Antagonist effects of the enantiomers of 3-PPP towards alpha 1-adrenoceptors coupled to inositol phospholipid breakdown in the rat cerebral cortex.
The effects of the two enantiomers of 3-PPP upon alpha 1-adrenergic and muscarinic receptors coupled to the inositol phospholipid (PI) breakdown response have been investigated. 3-PPP(-) and 3-PPP(+) were found to antagonize the noradrenaline (10 microM)-stimulated PI breakdown in rat cerebral cortical miniprisms with IC50 values of 18 and 61 microM, respectively. The dopamine receptor antagonists haloperidol and raclopride were also antagonists, with IC50 values of 0.4 and 25 microM, respectively. 3-PPP(-) and raclopride were found further to act as competitive antagonists, with pA2 values of 6.03 and 5.44, respectively. 3-PPP(-), 3-PPP(+) and haloperidol also antagonized the muscarinic receptor-mediated carbachol (50 microM)-stimulated PI breakdown in cortical miniprisms, albeit at high concentrations (IC50 values of 91, 170 and 28 microM, respectively) whereas raclopride produced only 24% inhibition at the highest concentration tested (100 microM).
D000818:Animals; D000978:Antiparkinson Agents / Q000494:pharmacology*; D001285:Atropine / Q000378:metabolism; D002217:Carbachol / Q000037:antagonists & inhibitors; D002540:Cerebral Cortex / Q000187:drug effects / Q000378:metabolism*; D006220:Haloperidol / Q000494:pharmacology; D066298:In Vitro Techniques; D007295:Inositol Phosphates / Q000378:metabolism*; D008297:Male; D009638:Norepinephrine / Q000037:antagonists & inhibitors; D010643:Phenoxybenzamine / Q000378:metabolism; D010880:Piperidines / Q000494:pharmacology*; D011224:Prazosin / Q000378:metabolism; D020891:Raclopride; D051381:Rats; D011919:Rats, Inbred Strains; D011942:Receptors, Adrenergic, alpha / Q000187:drug effects*; D012457:Salicylamides / Q000494:pharmacology; D013237:Stereoisomerism; D013403:Sugar Phosphates / Q000378:metabolism*
D000978:Antiparkinson Agents; D007295:Inositol Phosphates; D010880:Piperidines; D011942:Receptors, Adrenergic, alpha; D012457:Salicylamides; D013403:Sugar Phosphates; D010643:Phenoxybenzamine; D020891:Raclopride; D001285:Atropine; D002217:Carbachol; C026539:preclamol; D006220:Haloperidol; D009638:Norepinephrine; D011224:Prazosin