An opiate which potently and selectively activates μ opioid receptors (Ki = 0.16 nM) exclusively in the periphery; has antidiarrheal action; blocks voltage-sensitive sodium channels (IC50 = 270 nM) and high voltage-activated calcium channels (IC50 = 900 nM); comparable to morphine in blocking peripheral pain

Loperamide (hydrochloride) – 5 mg

Brand:
Cayman
CAS:
34552-83-5
Storage:
-20
UN-No:
De Minimis - 2811 / 6.1

Loperamide is an opiate which potently and selectively activates μ opioid receptors (Ki = 0.16 nM) exclusively in the periphery. Loperamide is an opiate which potently and selectively activates μ opioid receptors (Ki = 0.16 nM) exclusively in the periphery.{23761,23758} It is a much weaker agonist of the δ opioid receptor (Ki = 50 nM).{23761} Through its actions in the gut wall, loperamide has antidiarrheal action by increasing transit time and by altering intestinal transport of water and electrolytes.{23758,23756} It also blocks voltage-sensitive sodium channels (IC50 = 270 nM) and high voltage-activated calcium channels (IC50 = 900 nM), presumably through an inhibitory effect on calmodulin.{23759,23760,23758} Loperamide is comparable to morphine in blocking peripheral pain in rats.{23757}  

 

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Description

An opiate which potently and selectively activates μ opioid receptors (Ki = 0.16 nM) exclusively in the periphery; has antidiarrheal action; blocks voltage-sensitive sodium channels (IC50 = 270 nM) and high voltage-activated calcium channels (IC50 = 900 nM); comparable to morphine in blocking peripheral pain

Formal name: 4-(4-chlorophenyl)-4-hydroxy-N,N-dimethyl-α,α-diphenyl-1-piperidinebutanamide, monohydrochloride

Synonyms:  NSC 696356|PJ 185|R 18553

Molecular weight: 513.5

CAS: 34552-83-5

Purity: ≥98%

Formulation: A crystalline solid

Application|Mass Spectrometry||Product Type|Biochemicals|Analytical Standards||Product Type|Biochemicals|Drugs of Abuse||Research Area|Forensic Chemistry & Toxicology|Opioids

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