Discovery of drugs to treat cocaine dependence: behavioral and neurochemical effects of atypical dopamine transport inhibitors
Stimulant drugs acting at the dopamine transporter (DAT), like cocaine, are widely abused,
yet effective medical treatments for this abuse have not been found. Analogs of benztropine …
yet effective medical treatments for this abuse have not been found. Analogs of benztropine …
Atypical dopamine uptake inhibitors that provide clues about cocaine's mechanism at the dopamine transporter
A Hauck Newman, JL Katz - Transporters as Targets for Drugs, 2009 - Springer
The dopamine transporter (DAT) has been a primary target for cocaine abuse/addiction
medicationdiscovery. However predicted addiction liability and limited clinical evaluation …
medicationdiscovery. However predicted addiction liability and limited clinical evaluation …
Dopamine transporter binding without cocaine-like behavioral effects: synthesis and evaluation of benztropine analogs alone and in combination with cocaine in …
JL Katz, GE Agoston, KL Alling, RH Kline… - …, 2001 - Springer
Rationale: Previous SAR studies demonstrated that small halogen substitutions on the
diphenylether system of benztropine (BZT), such as a para-Cl group, retained high affinity at …
diphenylether system of benztropine (BZT), such as a para-Cl group, retained high affinity at …
Identification of a dopamine transporter ligand that blocks the stimulant effects of cocaine
RI Desai, TA Kopajtic, M Koffarnus… - Journal of …, 2005 - Soc Neuroscience
There is a large unmet medical need for cocaine addiction treatments. Studies have
indicated that the dopamine transporter (DAT) is the primary biological target of cocaine, and …
indicated that the dopamine transporter (DAT) is the primary biological target of cocaine, and …
Relations between heterogeneity of dopamine transporter binding and function and the behavioral pharmacology of cocaine
Both in vitro binding studies and studies of dopamine uptake have indicated that there is a
heterogeneity of action of cocaine and cocaine analogs. Both high-and low-affinity binding …
heterogeneity of action of cocaine and cocaine analogs. Both high-and low-affinity binding …
Effects of N-substituted analogs of benztropine: diminished cocaine-like effects in dopamine transporter ligands
JL Katz, TA Kopajtic, GE Agoston… - Journal of Pharmacology …, 2004 - ASPET
Previous studies demonstrated that analogs of benztropine (BZT) possess high affinity for
the dopamine transporter, inhibit dopamine uptake, but generally have behavioral effects …
the dopamine transporter, inhibit dopamine uptake, but generally have behavioral effects …
Probes for the dopamine transporter: New leads toward a cocaine‐abuse therapeutic—A focus on analogues of benztropine and rimcazole
AH Newman, S Kulkarni - Medicinal research reviews, 2002 - Wiley Online Library
In an attempt to discover a cocaine‐abuse pharmacotherapeutic, extensive investigation has
been directed toward elucidating the molecular mechanisms underlying the reinforcing …
been directed toward elucidating the molecular mechanisms underlying the reinforcing …
Pharmacological characterization of a dopamine transporter ligand that functions as a cocaine antagonist
An N-butyl analog of benztropine, JHW007 [N-(n-butyl)-3 α-[bis (4′-fluorophenyl) methoxy]-
tropane], binds to dopamine transporters (DAT) but has reduced cocaine-like behavioral …
tropane], binds to dopamine transporters (DAT) but has reduced cocaine-like behavioral …
Combinations of cocaine with other dopamine uptake inhibitors: assessment of additivity
Drugs that inhibit dopamine (DA) reuptake through actions at the dopamine transporter
(DAT) have been proposed as candidates for development as pharmacotherapies for …
(DAT) have been proposed as candidates for development as pharmacotherapies for …
Behavioral and neurochemical effects of the dopamine transporter ligand 4-chlorobenztropine alone and in combination with cocaine in vivo
The current studies evaluated the novel diphenylmethoxytropane analog 4-
chlorobenztropine (4-Cl-BZT), cocaine, and combinations of the two drugs for their abilities …
chlorobenztropine (4-Cl-BZT), cocaine, and combinations of the two drugs for their abilities …