AR-A 2 (AR-A 000002)

AR-A 2 (AR-A 000002) 是一种选择性 5-HT1B 受体拮抗剂，对豚鼠皮层 5HT1B/1D 和重组豚鼠 5-HT1B 受体具有高亲和力（Ki=0.24 和 0.47 nM），具有 10 倍的亲和力。对豚鼠 5-HT1D 受体的亲和力较低 (Ki, 5 nM)，对豚鼠 5-HT1B 受体的 EC50 为 4.5 nM； AR-A 2 (AR-A 000002) 可用于抑郁和焦虑的研究。

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Background

AR-A 2 is a selective 5-HT1B receptor antagonist, with high affinity to guinea pig cortex 5HT1B/1D and recombinant guinea pig 5-HT1B receptors (Ki=0.24 and 0.47 nM) and with 10-fold lower affinity to guinea pig 5-HT1D receptor (Ki, 5 nM), and shows an EC50 of 4.5 nM for the guinea pig 5-HT1B receptor; AR-A 2 can be used in the research of depression and anxiety.

AR-A 2 (AR-A000002) is a selective 5-HT1B receptor antagonist, with high affinity to guinea pig cortex 5HT1B/1D and recombinant guinea pig 5-HT1B receptors (Ki=0.24 and 0.47 nM) and with 10-fold lower affinity to guinea pig 5-HT1D receptors (Ki, 5 nM), and shows an EC50 of 4.5 nM for the guinea pig 5-HT1B receptor. AR-A 2 also binds to the rat cortical 5HT1B/1D receptor (Ki, 20 nM), rat cortex 5-HT2A receptor (Ki, 339 nM), rat hippocampus 5-HT1A receptor (Ki, 3070 nM). In addition, AR-A 2 also exhibits affinity for dopamine D2 (Ki, 330 nM) and α1-adrenoceptors (Ki, 490 nM)[1].

[1]. Ahlgren C, et al. In vitro characterization of AR-A000002, a novel 5-hydroxytryptamine(1B) autoreceptor antagonist. Eur J Pharmacol. 2004 Sep 19;499(1-2):67-75.