SB-616234-A

SB-616234-A is a selective and orally bioavailable 5-HT1B receptor antagonist, with anxiolytic and antidepressant activity.

Product information

CAS Number: 908601-49-0

Molecular Weight: 574.11

Formula: C32H36ClN5O3

Chemical Name: 6-[(3R,5S)-3,5-dimethylpiperazin-1-yl]-5-methoxy-1-[2'-methyl-4'-(5-methyl-1,2,4-oxadiazol-3-yl)-[1,1'-biphenyl]-4-carbonyl]-2,3-dihydro-1H-indole hydrochloride

Smiles: Cl.COC1=CC2CCN(C(=O)C3C=CC(=CC=3)C3=CC=C(C=C3C)C3=NOC(C)=N3)C=2C=C1N1C[C@H](C)N[C@H](C)C1

InChiKey: VPWVEPYFVFBHQR-XKFLBXONSA-N

InChi: InChI=1S/C32H35N5O3.ClH/c1-19-14-26(31-34-22(4)40-35-31)10-11-27(19)23-6-8-24(9-7-23)32(38)37-13-12-25-15-30(39-5)29(16-28(25)37)36-17-20(2)33-21(3)18-36;/h6-11,14-16,20-21,33H,12-13,17-18H2,1-5H3;1H/t20-,21+;

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 10 mg/mL (17.42 mM; Need ultrasonic).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

SB-616234-A possesses high affinity for human 5-HT1B receptors stably expressed in Chinese hamster ovary (CHO) cells (pKi 8.3 ± 0.2), and is over 100-fold selective for a range of molecular targets except h5-HT1D receptors (pKi 6.6 ± 0.1). Similarly, affinity (pKi) for rat and guinea pig striatal 5-HT1B receptors is 9.2 ± 0.1. In [35S]-GTPγS binding studies in the human recombinant cell line, SB-616234-A acts as a high affinity antagonist with a pA2 value of 8.6 ± 0.2 whilst providing no evidence of agonist activity in this system. In [35S]-GTPγS binding studies in rat striatal membranes, SB-616234-A acts as a high affinity antagonist with an apparent pKB of 8.4 ± 0.5, again whilst providing no evidence of agonist activity in this system. SB-616234-A (1 μM) potentiates electrically stimulated [3H]-5-HT release from guinea pig and rat cortical slices (S2/S1 ratios of 1.8 and 1.6, respectively).

In Vivo:

SB-616234-A reverses the 5-HT1/7 receptor agonist, SKF-99101H-induced hypothermia in guinea pigs in a dose related manner with an ED50 of 2.4 mg/kg p.o. SB-616234-A produces dose-related anxiolytic effects in both rat and guinea pig maternal separation-induced vocalisation models with an ED50 of 1.0 and 3.3 mg/kg i.p., respectively. SB-616234-A (0.3-30 mg/kg p.o.) causes a dose-dependent inhibition of ex vivo [3H]-GR125743 binding to rat striatal 5-HT1B receptors with an ED50 of 2.83 ± 0.39 mg/kg p.o.

Products are for research use only. Not for human use.