The affinity of Eptapirone (F11440) for 5-HT1A binding sites (pKi, 8.33) was higher than that of buspirone (pKi, 7.50), and somewhat lower than that of flesinoxan (pKi, 8.91). In vivo, Eptapirone (F11440) was 4- to 20-fold more potent than flesinoxan, and 30- to 60-fold more potent than buspirone, in exerting 5-HT1A agonist activity at pre- and postsynaptic receptors in rats (measured by, for example, its ability to decrease hippocampal extracellular serotonin (5-HT) levels and to increase plasma corticosterone levels, respectively).
|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: 5 mg/mL (Need ultrasonic)|
The use of sleep measures to compare a new 5HT1A agonist with buspirone in humans.
Wilson SJ, et al. J Psychopharmacol. 2005 Nov;19(6):609-13. PMID: 16272182.
F 11440, a potent, selective, high efficacy 5-HT1A receptor agonist with marked anxiolytic and antidepressant potential.
Koek W, et al. J Pharmacol Exp Ther. 1998 Oct;287(1):266-83. PMID: 9765347.
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Idalopirdine hydrochloride is a potent and selective 5-HT6 receptor antagonist with a Ki value of 0.83 nM.
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