Clorotepine

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Clorotepine
Clorotepine.svg
Systematic (IUPAC) name
1-(8-chloro-10,11-dihydrodibenzo[b,f]thiepin-10-yl)-4-methylpiperazine
Clinical data
Legal status
  • ℞ (Prescription only)
Routes of
administration		 Oral
Identifiers
CAS Number 13448-22-1
4789-68-8 (maleate)
42505-79-3 (mesylate)
ATC code None
PubChem CID: 1238
ChemSpider 1201
UNII E65W20MU7A
ChEMBL CHEMBL64249
Synonyms VUFB-6281; VUFB-10030
Chemical data
Formula C19H21ClN2S
Molecular mass 344.901 g/mol
  • Clc4cc2c(Sc1ccccc1CC2N3CCN(C)CC3)cc4
  • InChI=1S/C19H21ClN2S/c1-21-8-10-22(11-9-21)17-12-14-4-2-3-5-18(14)23-19-7-6-15(20)13-16(17)19/h2-7,13,17H,8-12H2,1H3
  • Key:XRYLGRGAWQSVQW-UHFFFAOYSA-N

Clorotepine (INN; brand names Clotepin, Clopiben), also known as octoclothepin or octoclothepine, is a very potent atypical antipsychotic and central depressant of the tricyclic series which was derived from perathiepin in 1965 and soon thereafter marketed in the Czech Republic by Spofa for the treatment of schizophrenic psychosis.[1][2][3][4] It is known to have high affinity for the D1,[5] D2,[6] D3,[6] D4,[6] 5-HT2A,[5] 5-HT2B,[7] 5-HT2C,[7] 5-HT6,[8] 5-HT7,[8] α1A-adrenergic,[9] α1B-adrenergic,[9] α1D-adrenergic,[9] and H1 receptors,[10] where it has been it has been confirmed to act as an antagonist (or inverse agonist) at most sites (and likely is as such at all of them based on structure-activity relationships), and it also blocks the reuptake of norepinephrine via inhibition of the norepinephrine transporter.[11] Due to its very potent activity at the D2 receptor, along with tefludazine, clorotepine was used as the basis for developing a 3-dimensional (3D) pharmacophore for D2 receptor antagonists.[12]

See also

References

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  12. ↑ Lua error in package.lua at line 80: module 'strict' not found.
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