SB-616234-A

SKU: orb1309125

Description

SB-616234-A is a potent, selective, and orally bioavailable 5-HT1B receptor antagonist. It exhibits anxiolytic and antidepressant properties in preclinical models, making it a useful research tool for studying serotonin signaling in neuropsychiatric disorders both in vitro and in vivo.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 908601-49-0
• MW: 574.11
• Purity: 99.72% (May vary between batches)
• Formula: C₃₂H₃₆ClN₅O₃
• SMILES: Cl.COc1cc2CCN(C(=O)c3ccc(cc3)-c3ccc(cc3C)-c3noc(C)n3)c2cc1N1C[C@H](C)N[C@H](C)C1
• Target: 5-HT Receptor
• Solubility: DMSO:5.79 mg/mL (10.09 mM)

Bioactivity

• 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.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.
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• 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).
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

SB 616234 A, SB616234A, SB-616234A, SB-616234-A, Serotonin Receptor, 5-HT1B, 5-HT Receptor, 5HT Receptor, 5-hydroxytryptamine Receptor, 5HTReceptor, Inhibitor, inhibit

Compound Identifiers

PubChem CID

11685613