WAY-100635 is a potent and selective 5-hydroxytryptamine1A antagonist with an IC50 of 0.95 ?0.12 nM for 5-HT. Intravenous administration of WAY-100635 (0.025-0.5 mg/kg) markedly improved neuronal activity. The stimulatory action of WAY-100635 was evident during wakefulness (when serotonergic neurons typically display a relatively high level of activity) but not during sleep (when serotonergic neurons display little or no spontaneous activity). WAY-100635 at doses as low as 0.1 mg/kg i.v. completely blocked the action of 8-hydroxy-2- (di-n-propylamino)tetralin. The antagonist action of WAY-100635 at 5-HT1A autoreceptors closely paralleled its ability to increase neuronal activity. WAY-100635 affected neither the blackage of action potential frequency adaptation and slow afterhyperpolarization produced by 5-HT (15 μM) nor the hyperpolarization and decrease in membrane input resistance evoked by bath application of GABA (B) receptor agonist baclofen (10 μM).
|Preparation method||Making extracellular recordings with glass microelectrodes filled with 2 M NaC1 (12 MΩ-15 MΩ). Identifing the cells as 5-HT neurons according to the following criteria: biphasic action potentials of 2 msec to 3 msec in duration, slow (0.5 Hz - 2.0 Hz) and regular pattern of discharge. Firing is evoked in the otherwise silent neurons by adding the alpha-l adrenergic agonist phenylephrine (3 μM) to the superfusing ACSF. Recoring baseline activity for at least 10 minutes before application of the different drugs. The electric signals are fed into a high-input impedance amplifier, an oscilloscope and an electronic ratemeter triggered by individual action potentials connected to an A/D converter and a personal computer. Using dedicated software, the integrated firing rate is recorded, computed and displayed on a chart recorder as consecutive 10-sec samples. Evaluting the effects of agonists by comparing the mean discharge frequency recorded during the 2 minutes that preceded WAY 100635 application with that recorded at the peak of WAY 100635 action (usually 2-5 minutes after the beginning of application). When the agonists are applied in the presence of the antagonist, the effect of the agonist is compared to baseline firing rate and to the frequency recorded during superfusion of the antagonist alone. The antagonist is left to equilibrate for 10 minutes to 25 minutes before retesting of the action of agonists.|
|Concentrations||1 nM -5 nM|
|Incubation time||2 minutes -5 minutes|
|Animal models||Male CD1 mice with 25-30 g body weight|
|Dosages||250 μL (30.4 μCi/mL)|
|Administration||Administered via i.v.|
|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 80 mg/mL|
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