141533-35-9

SDZ-216525 is a 5-HT1A receptor antagonist which significantly inhibits the tracheal contractions induced both by NKA (10 nM-3 microM) and 5-HT (10 nM-10 microM) (n=4-10).

SDZ 216-525 is a selective silent antagonist of 5-HT1A receptor[1][2].

[1] Boddeke H W G M, et al. Agonist/antagonist interactions with cloned human 5-HT 1A receptors: variations in intrinsic activity studied in transfected HeLa cells[J]. Naunyn-Schmiedeberg's archives of pharmacology, 1992, 345: 257-263. DOI:10.1007/BF00168684
[2] Sharp T, et al. The novel 5‐HT1A receptor antagonist, SDZ 216–525, decreases 5‐HT release in rat hippocampus in vivo[J]. British journal of pharmacology, 1993, 109(3): 699-702. DOI:10.1111/j.1476-5381.1993.tb13630.x