1. GPCR/G Protein
    Neuronal Signaling
  2. 5-HT Receptor
  3. AR-A 2

AR-A 2 (Synonyms: AR-A 000002)

Cat. No.: HY-107018
Handling Instructions

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.

For research use only. We do not sell to patients.

AR-A 2 Chemical Structure

AR-A 2 Chemical Structure

CAS No. : 220051-79-6

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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.

IC50 & 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]

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].

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
Molecular Weight

448.60

Formula

C₂₇H₃₆N₄O₂

CAS No.

220051-79-6

SMILES

CC1=CC=C(N2CCN(C)CC2)C3=C1CC[[email protected]@H](NC(C4=CC=C(N5CCOCC5)C=C4)=O)C3

Shipping

Room temperature in continental US; may vary elsewhere

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AR-A 2
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HY-107018
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AR-A 2

Cat. No.: HY-107018