Loperamide HCl 34552-83-5

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Molecular Weight: 513.5 Loperamide HCl is an opioid-receptor agonist with an ED50 of 0.15 mg/kg.

Biological Activity

Loperamide is an opioid-receptor agonist with an ED50 of 0.15 mg/kg. It acts on the μ-opioid receptors in the myenteric plexus of the large intestine; by itself it does not affect the central nervous system like other opioids. It works by decreasing the activity of the myenteric plexus, which, like m orphine, decreases the tone of the longitudinal smooth muscles but increases tone of circular smooth muscles of the intestinal wall. This increases the amount of time substances stay in the intestine, allowing for more water to be absorbed out of the fecal matter. Loperamide also decreases colonic mass movements and suppresses the gastrocolic reflex.






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)	513.5
Formula	C29H33ClN2O2.HCl
CAS No.	34552-83-5

Storage	3 years -20℃Powder
	6 months-80℃in solvent (DMSO, water, etc.)
Synonyms	ADL 2-1294

Solubility (25°C) *	In vitro	DMSO	22 mg/mL (42.84 mM)
		Water	<1 mg/mL (
		Ethanol	4 mg/mL (7.78 mM)

Chemical Name	4-(4-chlorophenyl)-4-hydroxy-N,N-dimethyl-α,α-diphenyl-1-piperidinebutanamide, hydrochloride (1:1)

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Product Categories : Neuronal Signaling > Opioid Receptor Inhibitor