Ritanserin

Ritanserin
Clinical data
ATC code	none;
Identifiers
	IUPAC name 6-[2-[4-[bis(4-fluorophenyl)methylidene]piperidin-1-yl]ethyl]-7-methyl-[1,3]thiazolo[2,3-b]pyrimidin-5-one;
CAS Number	87051-43-2 ;
PubChem CID	5074;
IUPHAR/BPS	97;
ChemSpider	4896 ;
UNII	145TFV465S;
ChEBI	CHEBI:64195 ;
ChEMBL	ChEMBL267777 ;
CompTox Dashboard (EPA)	DTXSID9042594 ;
ECHA InfoCard	100.163.772
Chemical and physical data
Formula	C27H25F2N3OS
Molar mass	477.57 g·mol−1
3D model (JSmol)	Interactive image;
	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 ; Key:JUQLTPCYUFPYKE-UHFFFAOYSA-N ;
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Ritanserin (INN, USAN, BAN) is a serotonin receptor antagonist which was never marketed for clinical use but has been used in scientific research.^[1]

Research

Ritanserin was tested in clinical trials for schizophrenia^[2] and migraine.^[3]

Ritanserin acts as a selective 5-HT_2A (K_i = 0.45 nM) and 5-HT_2C receptor (K_i = 0.71 nM) antagonist.^[2]^[4] 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).^[4] The affinity of ritanserin for the 5-HT_1A receptor is less than 1 μM.^[4] 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.^[5]

The atypical antipsychotic risperidone was developed from ritanserin.^[6]

^ Dr. Ian Morton; I.K. Morton; Judith M. Hall (31 October 1999). Concise Dictionary of Pharmacological Agents: Properties and Synonyms. Springer Science & Business Media. pp. 249–. ISBN 978-0-7514-0499-9.
^ ^a ^b Akhondzadeh S, Malek-Hosseini M, Ghoreishi A, Raznahan M, Rezazadeh SA (September 2008). "Effect of ritanserin, a 5HT2A/2C antagonist, on negative symptoms of schizophrenia: A double-blind randomized placebo-controlled study". Progress in Neuro-Psychopharmacology & Biological Psychiatry. 32 (8): 1879–83. doi:10.1016/j.pnpbp.2008.08.020. PMID 18801405. S2CID 12270281.
^ Nappi, G; Sandrini, G; Granella, F; Ruiz, L; Cerutti, G; Facchinetti, F; Blandini, F; Manzoni, GC (June 1990). "A new 5-HT2 antagonist (ritanserin) in the treatment of chronic headache with depression. A double-blind study vs amitriptyline". Headache. 30 (7): 439–44. doi:10.1111/j.1526-4610.1990.hed3007439.x. hdl:11380/740716. PMID 2119355.
^ ^a ^b ^c Leysen JE, Gommeren W, Van Gompel P, Wynants J, Janssen PF, Laduron PM (1985). "Receptor-binding properties in vitro and in vivo of ritanserin: A very potent and long acting serotonin-S2 antagonist". Mol Pharmacol. 27 (6): 600–11. PMID 2860558.
^ Harmful Non-Indigenous Species in the United States. DIANE Publishing. 1 February 1993. pp. 361–. ISBN 978-0-7881-0441-1.
^ Bentham Science Publishers (May 1994). Current Medicinal Chemistry. Bentham Science Publishers. pp. 52–.

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