Ritanserin
Synonym(s):6-[2-[4-(bis(4-Fluorophenyl)methylene]-1-piperidinyl]ethyl]-7-methyl-5H-thiazolo[3,2-a]pyrimidin-5-one
- CAS NO.:87051-43-2
- Empirical Formula: C27H25F2N3OS
- Molecular Weight: 477.57
- MDL number: MFCD00069341
- SAFETY DATA SHEET (SDS)
- Update Date: 2023-09-04 15:51:00
What is Ritanserin?
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.
The Uses of Ritanserin
Ritanserin has been used in behavioral testing and as a serotonin 2A receptor (5-HT2A)-receptor antagonist.
The Uses of Ritanserin
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).
What are the applications of Application
Ritanserin is potent and long-acting 5-HT2 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
Properties of Ritanserin
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 for Ritanserin
Signal word | Warning |
Pictogram(s) |
Exclamation Mark Irritant GHS07 |
GHS Hazard Statements |
H315:Skin corrosion/irritation H319:Serious eye damage/eye irritation H335:Specific target organ toxicity, single exposure;Respiratory tract irritation |
Precautionary Statement Codes |
P261:Avoid breathing dust/fume/gas/mist/vapours/spray. P264:Wash hands thoroughly after handling. P264:Wash skin thouroughly after handling. P271:Use only outdoors or in a well-ventilated area. P280:Wear protective gloves/protective clothing/eye protection/face protection. P302+P352:IF ON SKIN: wash with plenty of soap and water. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing. |
Computed Descriptors for Ritanserin
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