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Article

Mechanism of inverse agonist action of sarpogrelate at the constitutively active mutant of human 5-HT2A receptor revealed by molecular modeling.

Biological & pharmaceutical bulletin - 1 Jan 2012

Hossain Murad, Muntasir Habib Abul, Ishiguro Masaji, Bhuiyan Mohiuddin Ahmed, Rashid Mamunur, Sugihara Takumichi, Nagatomo Takafumi

Abstract excerpt

We previously reported that sarpogrelate, a selective 5-HT2A antagonist, showed a potent inverse agonist activity to constitutively active mutant (C322K) of human 5-HT2A receptor (5-HT2AR). However, it remains to be unknown about the actual mechanism of this mutant for its constitutive activation as well as inverse agonist activity of sarpogrelate. Our model shows that mutation (C322K) of 5-HT2AR causes...

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PMID: 22975508
DOI: 10.1248/bpb.b12-00401

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