Ketanserin

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种高亲和力、非选择性 5-HT2 受体拮抗剂，5-HT2A 的 Ki 值为 2-3 nM，5-HT2C 的 Ki 值为 28 nM。

A high-affinity, non-selective antagonist of 5-HT2 receptor with Ki of 2-3 nM for 5-HT2A and 28 nM for 5-HT2C; also has a high affinity antagonist for the H1 receptor (Ki= 2 nM) and α1-adrenergic receptor (Ki=40 nM); an antihypertensive agent.Hypertension Approved(In Vitro):Ketanserin at 0.3 μM inhibits the voltage-dependent step current (IhERG.step) and tail current (IhERG.tail) of hERG channels with a 5-min exposure. The synergistic effect observed for AA with 5-HT is, also, blocked by the 5-HT receptor blockers cyproheptadine (IC50=22.0±7 μM), Ketanserin (IC50=152±23 μM). Ketanserin (50-350 μM) inhibits the synergism by blocking the receptor in a dose-dependent manner. The IC50 value of Cyproheptadine is 22±7 μM and Ketanserin is 152±23 μM. Ketanserin inhibits platelet aggregation with an IC50 of 240 (169-339) nM.(In Vivo):Ketanserin is a 5-HT2A receptor antagonist. Ketanserin significantly reduces BDNF protein levels in numerous brain regions (CA1 and CA3 of the hippocampus, prefrontal cortex, central amygdaloid nucleus, dorsomedial hypothalamic nucleus, dentate gyrus, shell of the nucleus accumbens and midbrain periaqueductal gray). 5-HT2A antagonist Ketanserin can significantly reduce BDNF mRNA levels in various brain regions.

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R41468

GPCR/G Protein

5-HT Receptor

5-HT2A|5-HT2C(Human)|5-HT2C(Rat)

Cardiovascular Disease

Hypertension

74050-98-9

395.4268

C22H22FN3O3

>98% (HPLC)

DMSO: 8 mg/mL

O=C(N1CCN2CCC(C(C3=CC=C(F)C=C3)=O)CC2)NC4=C(C=CC=C4)C1=O

2,4(1H,3H)-Quinazolinedione, 3-[2-[4-(4-fluorobenzoyl)-1-piperidinyl]ethyl]-

(-20℃)

With Ice Pack

≥ 2 years