Title: Lazabemide
CAS Registry Number: 103878-84-8
CAS Name: N-(2-Aminoethyl)-5-chloro-2-pyridinecarboxamide
Additional Names: N-(2-aminoethyl)-5-chloropicolinamide
Molecular Formula: C8H10ClN3O
Molecular Weight: 199.64
Percent Composition: C 48.13%, H 5.05%, Cl 17.76%, N 21.05%, O 8.01%
Literature References: Member of a novel class of potent, reversible, and extremely selective monoamine oxidase type B (MAO-B) inhibitors. Prepn: R. Imhof, E. Kyburz, GB 2163746; eidem, US 4764522 (1986, 1988 both to Hoffmann-LaRoche). HPLC determn in plasma: R. Wyss, W. Philipp, J. Chromatogr. 507, 187 (1990). Neurochemical profile: W. E. Haefely et al., Adv. Neurol. 53, 505 (1990). Enzyme binding studies: J. Saura et al., J. Neurosci. 12, 1977 (1992). Clinical trial: Parkinson Study Group, Ann. Neurol. 33, 350 (1993).
Derivative Type: Monohydrochloride
CAS Registry Number: 103878-83-7
Manufacturers' Codes: Ro-19-6327
Molecular Formula: C8H10ClN3O.HCl
Molecular Weight: 236.10
Percent Composition: C 40.70%, H 4.70%, Cl 30.03%, N 17.80%, O 6.78%
Properties: Crystals from methanol/ether, mp 193-195°. Partition coefficient (n-octanol/water) ~0.1. pKa 8.9. LD50 orally in mice: 1000-2000 mg/kg (Imhof, Kyburz, 1986).
Melting point: mp 193-195°
pKa: pKa 8.9
Log P: Partition coefficient (n-octanol/water) ~0.1
Toxicity data: LD50 orally in mice: 1000-2000 mg/kg (Imhof, Kyburz, 1986)
Therap-Cat: Antiparkinsonian.
Keywords: Antiparkinsonian; Monoamine Oxidase Inhibitor. |