Aptiganel

Title: Aptiganel
CAS Registry Number: 137159-92-3
CAS Name: N-(3-Ethylphenyl)-N-methyl-N¢-1-naphthalenylguanidine
Additional Names: N-(1-naphthyl)-N¢-(3-ethylphenyl)-N¢-methylguanidine; aptaguanal
Molecular Formula: C20H21N3
Molecular Weight: 303.40
Percent Composition: C 79.17%, H 6.98%, N 13.85%
Literature 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).
Derivative Type: Hydrochloride
CAS Registry Number: 137160-11-3
Manufacturers' Codes: CNS-1102
Trademarks: Cerestat (Cambridge Neurosci.)
Molecular Formula: C20H21N3.HCl
Molecular Weight: 339.86
Percent Composition: C 70.68%, H 6.52%, N 12.36%, Cl 10.43%
Properties: Off-white needles from ethanol + diethyl ether, mp 223-225°.
Melting point: mp 223-225°
Therap-Cat: Neuroprotective.
Keywords: Neuroprotective; NMDA Receptor Antagonist.
Apyrase Aquaporins Arabinose Arabitol Arachidic Acid

Aptiganel
Aptiganel.svg
Systematic (IUPAC) name
1-(3-ethylphenyl)-1-methyl-2-naphthalen-1-ylguanidine
Clinical data
Legal status Uncontrolled
Identifiers
CAS number 137159-92-3 N
ATC code None
PubChem CID 60840
ChemSpider 54827 YesY
UNII 46475LV84I YesY
ChEMBL CHEMBL92484 YesY
Chemical data
Formula C20H21N3 
Mol. mass 303.401 g/mol
 N (what is this?)  (verify)

Aptiganel (Cerestat; CNS-1102) is a drug which acts as a noncompetitive NMDA antagonist.[1] It has neuroprotective effects and was researched for potential use in the treatment of stroke,[2] but despite positive results in animal studies,[3] human trials showed limited efficacy,[4] as well as undesirable side effects such as sedation and hallucinations,[5][6] and clinical development was ultimately not continued.[7]