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

Safety Information

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)

MSDS

• Language:English Provider:SigmaAldrich

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 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).

Uses

Ritanserin has been used in behavioral testing and as a serotonin 2A receptor (5-HT2A)-receptor antagonist.

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.

storage

Store at +4°C

Ritanserin(87051-43-2)Related Product Information

• 1-Fluoro-4-(1-methylethenyl)benzene
• Ritanserin
• 4-Pyrimidinol
• 4-[(4-Fluorophenyl)methylene]piperidine
• 4-Hydroxy-6-methylpyrimidine
• 2-Methylthio-4-pyrimidinol
• 4,4'-Difluorodiphenylmethane
• 6-Methyl-2-(methylthio)pyrimidin-4-ol
• 4-Fluorostyrene
• N,N-DIMETHYLMETHACRYLAMIDE
• DIACYLGLYCEROL KINASE INHIBITOR I
• 4-(DIPHENYLMETHYLENE)PIPERIDINE
• 1-Methyl-4-methylene-piperidine
• 4(3H)-Pyrimidinone, 5-methyl-2-(methylthio)-
• 1,1-BIS(4-FLUOROPHENYL)-1-BUTENE
• 7-METHYL-5H-[1,3]THIAZOLO[3,2-A]PYRIMIDIN-5-ONE
• N,N'-DIMETHYLCARBAMIMINOTHIOIC ACID METHYL ESTER
• Ketanserin/Ritanserin/Sufrexal/Serefrex