Inhibitory effect of idazoxan on forskolin-stimulated adenylate cyclase activity through 5-hydroxytryptamine1A receptors.
The binding affinity of the alpha 2-adrenoceptor antagonist idazoxan (CAS 79944-56-2) to 5-hydroxytryptamine1A (5-HT1A) receptors and its effect on the forskolin-stimulated adenylate cyclase activity in the rat hippocampus were examined. Idazoxan had moderate affinity for the 5-HT1A receptors. It inhibited the forskolin-stimulated adenylate cyclase activity to the same extent as 5-HT. The 5-HT1A receptor antagonist spiperone shifted the concentration-response curve of idazoxan to the right in a parallel manner. These results indicate that idazoxan is a 5-HT1A agonist.
Kawai
N
N
Department of Psychopharmacology, Tokyo Institute of Psychiatry, Japan.
Yamamoto
T
T
Baba
A
A
Yamamoto
H
H
Moroji
T
T
D017371:8-Hydroxy-2-(di-n-propylamino)tetralin / Q000494:pharmacology; D000262:Adenylyl Cyclases / Q000378:metabolism*; D000317:Adrenergic alpha-Antagonists / Q000493:pharmacokinetics / Q000494:pharmacology*; D000818:Animals; D005576:Colforsin / Q000037:antagonists & inhibitors* / Q000494:pharmacology; D004146:Dioxanes / Q000493:pharmacokinetics / Q000494:pharmacology*; D006624:Hippocampus / Q000187:drug effects / Q000201:enzymology; D019329:Idazoxan; D066298:In Vitro Techniques; D008297:Male; D008566:Membranes / Q000187:drug effects / Q000201:enzymology / Q000378:metabolism; D051381:Rats; D017208:Rats, Wistar; D018341:Receptors, Adrenergic, alpha-2 / Q000187:drug effects / Q000378:metabolism; D011985:Receptors, Serotonin / Q000187:drug effects* / Q000378:metabolism
D000317:Adrenergic alpha-Antagonists; D004146:Dioxanes; D018341:Receptors, Adrenergic, alpha-2; D011985:Receptors, Serotonin; D005576:Colforsin; D017371:8-Hydroxy-2-(di-n-propylamino)tetralin; D000262:Adenylyl Cyclases; D019329:Idazoxan