An antagonist of nAChRs and muscarinic M2 and M3 receptors (ED50s = 0.08

Mivacurium (chloride) – 10 mg

Brand:
Cayman
CAS:
106861-44-3
Storage:
-20
UN-No:
Non-Hazardous - /

Mivacurium is an antagonist of nicotinic acetylcholine receptors (nAChRs) and muscarinic M2 and M3 receptors (ED50s = 0.08, 0.3, and 0.1 mg/kg for ex vivo human skeletal muscle nAChRs, guinea pig cardiac M2 receptors, and guinea pig bronchial M3 receptors, respectively).{40374} It inhibits acetylcholine-induced activation of neuronal nAChRs (IC50s = 69.04, 3.71, 1.52, and 2.90 for human α3β2-, α3β4-, α4β2-, and α7-containing nAChRs expressed in Xenopus oocytes).{40375} Mivacurium also inhibits adult human muscular α1β1εδ-containing nAChRs (IC50 = 3.69 nM in Xenopus oocytes expressing the human recombinant receptor). In vivo, mivacurium inhibits bradycardia and bronchoconstriction induced by vagal stimulation or acetylcholine in guinea pigs.{40374} It also induces neuromuscular blockade (ED95 = 80 μg/kg) in sheep with a more rapid onset time than atracurium (Item No. 17796) and vecuronium (Item No. 15603).{40376} Formulations containing mivacurium have been used for pediatric anesthesia.{40377}  

 

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Description

An antagonist of nAChRs and muscarinic M2 and M3 receptors (ED50s = 0.08, 0.3, and 0.1 mg/kg for ex vivo human skeletal muscle nAChRs, guinea pig cardiac M2 receptors, and guinea pig bronchial M3 receptors, respectively); inhibits acetylcholine-induced activation of neuronal nAChRs (IC50s = 69.04, 3.71, 1.52, and 2.90 for human α3β2-, α3β4-, α4β2-, and α7-containing nAChRs expressed in Xenopus oocytes); inhibits adult human muscular α1β1εδ-containing nAChRs (IC50 = 3.69 nM in Xenopus oocytes expressing the human recombinant receptor); inhibits bradycardia and bronchoconstriction induced by vagal stimulation or acetylcholine in guinea pigs; induces neuromuscular blockade in sheep (ED95 = 80 μg/kg)

Formal name: (1R,1’R)-2,2’-[[(4E)-1,8-dioxo-4-octene-1,8-diyl]bis(oxy-3,1-propanediyl)]bis[1,2,3,4-tetrahydro-6,7-dimethoxy-2-methyl-1-[(3,4,5-trimethoxyphenyl)methyl] isoquinolinium, dichloride

Synonyms: 

Molecular weight: 1,100.20

CAS: 106861-44-3

Purity: ≥95%

Formulation: A solid

Product Type|Biochemicals|Ion Channel Modulation|Blockers||Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Cardiovascular System|Heart|Arrhythmia||Research Area|Neuroscience

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