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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 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.
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.
![]() | |
Clinical data | |
---|---|
ATC code |
|
Legal status | |
Legal status |
|
Identifiers | |
| |
CAS Number | |
PubChem CID | |
ChemSpider | |
UNII | |
ChEMBL | |
CompTox Dashboard ( EPA) | |
Chemical and physical data | |
Formula | C20H21N3 |
Molar mass | 303.409 g·mol−1 |
3D model ( JSmol) | |
| |
| |
![]() ![]() |
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.
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.