[sun-shine]

MK3207(mk-3207);
cas#957118-49-9;
purity:98%;
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Biological Activity of MK 3207:
MK3207 is a potent and orally bioavailable CGRP receptor antagonist. In vitro, it is a potent antagonist of the human and rhesus CGRP receptors (Ki = 0.024 nM). In common with other CGRP receptor antagonists MK-3207 displays lower affinity for CGRP receptors from other species including canine and rodent. As a consequence of species selectivity the in vivo potency was assessed in a rhesus pharmacodynamic assay measuring capsaicin-induced changes in forearm dermal blood flow via laser Doppler imaging. MK-3207 produced a concentration-dependent inhibition of dermal vasodilation with plasma concentrations of 0.8 and 7 nM required to block 50 and 90% of the blood flow increase, respectively.