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| Ritanserin Basic information |
| Product Name: | Ritanserin | | Synonyms: | 6-[2-[4-(bis(4-fluorophenyl)methylene]-1-piperidinyl]ethyl]-7-methyl-5h-thiazolo[3,2-a]pyrimidin-5-one;RITANSERIN SEROTONIN ANTAGONIST;6-[2-[4-[Bis(4-fluorophenyl)methylene]-piperidino]ethyl]-7-methyl-5H-thiazolo-[3,2-a]pyrimidin-5-one;6-[2-[4-[Bis(4-fluorophenyl)methylene]piperidin-1-yl]ethyl]-7-methyl-5H-thiazolo[3,2-a]pyrimidin-5-one;6-[2-[4-[Bis(4-fluorophenyl)Methylidene]piperidin-1-yl]ethyl]-7-Methyl-[1,3]thia;Tiserton;6-[2-[4-[Bis(4-fluorophenyl)Methylidene]piperidin-1-yl]ethyl]-7-Methyl-[1,3]thiazolo[2,3-b]pyriMidin-5-one HCl;6-(2-(4-(Bis(4-fluorophenyl)methylene)piperidin-1-yl)-ethyl)-7-methyl-5H-thiazolo[3,2-a]pyrimidin | | CAS: | 87051-43-2 | | MF: | C27H25F2N3OS | | MW: | 477.57 | | EINECS: | | Product Categories: | Aromatics;Heterocycles;API;Intermediates & Fine Chemicals;Pharmaceuticals;Sulfur & Selenium Compounds;Serotonin receptor | | Mol File: | 87051-43-2.mol |
| Ritanserin Chemical Properties |
| Melting point | 145.5° | | Boiling point | 618.7±65.0 °C(Predicted) | | density | 1.30±0.1 g/cm3(Predicted) | | storage temp. | Sealed in dry,2-8°C | | solubility | methanol: >10 mg/mL | | form | solid | | pka | 7.74±0.20(Predicted) | | color | white |
| Hazard Codes | Xi | | Risk Statements | 36/37/38 | | Safety Statements | 22-26-36 | | WGK Germany | 3 | | Toxicity | LD50 in male, female mice, rats, dogs (mg/kg): 28.2, 28.2, 20.0, 22.2, 24.1, 33.2 i.v.; 626, 993, 956, 515, ~1280, 640-1280 orally (Awouters) |
| Ritanserin Usage And Synthesis |
| Description | Ritanserin, also known by its developmental code name R-55667, is a serotonin antagonist medication described as an anxiolytic, antidepressant, antiparkinsonian agent, and antihypertensive agent. It was never marketed for medical use due to safety problems but has been used in scientific research to study the serotonin system. | | Uses | Ritanserin has been used in behavioral testing and as a serotonin 2A receptor (5-HT2A)-receptor antagonist. | | Uses | Ritanserin and other 5HT2A/2C receptor antagonists have shown in clinical trial to promote slow-wave sleep in chronic primary insomnia or generalized anxiety disorder (Mayer, 2003). | | Definition | ChEBI: Ritanserin is a thiazolopyrimidine that is 5H-[1,3]thiazolo[3,2-a]pyrimidin-5-one which is substituted at position 7 by a methyl group and at position 6 by a 2-{4-[bis(4-fluorophenyl)methylidene]piperidin-1-yl}ethyl group. A potent and long-acting seratonin (5-hydroxytryptamine, 5-HT) antagonist of the subtype 5-HT2 (Ki = 0.39 nM), it is used in the treatment of a variety of disorders including anxiety, depression and schizophrenia. It has little sedative action. It has a role as a dopaminergic antagonist, a serotonergic antagonist, an antipsychotic agent, an anxiolytic drug, an antidepressant and an EC 3.4.21.26 (prolyl oligopeptidase) inhibitor. It is an organofluorine compound, a member of piperidines and a thiazolopyrimidine. | | Brand name | Tiserton (Janssen). | | Hazard | A poison.
| | Biological Activity | Ritanserin acts as a potent and long-acting 5-HT 2 receptor; antagonist (Ki = 0.39nM).Anxiolytic in vivo .It has relatively low affinity for the H1, D2, α1-adrenergic, and α2-adrenergic receptors (39-, 77-, 107-, and 166-fold lower relative to 5-HT2A, respectively). | | Biochem/physiol Actions | Potent 5-HT2A serotonin receptor antagonist/inverse agonist that crosses the blood-brain barrier. |
| Ritanserin Preparation Products And Raw materials |
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