Medetomidine HCl 86347-15-1

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Molecular Weight: 236.74 Medetomidine is a selective α2-adrenoceptor agonist, with Ki of 1.08 nM, exhibts 1620-fold selectivity over α1-adrenoceptor.

Medetomidine is a selectiveα2-adrenoceptor agonist, with Ki of 1.08 nM, exhibits 1620-fold selectivity over α1-adrenoceptor, has
very weak or no binding to other neurotransmitter receptors.

In anesthetized rats, medetomidine (1-100 μg/kg, i.v.) induces a
dose-dependent, relatively short-lived reduction in blood pressure and
heart rate. In the pithed rat, medetomidine shows very potent
vasopressor (PD50 1.7 μg/kg) and sympatho-inhibitory (ID50 1.6 μg/kg)
effects without affecting basal heart rate. Medetomidine
induces dose-dependent sedation, which at high doses (>100μg/kg)
includes loss of the righting reflex and hypothermia. Medetomidine
induces a decreases in the turnover rate of biogenic amines in the
brain, dose-dependently inhibits norepinephrine (NE) turnover, inhibits
brain dopamine turnover at high doses, decreases serotonin turnover.





Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

Species	Baboon	Dog	Monkey	Rabbit	Guinea pig	Rat	Hamster	Mouse
Weight (kg)	12	10	3	1.8	0.4	0.15	0.08	0.02
Body Surface Area (m2)	0.6	0.5	0.24	0.15	0.05	0.025	0.02	0.007
Km factor	20	20	12	12	8	6	5	3

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.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×	mouse Km(3)	= 11.2 mg/kg
	rat Km(6)

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Product Categories : Neuronal Signaling > Adrenergic Receptor Inhibitor