Английская Википедия:Aptiganel
Шаблон:Short description Шаблон: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
Шаблон:Hallucinogens Шаблон:Ionotropic glutamate receptor modulators
- ↑ Шаблон:Cite journal
- ↑ Шаблон:Cite journal
- ↑ Шаблон:Cite journal
- ↑ Шаблон:Cite journal
- ↑ Шаблон:Cite journal
- ↑ Шаблон:Cite journal
- ↑ Шаблон:Cite journal
- ↑ 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
- ↑ Шаблон:Cite journal
- ↑ Шаблон:Cite patent; E. Weber, J. F. W. Keana, Шаблон:US patent (1993 to State of Oregon)
