SB-616234A
- CAS No.
- 908601-49-0
- Chemical Name:
- SB-616234A
- Synonyms
- SB-616234A;inhibit,5-hydroxytryptamine Receptor,SB 616234 A,Inhibitor,5-HT Receptor,Serotonin Receptor,SB616234A
- CBNumber:
- CB73175584
- Molecular Formula:
- C32H36ClN5O3
- Molecular Weight:
- 574.12
- MDL Number:
- MFCD31382381
- MOL File:
- 908601-49-0.mol
SB-616234A price
Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
---|---|---|---|---|---|---|---|
ChemScene | CS-6686 | SB-616234-A 98.14% | 908601-49-0 | 5mg | $650 | 2021-12-16 | Buy |
ChemScene | CS-6686 | SB-616234-A 98.14% | 908601-49-0 | 10mg | $1150 | 2021-12-16 | Buy |
ChemScene | CS-6686 | SB-616234-A 98.14% | 908601-49-0 | 25mg | $2450 | 2021-12-16 | Buy |
ChemScene | CS-6686 | SB-616234-A 98.14% | 908601-49-0 | 50mg | $3850 | 2021-12-16 | Buy |
ChemScene | CS-6686 | SB-616234-A 98.14% | 908601-49-0 | 100mg | $5850 | 2021-12-16 | Buy |
SB-616234A Chemical Properties,Uses,Production
Description
SB-616234A is a selective and orally bioavailable 5-HT1B receptor antagonist, with anxiolytic and antidepressant activity.
SB-616234A 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-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].
SB-616234A 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-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]. SB-616234A (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[1].
References
[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.
SB-616234A Preparation Products And Raw materials
Raw materials
Preparation Products
SB-616234A Suppliers
Supplier | Tel | Country | ProdList | Advantage | |
---|---|---|---|---|---|
TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 19892 | 58 |
MedChemexpress LLC | 021-58955995 | sales@medchemexpress.cn | United States | 4863 | 58 |
Shanghai Beckham Medical Technology Co., Ltd | 021-13816613772 13816613772 | huahero21@sina.com | China | 384 | 55 |
Fan De(Beijing) Biotechnology Co., Ltd. | 15911056312 | liming@bio-fount.com | China | 9730 | 58 |
TargetMol Chemicals Inc. | 4008200310 | marketing@tsbiochem.com | China | 23963 | 58 |
Nanjing Shizhou Biology Technology Co.,Ltd | 025-85560043 15850508050 | cindy.huang@synzest.com | China | 12007 | 58 |