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SB-616234-A

Catalog No. T12847 CAS 908601-49-0

Synonyms: SB-616234A

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

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SB-616234-A, CAS 908601-49-0

Pack Size	Availability	Price/USD
1 mg	In stock	$ 212.00
5 mg	In stock	$ 538.00
10 mg	In stock	$ 778.00
25 mg	In stock	$ 1,180.00
50 mg	In stock	$ 1,590.00
100 mg	In stock	$ 2,180.00
1 mL * 10 mM (in DMSO)	In stock	$ 679.00

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Biological Description

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Description	SB-616234-A is a selective and orally bioavailable antagonist of 5-HT1B receptor, with anxiolytic and antidepressant activity.
In vitro	SB-616234A possesses high affinity for human 5-HT1B receptors stably expressed in Chinese hamster ovary (CHO) cells (pKi 8.3 ± 0.2). Similarly, rat and guinea pig striatal 5-HT1B receptors affinity (pKi) of 9.2 ± 0.1. In [35S]-GTPγS binding studies in the human recombinant cell line, SB-616234A 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-616234A 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-616234A (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)[2].
In vivo	SB-616234A reverses the agonist of 5-HT1/7 receptor, SKF-99101H-induced hypothermia in guinea pigs in a dose related manner with an ED50 of 2.4 mg/kg p.o. SB-616234A 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[1].a dose-dependent inhibition of ex vivo [3H]-GR125743 binding to rat striatal 5-HT1B receptors caused by SB-616234A (0.3-30 mg/kg p.o.) with an ED50 of 2.83 ± 0.39 mg/kg p.o[1].

Synonyms	SB-616234A
Molecular Weight	574.11
Formula	C32H36ClN5O3
CAS No.	908601-49-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 5.79 mg/ml (10.08 mM), Sonication is recommended.

References and Literature

1. Lee A.Dawson, et al. Characterisation of the selective 5-HT1B receptor antagonist SB-616234-A (1-[6-(cis-3,5-dimethylpiperazin-1-yl)-2,3-dihydro-5-methoxyindol-1-yl]-1-[2′-methyl-4′-(5-methyl-1,2,4-oxadiazol-3-yl)biphenyl-4-yl]methanone hydrochloride): In vivo neurochemical and behavioural evidence of anxiolytic/antidepressant activity. Neuropharmacology Volume 50, Issue 8, June 2006, Pages 975-983 2. Scott C, et al. SB-616234-A (1-[6-(cis-3,5-dimethylpiperazin-1-yl)-2,3-dihydro-5-methoxyindol-1-yl]-1-[2'methyl-4'-(5-methyl-1,2,3-oxadiazol-3-yl)biphenyl-4-yl]methanone hydrochloride): a novel, potent and selective 5-HT1B receptor antagonist. Neuropharmacology. 2006 Jun;50(8):984-90. Epub 2006 Mar 20.

Related compound libraries

This product is contained In the following compound libraries：

GPCR Compound Library Membrane Protein-targeted Compound Library Inhibitor Library Anti-Cancer Compound Library Neuronal Signaling Compound Library Antidepressant Compound Library Bioactive Compound Library Bioactive Compounds Library Max Neurotransmitter Receptor Compound Library Orally Active Compound Library

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Keywords

SB-616234-A 908601-49-0 GPCR/G Protein Neuroscience 5-HT Receptor inhibit 5-hydroxytryptamine Receptor SB 616234 A Inhibitor SB-616234A Serotonin Receptor SB616234A inhibitor

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