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Tytuł :
Synthesis and biological evaluation of tropane-like 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine (GBR 12909) analogues.
Autorzy :
Zhang Y; Laboratory of Medicinal Chemistry, Building 8, Room B1-22, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, Maryland 20892-0815, USA.
Joseph DB
Bowen WD
Flippen-Anderson JL
Dersch CM
Rothman RB
Jacobson AE
Rice KC
Pokaż więcej
Źródło :
Journal of medicinal chemistry [J Med Chem] 2001 Nov 08; Vol. 44 (23), pp. 3937-45.
Typ publikacji :
Journal Article; Research Support, U.S. Gov't, Non-P.H.S.; Research Support, U.S. Gov't, P.H.S.
MeSH Terms :
Nerve Tissue Proteins*
Dopamine/*metabolism
Dopamine Uptake Inhibitors/*chemical synthesis
Membrane Transport Proteins/*metabolism
Piperazines/*chemistry
Tropanes/*chemical synthesis
Animals ; Brain/metabolism ; Carrier Proteins/metabolism ; Crystallography, X-Ray ; Dopamine Plasma Membrane Transport Proteins ; Dopamine Uptake Inhibitors/chemistry ; Dopamine Uptake Inhibitors/metabolism ; In Vitro Techniques ; Male ; Membrane Glycoproteins/metabolism ; Rats ; Rats, Sprague-Dawley ; Receptor, Muscarinic M1 ; Receptors, Muscarinic/metabolism ; Serotonin/metabolism ; Serotonin Plasma Membrane Transport Proteins ; Structure-Activity Relationship ; Tropanes/chemistry ; Tropanes/metabolism
Czasopismo naukowe
Tytuł :
Effect of N-alkyl and N-alkenyl substituents in noroxymorphindole, 17-substituted-6,7-dehydro-4,5alpha-epoxy-3,14-dihydroxy-6,7:2',3'-indolomorphinans, on opioid receptor affinity, selectivity, and efficacy.
Autorzy :
McLamore S; Laboratory of Medicinal Chemistry, Building 8, Room B1-23, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, Maryland 20892-0815, USA.
Ullrich T
Rothman RB
Xu H
Dersch C
Coop A
Davis P
Porreca F
Jacobson AE
Rice KC
Pokaż więcej
Źródło :
Journal of medicinal chemistry [J Med Chem] 2001 Apr 26; Vol. 44 (9), pp. 1471-4.
Typ publikacji :
Journal Article
MeSH Terms :
Morphinans/*chemical synthesis
Receptors, Opioid/*metabolism
Animals ; Binding, Competitive ; Electric Stimulation ; Guanosine 5'-O-(3-Thiotriphosphate)/metabolism ; Guinea Pigs ; Ileum/drug effects ; Ileum/physiology ; In Vitro Techniques ; Male ; Mice ; Morphinans/chemistry ; Morphinans/metabolism ; Morphinans/pharmacology ; Muscle Contraction/drug effects ; Muscle, Smooth/drug effects ; Narcotic Antagonists ; Radioligand Assay ; Receptors, Opioid, delta/antagonists & inhibitors ; Receptors, Opioid, delta/metabolism ; Receptors, Opioid, kappa/antagonists & inhibitors ; Receptors, Opioid, kappa/metabolism ; Receptors, Opioid, mu/antagonists & inhibitors ; Receptors, Opioid, mu/metabolism ; Structure-Activity Relationship ; Vas Deferens/drug effects ; Vas Deferens/physiology
Czasopismo naukowe
Tytuł :
Design, synthesis, and monoamine transporter binding site affinities of methoxy derivatives of indatraline.
Autorzy :
Gu XH; Laboratory of Medicinal Chemistry, Building 8, Room B1-23, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, Maryland 20892-0815, USA.
Yu H
Jacobson AE
Rothman RB
Dersch CM
George C
Flippen-Anderson JL
Rice KC
Pokaż więcej
Źródło :
Journal of medicinal chemistry [J Med Chem] 2000 Dec 14; Vol. 43 (25), pp. 4868-76.
Typ publikacji :
Journal Article; Research Support, U.S. Gov't, Non-P.H.S.; Research Support, U.S. Gov't, P.H.S.
MeSH Terms :
Membrane Transport Proteins*
Nerve Tissue Proteins*
Symporters*
Carrier Proteins/*metabolism
Dopamine/*metabolism
Indans/*chemical synthesis
Membrane Glycoproteins/*metabolism
Methylamines/*chemical synthesis
Neurotransmitter Uptake Inhibitors/*chemical synthesis
Norepinephrine/*metabolism
Serotonin/*metabolism
Animals ; Binding, Competitive ; Crystallography, X-Ray ; Dopamine Plasma Membrane Transport Proteins ; Drug Design ; Indans/chemistry ; Indans/metabolism ; Methylamines/chemistry ; Methylamines/metabolism ; Neurotransmitter Uptake Inhibitors/chemistry ; Neurotransmitter Uptake Inhibitors/metabolism ; Norepinephrine Plasma Membrane Transport Proteins ; Radioligand Assay ; Serotonin Plasma Membrane Transport Proteins ; Structure-Activity Relationship
Czasopismo naukowe
Tytuł :
Synthesis and transporter binding properties of bridged piperazine analogues of 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine (GBR 12909).
Autorzy :
Zhang Y; Laboratory of Medicinal Chemistry, Building 8, Room B1-22, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, Maryland 20892-0815, USA.
Rothman RB
Dersch CM
de Costa BR
Jacobson AE
Rice KC
Pokaż więcej
Źródło :
Journal of medicinal chemistry [J Med Chem] 2000 Dec 14; Vol. 43 (25), pp. 4840-9.
Typ publikacji :
Journal Article; Research Support, U.S. Gov't, P.H.S.
MeSH Terms :
Membrane Transport Proteins*
Nerve Tissue Proteins*
Bridged Bicyclo Compounds, Heterocyclic/*chemical synthesis
Carrier Proteins/*metabolism
Dopamine/*metabolism
Dopamine Uptake Inhibitors/*chemical synthesis
Heterocyclic Compounds, Bridged-Ring/*chemical synthesis
Indoles/*chemical synthesis
Piperazines/*chemical synthesis
Animals ; Brain/metabolism ; Bridged Bicyclo Compounds, Heterocyclic/chemistry ; Bridged Bicyclo Compounds, Heterocyclic/metabolism ; Bridged Bicyclo Compounds, Heterocyclic/pharmacology ; Dopamine Plasma Membrane Transport Proteins ; Dopamine Uptake Inhibitors/chemistry ; Dopamine Uptake Inhibitors/metabolism ; Dopamine Uptake Inhibitors/pharmacology ; Heterocyclic Compounds, Bridged-Ring/chemistry ; Heterocyclic Compounds, Bridged-Ring/metabolism ; Heterocyclic Compounds, Bridged-Ring/pharmacology ; In Vitro Techniques ; Indoles/chemistry ; Indoles/metabolism ; Indoles/pharmacology ; Membrane Glycoproteins/metabolism ; Piperazines/chemistry ; Piperazines/metabolism ; Piperazines/pharmacology ; Radioligand Assay ; Rats ; Serotonin/metabolism ; Serotonin Plasma Membrane Transport Proteins ; Structure-Activity Relationship ; Synaptosomes/metabolism
Czasopismo naukowe
Tytuł :
Probes for narcotic receptor-mediated phenomena. 27. Synthesis and pharmacological evaluation of selective delta-opioid receptor agonists from 4-[(alphaR)-alpha-(2S,5R)-4-substituted-2, 5-dimethyl-1-piperazinyl-3-methoxybenzyl]-N,N-diethylbenzamides and their enantiomers.
Autorzy :
Furness MS; Laboratory of Medicinal Chemistry, Building 8, Room B1-22, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, Maryland 20892-0815, USA.
Zhang X
Coop A
Jacobson AE
Rothman RB
Dersch CM
Xu H
Porreca F
Rice KC
Pokaż więcej
Źródło :
Journal of medicinal chemistry [J Med Chem] 2000 Aug 10; Vol. 43 (16), pp. 3193-6.
Typ publikacji :
Journal Article
MeSH Terms :
Benzamides/*chemical synthesis
Piperazines/*chemical synthesis
Receptors, Opioid, delta/*agonists
Animals ; Benzamides/chemistry ; Benzamides/pharmacology ; Binding, Competitive ; Brain/metabolism ; Guanosine 5'-O-(3-Thiotriphosphate)/metabolism ; Guinea Pigs ; In Vitro Techniques ; Ligands ; Narcotic Antagonists/chemical synthesis ; Narcotic Antagonists/chemistry ; Narcotic Antagonists/pharmacology ; Piperazines/chemistry ; Piperazines/pharmacology ; Rats ; Receptors, Opioid, delta/metabolism ; Receptors, Opioid, kappa/metabolism ; Receptors, Opioid, mu/metabolism ; Stereoisomerism ; Structure-Activity Relationship
Czasopismo naukowe
Tytuł :
Probes for narcotic receptor mediated phenomena. 26. Synthesis and biological evaluation of diarylmethylpiperazines and diarylmethylpiperidines as novel, nonpeptidic delta opioid receptor ligands.
Autorzy :
Zhang X; Laboratory of Medicinal Chemistry, Building 8, Room B1-23, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, Maryland 20892, USA.
Rice KC
Calderon SN
Kayakiri H
Smith L
Coop A
Jacobson AE
Rothman RB
Davis P
Dersch CM
Porreca F
Pokaż więcej
Źródło :
Journal of medicinal chemistry [J Med Chem] 1999 Dec 30; Vol. 42 (26), pp. 5455-63.
Typ publikacji :
Journal Article; Research Support, U.S. Gov't, P.H.S.
MeSH Terms :
Piperazines/*chemical synthesis
Piperazines/*pharmacology
Receptors, Opioid, delta/*drug effects
Animals ; Brain/drug effects ; Brain/metabolism ; Guinea Pigs ; In Vitro Techniques ; Ligands ; Magnetic Resonance Spectroscopy ; Male ; Mass Spectrometry ; Mice ; Mice, Inbred ICR ; Molecular Probes ; Muscle Contraction/drug effects ; Muscle, Smooth/drug effects ; Muscle, Smooth/physiology ; Piperazines/metabolism ; Radioligand Assay ; Rats ; Receptors, Opioid, delta/metabolism ; Receptors, Opioid, delta/physiology ; Structure-Activity Relationship
Czasopismo naukowe
Tytuł :
Oxygenated analogues of 1-[2-(Diphenylmethoxy)ethyl]- and 1-[2-[Bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazines (GBR 12935 and GBR 12909) as potential extended-action cocaine-abuse therapeutic agents.
Autorzy :
Lewis DB; Laboratory of Medicinal Chemistry, Building 8, Room B1-23, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, Maryland 20892, USA.
Matecka D
Zhang Y
Hsin LW
Dersch CM
Stafford D
Glowa JR
Rothman RB
Rice KC
Pokaż więcej
Źródło :
Journal of medicinal chemistry [J Med Chem] 1999 Dec 02; Vol. 42 (24), pp. 5029-42.
Typ publikacji :
Journal Article; Research Support, U.S. Gov't, P.H.S.
MeSH Terms :
Membrane Glycoproteins*
Membrane Transport Proteins*
Nerve Tissue Proteins*
Cocaine-Related Disorders/*drug therapy
Dopamine Uptake Inhibitors/*chemical synthesis
Piperazines/*chemical synthesis
Piperazines/*chemistry
Animals ; Carrier Proteins/metabolism ; Delayed-Action Preparations ; Dopamine/metabolism ; Dopamine Plasma Membrane Transport Proteins ; Hydroxylation ; Ligands ; Macaca mulatta ; Male ; Methylation ; Molecular Structure ; Oxygen/chemistry ; Piperazines/metabolism ; Piperazines/pharmacology ; Rats ; Structure-Activity Relationship ; Tritium
Czasopismo naukowe
Tytuł :
Synthesis, opioid receptor binding, and biological activities of naltrexone-derived pyrido- and pyrimidomorphinans.
Autorzy :
Ananthan S; Organic Chemistry Department, Southern Research Institute, Birmingham, Alabama 35255, USA. />Kezar HS 3rd
Carter RL
Saini SK
Rice KC
Wells JL
Davis P
Xu H
Dersch CM
Bilsky EJ
Porreca F
Rothman RB
Pokaż więcej
Źródło :
Journal of medicinal chemistry [J Med Chem] 1999 Sep 09; Vol. 42 (18), pp. 3527-38.
Typ publikacji :
Journal Article; Research Support, U.S. Gov't, P.H.S.
MeSH Terms :
Morphinans/*chemical synthesis
Morphine/*pharmacology
Naltrexone/*chemistry
Receptors, Opioid/*metabolism
Analgesics/chemical synthesis ; Analgesics/pharmacology ; Animals ; Binding, Competitive ; Brain/drug effects ; Enkephalin, Ala(2)-MePhe(4)-Gly(5)- ; Enkephalin, Leucine-2-Alanine/metabolism ; Enkephalins/metabolism ; Guinea Pigs ; Ileum/drug effects ; Male ; Mice ; Mice, Inbred Strains ; Morphinans/pharmacology ; Muscle Contraction/drug effects ; Protein Binding ; Rats ; Vas Deferens/drug effects
Czasopismo naukowe
Tytuł :
delta Opioid affinity and selectivity of 4-hydroxy-3-methoxyindolomorphinan analogues related to naltrindole.
Autorzy :
Coop A; Laboratory of Medicinal Chemistry, Building 8, Room B1-23, National Institute of Diabetes, Digestive and Kidney Diseases, National Institutes of Health, Bethesda, Maryland 20892, USA.
Rothman RB
Dersch C
Partilla J
Porreca F
Davis P
Jacobson AE
Rice KC
Pokaż więcej
Źródło :
Journal of medicinal chemistry [J Med Chem] 1999 May 06; Vol. 42 (9), pp. 1673-9.
Typ publikacji :
Journal Article
MeSH Terms :
Indoles/*chemical synthesis
Naltrexone/*analogs & derivatives
Narcotic Antagonists/*chemical synthesis
Receptors, Opioid, delta/*metabolism
Animals ; Binding, Competitive ; Brain/metabolism ; Guanosine 5'-O-(3-Thiotriphosphate)/metabolism ; Ileum/drug effects ; Ileum/physiology ; In Vitro Techniques ; Indoles/chemistry ; Indoles/pharmacology ; Ligands ; Male ; Mice ; Mice, Inbred ICR ; Muscle Contraction/drug effects ; Muscle, Smooth/drug effects ; Muscle, Smooth/physiology ; Naltrexone/chemical synthesis ; Naltrexone/chemistry ; Naltrexone/pharmacology ; Narcotic Antagonists/chemistry ; Narcotic Antagonists/pharmacology ; Rabbits ; Receptors, Opioid, delta/antagonists & inhibitors ; Vas Deferens/drug effects ; Vas Deferens/physiology
Czasopismo naukowe
Tytuł :
Characterization of novel N,N'-disubstituted piperazines as sigma receptor ligands.
Autorzy :
Zhang Y; Laboratory of Medicinal Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, 8 Center Drive, MSC 0815, Bethesda, Maryland 20892-0815, USA.
Williams W
Torrence-Campbell C
Bowen WD
Rice KC
Pokaż więcej
Źródło :
Journal of medicinal chemistry [J Med Chem] 1998 Dec 03; Vol. 41 (25), pp. 4950-7.
Typ publikacji :
Journal Article; Research Support, U.S. Gov't, P.H.S.
MeSH Terms :
Piperazines/*chemical synthesis
Receptors, sigma/*metabolism
Animals ; Brain/metabolism ; Guinea Pigs ; In Vitro Techniques ; Ligands ; Liver/metabolism ; Piperazines/chemistry ; Piperazines/metabolism ; Radioligand Assay ; Rats ; Structure-Activity Relationship
Czasopismo naukowe
Tytuł :
Synthesis, opioid receptor binding, and bioassay of naltrindole analogues substituted in the indolic benzene moiety.
Autorzy :
Ananthan S; Organic Chemistry Department, Southern Research Institute, Birmingham, Alabama 35255, USA. />Johnson CA
Carter RL
Clayton SD
Rice KC
Xu H
Davis P
Porreca F
Rothman RB
Pokaż więcej
Źródło :
Journal of medicinal chemistry [J Med Chem] 1998 Jul 16; Vol. 41 (15), pp. 2872-81.
Typ publikacji :
Comparative Study; Journal Article; Research Support, U.S. Gov't, P.H.S.
MeSH Terms :
Indoles*/chemical synthesis
Indoles*/pharmacology
Morphinans*/chemical synthesis
Morphinans*/pharmacology
Narcotic Antagonists*/chemical synthesis
Narcotic Antagonists*/metabolism
Narcotic Antagonists*/pharmacology
Naltrexone/*analogs & derivatives
Receptors, Opioid/*metabolism
Animals ; Brain/drug effects ; Brain/metabolism ; Guinea Pigs ; Ileum/drug effects ; Ileum/physiology ; Ligands ; Male ; Mice ; Muscle Contraction/drug effects ; Muscle, Smooth/drug effects ; Muscle, Smooth/physiology ; Naltrexone/metabolism ; Naltrexone/pharmacology ; Rats ; Receptors, Opioid/agonists ; Receptors, Opioid, delta/agonists ; Receptors, Opioid, delta/antagonists & inhibitors ; Receptors, Opioid, delta/metabolism ; Receptors, Opioid, kappa/agonists ; Receptors, Opioid, kappa/antagonists & inhibitors ; Receptors, Opioid, kappa/metabolism ; Receptors, Opioid, mu/agonists ; Receptors, Opioid, mu/antagonists & inhibitors ; Receptors, Opioid, mu/metabolism ; Structure-Activity Relationship ; Vas Deferens/drug effects ; Vas Deferens/physiology
Czasopismo naukowe
Tytuł :
Probes for narcotic receptor-mediated phenomena. 25. Synthesis and evaluation of N-alkyl-substituted (alpha-piperazinylbenzyl)benzamides as novel, highly selective delta opioid receptor agonists.
Autorzy :
Katsura Y; Laboratory of Medicinal Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, Maryland 20892, USA.
Zhang X
Homma K
Rice KC
Calderon SN
Rothman RB
Yamamura HI
Davis P
Flippen-Anderson JL
Xu H
Becketts K
Foltz EJ
Porreca F
Pokaż więcej
Źródło :
Journal of medicinal chemistry [J Med Chem] 1997 Aug 29; Vol. 40 (18), pp. 2936-47.
Typ publikacji :
Journal Article; Research Support, U.S. Gov't, Non-P.H.S.; Research Support, U.S. Gov't, P.H.S.
MeSH Terms :
Benzamides/*chemical synthesis
Narcotics/*agonists
Narcotics/*chemical synthesis
Piperazines/*chemical synthesis
Receptors, Opioid, delta/*agonists
Alkylation ; Animals ; Benzamides/chemistry ; Benzamides/pharmacology ; Brain/metabolism ; CHO Cells ; Cell Membrane/metabolism ; Cricetinae ; Crystallography, X-Ray ; Guinea Pigs ; Humans ; Kinetics ; Male ; Mice ; Mice, Inbred ICR ; Models, Molecular ; Molecular Conformation ; Molecular Structure ; Muscle Contraction/drug effects ; Muscle, Smooth/drug effects ; Muscle, Smooth/physiology ; Narcotics/chemistry ; Narcotics/pharmacology ; Piperazines/chemistry ; Piperazines/pharmacology ; Radioligand Assay ; Rats ; Receptors, Opioid, delta/metabolism ; Receptors, Opioid, mu/metabolism ; Structure-Activity Relationship ; Transfection ; Vas Deferens/drug effects ; Vas Deferens/physiology
Czasopismo naukowe
Tytuł :
Heteroaromatic analogs of 1-[2-(diphenylmethoxy)ethyl]- and 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazines (GBR 12935 and GBR 12909) as high-affinity dopamine reuptake inhibitors.
Autorzy :
Matecka D; Laboratory of Medicinal Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, Maryland 20892, USA.
Lewis D
Rothman RB
Dersch CM
Wojnicki FH
Glowa JR
DeVries AC
Pert A
Rice KC
Pokaż więcej
Źródło :
Journal of medicinal chemistry [J Med Chem] 1997 Feb 28; Vol. 40 (5), pp. 705-16.
Typ publikacji :
Journal Article; Research Support, U.S. Gov't, P.H.S.
MeSH Terms :
Membrane Transport Proteins*
Nerve Tissue Proteins*
Carrier Proteins/*metabolism
Dopamine Uptake Inhibitors/*pharmacology
Piperazines/*pharmacology
Animals ; Cocaine/administration & dosage ; Cocaine/analogs & derivatives ; Cocaine/metabolism ; Dopamine/metabolism ; Dopamine Plasma Membrane Transport Proteins ; Dopamine Uptake Inhibitors/chemical synthesis ; Dopamine Uptake Inhibitors/chemistry ; Dopamine Uptake Inhibitors/metabolism ; Feeding Behavior/drug effects ; Ligands ; Macaca mulatta ; Magnetic Resonance Spectroscopy ; Membrane Glycoproteins/metabolism ; Molecular Structure ; Motor Activity/drug effects ; Pentazocine/metabolism ; Piperazines/chemical synthesis ; Piperazines/chemistry ; Piperazines/metabolism ; Rats ; Serotonin Plasma Membrane Transport Proteins ; Structure-Activity Relationship
Czasopismo naukowe
Tytuł :
Probes for narcotic receptor mediated phenomena. 23. Synthesis, opioid receptor binding, and bioassay of the highly selective delta agonist (+)-4-[(alpha R)-alpha-((2S,5R)-4-Allyl-2,5-dimethyl-1-piperazinyl)-3-methoxybenzyl]- N,N-diethylbenzamide (SNC 80) and related novel nonpeptide delta opioid receptor ligands.
Autorzy :
Calderon SN; Laboratory of Medicinal Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, Maryland 20892, USA.
Rice KC
Rothman RB
Porreca F
Flippen-Anderson JL
Kayakiri H
Xu H
Becketts K
Smith LE
Bilsky EJ
Davis P
Horvath R
Pokaż więcej
Źródło :
Journal of medicinal chemistry [J Med Chem] 1997 Feb 28; Vol. 40 (5), pp. 695-704.
Typ publikacji :
Journal Article; Research Support, U.S. Gov't, Non-P.H.S.; Research Support, U.S. Gov't, P.H.S.
MeSH Terms :
Benzamides/*chemical synthesis
Benzamides/*metabolism
Piperazines/*chemical synthesis
Piperazines/*metabolism
Receptors, Opioid, delta/*agonists
Animals ; Benzamides/chemistry ; Benzamides/pharmacology ; Binding, Competitive ; Brain/metabolism ; Crystallography, X-Ray ; Enkephalin, Ala(2)-MePhe(4)-Gly(5)- ; Enkephalin, Leucine-2-Alanine/metabolism ; Enkephalins/metabolism ; Guinea Pigs ; Ileum/metabolism ; Magnetic Resonance Spectroscopy ; Male ; Mice ; Molecular Conformation ; Molecular Structure ; Muscle Contraction/drug effects ; Piperazines/chemistry ; Piperazines/pharmacology ; Radioligand Assay ; Rats ; Receptors, Opioid, delta/metabolism ; Receptors, Opioid, mu/metabolism ; Stereoisomerism ; Vas Deferens/metabolism
Czasopismo naukowe
Tytuł :
Sustained decrease in cocaine-maintained responding in rhesus monkeys with 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-hydroxy-3-phenylpropyl) piperazinyl decanoate, a long-acting ester derivative of GBR 12909.
Autorzy :
Glowa JR; Department of Psychiatry, Uniformed Services University of the Health Sciences, Bethesda, Maryland 20814, USA.
Fantegrossi WE
Lewis DB
Matecka D
Rice KC
Rothman RB
Pokaż więcej
Źródło :
Journal of medicinal chemistry [J Med Chem] 1996 Nov 22; Vol. 39 (24), pp. 4689-91.
Typ publikacji :
Journal Article; Research Support, U.S. Gov't, P.H.S.
MeSH Terms :
Cocaine/*metabolism
Piperazines/*pharmacology
Animals ; Behavior, Animal/drug effects ; Decanoates/chemical synthesis ; Decanoates/pharmacology ; Dopamine Uptake Inhibitors ; Macaca mulatta ; Male ; Molecular Structure ; Piperazines/chemical synthesis ; Substance-Related Disorders/therapy
Czasopismo naukowe
Tytuł :
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).
Autorzy :
Matecka D; Laboratory of Medicinal Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, Maryland 20892, USA.
Rothman RB
Radesca L
de Costa BR
Dersch CM
Partilla JS
Pert A
Glowa JR
Wojnicki FH
Rice KC
Pokaż więcej
Źródło :
Journal of medicinal chemistry [J Med Chem] 1996 Nov 22; Vol. 39 (24), pp. 4704-16.
Typ publikacji :
Journal Article; Research Support, U.S. Gov't, P.H.S.
MeSH Terms :
Membrane Glycoproteins*
Membrane Transport Proteins*
Nerve Tissue Proteins*
Dopamine Uptake Inhibitors/*chemical synthesis
Piperazines/*chemical synthesis
Animals ; Carrier Proteins/drug effects ; Carrier Proteins/metabolism ; Cocaine/pharmacology ; Dopamine/metabolism ; Dopamine Plasma Membrane Transport Proteins ; Dopamine Uptake Inhibitors/pharmacology ; Drug Design ; Magnetic Resonance Spectroscopy ; Mass Spectrometry ; Molecular Conformation ; Molecular Structure ; Piperazines/metabolism ; Piperazines/pharmacology ; Rats ; Receptors, Drug/metabolism ; Serotonin/metabolism ; Substance-Related Disorders/therapy
Czasopismo naukowe
Tytuł :
Synthesis and evaluation of aryl-substituted N-(arylethyl)-N-methyl-2-(1-pyrrolidinyl)ethylamines and corresponding arylacetamides for sigma receptor affinity.
Autorzy :
Zhang Y; Laboratory of Medicinal Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, Maryland 20892-0815, USA.
Williams W
Bowen WD
Rice KC
Pokaż więcej
Źródło :
Journal of medicinal chemistry [J Med Chem] 1996 Aug 30; Vol. 39 (18), pp. 3564-8.
Typ publikacji :
Journal Article; Research Support, U.S. Gov't, P.H.S.
MeSH Terms :
Acetamides/*chemical synthesis
Ethylamines/*chemical synthesis
Receptors, sigma/*metabolism
Acetamides/metabolism ; Animals ; Ethylamines/metabolism ; Guinea Pigs ; In Vitro Techniques ; Rats ; Structure-Activity Relationship
Czasopismo naukowe
Tytuł :
Probes for narcotic receptor-mediated phenomena. 21. Novel derivatives of 3-(1,2,3,4,5,11-hexahydro-3-methyl-2,6-methano-6H-azocino[4,5-b]indol- 6-yl)-phenols with improved delta opioid receptor selectivity.
Autorzy :
Bertha CM; Laboratory of Medicinal Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, Maryland 20892, USA.
Ellis M
Flippen-Anderson JL
Porreca F
Rothman RB
Davis P
Xu H
Becketts K
Rice KC
Pokaż więcej
Źródło :
Journal of medicinal chemistry [J Med Chem] 1996 May 10; Vol. 39 (10), pp. 2081-6.
Typ publikacji :
Journal Article; Research Support, U.S. Gov't, Non-P.H.S.; Research Support, U.S. Gov't, P.H.S.
MeSH Terms :
Phenols/*pharmacology
Receptors, Opioid, delta/*drug effects
Analgesics/metabolism ; Animals ; Crystallography, X-Ray ; Guinea Pigs ; Ileum/drug effects ; Ileum/physiology ; In Vitro Techniques ; Male ; Mice ; Mice, Inbred ICR ; Molecular Probes ; Phenols/chemistry ; Radioligand Assay ; Receptors, Opioid, delta/metabolism ; Stereoisomerism ; Vas Deferens/drug effects ; Vas Deferens/physiology
Czasopismo naukowe
Tytuł :
(Aminoalkyl)indole isothiocyanates as potential electrophilic affinity ligands for the brain cannabinoid receptor.
Autorzy :
Yamada K; Laboratory of Medicinal Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, Maryland 20892, USA.
Rice KC
Flippen-Anderson JL
Eissenstat MA
Ward SJ
Johnson MR
Howlett AC
Pokaż więcej
Źródło :
Journal of medicinal chemistry [J Med Chem] 1996 May 10; Vol. 39 (10), pp. 1967-74.
Typ publikacji :
Journal Article; Research Support, U.S. Gov't, Non-P.H.S.; Research Support, U.S. Gov't, P.H.S.
MeSH Terms :
Brain/*metabolism
Isothiocyanates/*metabolism
Receptors, Drug/*metabolism
Adenylyl Cyclases/metabolism ; Animals ; Cell Line ; Cyclohexanols/metabolism ; Isothiocyanates/chemistry ; Magnetic Resonance Spectroscopy ; Mass Spectrometry/methods ; Radioligand Assay ; Rats ; Receptors, Cannabinoid
Czasopismo naukowe
Tytuł :
(E)-8-benzylidene derivatives of 2-methyl-5-(3-hydroxyphenyl)morphans: highly selective ligands for the sigma 2 receptor subtype.
Autorzy :
Bertha CM; Laboratory of Medicinal Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, Maryland 20892, USA.
Vilner BJ
Mattson MV
Bowen WD
Becketts K
Xu H
Rothman RB
Flippen-Anderson JL
Rice KC
Pokaż więcej
Źródło :
Journal of medicinal chemistry [J Med Chem] 1995 Nov 24; Vol. 38 (24), pp. 4776-85.
Typ publikacji :
Journal Article; Research Support, U.S. Gov't, P.H.S.
MeSH Terms :
Ligands*
Benzylidene Compounds/*chemistry
Benzylidene Compounds/*pharmacology
Receptors, sigma/*drug effects
Animals ; Benzylidene Compounds/chemical synthesis ; Binding Sites ; Brain/drug effects ; Brain/metabolism ; Guinea Pigs ; Male ; Radioligand Assay ; Rats ; Rats, Sprague-Dawley ; Receptors, sigma/metabolism ; Stereoisomerism ; Structure-Activity Relationship
Czasopismo naukowe

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