Ropinirole HCl 91374-20-8

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Molecular Weight: 296.84 Ropinirole a selective dopamine D2 receptors agonist with Ki of 29 nM.






Ropinirole scavenges free radicals and suppresses lipid peroxidation in the Fe2+–H2O2 reaction system.

Ropinirole (50 mg/kg, i.p.) causes biphasic spontaneous locomotor
activity in mice. Ropinirole (0.05-1.0 mg/kg SC) dose-dependently
inhibits the dyskinesias induced by
2-di-n-propylamino-5,6-di-hydroxytetralin in mice. Ropirtirole, at doses
of 1 and 10 μg, injected unilaterally directly into the striatum of the
rat causes marked, contralateral (away from the side of injection)
asymmetry and circling in mice. Ropinirole (0.05-1.0 mg/kg SC or 0.1
mg/kg PO) reverses all motor and behavioural deficits induced by MPTP in
marmosets. Ropinirole (2 mg/kg, i.p.) for 7 days
increases GSH, catalase and SOD activities in the striatum and protected
striatal dopaminergic neurons against 6-hydroxydopamine (6-OHDA) in
mice. Ropinirole (0.2 mg/kg, i.p.) improves the use of
previously akinetic forelimb and produced robust circling behavior in
lesioned rats with striatal over-expression of both D2R and D3R compared
to lesioned animals that received blank vector. The subtherapeutic dose
of ropinirole generates only modest motor effects in lesioned rats with
sole over-expression of D2R or D3R. Ropinirole (1-8 mg
t.i.d.) is rapidly and completely absorbed with oral bioavailability of
55%, clearance of 780 mL/min, elimination half-life of 6 hours in
healthy volunteer. Since the major route of elimination for Ropinirole
is by the CYP enzyme system, mainly by CYP1A2 and also by CYP3A4,
inhibition of the former and possibly the latter may reduce the agent`s
clearance and lead to drug accumulation. Ropinirole (0.25
mg-4.0 mg per day) treatment significantly improves patients' ability
to initiate sleep, the amount of stage 2 sleep and sleep adequacy
compared with placebo. Periodic limb movements with arousal per hour
decreases from 7.0 to 2.5 with ropinirole but increases from 4.2 to 6.0
with placebo. Periodic limb movements while awake per hour decreases
from 56.5 to 23.6 with ropinirole but increases from 46.6 to 56.1 with
placebo.






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)

Chemical Information

Molecular Weight (MW)	296.84
Formula	C16H24N2O.HCl
CAS No.	91374-20-8

Storage	3 years -20℃Powder
	6 months-80℃in solvent (DMSO, water, etc.)
Synonyms

Solubility (25°C) *	In vitro	DMSO	10 mg/mL (33.68 mM)
		Water	60 mg/mL (202.12 mM)
		Ethanol	<1 mg/mL (
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Name	4-(2-(dipropylamino)ethyl)indolin-2-one hydrochloride

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Product Categories : Neuronal Signaling > Dopamine Receptor Inhibitor