N-substituted benztropine analogs: selective dopamine transporter ligands with a fast onset of action and minimal cocaine-like behavioral effects

SM Li, TA Kopajtic, MJ O'Callaghan, GE Agoston… - … of Pharmacology and …, 2011 - ASPET
Previous studies suggested that differences between the behavioral effects of cocaine and
analogs of benztropine were related to the relatively slow onset of action of the latter …

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 …

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 …

Assessment of the influence of histaminergic actions on cocaine-like effects of 3α-diphenylmethoxytropane analogs

VC Campbell, TA Kopajtic, AH Newman… - Journal of Pharmacology …, 2005 - ASPET
Previous studies demonstrated that analogs of benztropine (BZT) possess high affinity for
the dopamine (DA) transporter (DAT) but generally have behavioral effects different from …

Behavioral and neurochemical effects of the dopamine transporter ligand 4-chlorobenztropine alone and in combination with cocaine in vivo

BK Tolliver, AH Newman, JL Katz, LB Ho, LM Fox… - … of Pharmacology and …, 1999 - ASPET
The current studies evaluated the novel diphenylmethoxytropane analog 4-
chlorobenztropine (4-Cl-BZT), cocaine, and combinations of the two drugs for their abilities …

Dopamine transporter-dependent and-independent striatal binding of the benztropine analog JHW 007, a cocaine antagonist with low abuse liability

TA Kopajtic, Y Liu, CK Surratt, DM Donovan… - … of Pharmacology and …, 2010 - ASPET
The benztropine analog N-(n-butyl)-3α-[bis (4′-fluorophenyl) methoxy]-tropane (JHW 007)
displays high affinity for the dopamine transporter (DAT), but unlike typical DAT ligands, has …

Comparative structure–activity relationships of benztropine analogues at the dopamine transporter and histamine H1 receptors

SS Kulkarni, TA Kopajtic, JL Katz… - Bioorganic & medicinal …, 2006 - Elsevier
Benztropine (BZT) and its analogues inhibit dopamine uptake and bind with moderate to
high affinity to the dopamine transporter (DAT). However, many of these compounds, in …

Pharmacological characterization of a dopamine transporter ligand that functions as a cocaine antagonist

RI Desai, DK Grandy, CR Lupica, JL Katz - Journal of Pharmacology and …, 2014 - ASPET
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 …

Stimulus generalization from cocaine to analogs with high in vitro affinity for dopamine uptake sites

EJ Cline, P Terry, FI Carroll, MJ Kuhar… - Behavioural …, 1992 - journals.lww.com
Previous research has shown that phenyltropane derivatives of cocaine are very potent
ligands for dopamine transporters in in vitro binding and uptake, and in in vivo binding …

A dopamine transport inhibitor with markedly low abuse liability suppresses cocaine self-administration in the rat

A Ferragud, C Velázquez-Sánchez… - …, 2009 - Springer
Rationale N-substituted benztropine analogs are potent dopamine uptake inhibitors that
display pharmacokinetic/dynamic properties consistent with the profile of a substitute …