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A selective 5-HT7 receptor antagonist. Extremely potent in vivo and in vitro. Chronic or acute (even single dose) administration of SB269970 induces functional desensitization of the 5-HT7 receptor system, which precedes changes in the receptor density. This mechanism may be responsible for the rapid antidepressant-like effect of the 5-HT7 antagonist in animal models. SB-269970 is an analogue of SB-258719 and has been shown to have at least 100 fold selectivity versus all other 5-HT receptor subtypes except the human 5-HT5A receptor (pKi values are 8.9, 7.2 and 6.0 for 5-HT7A, 5-HT5A and 5-HT1B).
Tokarski, K. et al. 2012. Pharmacol. Rep.64, 256. Thomas. D. R. et al. 2000. Br. J. Pharmacol.130, 409.
Lovell, P. J. et al. 2000. J. Med. Chem.43, 342. Forbes, I. T. et al. 1998. J. Med. Chem.41, 655.
Tokarski, K. et al. 2012. Pharmacol. Rep.64, 256. Thomas. D. R. et al. 2000. Br. J. Pharmacol.130, 409.
Lovell, P. J. et al. 2000. J. Med. Chem.43, 342. Forbes, I. T. et al. 1998. J. Med. Chem.41, 655.
数据表
Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.
A selective 5-HT7 receptor antagonist. Extremely potent in vivo and in vitro. Chronic or acute (even single dose) administration of SB269970 induces functional desensitization of the 5-HT7 receptor system, which precedes changes in the receptor density. This mechanism may be responsible for the rapid antidepressant-like effect of the 5-HT7 antagonist in animal models. SB-269970 is an analogue of SB-258719 and has been shown to have at least 100 fold selectivity versus all other 5-HT receptor subtypes except the human 5-HT5A receptor (pKi values are 8.9, 7.2 and 6.0 for 5-HT7A, 5-HT5A and 5-HT1B).
Form
Off-white solid
CAS number
261901-57-9
Chemical formula
C₁₈H₂₈N₂O₃S·HCl
Structure formula
Purity
≥98% by HPLC
Solubility
DMSO
Storage
Protect from light
+2°C to +8°C
Do Not Freeze
Ok to freeze
Special Instructions
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity
Standard Handling
References
Tokarski, K. et al. 2012. Pharmacol. Rep.64, 256. Thomas. D. R. et al. 2000. Br. J. Pharmacol.130, 409.
Lovell, P. J. et al. 2000. J. Med. Chem.43, 342. Forbes, I. T. et al. 1998. J. Med. Chem.41, 655.
