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HomeProduct name listRitanserin

Ritanserin

Synonym(s):6-[2-[4-(bis(4-Fluorophenyl)methylene]-1-piperidinyl]ethyl]-7-methyl-5H-thiazolo[3,2-a]pyrimidin-5-one

Ritanserin Structural

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 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).

The Uses of Ritanserin

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

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)
ghs
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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