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Ritanserin

Product Name
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
Formula Weight
477.57
MOL File
87051-43-2.mol
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Ritanserin Property

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
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Safety

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)
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P271Use only outdoors or in a well-ventilated area.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
R103
Product name
Ritanserin
Purity
powder
Packaging
25mg
Price
$150
Updated
2024/03/01
Sigma-Aldrich
Product number
R103
Product name
Ritanserin
Purity
powder
Packaging
100mg
Price
$240
Updated
2024/03/01
Cayman Chemical
Product number
21374
Product name
Ritanserin
Purity
≥98%
Packaging
5mg
Price
$36
Updated
2024/03/01
Cayman Chemical
Product number
21374
Product name
Ritanserin
Purity
≥98%
Packaging
10mg
Price
$61
Updated
2024/03/01
Sigma-Aldrich
Product number
R103
Product name
Ritanserin
Purity
powder
Packaging
250mg
Price
$837
Updated
2024/03/01
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Ritanserin Chemical Properties,Usage,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 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 Preparation Products And Raw materials

Raw materials

Preparation Products

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87051-43-2, RitanserinRelated Search:

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

  • 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
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  • Serotonin receptor