SB-272183 is a selective serotonin 5-HT1A, 5-HT1B, and 5-HT1D receptor antagonist. It shows high affinity for these receptors, with Ki values of 10 nM, 7.9 nM, and 2.0 nM, respectively, and with at least 30-fold selectivity over various other receptors. The drug was a partial agonist of the serotonin 5-HT1A, 5-HT1B, and 5-HT1D receptors in vitro, but showed only antagonistic activity ex vivo in native tissue. SB-272183 was first described in the scientific literature in 2001. It is said to have been the first selective serotonin 5-HT1A, 5-HT1B, and 5-HT1D receptor antagonist to be described.
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