NAS181 is a potent and selective antagonist of rat 5-HT 1B receptor, with a K i of 47 nM. NAS181 shows 13-fold selectivity for r5-HT 1B over bovine 5-HT 1B receptor (K i =630 nM). NAS181 increases the 5-HT turnover and the synaptic concentration of 5-HT by inhibiting terminal r5-HT 1B autoreceptors.
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