SB-269970 hydrochloride

SKU: orb1685634

Description

SB-269970 hydrochloride is a potent and selective 5-HT7 receptor antagonist (pKi = 8.3), demonstrating over 50-fold selectivity versus other receptor subtypes. It is widely used in neuroscience research to investigate the role of 5-HT7 receptors in vitro and in animal models related to sleep, cognition, and mood disorders.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 261901-57-9
• MW: 388.95
• Purity: 99.80%
• Formula: C₁₈H₂₈N₂O₃S·HCl
• SMILES: Cl.CC1CCN(CC[C@H]2CCCN2S(=O)(=O)c2cccc(O)c2)CC1
• Target: 5-HT Receptor
• Solubility: DMSO:12 mg/mL (30.85 mM);H2O:7.8 mg/mL (20.05 mM)

Bioactivity

• Target IC50:
  5-HT7:8.3(pKi)
• In Vivo:
  SB-269970 (10 mg/kg and 30 mg/kg) significantly reduces the effects of amphetamine by 25 and 27%, respectively, and blocks the effects of ketamine by 38% (10 mg/kg) and 30% (30 mg/kg). SB-269970 significantly reduces amphetamine-induced hyperactivity in wild-type mice and is without effects in 5-HT7 knockout mice. Systemic administration of SB-269970 (30 mg/kg) significantly reverses amphetamine disruption of PPI and did not enhance PPI by itself compared to control. SB-269970 significantly reverses the deficits induced by MK-801, but not by scopolamine. SB-269970 normalizes MK-801-induced glutamate but not dopamine release in the cortex. SB-269970 (in one medium dose of 0.5 or 1 mg/kg) exerts a specific antianxiety-like effect in the Vogel drinking test in rats, in the elevated plus-maze test in rats and in the four-plate test in mice. Moreover, SB-269970 (in one medium dose of 5 or 10 mg/kg) reveals antidepressant-like activity in the forced swimming and the tail suspension tests in mice. SB-269970 at doses of 0.3, 1 and 3 μg exhibits an anticonflict effect which is weaker than that of diazepam (40 μg), whereas SB-269970 at doses of 3 and 10 μg had marked anti-immobility action comparable to that of imipramine (0.1 μg).
• In Vitro:
  SB-269970 inhibits 5-CT-stimulated adenylyl cyclase activity in guinea-pig hippocampal membranes. SB-269970 (0.03 μM, 0.1 μM, 0.3 μM and 1 μM) produces a concentration-related rightward-shift of the 5-CT concentration-response curve with no significant alteration in the maximal response to 5-CT. SB-269970 (1 μM) has any effect on 5-HT efflux when superfused alone.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

5-HT Receptor, 5HT Receptor, 5-hydroxytryptamine Receptor, 5-HT7, 5HTReceptor, inhibit, Inhibitor, Serotonin Receptor, SB 269970, SB 269970 Hydrochloride, SB 269970 hydrochloride, SB269970, SB-269970, SB269970 HCl, SB269970 hydrochloride, SB269970 Hydrochloride, SB-269970 Hydrochloride, SB-269970A

Compound Identifiers

PubChem CID

11957684