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Formula | C20H21N3 |
Molar mass | 303.409 g·mol−1 |
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Aptiganel (Cerestat;CNS-1102) is an unsuccessful drug candidate which acts as a noncompetitiveNMDA antagonist, and that was under development by Cambridge Neuroscience, Inc as a treatment for stroke.[1] It hasneuroprotective effects and was researched for potential use in the treatment ofstroke,[2] but despite positive results in animal studies,[3] human trials showed limited efficacy,[4] as well as undesirable side effects such assedation andhallucinations,[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.
1-Naphthylamine is reacted withcyanogen bromide to give2. 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.