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Submit ReviewSB 204070 is a potent and selective 5-HT4 receptor antagonist (pIC50 = 10.1). Displays >5000-fold selectivity for 5-HT4 over 5-HT1A, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2C, and 5-HT3 receptors. Exhibits anxiolytic activity upon systemic administration in vivo.
Sold for research purposes under agreement from GlaxoSmithKline.
M. Wt | 419.34 |
Formula | C19H27ClN2O4.HCl |
Storage | Desiccate at RT |
Purity | ≥98% (HPLC) |
CAS Number | 148688-01-1 |
PubChem ID | 121880 |
InChI Key | YEQGKAOSYSXEPU-UHFFFAOYSA-N |
Smiles | ClC1=C(N)C(OCCO2)=C2C(C(OCC3CCN(CCCC)CC3)=O)=C1.Cl |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
References are publications that support the biological activity of the product.
Bingham et al (1995) Antagonism by SB 204070 of 5-HT-evoked contractions in the dog stomach: an in-vivo model of 5-HT4 receptor function. J.Pharm.Pharmacol. 47 219 PMID: 7602484
Gaster et al (1993) (1-Butyl-4-piperidinyl)methyl 8-amino-7-chloro-1,4-benzodioxane-5-carboxylate hydrochloride: a highly potent and selective 5-HT4 antagonist derived from metoclopr. J.Med.Chem. 36 4121 PMID: 8258837
Prins et al (2000) An improved in vitro bioassay for the study of 5-HT4 receptors in the human isolated large intestine circular muscle. Br.J.Pharmacol. 129 1601 PMID: 10780964
Keywords: SB 204070, SB 204070 supplier, Serotonin, serotonergics, selective, 5-HT4, receptors, antagonists, anxiolytics, SB204070, Receptors, 1373, Tocris Bioscience
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Written by Nicholas M. Barnes and John F. Neumaier, this review summarizes the various serotonin receptor subtypes and their importance in mediating the role of serotonin in numerous physiological and pharmacological processes. Compounds available from Tocris are listed.
Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.