758. Aptiganel

Nomenclature

CAS number: 137159-92-3
N-(3-Ethylphenyl)-N-methyl-N′-1-naphthalenylguanidine; N-(1-naphthyl)-N′-(3-ethylphenyl)-N′-methylguanidine; aptaguanal.
C20H21N3; mol wt 303.40.
C 79.17%, H 6.98%, N 13.85%.

Description and references

Noncompetitive NMDA-receptor antagonist. Prepn: E. Weber, J. F. W. Keana, WO 9112797; eidem, US 5262568 (1991, 1993 both to State of Oregon); N. L. Reddy et al., J. Med. Chem. 37, 260 (1994). Clinical pharmacology and kinetics: K. W. Muir et al., Ann. N.Y. Acad. Sci. 765, 279 (1995). Review of theoretical basis for use in stroke: K. W. Muir, K. R. Lees, Stroke 26, 503-513 (1995). Clinical trial in acute ischemic stroke: G. W. Albers et al., J. Am. Med. Assoc. 286, 2673 (2001).

Chemical structure

Derivative

Hydrochloride.

Nomenclature

CAS number: 137160-11-3
CNS-1102; Cerestat (Cambridge Neurosci.).
C20H21N3.HCl; mol wt 339.86.
C 70.68%, H 6.52%, N 12.36%, Cl 10.43%.

Properties

Off-white needles from ethanol + diethyl ether, mp 223-225°.

Therapeutic Category

Neuroprotective.

Keywords

Neuroprotective; NMDA Receptor Antagonist