ritanserin
Sign in to saveAlso known as R-55667, 6-(2-(4-(bis(p-fluorophenyl)methylene)-piperidino)ethyl)-7-methyl-5H-thiazolo-(3,2-a)pyrimidin-5-one, R 55,667
Ritanserin, also known by its developmental code name R-55667, is a serotonin receptor antagonist which was under development for the treatment of anxiety disorders and major depressive disorder but was never marketed. It was also investigated for treatment of insomnia, especially to enhance sleep quality by significantly increasing slow wave sleep by virtue of potent and concomitant serotonin 5-HT2A and 5-HT2C receptor antagonism. The drug is taken orally.
Research
1,405 papers- Ritanserin and alcohol abuse and dependence.Alcohol and alcoholism (Oxford, Oxfordshire). Supplement · 1994
- Identification of ritanserin analogs that display DGK isoform specificity.Biochemical pharmacology · 2022
- Ritanserin blocks Ca(V)1.2 channels in rat artery smooth muscles: electrophysiological, functional, and computational studies.Acta pharmacologica Sinica · 2020
- Ritanserin (R 55667) an original thymosthenic.Bollettino chimico farmaceutico · 1986
- Ritanserin, a novel agent targeting the mesenchymal subtype of glioblastomas.Neuro-oncology · 2018
via PubMed
Wikidata facts
- Subclass of
- chemical compound
- Mass
- 477.16864
Show 4 more facts
- chemical formula
- C₂₇H₂₅F₂N₃OS
- World Health Organisation international non-proprietary name
- ritanserin
- canonical SMILES
- CC1=C(C(=O)N2C=CSC2=N1)CCN3CCC(=C(C4=CC=C(C=C4)F)C5=CC=C(C=C5)F)CC3
- Commons category
- Ritanserin
via Wikidata · CC0
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Encyclopedic overview
12 sectionsContents
- Pharmacology
- Pharmacodynamics
- Pharmacokinetics
- Chemistry
- Synthesis
- History
- Society and culture
- Names
- Availability
- Research
- See also
- References
Ritanserin, also known by its developmental code name R-55667, is a serotonin receptor antagonist which was under development for the treatment of anxiety disorders and major depressive disorder but was never marketed. It was also investigated for treatment of insomnia, especially to enhance sleep quality by significantly increasing slow wave sleep by virtue of potent and concomitant serotonin 5-HT2A and 5-HT2C receptor antagonism. The drug is taken orally.
==Pharmacology== ===Pharmacodynamics=== Ritanserin acts as a selective 5-HT2A (Ki = 0.45 nM) and 5-HT2C receptor (Ki = 0.71 nM) antagonist. 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). The affinity of ritanserin for the 5-HT1A receptor is less than 1 μM. In addition to its affinity for the 5-HT2A and 5-HT2C receptors, ritanserin also binds to and antagonizes the 5-HT1D, 5-HT2B, 5-HT5A, 5-HT6, and 5-HT7 receptors.
Excerpted from Wikipedia’s “ritanserin” article, available under the CC BY-SA 4.0 licence.