YM 90K hydrochloride delays neuronal death in a global ischemia model and cerebral infarction in a focal ischemia model following postischemic administration. The novel AMPA receptor antagonist YM90K was effective in the treatment of focal cerebral ischaemic lesions. Activation of AMPA receptor may play a key role in the development of cerebral infarct in the early phase of ischaemia in rats. YM90K is a potent and competitive antagonist for AMPA receptors and the apparent affinity of competitive antagonists was reduced by cyclothiazide. Cyclothiazide can affect the interaction between receptors and both agonists and antagonists, suggesting that it might allosterically alter the affinity of agonists and competitive antagonists for their binding site on the AMPA receptor complex. YM 90K may be useful for the treatment of acute epileptic conditions such as status epilepticus. Moreover, it might prevent pathological neuronal plasticity resulting from status epilepticus, since it shows an antiepileptogenic effect and protects hippocampal neurons during kainate-induced generalized seizures.
| Molecular Weight | 309.67 |
| Formula | C11H7N5O4.HCl |
| CAS Number | 154164-30-4 |
| Solubility (25°C) | DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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