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Ritanserin

CAS No.
87051-43-2
Chemical Name:
Ritanserin
Synonyms
R 55667;Tiserton;RITANSERIN;RITANSERIN SEROTONIN ANTAGONIST;6-[2-[4-[Bis(4-fluorophenyl)Methylidene]piperidin-1-yl]ethyl]-7-Methyl-[1,3]thia;6-(2-(4-(Bis(4-fluorophenyl)methylene)piperidin-1-yl)-ethyl)-7-methyl-5H-thiazolo[3,2-a]pyrimi;6-[2-[4-[BIS(4-FLUOROPHENYL)-METHYLENE]-1-PIPERIDINYL]-ETHYL]-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;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
CBNumber:
CB6458180
Molecular Formula:
C27H25F2N3OS
Molecular Weight:
477.57
MDL Number:
MFCD00069341
MOL File:
87051-43-2.mol
MSDS File:
SDS
Last updated:2023-09-04 15:51:00

Ritanserin 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
FDA UNII 145TFV465S

SAFETY

Risk and Safety Statements

Symbol(GHS)  GHS hazard pictograms
GHS07
Signal word  Warning
Hazard statements  H315-H319-H335
Precautionary statements  P261-P264-P271-P280-P302+P352-P305+P351+P338
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)
NFPA 704
0
2 0

Ritanserin price More Price(21)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Sigma-Aldrich R103 Ritanserin powder 87051-43-2 25mg $150 2024-03-01 Buy
Sigma-Aldrich R103 Ritanserin powder 87051-43-2 100mg $240 2024-03-01 Buy
Cayman Chemical 21374 Ritanserin ≥98% 87051-43-2 5mg $36 2024-03-01 Buy
Cayman Chemical 21374 Ritanserin ≥98% 87051-43-2 10mg $61 2024-03-01 Buy
Sigma-Aldrich R103 Ritanserin powder 87051-43-2 250mg $837 2024-03-01 Buy
Product number Packaging Price Buy
R103 25mg $150 Buy
R103 100mg $240 Buy
21374 5mg $36 Buy
21374 10mg $61 Buy
R103 250mg $837 Buy

Ritanserin Chemical Properties,Uses,Production

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.

storage

Store at +4°C

Ritanserin Preparation Products And Raw materials

Raw materials

Preparation Products

Global( 79)Suppliers
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Shanghai Daken Advanced Materials Co.,Ltd
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Shanghai Acmec Biochemical Technology Co., Ltd.
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Ritanserin Spectrum

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 6-(2-(4-(Bis(4-fluorophenyl)methylene)piperidin-1-yl)-ethyl)-7-methyl-5H-thiazolo[3,2-a]pyrimi RITANSERIN 6-[2-[4-[BIS(4-FLUOROPHENYL)-METHYLENE]-1-PIPERIDINYL]-ETHYL]-5H-THIAZOLO[3,2-A]PYRIMIDIN-5-ONE 6-(2-[4-(BIS[4-FLUOROPHENYL]METHYLENE)-1-PIPERIDINYL]ETHYL)-7-METHYL-5H-THIAZOLO(3,2-A)PYRIMIDIN-5-ONE R 55667 5H-Thiazolo[3,2-a]pyrimidin-5-one, 6-[2-[4-[bis(4-fluorophenyl)methylene]-1-piperidinyl]ethyl]-7-methyl- Inhibitor,Histamine Receptor,5-hydroxytryptamine Receptor,inhibit,Serotonin Receptor,Ritanserin,R-55667,5-HT Receptor,R55667,Beta Receptor,Adrenergic Receptor,Dopamine Receptor 87051-43-2 C27H25F2N3OS Aromatics Heterocycles Intermediates & Fine Chemicals Pharmaceuticals Sulfur & Selenium Compounds API Serotonin receptor