Dopamine transport inhibitors based on GBR12909 and benztropine as potential medications to treat cocaine addiction

RB Rothman, MH Baumann, TE Prisinzano… - Biochemical …, 2008 - Elsevier
The discovery and development of medications to treat addiction and notably, cocaine
addiction, have been frustrated by both the complexity of the disorder and the lack of target …

Development of neurochemical normalization (“agonist substitution”) therapeutics for stimulant abuse: focus on the dopamine uptake inhibitor, GBR12909

T Prisinzano, KC Rice, MH Baumann… - Current Medicinal …, 2004 - ingentaconnect.com
At the present time, there are no drugs are approved in the US for the treatment of stimulant
abuse. Based on a diverse body of preclinical data, sometimes termed the “dopamine …

Dopamine transporter ligands: recent developments and therapeutic potential

SP Runyon, F Carroll - Current topics in medicinal chemistry, 2006 - ingentaconnect.com
The dopamine transporter (DAT) is a target for the development of pharmacotherapies for a
number of central disorders including Parkinson's disease, Alzheimer's disease …

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 …

Discovery of drugs to treat cocaine dependence: behavioral and neurochemical effects of atypical dopamine transport inhibitors

G Tanda, AH Newman, JL Katz - Advances in pharmacology, 2009 - Elsevier
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 …

Interaction of cocaine‐, benztropine‐, and GBR12909‐like compounds with wild‐type and mutant human dopamine transporters: molecular features that differentially …

KC Schmitt, J Zhen, P Kharkar, M Mishra… - Journal of …, 2008 - Wiley Online Library
The widely abused psychostimulant cocaine is thought to elicit its reinforcing effects
primarily via inhibition of the neuronal dopamine transporter (DAT). However, not all DAT …

[HTML][HTML] Novel benztropine (3a-(diphenylmethoxy) tropane) analogs as probes for the dopamine transporter

AH Newman, GE Agoston - Current medicinal chemistry, 1998 - books.google.com
The design, synthesis and pharmacological evaluation of novel dopamine transporter
ligands, based on Benztropine [30-(diphenylmethoxy) tropane], has been a focus of our …

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 …

Cocaine cross-sensitization to dopamine uptake inhibitors: unique effects of GBR12909

GI Elmer, A Brockington, DA Gorelick, FI Carrol… - Pharmacology …, 1996 - Elsevier
Repeated administration of cocaine will cross-sensitize the locomotor response to a variety
of psychomotor stimulants. The ability of cocaine to cross-sensitize the locomotor effects of …

The dopamine transporter and cocaine medication development: drug self-administration in nonhuman primates

LL Howell, KM Wilcox - Journal of Pharmacology and Experimental …, 2001 - ASPET
Despite intensive medication development efforts, no effective pharmacotherapy for cocaine
abuse has demonstrated efficacy for long-term use. Given the obvious importance of the …