1050. Benserazide

Nomenclature

CAS number: 322-35-0
dl-Serine 2-[(2,3,4-trihydroxyphenyl)methyl] hydrazide; N-(dl-seryl)-N′-(2,3,4-trihydroxybenzyl) hydrazine.
C10H15N3O5; mol wt 257.24.
C 46.69%, H 5.88%, N 16.33%, O 31.10%.

Description and references

Peripheral decarboxylase inhibitor. Prepn: BE 619015; Hegedüs, Zeller, US 3178476 (1962, 1965 both to Hoffmann-La Roche). Inhibition of dopa decarboxylase in vitro and in vivo: W. P. Burkard et al., Experientia 18, 411 (1962); eidem, Arch. Biochem. Biophys. 107, 187 (1964). Synergy with dopa in vivo: G. Bartholini et al., Nature 215, 852 (1967); G. Bartholini, A. Pletscher, J. Pharmacol. Exp. Ther. 161, 14 (1968). Clinical comparison with carbidopa, q.v.: I. Kuruma et al., J. Pharm. Pharmacol. 24, 289 (1972). Clinical and pharmacokinetic profile: M.-H. Marion et al., Adv. Neurol. 45, 493 (1987). Review of pharmacology and clinical efficacy of decarboxylase inhibitors: R. M. Pinder et al., Drugs 11, 329-377 (1976).

Chemical structure

Derivative

Hydrochloride.

Nomenclature

CAS number: 14919-77-8
Ro-4-4602.
C10H15N3O5.HCl; mol wt 293.70.
C 40.89%, H 5.49%, N 14.31%, O 27.24%, Cl 12.07%.

Properties

White crystalline powder, mp 146-148°. Sol in water.

Derivative

Combination with levodopa.

Nomenclature

CAS number: 37270-69-2
Co-beneldopa; Madopar (Roche); Madopark (Roche); Prolopa (Roche).

Therapeutic Category

In combination with levodopa as antiparkinsonian.

Keywords

Antiparkinsonian