NAS-181 (free base) [CAS 205242-61-1]

NAS181 free base is a potent and selective antagonist of rat 5-HT1B receptor, with a Ki of 47 nM. NAS181 free base shows 13-fold selectivity for r5-HT1B over bovine 5-HT1B receptor (Ki=630 nM) . NAS181 free base increases the 5-HT turnover and the synaptic concentration of 5-HT by inhibiting terminal r5-HT1B autoreceptors[1][2].

[205242-61-1]

C19H26N2O4

346.42

[C@@H]1(CNCCO1)COC2=C3C(C=C(CO3)CN4CCOCC4)=CC=C2

5-HT Receptor

5-HT1 Receptor

Room temperature