3552. Eltoprazine
Nomenclature
CAS number: 98224-03-4
1-(2,3-Dihydro-1,4-benzodioxin-5-yl)piperazine; 1-(1,4-benzodioxan-5-yl)piperazine. C12H16N2O2; mol wt 220.27.
C 65.43%, H 7.32%, N 12.72%, O 14.53%.
Description and references
Selective serotonin 5HT1 agonist; psychotropic agent with antiagressive activity. Prepn: J. Hartog et al., EP 138280; idem et al., EP 189612 (1985, 1986 both to Duphar). Prepd (not claimed): idem et al., US 4833142 (1989 to Duphar). Crystal structure: M. L. Verdonk et al., Acta Crystallogr. C48, 2271 (1992). Series of articles on pharmacology, receptor binding and mechanism of action: Drug Metab. Drug Interact. 8, 1-186 (1990). Pharmacokinetics: M. H. de Vries et al., Eur. J. Clin. Pharmacol. 41, 485 (1991). Clinical evaluation in self-injury: W. M. A. Verhoeven et al., Lancet 340, 1037 (1992); in violent psychiatric patients: J. Tiihonen et al., ibid. 341, 307 (1993).
Derivative
Hydrochloride.Nomenclature
CAS number: 98206-09-8
DU-28853. C12H16N2O2.HCl; mol wt 256.73.
C 56.14%, H 6.67%, N 10.91%, O 12.46%, Cl 13.81%.
Properties
Crystals from ethanol, mp 256-258°. Soly in water: 19 g/100 ml.Therapeutic Category
Serenic.
Keywords
Serenic; Serotonin Receptor Agonist