B-HT 920 activates dopamine D2 receptors coupled to inhibition of adenylate cyclase activity.

Authors: Onali P; Olianas MC

Abstract: In homogenates of female rat anterior pituitary, the azepine derivative B-HT 920 inhibited the forskolin-stimulated adenylate cyclase activity with an EC50 value of 0.35 microM. In male rat anterior pituitary, B-HT 920 curtailed the stimulation of adenylate cyclase activity by vasoactive intestinal peptide with an EC50 of 0.20 microM. In synaptic plasma membranes of rat striatum, B-HT 920 significantly reduced basal adenylate cyclase activity with an EC50 of 0.68 microM. Both in pituitary and striatum, the B-HT 920 inhibition was counteracted by the dopamine (DA) D2 receptor antagonist 1-sulpiride, but not by the alpha 2-adrenergic antagonist yohimbine. These results indicate that B-HT 920 is capable of activating DA D2 receptors negatively coupled to adenylate cyclase activity.

Keywords: Adenylate Cyclase/*metabolism; Animals; Azepines/*pharmacology; Corpus Striatum/cytology/enzymology/metabolism; Dopamine Agents/*pharmacology; Female; Male; Pituitary Gland, Anterior/cytology/enzymology/metabolism; Rats; Rats, Inbred Strains; Receptors, Dopamine/*drug effects; Receptors, Dopamine D2; Sulpiride/pharmacology; Yohimbine/pharmacology
Journal: Journal of neural transmission. General section
Volume: 88
Issue: 2
Pages: 95-104
Date: Jan. 1, 1992
PMID: 1352980
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Citation:

Onali P, Olianas MC (1992) B-HT 920 activates dopamine D2 receptors coupled to inhibition of adenylate cyclase activity. Journal of neural transmission. General section 88: 95-104.



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