BDBM50082392 piperidine based analogue of cocaine CHEMBL324631 PIPERIDINE BASED ANALOGUE OF COCAINE (STRUCTURAL MIX)
BDBM50082393 piperidine based analogue of cocaine CHEMBL441075
CAS_50-36-2 COCAINE NSC_446220 BDBM86207
BDBM22418 Cocaine (-) methyl (1R,2R,3S,5S)-3-(benzoyloxy)-8-methyl-8-azabicyclo[3.2.1]octane-2-carboxylate methyl (1R,2R,3S,5S)-8-methyl-3-[(phenylcarbonyl)oxy]-8-azabicyclo[3.2.1]octane-2-carboxylate Cocaine
(1R,2R,3S,5S)-methyl 3-(benzoyloxy)-8-methyl-8-azabicyclo[3.2.1]octane-2-carboxylate (3S,5R)-3-Benzoyloxy-8-methyl-8-aza-bicyclo[3.2.1]octane-2-carboxylic acid methyl ester (2R,3S,5R)-3-Benzoyloxy-8-methyl-8-aza-bicyclo[3.2.1]octane-2-carboxylic acid methyl ester 3-Benzoyloxy-8-methyl-8-aza-bicyclo[3.2.1]octane-2-carboxylic acid methyl ester (R)-3-Benzoyloxy-8-methyl-8-aza-bicyclo[3.2.1]octane-2-carboxylic acid methyl ester (2R,3S)-3-Benzoyloxy-8-methyl-8-aza-bicyclo[3.2.1]octane-2-carboxylic acid methyl ester CHEMBL120901 8-Methyl-8-aza-bicyclo[3.2.1]octane-2,3-dicarboxylic acid 2-methyl ester 3-phenyl ester(cocaine) (1S,2R,3S,5R)-methyl 3-(benzoyloxy)-8-methyl-8-aza-bicyclo[3.2.1]octane-2-carboxylate 3-Benzoyloxy-8-methyl-8-aza-bicyclo[3.2.1]octane-2-carboxylic acid ethyl ester R-3-Benzoyloxy-8-methyl-8-aza-bicyclo[3.2.1]octane-2-carboxylic acid methyl ester (2R,3S,8S)-3-Benzoyloxy-8-methyl-8-aza-bicyclo[3.2.1]octane-2-carboxylic acid methyl ester (3S,8R)-3-Benzoyloxy-8-methyl-8-aza-bicyclo[3.2.1]octane-2-carboxylic acid methyl ester (S)-3-Benzoyloxy-8-methyl-8-aza-bicyclo[3.2.1]octane-2-carboxylic acid methyl ester methyl 8-methyl-3-phenylcarbonyloxy-(5R)-8-azabicyclo[3.2.1]octane-2-carboxylate (R)-3-Benzoyloxy-2-methoxycarbonyl-8-methyl-8-azonia-bicyclo[3.2.1]octane S-3-Benzoyloxy-8-methyl-8-aza-bicyclo[3.2.1]octane-2-carboxylic acid methyl ester (1R,2R,3S,5S)-methyl 3-(benzoyloxy)-8-methyl-8-aza-bicyclo[3.2.1]octane-2-carboxylate (-)-(1R,2R,3S,5S)-methyl 3-(benzoyloxy)-8-methyl-8-aza-bicyclo[3.2.1]octane-2-carboxylate 3-(4-Fluoro-phenyl)-8-methyl-8-aza-bicyclo[3.2.1]octane-2-carboxylic acid methyl ester(Cocaine) (2R,3S,8R)-3-Benzoyloxy-8-methyl-8-aza-bicyclo[3.2.1]octane-2-carboxylic acid methyl ester (cocaine)3-Benzoyloxy-8-methyl-8-aza-bicyclo[3.2.1]octane-2-carboxylic acid methyl ester BDBM50084717 COCAINE (+)-(1R,2R,3S,5S)-methyl 3-(benzoyloxy)-8-methyl-8-aza-bicyclo[3.2.1]octane-2-carboxylate methyl 8-methyl-3-phenylcarbonyloxy-(3S)-8-azabicyclo[3.2.1]octane-2-carboxylate methyl 8-methyl-3-phenylcarbonyloxy-(3S,5R)-8-azabicyclo[3.2.1]octane-2-carboxylate 3-Benzoyloxy-6-methyl-6-aza-bicyclo[3.2.2]nonane-4-carboxylic acid methyl ester (1R,2R,3S,5S)-methyl 3-(benzyloxy)-8-methyl-8-aza-bicyclo[3.2.1]octane-2-carboxylate 3-Benzoyloxy-8-methyl-8-aza-bicyclo[3.2.1]octane-2-carboxylic acid methyl ester(Cocaine(-)) 3-Benzoyloxy-8-methyl-8-aza-bicyclo[3.2.1]octane-2-carboxylic acid methyl ester(Cocaine) (2R,3S)-3-Benzoyloxy-2-methoxycarbonyl-8-methyl-8-azonia-bicyclo[3.2.1]octane 3-Naphthalen-2-yl-8-oxa-bicyclo[3.2.1]oct-2-ene-2-carboxylic acid methyl ester 4-(4-Chloro-benzyl)-2-(1-methyl-azepan-4-yl)-2H-phthalazin-1-one
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- ChEMBL_49336 Inhibition [3H]-cocaine binding to Cocaine receptor in rat striatal membranes.
- ChEMBL_49347 Inhibition of [3H]cocaine binding to Cocaine receptor in rat striatal membranes
- ChEBML_49342 Competitive inhibition against [3H]cocaine binding to cocaine receptor in bovine striatal tissue
- ChEMBL_49342 Competitive inhibition against [3H]cocaine binding to cocaine receptor in bovine striatal tissue
- ChEMBL_216233 Functional cocaine antagonism was evaluated by inhibition of [3H]dopamine reuptake at a concentration of 100 nM with cocaine
- ChEMBL_216234 Functional cocaine antagonism was evaluated by inhibition of [3H]dopamine reuptake at a concentration of 30 nM with cocaine
- ChEMBL_216235 Functional cocaine antagonism was evaluated by inhibition of [3H]dopamine reuptake at a concentration of 300 nM with cocaine
- ChEMBL_62169 Inhibition of [3H]cocaine binding to the dopamine transporter.
- ChEMBL_62797 Inhibition of [3H]cocaine binding to the dopamine transporter.
- ChEMBL_216232 Functional cocaine antagonism was evaluated by inhibition of [3H]dopamine reuptake
- ChEMBL_486190 Displacement of [3H]WIN-from cocaine site of dopamine transporter
- ChEMBL_61838 Inhibition of [3H]cocaine binding to rat forebrain dopamine receptor
- ChEMBL_62162 Inhibition of [125I]RTI-55 cocaine binding to the dopamine transporter.
- ChEMBL_62791 Inhibition of [125I]RTI-55 cocaine binding to the dopamine transporter.
- ChEBML_49341 Concentration inhibiting [3H]cocaine binding site to rat striatal membranes.
- ChEMBL_49345 Tested for inhibition of [3H]cocaine binding to rat striatal P2 membranes
- ChEMBL_61839 Binding affinity of compound at site labeled by [3H]-cocaine in rat forebrain.
- ChEBML_49348 In vitro inhibitory activity towards [3H]cocaine binding to rat striatal tissue
- ChEMBL_49348 In vitro inhibitory activity towards [3H]cocaine binding to rat striatal tissue
- ChEMBL_62178 Tested for radioligand [3H]cocaine displacement from dopamine transporter in rat forebrain
- ChEMBL_62321 Displacement of [3H]mazindol from cocaine binding site on Dopamine transporter (DAT)
- ChEMBL_62809 Antagonism of cocaine''s inhibition of [3H]DA uptake at the dose of 200 nM
- ChEMBL_62810 Antagonism of cocaine''s inhibition of [3H]DA uptake at the dose of 500 nM
- ChEMBL_62811 Antagonism of cocaine''s inhibition of [3H]DA uptake at the dose of 50 nM
- ChEBML_61992 Affinity against cocaine binding site of dopamine transporter in rat striatum using [3H]2b as radioligand.
- ChEMBL_62653 ability to displace [3H]- Mazindol binding to cocaine binding sites on Dopamine transporter of rat striatal membranes
- ChEMBL_62943 Binding Affinity to cocaine site of dopamine transporter in caudate nuclei which was homogenized and incubated with [3H]mazindol.
- ChEMBL_62944 Binding Affinity to cocaine site of dopamine transporter in caudate nuclei which was homogenized and incubated with [3H]mazindol.
- ChEMBL_62958 Binding Affinity to cocaine site of Dopamine transporter in caudate nuclei which was homogenized and incubated with [3H]mazindol.
- ChEMBL_61488 Compound was evaluated for inhibition of specifically bound [3H]- cocaine (2.7 nM) against Dopamine transporter in cynomolgus monkeys
- ChEMBL_49340 Binding affinity was determined against cocaine receptor by measuring the ability of compound to displace bound [3H]-3 from rat caudate-putamen tissue
- ChEMBL_62016 Inhibition of [3H]WIN-35428 binding to the cocaine binding site on the dopamine transporter (DAT) in synaptosomal membrane preparations from rat striatal tissue.
- ChEMBL_62639 Inhibition of [3H]WIN-35428 binding to the cocaine binding site on the dopamine transporter (DAT) in synaptosomal membrane preparations from rat striatal tissue
- ChEMBL_49339 Binding affinity was determined against cocaine binding site by measuring the ability of compound to displace bound [3H]dopamine from rat caudate-putamen tissue
- HTS Image-Based Screen for Selective Agonists of the KOR Receptor Data Source: Sanford-Burnham Center for Chemical Genomics (SBCCG) Source Affiliation: Sanford-Burnham Medical Research Institute (SBMRI, San Diego, CA) Network: NIH Molecular Libraries Probe Production Centers Network (MLPCN) Grant Number: 1X01DA026208-01 Assay Provider: Dr. Lawrance Barak, Duke University, Durham, NC Drug addiction is a disease originating in the central nervous system that produces compulsive behaviors despite the negative consequences that may result. Major addictive drugs of abuse include components of tobacco, opiates, marijuana, ethanol, cocaine, and derivatives of amphetamines. While the addictive behaviors produced by these substances may be generally similar, the drugs act at different receptor sites in the brain. Recent studies have shown that opioid receptors play a role regulating the addictive behaviors of other receptors that interact with illicit and legal substances of abuse. Opioid receptors are composed of multiple subtypes whose contributions to a
- HTS Image-Based Screen for Selective Antagonists of the KOR Receptor Data Source: Sanford-Burnham Center for Chemical Genomics (SBCCG) Source Affiliation: Sanford-Burnham Medical Research Institute (SBMRI, San Diego, CA) Network: NIH Molecular Libraries Probe Production Centers Network (MLPCN) Grant Number: 1X01DA026208-01 Assay Provider: Dr. Lawrance Barak , Duke University, Durham NC Drug addiction is a disease originating in the central nervous system that produces compulsive behaviors despite the negative consequences that may result. Major addictive drugs of abuse include components of tobacco, opiates, marijuana, ethanol, cocaine, and derivatives of amphetamines. While the addictive behaviors produced by these substances may be generally similar, the drugs act at different receptor sites in the brain. Recent studies have shown that opioid receptors play a role regulating the addictive behaviors of other receptors that interact with illicit and legal substances of abuse. Opioid receptors are composed of multiple subtypes whose contributions to a
- SAR analysis of small molecule agonists of the kappa opioid receptor via a luminescent beta-arrestin assay - Set 2 Data Source: Sanford-Burnham Center for Chemical Genomics (SBCCG) Source Affiliation: Sanford-Burnham Medical Research Institute (SBMRI, San Diego, CA) Network: NIH Molecular Libraries Production Centers Network (MLPCN) Grant Number: 1X01DA026208-01 Assay Provider: Dr. Lawrance Barak , Duke University, Durham NC Drug addiction is a disease originating in the central nervous system that produces compulsive behaviors despite the negative consequences that may result. Major addictive drugs of abuse include components of tobacco, opiates, marijuana, ethanol, cocaine, and derivatives of amphetamines. While the addictive behaviors produced by these substances may be generally similar, the drugs act at different receptor sites in the brain. Recent studies have shown that opioid receptors play a role regulating the addictive behaviors of other receptors that interact with illicit and legal substances of abuse. Opioid receptors are composed of multiple subtypes whose contributions to addicti
- SAR analysis of small molecule agonists of the kappa opioid receptor via a luminescent beta-arrestin assay - Set 3 Data Source: Sanford-Burnham Center for Chemical Genomics (SBCCG) Source Affiliation: Sanford-Burnham Medical Research Institute (SBMRI, San Diego, CA) Network: NIH Molecular Libraries Production Centers Network (MLPCN) Grant Number: 1X01DA026208-01 Assay Provider: Dr. Lawrance Barak , Duke University, Durham NC Drug addiction is a disease originating in the central nervous system that produces compulsive behaviors despite the negative consequences that may result. Major addictive drugs of abuse include components of tobacco, opiates, marijuana, ethanol, cocaine, and derivatives of amphetamines. While the addictive behaviors produced by these substances may be generally similar, the drugs act at different receptor sites in the brain. Recent studies have shown that opioid receptors play a role regulating the addictive behaviors of other receptors that interact with illicit and legal substances of abuse. Opioid receptors are composed of multiple subtypes whose contributions to addicti
- SAR analysis of small molecule agonists of the kappa opioid receptor via a luminescent beta-arrestin assay Data Source: Sanford-Burnham Center for Chemical Genomics (SBCCG) Source Affiliation: Sanford-Burnham Medical Research Institute (SBMRI, San Diego, CA) Network: NIH Molecular Libraries Production Centers Network (MLPCN) Grant Number: 1X01DA026208-01 Assay Provider: Dr. Lawrance Barak , Duke University, Durham NC Drug addiction is a disease originating in the central nervous system that produces compulsive behaviors despite the negative consequences that may result. Major addictive drugs of abuse include components of tobacco, opiates, marijuana, ethanol, cocaine, and derivatives of amphetamines. While the addictive behaviors produced by these substances may be generally similar, the drugs act at different receptor sites in the brain. Recent studies have shown that opioid receptors play a role regulating the addictive behaviors of other receptors that interact with illicit and legal substances of abuse. Opioid receptors are composed of multiple subtypes whose contributions to addicti
- SAR analysis of small molecule antagonists of the kappa opioid receptor via a luminescent beta-arrestin assay - Set 3 Data Source: Burnham Center for Chemical Genomics (BCCG) Source Affiliation: Burnham Institute for Medical Research (BIMR, La Jolla, CA) Network: NIH Molecular Libraries Probe Production Centers Network (MLPCN) Grant Number: 1X01DA026208-01 Assay Provider: Dr. Lawrance Barak , Duke University, Durham NC Drug addiction is a disease originating in the central nervous system that produces compulsive behaviors despite the negative consequences that may result. Major addictive drugs of abuse include components of tobacco, opiates, marijuana, ethanol, cocaine, and derivatives of amphetamines. While the addictive behaviors produced by these substances may be generally similar, the drugs act at different receptor sites in the brain. Recent studies have shown that opioid receptors play a role regulating the addictive behaviors of other receptors that interact with illicit and legal substances of abuse. Opioid receptors are composed of multiple subtypes whose contributions to addictive behavio
- SAR analysis of small molecule antagonists of the kappa opioid receptor via a luminescent beta-arrestin assay - Set 4 Data Source: Burnham Center for Chemical Genomics (BCCG) Source Affiliation: Burnham Institute for Medical Research (BIMR, La Jolla, CA) Network: NIH Molecular Libraries Probe Production Centers Network (MLPCN) Grant Number: 1X01DA026208-01 Assay Provider: Dr. Lawrance Barak , Duke University, Durham NC Drug addiction is a disease originating in the central nervous system that produces compulsive behaviors despite the negative consequences that may result. Major addictive drugs of abuse include components of tobacco, opiates, marijuana, ethanol, cocaine, and derivatives of amphetamines. While the addictive behaviors produced by these substances may be generally similar, the drugs act at different receptor sites in the brain. Recent studies have shown that opioid receptors play a role regulating the addictive behaviors of other receptors that interact with illicit and legal substances of abuse. Opioid receptors are composed of multiple subtypes whose contributions to addictive behavio
- SAR analysis of small molecule antagonists of the kappa opioid receptor via a luminescent beta-arrestin assay - Set 5 Data Source: Sanford-Burnham Center for Chemical Genomics (SBCCG) Source Affiliation: Sanford-Burnham Medical Research Institute (SBMRI, San Diego, CA) Network: NIH Molecular Libraries Probe Production Centers Network (MLPCN) Grant Number: 1X01DA026208-01 Assay Provider: Dr. Lawrance Barak , Duke University, Durham NC Drug addiction is a disease originating in the central nervous system that produces compulsive behaviors despite the negative consequences that may result. Major addictive drugs of abuse include components of tobacco, opiates, marijuana, ethanol, cocaine, and derivatives of amphetamines. While the addictive behaviors produced by these substances may be generally similar, the drugs act at different receptor sites in the brain. Recent studies have shown that opioid receptors play a role regulating the addictive behaviors of other receptors that interact with illicit and legal substances of abuse. Opioid receptors are composed of multiple subtypes whose contributions to ad
- SAR analysis of small molecule antagonists of the kappa opioid receptor via a luminescent beta-arrestin assay - Set 6 Data Source: Sanford-Burnham Center for Chemical Genomics (SBCCG) Source Affiliation: Sanford-Burnham Medical Research Institute (SBMRI, San Diego, CA) Network: NIH Molecular Libraries Probe Production Centers Network(MLPCN)Grant Number: 1X01DA026208-01 Assay Provider: Dr. Lawrance Barak , Duke University, Durham NC Drug addiction is a disease originating in the central nervous system that produces compulsive behaviors despite the negative consequences that may result. Major addictive drugs of abuse include components of tobacco, opiates, marijuana, ethanol, cocaine, and derivatives of amphetamines. While the addictive behaviors produced by these substances may be generally similar, the drugs act at different receptor sites in the brain. Recent studies have shown that opioid receptors play a role regulating the addictive behaviors of other receptors that interact with illicit and legal substances of abuse. Opioid receptors are composed of multiple subtypes whose contributions to addi
- SAR analysis of small molecule antagonists of the kappa opioid receptor via a luminescent beta-arrestin assay Data Source: Sanford-Burnham Center for Chemical Genomics (SBCCG) Source Affiliation: Sanford-Burnham Medical Research Institute (SBMRI, San Diego, CA) Network: NIH Molecular Libraries Production Centers Network (MLPCN) Grant Number: 1X01DA026208-01 Assay Provider: Dr. Lawrance Barak , Duke University, Durham NC Drug addiction is a disease originating in the central nervous system that produces compulsive behaviors despite the negative consequences that may result. Major addictive drugs of abuse include components of tobacco, opiates, marijuana, ethanol, cocaine, and derivatives of amphetamines. While the addictive behaviors produced by these substances may be generally similar, the drugs act at different receptor sites in the brain. Recent studies have shown that opioid receptors play a role regulating the addictive behaviors of other receptors that interact with illicit and legal substances of abuse. Opioid receptors are composed of multiple subtypes whose contributions to addictiv
- uHTS identification of small molecule antagonists of the kappa opioid receptor via a luminescent beta-arrestin assay Data Source: Sanford-Burnham Center for Chemical Genomics (SBCCG) Source Affiliation: Sanford-Burnham Medical Research Institute (SBMRI, San Diego, CA) Network: NIH Molecular Libraries Production Centers Network (MLPCN) Grant Number: 1X01DA026208-01 Assay Provider: Dr. Lawrance Barak , Duke University, Durham NC Drug addiction is a disease originating in the central nervous system that produces compulsive behaviors despite the negative consequences that may result. Major addictive drugs of abuse include components of tobacco, opiates, marijuana, ethanol, cocaine, and derivatives of amphetamines. While the addictive behaviors produced by these substances may be generally similar, the drugs act at different receptor sites in the brain. Recent studies have shown that opioid receptors play a role regulating the addictive behaviors of other receptors that interact with illicit and legal substances of abuse. Opioid receptors are composed of multiple subtypes whose contributions to addictiv
- Dopamine Transporter Binding Assay Brains from male Sprague-Dawley rats weighing 200-225 g (Taconic Labs) were removed, striatum dissected and quickly frozen. Membranes were prepared by homogenizing tissues in 20 volumes (w/v) of ice cold modified sucrose phosphate buffer (0.32 M sucrose, 7.74 mM Na2HPO4, 2.26 mM NaH2PO4, pH adjusted to 7.4) using a Brinkman Polytron (setting 6 for 20 sec) and centrifuged at 20,000ug for 10 min at 4° C. The resulting pellet was resuspended in buffer, recentrifuged and resuspended in buffer to a concentration of 10 mg/ml. Ligand binding experiments were conducted in assay tubes containing 0.5 ml sucrose phosphate buffer for 120 min on ice. Each tube contained 0.5 nM 3H WIN 35428 (specific activity 84 Ci/mmol) and 1.0 mg striatal tissue (original wet weight). Nonspecific binding was determined using 0.1 mM cocaine HCl. Incubations were terminated by rapid filtration through Whatman GF/B filters, presoaked in 0.05% PEI (polyethyleneimine), using a Brandel R48 filtering manifold (Brandel Instruments Gaithersburg, Md.). The filters were washed twice with 5 ml cold buffer and transferred to scintillation vials.
- Binding Assay Dopamine Transporter Binding Assay. Brains from male Sprague-Dawley rats weighing 200-225 g (Taconic Labs) were removed, striatum dissected and quickly frozen. Membranes were prepared by homogenizing tissues in 20 volumes (w/v) of ice cold modified sucrose phosphate buffer (0.32 M sucrose, 7.74 mM Na2HPO4, 2.26 mM NaH2PO4, pH adjusted to 7.4) using a Brinkman Polytron (setting 6 for 20 sec) and centrifuged at 20,000×g for 10 min at 4° C. The resulting pellet was resuspended in buffer, recentrifuged and resuspended in buffer to a concentration of 10 mg/ml. Ligand binding experiments were conducted in assay tubes containing 0.5 ml sucrose phosphate buffer for 120 min on ice. Each tube contained 0.5 nM 3H WIN 35428 (specific activity 84 Ci/mmol) and 1.0 mg striatal tissue (original wet weight). Nonspecific binding was determined using 0.1 mM cocaine HCl. Incubations were terminated by rapid filtration through Whatman GF/B filters, presoaked in 0.05% PEI (polyethyleneimine), using a Brandel R48 filtering manifold (Brandel Instruments Gaithersburg, Md.). The filters were washed twice with 5 ml cold buffer and transferred to scintillation vials. Beckman Ready Safe (3.0 ml) was added and the vials were counted the next day using a Beckman 6000 liquid scintillation counter (Beckman Coulter Instruments, Fullerton, Calif.). Data were analyzed by using GraphPad Prism software (San Diego, Calif.).