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Description: Potent 5-HT2 antagonist
Chemical Name: 6-[2-[4-[Bis(4-fluorophenyl)methylene]-1-piperidinyl]ethyl]-7-methyl-5H-thiazolo[3,2-a]pyrimidin-5-one
Purity: ≥98% (HPLC)
Biological Activity for Ritanserin
Ritanserin is a potent and long-acting 5-HT2 receptor antagonist (Ki = 0.39 nM). Anxiolytic in vivo.
Compound Libraries for Ritanserin
Ritanserin is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for Ritanserin
| M. Wt | 477.57 |
| Formula | C27H25F2N3OS |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 87051-43-2 |
| PubChem ID | 5074 |
| InChI Key | JUQLTPCYUFPYKE-UHFFFAOYSA-N |
| Smiles | O=C1N3C(SC=C3)=NC(C)=C1CCN4CC/C(CC4)=C(C5=CC=C(F)C=C5)/C2=CC=C(F)C=C2 |
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.
Solubility Data for Ritanserin
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| ethanol | 11.94 | 25 | |
| DMSO | 47.76 | 100 |
Preparing Stock Solutions for Ritanserin
The following data is based on the product molecular weight 477.57. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.09 mL | 10.47 mL | 20.94 mL |
| 5 mM | 0.42 mL | 2.09 mL | 4.19 mL |
| 10 mM | 0.21 mL | 1.05 mL | 2.09 mL |
| 50 mM | 0.04 mL | 0.21 mL | 0.42 mL |
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Product Datasheets for Ritanserin
References for Ritanserin
References are publications that support the biological activity of the product.
Janssen (1985) Pharmacology of potent and selective S2-serotonergic antagonists. J.Cardiovasc.Pharmacol. 7 S2 PMID: 2412048
Leysen et al (1985) Receptor-binding properties in vitro and in vivo of ritanserin. Mol.Pharmacol. 27 600 PMID: 2860558
Watanabe et al (1992) Syntheses and 5-HT2 antagonist activity of bicyclic 1,2,4-triazol-3(2H)-one and 1,3,5-triazine-2,4(3H)-dione derivatives. J.Med.Chem. 35 189 PMID: 1732528
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Keywords: Ritanserin, Ritanserin supplier, Potent, 5-HT2, antagonists, Non-Selective, Serotonin, Receptors, Non-selective, 1955, Tocris Bioscience
7 Citations for Ritanserin
Citations are publications that use Tocris products. Selected citations for Ritanserin include:
Mondal et al (2013) Mechanism of ghrelin-induced gastric contractions in Suncus murinus (house musk shrew): involvement of intrinsic primary afferent neurons. PLoS One 8 e60365 PMID: 23565235
Jahchan et al (2013) A drug repositioning approach identifies tricyclic antidepressants as inhibitors of small cell lung cancer and other neuroendocrine tumors. Cancer Discov 3 1364 PMID: 24078773
Chen et al (2012) Mechanism of all-trans-retinal toxicity with implications for stargardt disease and age-related macular degeneration. J Biol Chem 287 5059 PMID: 22184108
Bracha et al (2013) The expression and role of serotonin receptor 5HTR2A in canine osteoblasts and an osteosarcoma cell line. Physiol Behav 9 251 PMID: 24330646
Shimizu et al (2017) Brain serotoninergic nervous system is involved in bombesin-induced frequent urination through brain 5-HT7 receptors in rats. Br J Pharmacol 174 3072 PMID: 28675470
Alsene and Bakshi (2011) Pharmacological stimulation of locus coeruleus reveals a new antipsychotic-responsive pathway for deficient sensorimotor gating. Neuropsychopharmacology 36 1656 PMID: 21508929
Hampson et al (2007) Stimulation of glycogen synthesis and inactivation of phosphorylase in hepatocytes by serotonergic mechanisms, and counter-regulation by atypical antipsychotic drugs. Diabetologia 50 1743 PMID: 17579833
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
5-HT Receptors Scientific Review
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.