PNU-282987 is a highly selective α7 nicotinic acetylcholine receptor (α7 nAChR) agonist with Ki of 27 nM. PNU-282987 has no detectable agonist activity and negligible antagonist activity at the neuromuscular junction form of the receptor (α1β1γδ), the predominant ganglionic nAChR (α3β4), and the α4β2 subtype. PNU-282987 is found to be a functional antagonist of the 5-HT3 receptor with IC50 of ~4.5 μM. PNU-282987 displays potent activity at both α7-5HT3 chimera and native α7 nAChR. PNU-282987 is shown to open native alpha7 nAChRs in cultured rat neurons in a concentration-dependent manner, which can be blocked by MLA. Consistently, PNU-282987 reverse an amphetamine-induced gating deficit in rats. PNU-282987 is inactive against a panel of 32 receptors at 1 μM, except 5-HT3 receptors with Ki of 930 nM. PNU-282987 enhances GABAergic synaptic activity when applied to hippocampal slices. Furthermore, PNU-282987 improves the inherent hippocampal gating deficit occurring in a subpopulation of anesthetized rats, and enhances amphetamine-induced hippocampal θ oscillation.Systemic administration of PNU-282987 significantly enhances the power (by 40%) of hippocampal theta oscillation induced by electrical stimulation of the brainstem reticular formation in anaesthetized rats, suggesting that precognitive actions of alpha7 nAChR agonists could be mediated, at least in part, by modulation of hippocampal oscillatory activity.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
|Solubility||DMSO: ≥ 30 mg/mL|
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