Ritanserin

Ritanserin

Systematic (IUPAC) name
6-[2-[4-[bis(4-fluorophenyl)methylidene]piperidin-1-yl]ethyl]-7-methyl-[1,3]thiazolo[2,3-b]pyrimidin-5-one
Identifiers
CAS Number	87051-43-2 Y
ATC code	none
PubChem	CID: 5074
IUPHAR/BPS	97
ChemSpider	4896 N
UNII	145TFV465S Y
ChEBI	CHEBI:64195 N
ChEMBL	CHEMBL267777 N
Chemical data
Molecular mass	477.569 g/mol
SMILES CC1=C(C(=O)N2C=CSC2=N1)CCN3CCC(=C(C4=CC=C(C=C4)F)C5=CC=C(C=C5)F)CC3
InChI InChI=1S/C27H25F2N3OS/c1-18-24(26(33)32-16-17-34-27(32)30-18)12-15-31-13-10-21(11-14-31)25(19-2-6-22(28)7-3-19)20-4-8-23(29)9-5-20/h2-9,16-17H,10-15H2,1H3 N Key:JUQLTPCYUFPYKE-UHFFFAOYSA-N N
NY (what is this?)  (verify)

Ritanserin (INN, USAN, BAN) is a serotonin receptor antagonist which was never marketed for clinical use but has been used in scientific research.

Research

Ritanserin was tested in clinical trials for schizophrenia and migraine.

Pharmacology

Ritanserin acts as a selective 5-HT_2A (K_i = 0.45 nM) and 5-HT_2C receptor (K_i = 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-HT_2A, respectively). The affinity of ritanserin for the 5-HT_1A receptor is than 1 µM. In addition to its affinity for the 5-HT_2A and 5-HT_2C receptors, ritanserin also binds to and antagonizes the 5-HT_1D, 5-HT_2B, 5-HT_5A, 5-HT₆, and 5-HT₇ receptors.

The atypical antipsychotic risperidone was developed from ritanserin.

See also

• Ketanserin