Aptiganel
Template:Short description Template:Drugbox
Aptiganel (Cerestat; CNS-1102) is an unsuccessful drug candidate which acts as a noncompetitive NMDA antagonist, and that was under development by Cambridge Neuroscience, Inc as a treatment for stroke.[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]
The drug's failure led to the collapse of Cambridge Neuroscience in 1998[8] and its eventual sale to CeNeS Pharmaceuticals in 2000.[9]
Other guanidine substances that the company had been bowling on was Cns-1145 & CNS1237.
Synthesis
1-Naphthylamine is reacted with cyanogen bromide to give 2. Treatment of this intermediate with 3-ethyl-N-methylaniline leads to addition to the cyano group and formation of the corresponding diaryl guanidine, aptiganel, 3.
See also
- Ditolylguanidine
- CNS1237 shares predominantly most of the same structural entities.
References
<templatestyles src="Reflist/styles.css" />
- ↑ Script error: No such module "Citation/CS1".
- ↑ Script error: No such module "Citation/CS1".
- ↑ Script error: No such module "Citation/CS1".
- ↑ Script error: No such module "Citation/CS1".
- ↑ Script error: No such module "Citation/CS1".
- ↑ Script error: No such module "Citation/CS1".
- ↑ Script error: No such module "Citation/CS1".
- ↑ Staff, Boston Business Journal. May 7, 1998. CNSI appoints new president, CEO
- ↑ Staff, ICIS. 23 May 2000 CeNeS to buy US neuroscience firm CNSI for $44m
- ↑ Script error: No such module "Citation/CS1".
- ↑ <templatestyles src="Citation/styles.css"/>Template:Citation/make link, Weber, Eckard & Keana, John F. W., "Tri- and tetra-substituted guanidines and their use as excitatory amino acid antagonists", published Script error: No such module "auto date formatter"., assigned to University of Oregon and Oregon Health Sciences UniversityScript error: No such module "Check for unknown parameters".; E. Weber, J. F. W. Keana, U.S. patent 5262568 (1993 to State of Oregon)
Script error: No such module "Check for unknown parameters".
Script error: No such module "Navbox". Template:Ionotropic glutamate receptor modulators