| Description |
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.
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| Related Catalog |
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| Target |
EC50: 4.5 nM (guinea pig 5-HT1B receptor)[1] Ki: 0.24 nM (guinea pig cortex 5HT1B/1D), 0.47 nM (recombinant guinea pig 5-HT1B receptor), 5 nM (guinea pig 5-HT1D receptor), 20 nM (rat cortical 5HT1B/1D receptor), 339 nM (rat cortex 5-HT2A receptor), 3070 nM (Rat hippocampus 5-HT1A receptor), 330 nM (dopamine D2), 490 nM (α1-adrenoceptor)[1]
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| In Vitro |
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].
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| References |
[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.
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