Disease relevance of Aptiganel

• The present study evaluated the neuroprotective efficacy of three noncompetitive NMDA receptor antagonists: Gacyclidine (GK-11), a new compound, Dizocilpine (MK-801), and Cerestat (CNS-1102) in a rat spinal cord contusion model [1].
• Recent studies have demonstrated a neuroprotective effect of the noncompetitive N-methyl-D-aspartate receptor antagonist aptiganel HCl (Cerestat) in focal cerebral ischemia [2].

Psychiatry related information on Aptiganel

• Conversely, cerestat (0.3, 1, and 3 mg/kg, sc) injected at 10 and 120 min postocclusion significantly reduced the ischemic volume at the dose of 1 mg/kg, and, at the same dose, significantly attenuated behavioural deficits in the body proprioception and in the forelimb flexion tests [3].

High impact information on Aptiganel

• Cerestat and other NMDA antagonists in ischemic stroke [4].
• This study investigated the ability of NBQX, an AMPA receptor antagonist, and cerestat, a NMDA receptor antagonist, to counteract neurological deficits and morphological damage induced by permanent occlusion of the left middle cerebral artery (MCAO model) in the rat [3].
• Effects of cerestat and NBQX on functional and morphological outcomes in rat focal cerebral ischemia [3].
• Cerestat reduced contusion volume from 77.3 +/- 5.8 mm3 to 66.8 +/- 3.9 mm3 (p < 0.05) [5].

Biological context of Aptiganel

• This study investigates the influence of Cerestat on contusion volume, post-traumatic brain edema and intracranial pressure (ICP) following Controlled Cortical Impact Injury (CCII) [5].

Associations of Aptiganel with other chemical compounds

• 2. Memantine and cerestat produced complete inhibition of ACh-induced inward currents with affinities similar to that reported for native NMDA receptors [6].

References