NAS181

rat 5-HT1B receptor antagonist

NAS-181 free base is a 5-HT(1B) receptor antagonist.

Tofacitinib maleate, also known as tasocitinib, CP-690550, is a Janus kinase (JAK) inhibitor. Tofacitinib maleate modulates the signaling pathway at the point of JAKs, preventing the phosphorylation and activation of STATs. JAK enzymes transmit cytokine signaling through pairing of JAKs (e.g., JAK1 JAK3, JAK1 JAK2, JAK1 TyK2, JAK2 JAK2). Tofacitinib maleate inhibited the in vitro activities of JAK1 JAK2, JAK1 JAK3, and JAK2 JAK2 combinations with IC50 of 406, 56, and 1377 nM, respectively.

NAS-181 是一种选择性大鼠 5-羟色胺 1B (r5-HT1B) 的有效拮抗剂 (Ki: 47 nM)。NAS-181 可以加强大鼠脑区 5-HTP 的积累。