6141. Metitepine

Nomenclature

CAS number: 20229-30-5
1-[10,11-Dihydro-8-(methylthio)dibenzo[b,f]thiepin-10-yl]-4-methylpiperazine; 8-methylthio-10-(4-methylpiperazino)-10,11-dihydrodibenzo[b,f]thiepine; methiothepine; methiothepin; Ro-8-6837.
C20H24N2S2; mol wt 356.55.
C 67.37%, H 6.78%, N 7.86%, S 17.99%.

Description and references

Serotonin (5-HT2) receptor antagonist; also exhibits affinity for 5-HT1-receptors. Prepn: NL 6608618; M. Protiva et al., US 3379729 (1966, 1968 both to SPOFA); and pharmacology: K. Pelz et al., Collect. Czech. Chem. Commun. 33, 1895 (1968); J. O. Jilek et al., ibid. 39, 3338 (1974). Receptor-blocking study: M.-A. Monachon et al., Arch. Pharmacol. 274, 192 (1972). Use in classification of 5-HT receptors: P. B. Bradley et al., Neuropharmacology 25, 563 (1986); E. J. Mylecharane, Clin. Exp. Pharmacol. Physiol. 16, 517 (1989).

Chemical structure

Properties

Crystals from ethanol, mp 88-89°.

Derivative

Maleate.

Nomenclature

CAS number: 19728-88-2
C20H24N2S2.C4H4O4; mol wt 472.62.
C 60.99%, H 5.97%, N 5.93%, S 13.57%, O 13.54%.

Properties

Crystals from ethanol, mp 171-173°. LD5O in mice (mg/kg): 51 i.v.; 94 orally (Jilek).

Use

Biochemical tool in serotonin receptor binding studies.