Evidence for antagonist activity of the dopamine D3 receptor partial agonist, BP 897, at human dopamine D3 receptor
by
Wood MD, Boyfield I, Nash DJ, Jewitt FR, Avenell KY, Riley GJ.
Department of Neuroscience Research,
SmithKline Beecham Pharmaceuticals,
New Frontiers Science Park, Third Avenue,
Essex, CM19 5AW, Harlow, UK.
[email protected]
Eur J Pharmacol 2000 Oct 27;407(1-2):47-51


ABSTRACT

The dopaminergic system has long been implicated in the mechanisms of reward and addiction. 1-(4-(2-Naphthoylamino)butyl)-4-(2-methoxyphenyl)-1A-piperazine HCl (BP 897) has been claimed to be a selective dopamine D3 receptor partial agonist and has recently been shown to inhibit cocaine-seeking behaviour, suggesting a role for dopamine D3 receptor agonists in the treatment of addiction. We have previously characterised the pharmacological profile of the human dopamine D3 and D2(long) receptors using microphysiometry and radioligand binding and we have now studied the interaction of BP 897 with the dopamine D2 and D3 receptors using these methods. At both human dopamine D3 and D2 receptors, BP 897 lacked agonist activity but was a potent and selective antagonist with pK(b) values of 8.05+/-0.16 (4) and 9.43+/-0.22 (4) at human dopamine D2 and D3 receptors, respectively. These results, therefore, suggest that it may be the dopamine D3 receptor antagonist properties of BP 897 which have potential in the treatment of addiction and withdrawal.


D3
BP 897
Dopamine
Supercoke
GBR12909
GABAergics
Oral cocaine
Cocaine hotspots
Dopaminergic agents
The coke-craving brain
Monoamines, cocaine and rats
Freebasing flies go hyperkinetic
Dopamine D3, sensitization and psychosis
BP 897, dopamine D3 agonists and cocaine use
BP 897, a selective dopamine D(3) receptor ligand


01 02 03 04 05 06 07 08 09 10 11 12
13 14 15 16 17 18 19 20 21 22 23 24


Refs
HOME
HedWeb
BLTC Research
Wirehead Hedonism
Paradise-Engineering
Utopian Pharmacology
The Hedonistic Imperative
When Is It Best to Take Crack Cocaine?

swan image
The Good Drug Guide
The Responsible Parent's Guide To
Healthy Mood Boosters For All The Family