SDZ PSD 958, a novel D1 receptor antagonist with potential limbic selectivity.

Abstract	SDZ PSD 958, a novel benzo[g]quinoxaline derivative exhibits the properties of a potent orally active selective D1 receptor antagonist. It has high affinity for D1-like receptors (D1, D5; pKi = 9.7-9.8) labelled by [3H]SCH23390 and is at least 400 fold less active at D2-like receptors (i.e. D2, D4) labelled by [3H]spiperone. Effects in functional tests are consistent with D1 receptor antagonist properties. SDZ PSD 958 inhibited apomorphine-induced rearing in mice and prevented prolongation of novelty-induced locomotion in rats elicited by the selective D1 receptor agonist CY 208-243. By contrast, SDZ PSD 958 did not induce catalepsy and only weakly inhibited apomorphine-induced stereotyped gnawing in rats. This suggests that SDZ PSD 958 preferentially inhibits responses mediated by dopamine systems innervating the limbic system.
Authors	R Markstein, P Gull, C Rüdeberg, S Urwyler, A L Jaton, K McAllister, A K Dixon, D Hoyer
Journal	Journal of neural transmission (Vienna, Austria : 1996) (J Neural Transm (Vienna)) Vol. 103 Issue 3 Pg. 261-76 ( 1996) ISSN: 0300-9564 [Print] Austria
PMID	8739838 (Publication Type: Journal Article)
Chemical References	Dopamine Antagonists Quinoxalines Receptors, Dopamine D1 SDZ PSD 958 Prolactin Adenylyl Cyclases Apomorphine Acetylcholine
Topics	Acetylcholine (metabolism) Adenylyl Cyclases (metabolism) Animals Apomorphine (antagonists & inhibitors) Basal Ganglia Diseases (chemically induced, physiopathology) Catalepsy (chemically induced, psychology) Cattle Dopamine Antagonists (metabolism, pharmacology) Humans In Vitro Techniques Limbic System (drug effects, metabolism) Male Mice Motor Activity (drug effects) Prolactin (blood) Quinoxalines (pharmacokinetics, pharmacology) Radioligand Assay Rats Rats, Inbred Strains Rats, Sprague-Dawley Receptors, Dopamine D1 (agonists, antagonists & inhibitors) Retina (drug effects, enzymology) Sympathectomy, Chemical

Join CureHunter, for free Research Interface BASIC access!

Take advantage of free CureHunter research engine access to explore the best drug and treatment options for any disease. Find out why thousands of doctors, pharma researchers and patient activists around the world use CureHunter every day.

Realize the full power of the drug-disease research graph!