in trained rats(post injection interval 15 min) | 1992 | Journal of medicinal chemistry, Dec-11, Volume: 35, Issue:25 | Structure-activity relationship studies of cocaine: replacement of the C-2 ester group by vinyl argues against H-bonding and provides an esterase-resistant, high-affinity cocaine analogue. |
| AID145373 | Ratio of uptake inhibition to binding affinity to human Norepinephrine transporter (IC50/Ki) | 2003 | Bioorganic & medicinal chemistry letters, Jul-07, Volume: 13, Issue:13 | Bivalent biogenic amine reuptake inhibitors. |
| AID61819 | Compound was evaluated for inhibition of [3H]DA uptake in HEK-hDAT cells expressing Human dopamine Transporter | 2000 | Journal of medicinal chemistry, May-18, Volume: 43, Issue:10 | Novel conformationally constrained tropane analogues by 6-endo-trig radical cyclization and stille coupling - switch of activity toward the serotonin and/or norepinephrine transporter. |
| AID192881 | Number of animals(n) completing 20 responses on either lever out of the number of animals tested (N) at dose 10 mg/kg evaluated by temporal tests in trained rats(post injection interval 120 min); n/N=7/7 | 1992 | Journal of medicinal chemistry, Dec-11, Volume: 35, Issue:25 | Structure-activity relationship studies of cocaine: replacement of the C-2 ester group by vinyl argues against H-bonding and provides an esterase-resistant, high-affinity cocaine analogue. |
| AID204709 | Ability to inhibit reuptake of serotonin ([3H]5-HT) at serotonin transporter of rat midbrian | 2003 | Bioorganic & medicinal chemistry letters, Oct-20, Volume: 13, Issue:20 | Synthesis and pharmacological evaluation of (Z)-9-(heteroarylmethylene)-7-azatricyclo[4.3.1.0(3,7)]decanes: thiophene analogues as potent norepinephrine transporter inhibitors. |
| AID444358 | Displacement of [3H]WIN-35428 from DAT in rat brain | 2009 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 19, Issue:24 | Synthesis and monoamine transporter affinity of 3alpha-arylmethoxy-3beta-arylnortropanes. |
| AID444657 | Effect on behavioural activity in ip dosed rat assessed as cocaine-induced lever response pretreated with cocaine by drug-discrimination studies | 2009 | Journal of medicinal chemistry, Nov-12, Volume: 52, Issue:21 | Synthesis and biological evaluation of bupropion analogues as potential pharmacotherapies for cocaine addiction. |
| AID281821 | Locomotor activity in CD1 mouse assessed as stimulation at 100 mg/kg, ip after 1 hr relative to control | 2004 | Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25 | Monoamine transporter binding, locomotor activity, and drug discrimination properties of 3-(4-substituted-phenyl)tropane-2-carboxylic acid methyl ester isomers. |
| AID196575 | Inhibition of [3H]dopamine reuptake in rat cytosol | 2001 | Bioorganic & medicinal chemistry letters, Sep-03, Volume: 11, Issue:17 | Rational design and synthesis of novel 2,5-disubstituted cis- and trans-piperidine derivatives exhibiting differential activity for the dopamine transporter. |
| AID65495 | Inhibitory constant towards reuptake of [125I]-13 from dopamine transporter in rat striatal membranes | 1994 | Journal of medicinal chemistry, May-13, Volume: 37, Issue:10 | Synthesis and characterization of radioiodinated N-(3-iodopropen-1-yl)-2 beta-carbomethoxy-3 beta-(4-chlorophenyl)tropanes: potential dopamine reuptake site imaging agents. |
| AID444517 | Displacement of [125I]RTI55 from cloned human DAT expressed in HEK293 cells | 2009 | Journal of medicinal chemistry, Nov-12, Volume: 52, Issue:21 | Synthesis and biological evaluation of bupropion analogues as potential pharmacotherapies for cocaine addiction. |
| AID181502 | Ability to inhibit [3H]dopamine uptake was measured in a chopped tissue assay | 2002 | Journal of medicinal chemistry, Mar-14, Volume: 45, Issue:6 | Synthesis and biological evaluation of 2-substituted 3beta-tolyltropane derivatives at dopamine, serotonin, and norepinephrine transporters. |
| AID204197 | Inhibition of [125I]RTI-55 binding to serotonin transporter (SERT) expressed in HEK cells | 1999 | Journal of medicinal chemistry, Sep-09, Volume: 42, Issue:18 | Design, synthesis, and biological evaluation of novel non-piperazine analogues of 1-[2-(diphenylmethoxy)ethyl]- and 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazines as dopamine transporter inhibitors. |
| AID204376 | Inhibition of [3H]paroxetine binding to 5-hydroxytryptamine (5-HT) transporter | 1994 | Journal of medicinal chemistry, Apr-15, Volume: 37, Issue:8 | Secondary amine analogues of 3 beta-(4'-substituted phenyl)tropane-2 beta-carboxylic acid esters and N-norcocaine exhibit enhanced affinity for serotonin and norepinephrine transporters. |
| AID64508 | Inhibition of [125I]RTI-55 binding to dopamine transporter | 2000 | Journal of medicinal chemistry, Jan-27, Volume: 43, Issue:2 | Novel 3-aminomethyl- and 4-aminopiperidine analogues of 1-[2-(diphenylmethoxy)ethyl]-4-(3-phenylpropyl)piperazines: synthesis and evaluation as dopamine transporter ligands. |
| AID281823 | Locomotor activity in CD1 mouse assessed as stimulation at 100 mg/kg, ip after 3 hrs relative to control | 2004 | Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25 | Monoamine transporter binding, locomotor activity, and drug discrimination properties of 3-(4-substituted-phenyl)tropane-2-carboxylic acid methyl ester isomers. |
| AID204374 | Inhibition of [3H]paroxetine binding at serotonin transporter was determined | 2003 | Journal of medicinal chemistry, May-08, Volume: 46, Issue:10 | 2002 Medicinal Chemistry Division Award address: monoamine transporters and opioid receptors. Targets for addiction therapy. |
| AID281813 | Locomotor activity in CD1 mouse assessed as stimulation at 10 mg/kg, ip after 1 hr relative to control | 2004 | Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25 | Monoamine transporter binding, locomotor activity, and drug discrimination properties of 3-(4-substituted-phenyl)tropane-2-carboxylic acid methyl ester isomers. |
| AID281814 | Locomotor activity in CD1 mouse assessed as stimulation at 10 mg/kg, ip after 2 hrs relative to control | 2004 | Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25 | Monoamine transporter binding, locomotor activity, and drug discrimination properties of 3-(4-substituted-phenyl)tropane-2-carboxylic acid methyl ester isomers. |
| AID65006 | Inhibitory activity against radioligand [3H]WIN-35428 binding at the dopamine transporter | 1998 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 8, Issue:24 | Synthesis and transporter binding properties of (R)-2 beta, 3 beta- and (R)-2 alpha, 3 alpha-diaryltropanes. |
| AID29423 | HPLC capacity factor (k') | 2002 | Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13 | Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data. |
| AID145365 | Displacement of [125I]RT155 binding in HEK cells expressing human NET | 2003 | Bioorganic & medicinal chemistry letters, Nov-17, Volume: 13, Issue:22 | Synthesis and biological activity of 2-carbomethoxy-3-catechol-8-azabicyclo[3.2.1]octanes. |
| AID1443752 | Inhibition of mouse DAT expressed in HEK293 cells assessed as reduction in [3H]-DA uptake | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | Scaffold Repurposing of Nucleosides (Adenosine Receptor Agonists): Enhanced Activity at the Human Dopamine and Norepinephrine Sodium Symporters. |
| AID111830 | Ability to reverse electroconvulsive shock induced amnesia in mice, after administering intraperitoneally at a dose of 2.5 mg/kg | 1984 | Journal of medicinal chemistry, May, Volume: 27, Issue:5 | Amnesia-reversal activity of a series of N-[(disubstituted-amino)alkyl] -2-oxo-1-pyrrolidineacetamides, including pramiracetam. |
| AID283002 | Displacement of [3H]WIN-35428 from DAT | 2005 | Journal of medicinal chemistry, Nov-17, Volume: 48, Issue:23 | Synthesis and monoamine transporter binding properties of 2,3-diaryltropanes. |
| AID229515 | Ratio of IC50 value against Serotonin transporter to that of dopamine transporter | 1995 | Journal of medicinal chemistry, Jan-20, Volume: 38, Issue:2 | Cocaine and 3 beta-(4'-substituted phenyl)tropane-2 beta-carboxylic acid ester and amide analogues. New high-affinity and selective compounds for the dopamine transporter. |
| AID192880 | Number of animals(n) completing 20 responses on either lever out of the number of animals tested (N) at dose 10 mg/kg evaluated by dose-response tests in trained rats(post injection interval 15 min); n/N=7/7 | 1992 | Journal of medicinal chemistry, Dec-11, Volume: 35, Issue:25 | Structure-activity relationship studies of cocaine: replacement of the C-2 ester group by vinyl argues against H-bonding and provides an esterase-resistant, high-affinity cocaine analogue. |
| AID19563 | Compound was evaluated for pseudo Hill coefficients (nH) in cynomolgus monkeys | 1991 | Journal of medicinal chemistry, May, Volume: 34, Issue:5 | Synthesis and receptor binding of N-substituted tropane derivatives. High-affinity ligands for the cocaine receptor. |
| AID444361 | Selectivity ratio of Ki for rat DAT to Ki for SERT | 2009 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 19, Issue:24 | Synthesis and monoamine transporter affinity of 3alpha-arylmethoxy-3beta-arylnortropanes. |
| AID281867 | Activity in CD1 mouse assessed as stereotypy at 100 mg/kg, ip after 4 hrs | 2004 | Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25 | Monoamine transporter binding, locomotor activity, and drug discrimination properties of 3-(4-substituted-phenyl)tropane-2-carboxylic acid methyl ester isomers. |
| AID243060 | Selectivity for inhibition of serotonin and dopamine transporters | 2005 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 15, Issue:4 | Synthesis and monoamine transporter affinity of new 2beta-carbomethoxy-3beta-[4-(substituted thiophenyl)]phenyltropanes: discovery of a selective SERT antagonist with picomolar potency. |
| AID194359 | Maximal locomotor activity of compound compared as a percent of cocaine's effect in rat by intraperitoneal administration | 2003 | Journal of medicinal chemistry, May-08, Volume: 46, Issue:10 | 2002 Medicinal Chemistry Division Award address: monoamine transporters and opioid receptors. Targets for addiction therapy. |
| AID179419 | Effect on cocaine inhibition of [3H]dopamine uptake | 1993 | Journal of medicinal chemistry, Nov-26, Volume: 36, Issue:24 | Methoxylation of cocaine reduces binding affinity and produces compounds of differential binding and dopamine uptake inhibitory activity: discovery of a weak cocaine "antagonist". |
| AID1653649 | Displacement of [3H]WIN 35428 from human DAT Y156F mutant transiently expressed in COS7 cells | |||
| AID7945 | Percentage of tracer or metabolite (unchanged) in baboon plasma at 30 min after injection of the compound | 1992 | Journal of medicinal chemistry, Jun-12, Volume: 35, Issue:12 | Synthesis of carbon-11 labeled iodinated cocaine derivatives and their distribution in baboon brain measured using positron emission tomography. |
| AID145551 | Compound was evaluated for inhibition of [3H]NE uptake in HEK-hNET cells expressing Human norepinephrine transporter | 2000 | Journal of medicinal chemistry, May-18, Volume: 43, Issue:10 | Novel conformationally constrained tropane analogues by 6-endo-trig radical cyclization and stille coupling - switch of activity toward the serotonin and/or norepinephrine transporter. |
| AID360443 | Inhibition of [3H]dopamine uptake at human DAT expressed in HEK293 cells | 2007 | The Journal of biological chemistry, Mar-23, Volume: 282, Issue:12 | Localization of cocaine analog [125I]RTI 82 irreversible binding to transmembrane domain 6 of the dopamine transporter. |
| AID42844 | Competitive inhibition against [3H]dopamine uptake in bovine striatal tissue | 1990 | Journal of medicinal chemistry, Jul, Volume: 33, Issue:7 | Synthesis of 3-arylecgonine analogues as inhibitors of cocaine binding and dopamine uptake. |
| AID64870 | Inhibition of [3H]WIN-35428 binding to rat striatal membrane dopamine transporter | 1991 | Journal of medicinal chemistry, Mar, Volume: 34, Issue:3 | Synthesis and ligand binding of cocaine isomers at the cocaine receptor. |
| AID7931 | Percentage of tracer or metabolite (CO2) in baboon plasma at 10 min after injection of the compound | 1992 | Journal of medicinal chemistry, Jun-12, Volume: 35, Issue:12 | Synthesis of carbon-11 labeled iodinated cocaine derivatives and their distribution in baboon brain measured using positron emission tomography. |
| AID65193 | Binding affinity for [3H]DA (Dopamine transporter) uptake by striated synaptosomes | 1998 | Journal of medicinal chemistry, Dec-03, Volume: 41, Issue:25 | Synthesis and biological properties of new 2beta-alkyl- and 2beta-aryl-3-(substituted phenyl)tropane derivatives: stereochemical effect of C-3 on affinity and selectivity for neuronal dopamine and serotonin transporters. |
| AID178218 | Effective dose of compound required to produce maximal locomotor activity in rat by intraperitoneal administration | 2003 | Journal of medicinal chemistry, May-08, Volume: 46, Issue:10 | 2002 Medicinal Chemistry Division Award address: monoamine transporters and opioid receptors. Targets for addiction therapy. |
| AID65490 | Inhibition of [3H]DA uptake by rat striatal dopamine transporter | 1995 | Journal of medicinal chemistry, Jan-20, Volume: 38, Issue:2 | Cocaine and 3 beta-(4'-substituted phenyl)tropane-2 beta-carboxylic acid ester and amide analogues. New high-affinity and selective compounds for the dopamine transporter. |
| AID295522 | Inhibition of [3H]dopamine uptake at DAT in Sprague-Dawley rat striatum synaptosome | 2007 | Bioorganic & medicinal chemistry, Jun-01, Volume: 15, Issue:11 | 3-{2-[Bis-(4-fluorophenyl)methoxy]ethyl}-6-substituted-3,6-diazabicyclo[3.1.1]heptanes as novel potent dopamine uptake inhibitors. |
| AID204357 | Compound was tested for binding affinity to Serotonin transporter sites in homogenates prepared from rat cortical membranes using [3H]paroxetine as radioligand | 1991 | Journal of medicinal chemistry, Oct, Volume: 34, Issue:10 | [123I]-2 beta-carbomethoxy-3 beta-(4-iodophenyl)tropane: high-affinity SPECT radiotracer of monoamine reuptake sites in brain. |
| AID451842 | Inhibition of [3H]NE reuptake at human NET expressed in HEK cells | 2009 | Bioorganic & medicinal chemistry, Oct-01, Volume: 17, Issue:19 | Inhibition of serotonin and norepinephrine reuptake and inhibition of phosphodiesterase by multi-target inhibitors as potential agents for depression. |
| AID64697 | Binding affinity towards dopamine transporter in rat striatum using [3H]WIN-35 428 as radioligand | 2003 | Journal of medicinal chemistry, Mar-27, Volume: 46, Issue:7 | High affinity hydroxypiperidine analogues of 4-(2-benzhydryloxyethyl)-1-(4-fluorobenzyl)piperidine for the dopamine transporter: stereospecific interactions in vitro and in vivo. |
| AID232436 | Ratio of inhibition of reuptake of norepinephrine to dopamine | 2000 | Journal of medicinal chemistry, May-18, Volume: 43, Issue:10 | Novel conformationally constrained tropane analogues by 6-endo-trig radical cyclization and stille coupling - switch of activity toward the serotonin and/or norepinephrine transporter. |
| 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. |
| 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. |
| AID111824 | Ability to reverse electroconvulsive shock (ECS) induced amnesia in mice, after administering intraperitoneally, at a dose of 0.31 mg/kg | 1984 | Journal of medicinal chemistry, May, Volume: 27, Issue:5 | Amnesia-reversal activity of a series of N-[(disubstituted-amino)alkyl] -2-oxo-1-pyrrolidineacetamides, including pramiracetam. |
| AID234003 | Selectivity for dopamine and serotonin transporters | 1996 | Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20 | Synthesis and transporter binding properties of 3 beta-(4'-alkyl-, 4'-alkenyl-, and 4'-alkynylphenyl)nortropane-2 beta-carboxylic acid methyl esters: serotonin transporter selective analogs. |
| AID237338 | Calculated partition coefficient (clogP) | 2004 | Journal of medicinal chemistry, Oct-07, Volume: 47, Issue:21 | Further structurally constrained analogues of cis-(6-benzhydrylpiperidin-3-yl)benzylamine with elucidation of bioactive conformation: discovery of 1,4-diazabicyclo[3.3.1]nonane derivatives and evaluation of their biological properties for the monoamine tr |
| AID1387460 | Displacement of [125I]RTI-55 from human NET expressed in HEK293 cell membranes | 2018 | Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20 | Synthesis and Discovery of Arylpiperidinylquinazolines: New Inhibitors of the Vesicular Monoamine Transporter. |
| AID204551 | Binding affinity towards serotonin transporter 5-HTT was determined using [3H]paroxetine radioligand. | 2004 | Journal of medicinal chemistry, Jan-15, Volume: 47, Issue:2 | Synthesis, monoamine transporter binding properties, and behavioral pharmacology of a series of 3beta-(substituted phenyl)-2beta-(3'-substituted isoxazol-5-yl)tropanes. |
| AID268231 | Inhibition of rat NET-mediated norepinephrine uptake in CHO cells | 2006 | Journal of medicinal chemistry, Jul-13, Volume: 49, Issue:14 | Development of peptidic dopamine transporter inhibitors via aromatic modification-mediated conformational restriction. |
| AID65648 | Inhibition of [3H]WIN-35428 binding to the dopamine transporter. | 1992 | Journal of medicinal chemistry, Mar-20, Volume: 35, Issue:6 | Cocaine receptor: biochemical characterization and structure-activity relationships of cocaine analogues at the dopamine transporter. |
| AID204630 | Binding affinity against Sigma receptor type 1 was determined by the displacement of [3H]pentazocine radioligand | 2003 | Journal of medicinal chemistry, Jun-19, Volume: 46, Issue:13 | Dual probes for the dopamine transporter and sigma1 receptors: novel piperazinyl alkyl-bis(4'-fluorophenyl)amine analogues as potential cocaine-abuse therapeutic agents. |
| AID145718 | Inhibitory activity against Norepinephrine transporter using 0.5 nM [3H]-radioligand | 1997 | Journal of medicinal chemistry, Apr-11, Volume: 40, Issue:8 | Synthesis and transporter binding properties of 2,3-diphenyltropane stereoisomers. Comparison to 3beta-phenyltropane-2beta-carboxylic acid esters. |
| AID232405 | Ratio of Ki at norepinephrine transporter and Ki at dopamine transporter. | 2002 | Journal of medicinal chemistry, Jul-18, Volume: 45, Issue:15 | SAR studies of piperidine-based analogues of cocaine. 4. Effect of N-modification and ester replacement. |
| AID161281 | Inhibition of human Potassium channel HERG expressed in mammalian cells | 2003 | Bioorganic & medicinal chemistry letters, Aug-18, Volume: 13, Issue:16 | Prediction of hERG potassium channel affinity by traditional and hologram qSAR methods. |
| AID444521 | Inhibition of [3H]serotonin reuptake at human SERT expressed in HEK293 cells | 2009 | Journal of medicinal chemistry, Nov-12, Volume: 52, Issue:21 | Synthesis and biological evaluation of bupropion analogues as potential pharmacotherapies for cocaine addiction. |
| AID234939 | Selectivity in uptake of 5-HT to that of DA | 2001 | Bioorganic & medicinal chemistry letters, Aug-20, Volume: 11, Issue:16 | Sar studies of piperidine-based analogues of cocaine. Part 3: oxadiazoles. |
| AID147739 | Ability to inhibit [3H]NE reuptake at norepinephrine transporter from rat brain | 2003 | Journal of medicinal chemistry, May-08, Volume: 46, Issue:10 | Biaryl analogues of conformationally constrained tricyclic tropanes as potent and selective norepinephrine reuptake inhibitors: synthesis and evaluation of their uptake inhibition at monoamine transporter sites. |
| AID395504 | Displacement of [3H]norepinephrine from human recombinant NET expressed in HEK293 cells by scintillation counting | 2009 | Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6 | Dual inhibitors of phosphodiesterase-4 and serotonin reuptake. |
| AID62290 | Compound was evaluated for its ability to displace [3H]mazindol binding from rat striatal membranes | 1992 | Journal of medicinal chemistry, Dec-11, Volume: 35, Issue:25 | Structure-activity relationship studies of cocaine: replacement of the C-2 ester group by vinyl argues against H-bonding and provides an esterase-resistant, high-affinity cocaine analogue. |
| AID204857 | Inhibition of [3H]-5-HT binding to serotonin transporter of rat brain synaptosomes | 2000 | Bioorganic & medicinal chemistry letters, Aug-07, Volume: 10, Issue:15 | Synthesis and biological evaluation of 1-azabicyclo-[3.2.1]octanes: new dopamine transporter inhibitors. |
| AID174465 | Percent response at dose 5 mg/kg evaluated by dose-response tests in trained rats(post injection interval 15 min) | 1992 | Journal of medicinal chemistry, Dec-11, Volume: 35, Issue:25 | Structure-activity relationship studies of cocaine: replacement of the C-2 ester group by vinyl argues against H-bonding and provides an esterase-resistant, high-affinity cocaine analogue. |
| AID234190 | Ratio of serotonin uptake to serotonin binding | 2000 | Journal of medicinal chemistry, Dec-28, Volume: 43, Issue:26 | Slow-onset, long-duration 3-(3',4'-dichlorophenyl)-1-indanamine monoamine reuptake blockers as potential medications to treat cocaine abuse. |
| AID174290 | Drug discrimination effect of compound in rats, expressed as percent of rats choosing the cocaine lever at dose 1.7 mg/kg (ip) | 2004 | Journal of medicinal chemistry, Jan-15, Volume: 47, Issue:2 | Synthesis, monoamine transporter binding properties, and behavioral pharmacology of a series of 3beta-(substituted phenyl)-2beta-(3'-substituted isoxazol-5-yl)tropanes. |
| AID64361 | Inhibition of [3H]DA uptake in HEK cells expressing dopamine transporter | 1999 | Journal of medicinal chemistry, Sep-09, Volume: 42, Issue:18 | Design, synthesis, and biological evaluation of novel non-piperazine analogues of 1-[2-(diphenylmethoxy)ethyl]- and 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazines as dopamine transporter inhibitors. |
| AID1387459 | Displacement of [125I]RTI-55 from human SERT expressed in HEK293 cell membranes | 2018 | Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20 | Synthesis and Discovery of Arylpiperidinylquinazolines: New Inhibitors of the Vesicular Monoamine Transporter. |
| AID1442394 | Induction of stimulus generalization in Sprague-Dawley rat trained to discriminate TDIQ assessed as appropriate responding level to training drug by two lever method | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | The 2014 Philip S. Portoghese Medicinal Chemistry Lectureship: The "Phenylalkylaminome" with a Focus on Selected Drugs of Abuse. |
| AID145388 | Inhibition of binding of [3H]nisoxetine to (NET) norepinephrine transporter in rat striatum | 2003 | Bioorganic & medicinal chemistry letters, May-05, Volume: 13, Issue:9 | Design, synthesis, and activity of novel cis- and trans-3,6-disubstituted pyran biomimetics of 3,6-disubstituted piperidine as potential ligands for the dopamine transporter. |
| AID184426 | To inhibit high affinity uptake of [3H]NE into nerve endings (synaptosomes) prepared from various regions of the rat brain. | 2000 | Journal of medicinal chemistry, Aug-24, Volume: 43, Issue:17 | Chemical synthesis and pharmacology of 6- and 7-hydroxylated 2-carbomethoxy-3-(p-tolyl)tropanes: antagonism of cocaine's locomotor stimulant effects. |
| AID603953 | In-vivo plasma to lung partition coefficients of the compound, logP(lung) in rat | 2008 | European journal of medicinal chemistry, Mar, Volume: 43, Issue:3 | Air to lung partition coefficients for volatile organic compounds and blood to lung partition coefficients for volatile organic compounds and drugs. |
| AID64511 | Compound was tested for inhibition of [125I]RTI-55 binding to dopamine transporter in HEK cells | 2003 | Bioorganic & medicinal chemistry letters, Jul-07, Volume: 13, Issue:13 | Bivalent biogenic amine reuptake inhibitors. |
| AID181665 | Compound is evaluated for [3H]dopamine uptake inhibition in rat forebrain | 1993 | Journal of medicinal chemistry, Apr-30, Volume: 36, Issue:9 | Synthesis and biological evaluation of 1-[1-(2-benzo[b]thienyl)cyclohexyl]piperidine homologues at dopamine-uptake and phencyclidine- and sigma-binding sites. |
| AID192997 | Number of animals(n) completing 20 responses on either lever out of the number of animals tested (N) at dose 2.5 mg/kg evaluated by dose-response tests in trained rats(post injection interval 15 min); n/N=7/7 | 1992 | Journal of medicinal chemistry, Dec-11, Volume: 35, Issue:25 | Structure-activity relationship studies of cocaine: replacement of the C-2 ester group by vinyl argues against H-bonding and provides an esterase-resistant, high-affinity cocaine analogue. |
| AID192879 | Number of animals(n) completing 20 responses on either lever out of the number of animals tested (N) at dose 1.25 mg/kg evaluated by dose-response tests in trained rats(post injection interval 15 min); n/N=7/7 | 1992 | Journal of medicinal chemistry, Dec-11, Volume: 35, Issue:25 | Structure-activity relationship studies of cocaine: replacement of the C-2 ester group by vinyl argues against H-bonding and provides an esterase-resistant, high-affinity cocaine analogue. |
| AID234940 | Selectivity in uptake of NE to that of 5-HT | 2001 | Bioorganic & medicinal chemistry letters, Aug-20, Volume: 11, Issue:16 | Sar studies of piperidine-based analogues of cocaine. Part 3: oxadiazoles. |
| AID213369 | The compound was tested for inhibition of [3H]-5-hydroxy tryptamine uptake in HEK cells by expressing cDNA for human tryptamine transporter | 2000 | Bioorganic & medicinal chemistry letters, Feb-07, Volume: 10, Issue:3 | Design, synthesis and biological evaluation of 7-azatricyclodecanes: analogues of cocaine. |
| AID64205 | Inhibition of [3H]3-beta-(4-fluorophenyl)tropane-2beta-carboxylic acid methyl ester binding to dopamine transporter of cynomolgus monkey striatum | 1993 | Journal of medicinal chemistry, Apr-02, Volume: 36, Issue:7 | Substituted 3-phenyltropane analogs of cocaine: synthesis, inhibition of binding at cocaine recognition sites, and positron emission tomography imaging. |
| AID52198 | Inhibitory effect of [3H]cocaine binding when pre incubation was conducted under reduced lighting | 1994 | Journal of medicinal chemistry, Jul-08, Volume: 37, Issue:14 | Synthesis of substituted 3-carbamoylecgonine methyl ester analogues: irreversible and photoaffinity ligands for the cocaine receptor/dopamine transporter. |
| AID239595 | Inhibition of high affinity uptake by the dopamine transporter from rat synaptosomal nerve endings by using [3H]DA as radioligand | 2004 | Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24 | Piperidine-based nocaine/modafinil hybrid ligands as highly potent monoamine transporter inhibitors: efficient drug discovery by rational lead hybridization. |
| AID296172 | Displacement of [125I]RTI55 from human NET expressed in COS1 cell membrane | 2007 | Bioorganic & medicinal chemistry, Jun-15, Volume: 15, Issue:12 | Synthesis, inhibition and binding of simple non-nitrogen inhibitors of monoamine transporters. |
| AID241744 | Displacement of [3H]paroxetine from Serotonin transporter of rat caudate putamen | 2005 | Journal of medicinal chemistry, May-05, Volume: 48, Issue:9 | Synthesis and pharmacology of 6-substituted benztropines: discovery of novel dopamine uptake inhibitors possessing low binding affinity to the dopamine transporter. |
| AID239623 | Inhibition of high affinity uptake by the norepinephrine transporter from rat synaptosomal nerve endings by using [3H]NE as radioligand | 2004 | Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24 | Piperidine-based nocaine/modafinil hybrid ligands as highly potent monoamine transporter inhibitors: efficient drug discovery by rational lead hybridization. |
| AID1324605 | Selectivity index, ratio of Ki for human DAT Y156F mutant expressed in COS7 cell membranes to Ki for human DAT expressed in COS7 cell membranes | 2016 | Journal of medicinal chemistry, 12-08, Volume: 59, Issue:23 | Novel and High Affinity 2-[(Diphenylmethyl)sulfinyl]acetamide (Modafinil) Analogues as Atypical Dopamine Transporter Inhibitors. |
| AID384546 | Binding affinity at DAT | 2008 | Journal of medicinal chemistry, May-08, Volume: 51, Issue:9 | Design and synthesis of 2- and 3-substituted-3-phenylpropyl analogs of 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine and 1-[2-(diphenylmethoxy)ethyl]-4-(3-phenylpropyl)piperazine: role of amino, fluoro, hydroxyl, methoxyl, methyl, m |
| AID111613 | Percent change from vehicle in locomotor activity in mice at 56 mg/kg (ip) in 1 h | 2004 | Journal of medicinal chemistry, Jan-15, Volume: 47, Issue:2 | Synthesis, monoamine transporter binding properties, and behavioral pharmacology of a series of 3beta-(substituted phenyl)-2beta-(3'-substituted isoxazol-5-yl)tropanes. |
| AID193666 | Half life of recovery for dopamine transporter in nucleus accumbens was determined | 2003 | Journal of medicinal chemistry, May-08, Volume: 46, Issue:10 | 2002 Medicinal Chemistry Division Award address: monoamine transporters and opioid receptors. Targets for addiction therapy. |
| AID268230 | Inhibition of rat DAT-mediated [3H]dopamine uptake in CHO cells | 2006 | Journal of medicinal chemistry, Jul-13, Volume: 49, Issue:14 | Development of peptidic dopamine transporter inhibitors via aromatic modification-mediated conformational restriction. |
| AID1443755 | Inhibition of [125I]RTI-55 binding to mouse DAT expressed in HEK293 cells preincubated for 10 mins followed by radioligand addition measured after 90 mins by micro beta scintillation counting analysis | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | Scaffold Repurposing of Nucleosides (Adenosine Receptor Agonists): Enhanced Activity at the Human Dopamine and Norepinephrine Sodium Symporters. |
| AID192993 | Number of animals(n) completing 20 responses on either lever out of the number of animals tested (N) at dose 10 mg/kg evaluated by temporal tests in trained rats(post injection interval 15 min); n/N=7/7 | 1992 | Journal of medicinal chemistry, Dec-11, Volume: 35, Issue:25 | Structure-activity relationship studies of cocaine: replacement of the C-2 ester group by vinyl argues against H-bonding and provides an esterase-resistant, high-affinity cocaine analogue. |
| AID174464 | Percent response at dose 2.5 mg/kg evaluated by dose-response tests in trained rats(post injection interval 15 min) | 1992 | Journal of medicinal chemistry, Dec-11, Volume: 35, Issue:25 | Structure-activity relationship studies of cocaine: replacement of the C-2 ester group by vinyl argues against H-bonding and provides an esterase-resistant, high-affinity cocaine analogue. |
| AID65491 | Inhibition of [3H]dopamine uptake at striatal nerve endings by dopamine transporter | 1999 | Bioorganic & medicinal chemistry letters, Dec-06, Volume: 9, Issue:23 | N-phenylalkyl-substituted tropane analogs of boat conformation with high selectivity for the dopamine versus serotonin transporter. |
| AID200769 | Inhibition of binding of [3H]- citalopram to Serotonin transporter (SERT) of rat cerebral cortex. | 2002 | Journal of medicinal chemistry, Jan-31, Volume: 45, Issue:3 | Expansion of structure-activity studies of piperidine analogues of 1-[2-(diphenylmethoxy)ethyl]-4-(3-phenylpropyl)piperazine (GBR 12935) compounds by altering substitutions in the N-benzyl moiety and behavioral pharmacology of selected molecules. |
| AID204226 | In vitro binding affinity at serotonin transporter in rat striatum by [3H]- citalopram displacement. | 2001 | Journal of medicinal chemistry, Mar-15, Volume: 44, Issue:6 | Structure-activity relationship studies of 4-[2-(diphenylmethoxy)ethyl]-1-benzylpiperidine derivatives and their N-analogues: evaluation of O-and N-analogues and their binding to monoamine transporters. |
| AID145888 | The compound was tested for binding affinity nisoxatine ligand | 1999 | Journal of medicinal chemistry, Oct-21, Volume: 42, Issue:21 | Structure-activity relationships at the monoamine transporters and sigma receptors for a novel series of 9-[3-(cis-3, 5-dimethyl-1-piperazinyl)propyl]carbazole (rimcazole) analogues. |
| AID444522 | Inhibition of [3H]norepinephrine reuptake at human NET expressed in HEK293 cells | 2009 | Journal of medicinal chemistry, Nov-12, Volume: 52, Issue:21 | Synthesis and biological evaluation of bupropion analogues as potential pharmacotherapies for cocaine addiction. |
| AID174367 | The compound was evaluated for its behavioral activity i.e., locomotor arousal in rat for a dose of 1 mg/kg in time interval of 1 hour | 1994 | Journal of medicinal chemistry, May-27, Volume: 37, Issue:11 | N-omega-fluoroalkyl analogs of (1R)-2 beta-carbomethoxy-3 beta-(4-iodophenyl)-tropane (beta-CIT): radiotracers for positron emission tomography and single photon emission computed tomography imaging of dopamine transporters. |
| AID781328 | pKa (acid-base dissociation constant) as determined by Luan ref: Pharm. Res. 2005 | 2014 | Pharmaceutical research, Apr, Volume: 31, Issue:4 | Comparison of the accuracy of experimental and predicted pKa values of basic and acidic compounds. |
| AID296174 | Inhibition of [3H]SER uptake in human SERT expressed in COS1 cell membrane | 2007 | Bioorganic & medicinal chemistry, Jun-15, Volume: 15, Issue:12 | Synthesis, inhibition and binding of simple non-nitrogen inhibitors of monoamine transporters. |
| AID194151 | Dopamine (DA) uptake | 1998 | Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6 | (-)-3 beta-Substituted ecgonine methyl esters as inhibitors for cocaine binding and dopamine uptake. |
| AID64864 | Inhibition of [3H]WIN-35428 binding to the dopamine transporter in rat striata. | 1996 | Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20 | Synthesis and transporter binding properties of 3 beta-(4'-alkyl-, 4'-alkenyl-, and 4'-alkynylphenyl)nortropane-2 beta-carboxylic acid methyl esters: serotonin transporter selective analogs. |
| AID65646 | Inhibition of [3H]GBR-12935 binding to the dopamine transporter. | 1992 | Journal of medicinal chemistry, Mar-20, Volume: 35, Issue:6 | Cocaine receptor: biochemical characterization and structure-activity relationships of cocaine analogues at the dopamine transporter. |
| AID444526 | Antidepressant activity in ip dosed mouse assessed as duration of locomotor activity | 2009 | Journal of medicinal chemistry, Nov-12, Volume: 52, Issue:21 | Synthesis and biological evaluation of bupropion analogues as potential pharmacotherapies for cocaine addiction. |
| AID248017 | Inhibitory concentration against [3H]-DA uptake in rat brain tissue | 2005 | Journal of medicinal chemistry, Mar-10, Volume: 48, Issue:5 | Synthesis and biological evaluation of meperidine analogues at monoamine transporters. |
| AID52193 | Potency ratio for Cocaine receptor (IC50 cocaine /IC50 compound) | 1998 | Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6 | (-)-3 beta-Substituted ecgonine methyl esters as inhibitors for cocaine binding and dopamine uptake. |
| AID65183 | Inhibition of high affinity uptake of [3H]-DA by dopamine transporter in nerve endings obtained from rat brain. | 2002 | Journal of medicinal chemistry, Jul-18, Volume: 45, Issue:15 | SAR studies of piperidine-based analogues of cocaine. 4. Effect of N-modification and ester replacement. |
| AID570374 | Displacement of [3H]nisoxetine from NET in Sprague-Dawley rat brain membranes | 2010 | ACS medicinal chemistry letters, Oct-10, Volume: 2, Issue:1 | Structure-Activity Relationships at the Monoamine Transporters for a Novel Series of Modafinil (2-[(diphenylmethyl)sulfinyl]acetamide) Analogues. |
| AID204389 | Selectivity for the Serotonin transporter using [3H]paroxetine binding assay | 1999 | Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23 | Synthesis and pharmacology of site-specific cocaine abuse treatment agents: 2-substituted-6-amino-5-phenylbicyclo[2.2.2]octanes. |
| AID65632 | In vitro ability to inhibit the [3H]WIN-35428 binding to cocaine binding site on dopamine transporter in rat striatal membranes irreversibly after one wash. | 1992 | Journal of medicinal chemistry, May-15, Volume: 35, Issue:10 | Probes for the cocaine receptor. Potentially irreversible ligands for the dopamine transporter. |
| AID243151 | Inhibitory concentration against potassium channel HERG | 2005 | Bioorganic & medicinal chemistry letters, Jun-02, Volume: 15, Issue:11 | A discriminant model constructed by the support vector machine method for HERG potassium channel inhibitors. |
| AID281810 | Locomotor activity in CD1 mouse assessed as stimulation at 3 mg/kg, ip after 2 hrs relative to control | 2004 | Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25 | Monoamine transporter binding, locomotor activity, and drug discrimination properties of 3-(4-substituted-phenyl)tropane-2-carboxylic acid methyl ester isomers. |
| AID234002 | Selectivity for norepinephrine and serotonin transporters | 1996 | Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20 | Synthesis and transporter binding properties of 3 beta-(4'-alkyl-, 4'-alkenyl-, and 4'-alkynylphenyl)nortropane-2 beta-carboxylic acid methyl esters: serotonin transporter selective analogs. |
| AID65352 | Displacement of [3H]WIN-35428 binding to the dopamine transporter (DAT) in Rat Caudate Putamen | 1997 | Journal of medicinal chemistry, Mar-14, Volume: 40, Issue:6 | 3'-Chloro-3 alpha-(diphenylmethoxy)tropane but not 4'-chloro-3 alpha-(diphenylmethoxy)tropane produces a cocaine-like behavioral profile. |
| AID147760 | Displacement of [125I]RTI-55 from human Norepinephrine transporter expressed in HEK cells | 2002 | Journal of medicinal chemistry, Sep-12, Volume: 45, Issue:19 | Mazindol analogues as potential inhibitors of the cocaine binding site at the dopamine transporter. |
| AID412739 | Displacement of [125I]RTI55 from human recombinant SERT expressed in HEK293 cells | 2009 | Bioorganic & medicinal chemistry, Jan-01, Volume: 17, Issue:1 | Stereoselective inhibition of serotonin re-uptake and phosphodiesterase by dual inhibitors as potential agents for depression. |
| AID145878 | Inhibition of 0.5 nM [3H]nisoxetine binding to Norepinephrine transporter | 2000 | Bioorganic & medicinal chemistry letters, Nov-06, Volume: 10, Issue:21 | 3alpha-(4-Substituted phenyl)nortropane-2beta-carboxylic acid methyl esters show selective binding at the norepinephrine transporter. |
| AID230871 | Ratio of affinity for serotonin transporter to that of dopamine transporter | 2004 | Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12 | Synthesis, molecular modeling, and biological studies of novel piperidine-based analogues of cocaine: evidence of unfavorable interactions proximal to the 3alpha-position of the piperidine ring. |
| AID111615 | Percent change from vehicle in locomotor activity in mice at 56 mg/kg (ip) in 3 h | 2004 | Journal of medicinal chemistry, Jan-15, Volume: 47, Issue:2 | Synthesis, monoamine transporter binding properties, and behavioral pharmacology of a series of 3beta-(substituted phenyl)-2beta-(3'-substituted isoxazol-5-yl)tropanes. |
| AID181689 | Compound was evaluated for its ability to antagonizing serotonin high affinity uptake was determined using [3H]5-HT on synaptosomes prepared from rat midbrain or parietal cortices. | 2000 | Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6 | Further SAR studies of piperidine-based analogues of cocaine. 2. Potent dopamine and serotonin reuptake inhibitors. |
| AID141706 | Binding affinity at muscarinic M1 receptor in rat brain by [3H]pirenzepine displacement. | 2004 | Journal of medicinal chemistry, Jun-17, Volume: 47, Issue:13 | Structure-activity relationships at monoamine transporters for a series of N-substituted 3alpha-(bis[4-fluorophenyl]methoxy)tropanes: comparative molecular field analysis, synthesis, and pharmacological evaluation. |
| AID296170 | Displacement of [125I]RTI55 from human DAT expressed in COS1 cell membrane | 2007 | Bioorganic & medicinal chemistry, Jun-15, Volume: 15, Issue:12 | Synthesis, inhibition and binding of simple non-nitrogen inhibitors of monoamine transporters. |
| AID204848 | Inhibition of [3H]5-HT Uptake in rat mid brain. | 2000 | Journal of medicinal chemistry, Feb-10, Volume: 43, Issue:3 | Discovery of a novel dopamine transporter inhibitor, 4-hydroxy-1-methyl-4-(4-methylphenyl)-3-piperidyl 4-methylphenyl ketone, as a potential cocaine antagonist through 3D-database pharmacophore searching. Molecular modeling, structure-activity relationshi |
| 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. |
| AID204542 | Inhibition of [125I]RTI-55 binding to Serotonin transporter of rat caudate membranes | 2002 | Bioorganic & medicinal chemistry letters, Aug-19, Volume: 12, Issue:16 | Identification of a novel partial inhibitor of dopamine transporter among 4-substituted 2-phenylquinazolines. |
| AID64869 | Inhibition of [3H]WIN-35428 binding to the cocaine binding site on the dopamine transporter (DAT) in synaptosomal membrane preparations from rat striatal tissue. | 2003 | Journal of medicinal chemistry, Apr-10, Volume: 46, Issue:8 | Synthesis and pharmacology of site specific cocaine abuse treatment agents: 8-substituted isotropane (3-azabicyclo[3.2.1]octane) dopamine uptake inhibitors. |
| AID273269 | Displacement of [3H]citalopram from SERT in Sprague-Dawley rat brain | 2006 | Journal of medicinal chemistry, Oct-19, Volume: 49, Issue:21 | Structure-activity relationship studies on a novel series of (S)-2beta-substituted 3alpha-[bis(4-fluoro- or 4-chlorophenyl)methoxy]tropane analogues for in vivo investigation. |
| AID540216 | Clearance in dog after iv administration | 2005 | Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7 | Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure. |
| AID195346 | Mean responses per minute at dose 10 mg/kg evaluated by temporal tests in trained rats(post injection interval 60 min) | 1992 | Journal of medicinal chemistry, Dec-11, Volume: 35, Issue:25 | Structure-activity relationship studies of cocaine: replacement of the C-2 ester group by vinyl argues against H-bonding and provides an esterase-resistant, high-affinity cocaine analogue. |
| AID412742 | Inhibition of [3H]5HT from human recombinant SERT expressed in HEK293 cells | 2009 | Bioorganic & medicinal chemistry, Jan-01, Volume: 17, Issue:1 | Stereoselective inhibition of serotonin re-uptake and phosphodiesterase by dual inhibitors as potential agents for depression. |
| AID205268 | Inhibition of binding of Batrachotoxinin [3H]BTX-B to high affinity sites on voltage dependent sodium channels in a vesicular preparation from guinea pig cerebral cortex at 10 uM | 1985 | Journal of medicinal chemistry, Mar, Volume: 28, Issue:3 | [3H]Batrachotoxinin A 20 alpha-benzoate binding to voltage-sensitive sodium channels: a rapid and quantitative assay for local anesthetic activity in a variety of drugs. |
| AID143640 | Inhibition of [3H]NE reuptake by human norepinephrine transporter expressed in HEK293 cells | 2000 | Journal of medicinal chemistry, Jan-27, Volume: 43, Issue:2 | Novel 3-aminomethyl- and 4-aminopiperidine analogues of 1-[2-(diphenylmethoxy)ethyl]-4-(3-phenylpropyl)piperazines: synthesis and evaluation as dopamine transporter ligands. |
| AID145541 | Binding affinity against norepinephrine cloned human transporter using 40-80 pM [125I]RTI | 2000 | Journal of medicinal chemistry, Dec-28, Volume: 43, Issue:26 | Slow-onset, long-duration 3-(3',4'-dichlorophenyl)-1-indanamine monoamine reuptake blockers as potential medications to treat cocaine abuse. |
| AID223307 | Effective dose for generalization to 10 mg/kg cocaine in rat (value is standard error of the population of 88 independent determinations) | 2000 | Journal of medicinal chemistry, Dec-28, Volume: 43, Issue:26 | Slow-onset, long-duration 3-(3',4'-dichlorophenyl)-1-indanamine monoamine reuptake blockers as potential medications to treat cocaine abuse. |
| AID1442374 | Induction of stimulus generalization in rat trained to discriminate S(+)methamphetamine assessed as appropriate responding level to training drug by two lever method | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | The 2014 Philip S. Portoghese Medicinal Chemistry Lectureship: The "Phenylalkylaminome" with a Focus on Selected Drugs of Abuse. |
| AID65012 | Inhibitory potency against [3H]DA uptake using [3H]WIN-35428 (WIN-) binding assay | 1999 | Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23 | Synthesis and pharmacology of site-specific cocaine abuse treatment agents: 2-substituted-6-amino-5-phenylbicyclo[2.2.2]octanes. |
| AID52200 | Tested for inhibition of [3H]cocaine binding to rat striatal P2 membranes | 1994 | Journal of medicinal chemistry, Jul-08, Volume: 37, Issue:14 | Synthesis of substituted 3-carbamoylecgonine methyl ester analogues: irreversible and photoaffinity ligands for the cocaine receptor/dopamine transporter. |
| AID273272 | Selectivity for Sprague-Dawley rat DAT over SERT | 2006 | Journal of medicinal chemistry, Oct-19, Volume: 49, Issue:21 | Structure-activity relationship studies on a novel series of (S)-2beta-substituted 3alpha-[bis(4-fluoro- or 4-chlorophenyl)methoxy]tropane analogues for in vivo investigation. |
| AID111600 | Percent change from vehicle in locomotor activity in mice at 17 mg/kg (ip) in 4 h | 2004 | Journal of medicinal chemistry, Jan-15, Volume: 47, Issue:2 | Synthesis, monoamine transporter binding properties, and behavioral pharmacology of a series of 3beta-(substituted phenyl)-2beta-(3'-substituted isoxazol-5-yl)tropanes. |
| AID127362 | Binding affinity against human monoclonal antibody (mAb) 2E2 by ELISA | 2004 | Journal of medicinal chemistry, Jan-01, Volume: 47, Issue:1 | Three-dimensional quantitative structure-activity relationship modeling of cocaine binding by a novel human monoclonal antibody. |
| AID64842 | Compound was tested for inhibitory activity to displace [3H]WIN-35428 at dopamine transporter in Rat Striatal Membranes. | 1997 | Journal of medicinal chemistry, Aug-01, Volume: 40, Issue:16 | Synthesis and ligand binding studies of 4'-iodobenzoyl esters of tropanes and piperidines at the dopamine transporter. |
| AID204066 | Inhibition of [3H]- 5-HT uptake in HEK cells expressing serotonin transporter | 1999 | Journal of medicinal chemistry, Sep-09, Volume: 42, Issue:18 | Design, synthesis, and biological evaluation of novel non-piperazine analogues of 1-[2-(diphenylmethoxy)ethyl]- and 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazines as dopamine transporter inhibitors. |
| AID65355 | Displacement of [3H]WIN-35248 from dopamine transporter (DAT) of rat striatal membrane | 2001 | Bioorganic & medicinal chemistry letters, Aug-20, Volume: 11, Issue:16 | Sar studies of piperidine-based analogues of cocaine. Part 3: oxadiazoles. |
| AID65508 | Binding affinity against dopamine transporter in rat caudate putamen tissue using [3H]WIN-35428 radioligand. | 1996 | Journal of medicinal chemistry, Nov-22, Volume: 39, Issue:24 | Synthesis and dopamine transporter affinity of 2-(methoxycarbonyl)-9-methyl-3-phenyl-9-azabicyclo[3.3.1]nonane derivatives. |
| AID64873 | Inhibition of binding of 3[H] WIN-35 428 to Dopamine transporter (DAT) of rat striatum. | 2002 | Journal of medicinal chemistry, Jan-31, Volume: 45, Issue:3 | Expansion of structure-activity studies of piperidine analogues of 1-[2-(diphenylmethoxy)ethyl]-4-(3-phenylpropyl)piperazine (GBR 12935) compounds by altering substitutions in the N-benzyl moiety and behavioral pharmacology of selected molecules. |
| AID1443750 | Inhibition of recombinant human SERT expressed in HEK293 cell membranes assessed as reduction in [3H]5-HT uptake incubated for 22 mins by micro beta scintillation counting analysis | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | Scaffold Repurposing of Nucleosides (Adenosine Receptor Agonists): Enhanced Activity at the Human Dopamine and Norepinephrine Sodium Symporters. |
| AID196579 | Tested for inhibition of [3H]-dopamine uptake into rat striatal synaptosomes | 1994 | Journal of medicinal chemistry, Jul-08, Volume: 37, Issue:14 | Synthesis of substituted 3-carbamoylecgonine methyl ester analogues: irreversible and photoaffinity ligands for the cocaine receptor/dopamine transporter. |
| AID145880 | Inhibition of [3H]NE uptake by rat frontal cortex Norepinephrine transporter | 1995 | Journal of medicinal chemistry, Jan-20, Volume: 38, Issue:2 | Cocaine and 3 beta-(4'-substituted phenyl)tropane-2 beta-carboxylic acid ester and amide analogues. New high-affinity and selective compounds for the dopamine transporter. |
| AID145531 | Ratio of IC50(NE) to the IC50(DA) | 1992 | Journal of medicinal chemistry, Jun-26, Volume: 35, Issue:13 | Isopropyl and phenyl esters of 3 beta-(4-substituted phenyl)tropan-2 beta-carboxylic acids. Potent and selective compounds for the dopamine transporter. |
| AID420668 | Inhibition of human ERG in MCF7 cells | 2009 | European journal of medicinal chemistry, May, Volume: 44, Issue:5 | GRIND-based 3D-QSAR and CoMFA to investigate topics dominated by hydrophobic interactions: the case of hERG K+ channel blockers. |
| AID243272 | Ability of compound to inhibit dopamine uptake of receptor was determined | 2005 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 15, Issue:8 | The role of QSAR in dopamine interactions. |
| AID65000 | Inhibitory activity against Dopamine transporter using 0.5 nM [3H]WIN-35428 as radioligand | 1997 | Journal of medicinal chemistry, Apr-11, Volume: 40, Issue:8 | Synthesis and transporter binding properties of 2,3-diphenyltropane stereoisomers. Comparison to 3beta-phenyltropane-2beta-carboxylic acid esters. |
| AID145711 | In vitro inhibitory activity against radioligand [3H]-nisoxatine binding to norepinephrine transporter (NET) in rat cortical tissue | 1997 | Journal of medicinal chemistry, Nov-21, Volume: 40, Issue:24 | 3 Beta-(4-ethyl-3-iodophenyl)nortropane-2 beta-carboxylic acid methyl ester as a high-affinity selective ligand for the serotonin transporter. |
| AID384955 | Intrinsic aqueous solubility at pH 10 by shake-flask method | 2008 | Journal of medicinal chemistry, May-22, Volume: 51, Issue:10 | Molecular characteristics for solid-state limited solubility. |
| AID181690 | Compound was evaluated for its ability to block the [3H]-Dopamine uptake in rat caudate-putamen | 1994 | Journal of medicinal chemistry, Jul-22, Volume: 37, Issue:15 | Novel 3 alpha-(diphenylmethoxy)tropane analogs: potent dopamine uptake inhibitors without cocaine-like behavioral profiles. |
| AID420090 | Ratio of Ki for [3H]dopamine uptake at rat dopamine transporter expressed in CHO cells to Ki for displacement of [3H]WIN-35428 from rat dopamine transporter expressed in CHO cells | 2009 | Bioorganic & medicinal chemistry, Jun-01, Volume: 17, Issue:11 | A novel photoaffinity ligand for the dopamine transporter based on pyrovalerone. |
| AID64377 | Displacement of [125I]- RTI-55 from Dopamine transporter expressed in HEK cells | 2002 | Journal of medicinal chemistry, Sep-12, Volume: 45, Issue:19 | Mazindol analogues as potential inhibitors of the cocaine binding site at the dopamine transporter. |
| AID241938 | Inhibition of [3H]WIN-35428 binding to rat striatal dopamine transporter | 2005 | Journal of medicinal chemistry, Jun-02, Volume: 48, Issue:11 | Synthesis and monoamine transporter binding properties of 3alpha-(substituted phenyl)nortropane-2beta-carboxylic acid methyl esters. Norepinephrine transporter selective compounds. |
| AID412740 | Displacement of [125I]RTI55 from human recombinant NET expressed in HEK293 cells | 2009 | Bioorganic & medicinal chemistry, Jan-01, Volume: 17, Issue:1 | Stereoselective inhibition of serotonin re-uptake and phosphodiesterase by dual inhibitors as potential agents for depression. |
| AID145879 | Inhibition of [3H]NE uptake at Norepinephrine transporter in rat parietal/occipital cortex was determined | 2001 | Bioorganic & medicinal chemistry letters, May-07, Volume: 11, Issue:9 | Pharmacophore-based discovery of 3,4-disubstituted pyrrolidines as a novel class of monoamine transporter inhibitors. |
| AID444359 | Displacement of [3H]citalopram from SERT in rat brain | 2009 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 19, Issue:24 | Synthesis and monoamine transporter affinity of 3alpha-arylmethoxy-3beta-arylnortropanes. |
| AID204063 | Inhibition of 5-HT uptake in HEK cells expressing human serotonin transporter (hSERT) | 2002 | Journal of medicinal chemistry, Sep-12, Volume: 45, Issue:19 | Mazindol analogues as potential inhibitors of the cocaine binding site at the dopamine transporter. |
| AID174291 | Drug discrimination effect of compound in rats, expressed as percent of rats choosing the cocaine lever at dose 10 mg/kg (ip) | 2004 | Journal of medicinal chemistry, Jan-15, Volume: 47, Issue:2 | Synthesis, monoamine transporter binding properties, and behavioral pharmacology of a series of 3beta-(substituted phenyl)-2beta-(3'-substituted isoxazol-5-yl)tropanes. |
| AID281816 | Locomotor activity in CD1 mouse assessed as stimulation at 10 mg/kg, ip after 4 hrs relative to control | 2004 | Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25 | Monoamine transporter binding, locomotor activity, and drug discrimination properties of 3-(4-substituted-phenyl)tropane-2-carboxylic acid methyl ester isomers. |
| AID281818 | Locomotor activity in CD1 mouse assessed as stimulation at 30 mg/kg, ip after 2 hrs relative to control | 2004 | Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25 | Monoamine transporter binding, locomotor activity, and drug discrimination properties of 3-(4-substituted-phenyl)tropane-2-carboxylic acid methyl ester isomers. |
| AID444523 | Antidepressant activity in ip dosed mouse assessed as stimulation of locomotor activity | 2009 | Journal of medicinal chemistry, Nov-12, Volume: 52, Issue:21 | Synthesis and biological evaluation of bupropion analogues as potential pharmacotherapies for cocaine addiction. |
| AID408565 | Displacement of [3H]nisoxetine from norepinephrine transporter | 2008 | Bioorganic & medicinal chemistry, May-15, Volume: 16, Issue:10 | Synthesis and receptor binding properties of 2beta-alkynyl and 2beta-(1,2,3-triazol)substituted 3beta-(substituted phenyl)tropane derivatives. |
| AID141717 | Displacement of [3H]pirenzepine from muscarinic acetylcholine receptor M1 of rat brain membrane | 2004 | Bioorganic & medicinal chemistry letters, Jun-21, Volume: 14, Issue:12 | The effect of 6-substituted-4',4"-difluorobenztropines on monoamine transporters and the muscarinic M1 receptor. |
| AID64677 | Ability to inhibit binding of [3H]WIN-35428 to dopamine transporter in rat caudate putamen | 2001 | Bioorganic & medicinal chemistry letters, Mar-26, Volume: 11, Issue:6 | Effects of two-carbon bridge region methoxylation of benztropine: discovery of novel chiral ligands for the dopamine transporter. |
| AID232156 | Ratio of 5-hydroxy tryptamine and dopamine transporter inhibition | 2000 | Bioorganic & medicinal chemistry letters, Feb-07, Volume: 10, Issue:3 | Design, synthesis and biological evaluation of 7-azatricyclodecanes: analogues of cocaine. |
| AID178216 | Effective dose of compound required to produce maximal locomotor activity in cocaine-trained rat by intraperitoneal administration | 2003 | Journal of medicinal chemistry, May-08, Volume: 46, Issue:10 | 2002 Medicinal Chemistry Division Award address: monoamine transporters and opioid receptors. Targets for addiction therapy. |
| AID204362 | Binding affinity at serotonin transporter in rat striatum by [3H]citalopram displacement. | 2003 | Journal of medicinal chemistry, May-22, Volume: 46, Issue:11 | Interaction of cis-(6-benzhydrylpiperidin-3-yl)benzylamine analogues with monoamine transporters: structure-activity relationship study of structurally constrained 3,6-disubstituted piperidine analogues of (2,2-diphenylethyl)-[1-(4-fluorobenzyl)piperidin- |
| AID1653651 | Selectivity ratio of Ki for displacement of [3H]WIN35428 from human DAT Y156F mutant transiently expressed in COS7 cells to Ki for displacement of [3H]WIN35428 from human DAT transiently expressed in COS7 cells | |||
| AID233625 | Ratio of binding affinity towards norepinephrine transporter to that of dopamine transporter | 2003 | Journal of medicinal chemistry, Mar-27, Volume: 46, Issue:7 | High affinity hydroxypiperidine analogues of 4-(2-benzhydryloxyethyl)-1-(4-fluorobenzyl)piperidine for the dopamine transporter: stereospecific interactions in vitro and in vivo. |
| AID65191 | Binding affinity against dopamine transporter was determined by the displacement of [3H]WIN-35428 radioligand in rat brain | 2003 | Journal of medicinal chemistry, Jun-19, Volume: 46, Issue:13 | Dual probes for the dopamine transporter and sigma1 receptors: novel piperazinyl alkyl-bis(4'-fluorophenyl)amine analogues as potential cocaine-abuse therapeutic agents. |
| AID444360 | Displacement of [3H]nisoxetine from NET in rat brain | 2009 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 19, Issue:24 | Synthesis and monoamine transporter affinity of 3alpha-arylmethoxy-3beta-arylnortropanes. |
| AID218899 | Functional cocaine antagonism was evaluated by inhibition of [3H]dopamine reuptake | 2001 | Bioorganic & medicinal chemistry letters, May-07, Volume: 11, Issue:9 | Pharmacophore-based discovery of 3,4-disubstituted pyrrolidines as a novel class of monoamine transporter inhibitors. |
| AID436601 | Displacement of [3H]nisoxetine from NET | 2009 | Bioorganic & medicinal chemistry, Jul-15, Volume: 17, Issue:14 | Synthesis and structure-activity relationship of 3beta-(4-alkylthio, -methylsulfinyl, and -methylsulfonylphenyl)tropane and 3beta-(4-alkylthiophenyl)nortropane derivatives for monoamine transporters. |
| AID1799064 | Radioligand Binding Assay (Ki) and Inhibition of Substrate Uptake (EC50/IC50) from Article 10.1021/jm8010993: \\Dual inhibitors of phosphodiesterase-4 and serotonin reuptake.\\ | 2009 | Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6 | Dual inhibitors of phosphodiesterase-4 and serotonin reuptake. |
| AID1799063 | PDE4 Enzyme Assay from Article 10.1021/jm8010993: \\Dual inhibitors of phosphodiesterase-4 and serotonin reuptake.\\ | 2009 | Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6 | Dual inhibitors of phosphodiesterase-4 and serotonin reuptake. |
| AID1798189 | Ligand Binding Assay from Article 10.1021/jm0703035: \\Synthesis, monoamine transporter binding, properties, and functional monoamine uptake activity of 3beta-[4-methylphenyl and 4-chlorophenyl]-2 beta-[5-(substituted phenyl)thiazol-2-yl]tropanes.\\ | 2007 | Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15 | Synthesis, monoamine transporter binding, properties, and functional monoamine uptake activity of 3beta-[4-methylphenyl and 4-chlorophenyl]-2 beta-[5-(substituted phenyl)thiazol-2-yl]tropanes. |
| AID1346931 | Rat DAT (Monoamine transporter subfamily) | 2004 | Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25 | Monoamine transporter binding, locomotor activity, and drug discrimination properties of 3-(4-substituted-phenyl)tropane-2-carboxylic acid methyl ester isomers. |
| AID977611 | Experimentally measured binding affinity data (Kd) for protein-ligand complexes derived from PDB | 2001 | Journal of molecular biology, Aug-03, Volume: 311, Issue:1 | Crystal structure of a cocaine-binding antibody. |
| AID977611 | Experimentally measured binding affinity data (Kd) for protein-ligand complexes derived from PDB | 2005 | Journal of molecular biology, Jun-10, Volume: 349, Issue:3 | Diversity in hapten recognition: structural study of an anti-cocaine antibody M82G2. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 5794 (19.08) | 18.7374 |
| 1990's | 7723 (25.44) | 18.2507 |
| 2000's | 6728 (22.16) | 29.6817 |
| 2010's | 7614 (25.08) | 24.3611 |
| 2020's | 2503 (8.24) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Trials | 1,096 (3.38%) | 5.53% |
| Reviews | 0 (0.00%) | 6.00% |
| Reviews | 2,179 (6.71%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Case Studies | 2,065 (6.36%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Observational | 48 (0.15%) | 0.25% |
| Other | 8 (100.00%) | 84.16% |
| Other | 27,073 (83.40%) | 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 | ||
|---|---|---|---|---|---|---|---|
| Extending Long-term Outcomes Through an Adaptive Aftercare Intervention [NCT02143063] | 274 participants (Actual) | Interventional | 2014-08-31 | Completed | |||
| Efeitos da Estimulacao Magnetica Transcrania de Repeticao ( EMTr) no Tratamento da Dependencia ao Uso de Cocaina [NCT01259362] | Phase 2 | 40 participants (Anticipated) | Interventional | 2010-03-31 | Recruiting | ||
| The Effect of Using a Fan With Aromatherapy in Breathlessness Patient in Terminally Illness: a Randomized Control Trial [NCT05625854] | 99 participants (Anticipated) | Interventional | 2022-11-25 | Enrolling by invitation | |||
| Drug Test Detection 24 Hours After Nasal Administration of Cocaine as a Local Vasoconstrictor Prior to Nasal Intubation [NCT05334056] | 27 participants (Actual) | Observational | 2023-03-22 | Completed | |||
| Influence of Craving Manipulation on Cocaine Self-Administration [NCT03954938] | Early Phase 1 | 2 participants (Actual) | Interventional | 2019-05-15 | Terminated(stopped due to COVID-19) | ||
| Intravitreal Injection Anesthesia - Comparison of Different Topical Agents. [NCT01224847] | 92 participants (Actual) | Interventional | 2009-10-31 | Completed | |||
| Influence of Methylphenidate and Duloxetine Maintenance on Pharmacodynamic Effects of Cocaine [NCT03519022] | Early Phase 1 | 9 participants (Actual) | Interventional | 2018-06-01 | Completed | ||
| Neurological Impacts of Artificial Sweeteners in the Context of Diet Sodas [NCT04048681] | 5 participants (Actual) | Interventional | 2019-08-06 | Completed | |||
| A Phase 1b, Randomized, Double-Blinded, Multiple-Dose, Placebo Controlled, Crossover Study To Evaluate The Safety, Tolerability And Pharmacokinetic Effects Of A Metyrapone And Oxazepam Combination (EMB-001) When Co-Administered With Cocaine [NCT02856854] | Phase 1 | 18 participants (Actual) | Interventional | 2016-07-31 | Completed | ||
| The Effects of Non-Nutritive Sweeteners on Energy Intake [NCT03579043] | 0 participants (Actual) | Interventional | 2018-05-22 | Withdrawn(stopped due to Lack of recruitment - no eligible participants.) | |||
| Topiramate-Phentermine Combinations for Cocaine Dependence [NCT02239913] | Phase 1 | 38 participants (Actual) | Interventional | 2014-09-30 | Completed | ||
| Open-label, Pharmacokinetics, Safety, and Tolerability Study of a Single Topical Dose of GOPRELTO® Nasal Solution for the Induction of Local Anesthesia in Pediatric Subjects From ≥12 Years to <17 Years of Age [NCT04792034] | Phase 4 | 20 participants (Anticipated) | Interventional | 2021-04-01 | Not yet recruiting | ||
| Intranasal Cocaine and Temperature Regulation During Exercise [NCT05809453] | Phase 1/Phase 2 | 20 participants (Anticipated) | Interventional | 2023-09-01 | Recruiting | ||
| Cocaine Use and General Anesthesia: A Prospective Study of Cardiovascular and Anesthetic Effects [NCT02692534] | 300 participants (Actual) | Observational | 2016-04-30 | Completed | |||
| A Randomized, Double-blind, Placebo-controlled, Dose of RBP-8000 Following IV Cocaine to Evaluate the Pharmacokinetics Parameters of RBP-8000 and Cocaine and to Assess the Effects of Drug on Cocaine-induced Physiologic and Behavioral Effects in Cocaine Ab [NCT01846481] | Phase 2 | 40 participants (Actual) | Interventional | 2013-04-30 | Completed | ||
| Study of Dexmedetomidine for the Reversal of Cocaine's Effects on Myocardial Perfusion [NCT01927640] | Early Phase 1 | 115 participants (Actual) | Interventional | 2013-02-01 | Completed | ||
| Determination of Clinically Significant Carbohydrates Added to Zero Calorie Drink Products [NCT00525694] | 12 participants (Actual) | Interventional | 2007-02-28 | Completed | |||
| Comparison of the Effect of Xylometazoline and Cocaine on Epistaxis When Administered as Local Vasoconstrictors Prior to Nasal Intubation [NCT05334017] | Phase 4 | 120 participants (Actual) | Interventional | 2022-09-08 | Completed | ||
| Effects of Aripiprazole on Cocaine Craving and Self-Administration [NCT00373880] | Phase 2 | 26 participants (Actual) | Interventional | 2005-04-30 | Completed | ||
| Investigation of Cocaine Addiction Using mGluR5 PET and fMRI [NCT03471182] | Phase 1 | 32 participants (Actual) | Interventional | 2018-02-26 | Completed | ||
| Establishing and Eliminating Cue-drug Associations in Human Cocaine Addiction [NCT01978457] | Phase 1 | 6 participants (Actual) | Interventional | 2012-10-31 | Terminated(stopped due to Not funded) | ||
| Tests of a Therapeutic Cocaine Vaccine [NCT00965263] | Phase 2 | 15 participants (Actual) | Interventional | 2003-03-31 | Completed | ||
| Coke Zero for the Zero: A Study Examining the Effect of Coke Zero Consumption on Night Call Inpatient Course and Mortality [NCT06155981] | 160 participants (Anticipated) | Interventional | 2023-12-01 | Not yet recruiting | |||
| Phase III Topical Application of Cocaine HCl 4% Solution on Safety/Efficacy & Cocaine HCl 4% & 10% Solution on Safety in Local Anesthesia for Diagnostic Procedures & Surgeries on or Through Accessible Mucous Membranes of the Nasal Cavities [NCT02500836] | Phase 3 | 646 participants (Actual) | Interventional | 2015-09-30 | Completed | ||
| Cocaine Relapse Prevention II [NCT00094315] | Phase 1 | 16 participants | Interventional | 2004-09-30 | Active, not recruiting | ||
| Potential Interactions Between IV Cocaine and RPR 102681 [NCT00067535] | Phase 1 | 16 participants (Actual) | Interventional | 2003-06-30 | Completed | ||
| Pharmacodynamic and Pharmacokinetic Interactions Between Intravenous Cocaine and Acetazolamide or Quinine [NCT01851473] | Phase 1 | 14 participants (Actual) | Interventional | 2012-10-24 | Completed | ||
| Phase 1, Double-Blind, Placebo-Controlled Assessment of Potential Interactions Between Intravenous Cocaine and Clavulanic Acid [NCT02563769] | Phase 1 | 10 participants (Actual) | Interventional | 2016-10-24 | Completed | ||
| Brain Imaging: Cocaine Effects & Medication Development [NCT00000270] | Phase 4 | 0 participants (Actual) | Interventional | 1995-12-30 | Withdrawn(stopped due to Study never opened; never enrolled participants) | ||
| Elucidating the Role of the Hypothalamic-Pituitary-Adrenal (HPA) Axis in the Mechanisms Underlying Cocaine Dependence [NCT00451230] | 15 participants | Interventional | 2005-06-30 | Completed | |||
| Cocaine and Sympathetic Nerve Activity in Humans [NCT00338546] | Phase 1 | 0 participants (Actual) | Interventional | Withdrawn | |||
| Behavioral Effects of Drugs (Inpatient): 42 (Cocaine and Zolmitriptan) [NCT05019430] | Early Phase 1 | 20 participants (Anticipated) | Interventional | 2021-10-15 | Recruiting | ||
| Phase I Drug Interaction and Self Administration Studies of Compounds for Cocaine Use Disorder [NCT02537873] | Phase 1 | 29 participants (Actual) | Interventional | 2015-07-31 | Completed | ||
| Influence of Orexin Antagonism on Motivation for Cocaine [NCT03937986] | Early Phase 1 | 8 participants (Actual) | Interventional | 2019-07-11 | Completed | ||
| Development of Human Laboratory Study Model of Cocaine Relapse Prevention [NCT00040066] | Phase 1 | 32 participants | Interventional | 2002-05-31 | Active, not recruiting | ||
| Pathophysiological Subtyping of Abnormalities in Cocaine Dependence [NCT00015275] | Phase 4 | 0 participants | Interventional | Completed | |||
| Comparison of Topical Vasoconstriction in Endoscopic Sinus Surgery: Cocaine Versus Adrenaline [NCT01706952] | Phase 4 | 45 participants (Actual) | Interventional | 2012-12-31 | Completed | ||
| Virtual Reality Cue Exposure Therapy for Cocaine Craving: an Innovative Cognitive and Behavioral Psychotherapy for Cocaine Use Disorder (Psychothérapie Innovante COmportementale et Cognitive Pour le Trouble d'Usage de Cocaïne; PICOC) [NCT05833529] | 54 participants (Anticipated) | Interventional | 2023-05-01 | Recruiting | |||
| Impact of a Non-Drug Choice on Cocaine Reinforcement [NCT01906346] | Early Phase 1 | 9 participants (Actual) | Interventional | 2014-01-31 | Completed | ||
| Effect of Zonisamide on Cocaine Reinforcement, Craving, and Relapse [NCT01137890] | Phase 1/Phase 2 | 19 participants (Actual) | Interventional | 2010-06-30 | Completed | ||
| Impulsivity and Stimulant Administration [NCT01978431] | Phase 1 | 29 participants (Actual) | Interventional | 2012-11-30 | Completed | ||
| Effects of Vigabatrin on Cocaine Self-Administration [NCT00373581] | Phase 2 | 1 participants (Actual) | Interventional | 2006-04-30 | Terminated(stopped due to Funding ran out) | ||
| Modafinil in a Human Laboratory Model of Cocaine Relapse [NCT01778010] | Phase 2 | 8 participants (Actual) | Interventional | 2009-03-31 | Completed | ||
| Human Dopamine Transported Imaging in Cocaine Abuse: 1 [NCT00000315] | Phase 1 | 0 participants | Interventional | 1996-11-30 | Completed | ||
| Acute Withdrawal From Smoked Cocaine [NCT00000292] | Phase 1 | 0 participants | Interventional | 1996-04-30 | Completed | ||
| Human Dopamine Transported Imaging in Cocaine Abuse: 2 [NCT00000316] | Phase 1 | 0 participants | Interventional | 1996-08-31 | Completed | ||
| Stress Hormones and Human Cocaine Use [NCT00000290] | Phase 1 | 0 participants | Interventional | 1997-05-31 | Completed | ||
| Complementary Combination Therapy for Cocaine Dependence [NCT02538744] | Phase 1 | 45 participants (Actual) | Interventional | 2015-08-31 | Completed | ||
| Impact of Sustained Release d-Amphetamine on Choice Between Cocaine and a Non-Drug Reinforcer [NCT02383043] | Early Phase 1 | 18 participants (Actual) | Interventional | 2015-02-01 | Completed | ||
| Safety and Tolerability of Cocaine During Phendimetrazine Maintenance [NCT02233647] | Early Phase 1 | 11 participants (Actual) | Interventional | 2014-09-30 | Completed | ||
| A Single-Blind, Randomized Study Comparing The Efficacy And Safety Of A Single Dose Of TNX-1300 To Placebo With Usual Care For The Treatment Of Signs And Symptoms Of Acute Cocaine Intoxication In Emergency Department Subjects (CATALYST Study) [NCT06045793] | Phase 2 | 60 participants (Anticipated) | Interventional | 2023-12-11 | Not yet recruiting | ||
| Treatment With Lorcaserin for Cocaine Use: The TLC Study [NCT03192995] | Phase 2 | 22 participants (Actual) | Interventional | 2018-01-01 | Terminated(stopped due to FDA alert regarding study drug safety) | ||
| [NCT02018263] | Phase 1 | 5 participants (Actual) | Interventional | 2013-10-31 | Completed | ||
| GLP-1 Agonism for Blocking Cocaine Euphoria and Self-Administration [NCT02302976] | Phase 1 | 13 participants (Actual) | Interventional | 2014-11-30 | Completed | ||
| Development and Evaluation of a Virtual Reality Application for Eliciting Craving and Its Physiological Arousal in Cocaine Users [NCT05557149] | 11 participants (Actual) | Interventional | 2021-03-31 | Completed | |||
| Motivation for Cocaine and Non-Drug Reinforcers: Targeting Glutamate Homeostasis [NCT02141620] | Early Phase 1 | 15 participants (Actual) | Interventional | 2014-05-31 | Completed | ||
| Phase 1, Double-Blind, Placebo-Controlled, Parallel-Group Study to Assess Potential Interactions Between Intravenous Cocaine and Oral Lorcaserin [NCT02393599] | Phase 1 | 20 participants (Actual) | Interventional | 2015-05-31 | Completed | ||
| The Effect of N-acetylcysteine (NAC) on Treatment of Alcohol and Cocaine Use Disorders: A Double-Blind Randomized Controlled Trial. [NCT03018236] | Phase 4 | 100 participants (Anticipated) | Interventional | 2017-01-31 | Recruiting | ||
| A Phase III Investigation of Topical Application of Cocaine HCl 4% and 10% on Safety and Efficacy in Local (Topical) Anesthesia for Diagnostic Procedures and Surgeries on or Through Accessible Mucous Membranes of the Nasal Cavities. [NCT01746940] | Phase 3 | 159 participants (Actual) | Interventional | 2014-03-31 | Terminated(stopped due to Trial operational issues.) | ||
| Behavioral Effects of Drugs (Inpatient): 31 (Cocaine and Phendimetrazine) [NCT02522325] | Phase 1 | 30 participants (Actual) | Interventional | 2015-08-31 | Completed | ||
| A Human Laboratory Assessment of the Safety and Potential Efficacy of SYN117 (Nepicastat) in Cocaine-dependent Volunteers Receiving Cocaine [NCT00656357] | Phase 1/Phase 2 | 20 participants (Actual) | Interventional | 2008-06-30 | Completed | ||
| [information is prepared from clinicaltrials.gov, extracted Sep-2024] | |||||||