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Article

Inverse agonism and neutral antagonism at a constitutively active alpha-1a adrenoceptor.

British journal of pharmacology - 1 Oct 2000

Zhu J, Taniguchi T, Takauji R, Suzuki F, Tanaka T, Muramatsu I

Abstract excerpt

We have studied the antagonist action of prazosin and KMD-3213 in a constitutively active mutant of the human alpha-1a adrenoceptor in which Ala(271) was substituted to Thr and was expressed in CHO cells. Inverse agonism was characterized by up-regulation of receptor density, a decrease in basal GTPgammaS binding, and a reduction in basal inositol-1,4,5-trisphosphate (IP(3)) level. According to the above...

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Identifiers

PMID: 11015306
DOI: 10.1038/sj.bjp.0703584
PMCID: PMC1572343

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-07.1.

Source receipt: pubmed, retrieved 7 Sept 2026.

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