Article
Inverse agonist activity of sarpogrelate, a selective 5-HT2A-receptor antagonist, at the constitutively active human 5-HT2A receptor.
Journal of pharmacological sciences - 1 Oct 2006
Muntasir Habib Abul, Bhuiyan Mohiuddin Ahmed, Ishiguro Masaji, Ozaki Masanobu, Nagatomo Takafumi
Abstract excerpt
Mutations producing constitutively active G-protein coupled receptors have been found in the pathophysiology of several diseases, implying that inverse agonists at the constitutively active receptors may have preferred therapeutic applications. Because of the involvement of 5-HT(2A) receptors in mediating many cardiovascular diseases, constitutively active mutants of the 5-HT(2A) receptor may be responsible for...
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