The enantiomers of SK&F 83566, a new selective D-1 dopamine antagonist, stereospecifically block stereotyped behaviour induced by apomorphine and by the selective D-2 agonist RU 24213.
The non-selective dopamine receptor agonist apomorphine and the selective D-2 receptor agonist RU24213 each induced a typical syndrome of stereotyped behaviour characterised by sniffing and locomotion. The syndrome and its associated behaviours induced by each agonist were dose-dependently antagonised by pretreatment with the R- but not with the S-enantiomer of the benzazepine SK&F 83566. R- but not S-SK&F 83566 stereoselectively blocks D-1 receptors with high affinity, while the enantiomers have a very weak affinity for D-2 receptors which shows negligible stereoselectivity. Therefore, enantioselective blockade of brain D-1 receptors appears able to influence the expression of behaviours initiated by D-2 receptor stimulation.
D015647:2,3,4,5-Tetrahydro-7,8-dihydroxy-1-phenyl-1H-3-benzazepine / Q000031:analogs & derivatives*; D000818:Animals; D001058:Apomorphine / Q000037:antagonists & inhibitors*; D001552:Benzazepines / Q000494:pharmacology*; D008297:Male; D009043:Motor Activity / Q000187:drug effects; D010627:Phenethylamines / Q000037:antagonists & inhibitors*; D051381:Rats; D011919:Rats, Inbred Strains; D011954:Receptors, Dopamine / Q000187:drug effects*; D013237:Stereoisomerism; D013239:Stereotyped Behavior / Q000187:drug effects*
D015647:2,3,4,5-Tetrahydro-7,8-dihydroxy-1-phenyl-1H-3-benzazepine; D001058:Apomorphine; D001552:Benzazepines; D010627:Phenethylamines; D011954:Receptors, Dopamine; C016868:N-n-propyl-N-phenylethyl-4(3-hydroxyphenyl)ethylamine hydrochloride; C044846:SKF83566