A muscarinic antagonist at the mAChRs

Aclidinium (bromide) – 10 mg

Brand:
Cayman
CAS:
320345-99-1
Storage:
-20
UN-No:
Non-Hazardous - /

Aclidinium (bromide) is a long-acting reversible antagonist at the muscarinic acetylcholine receptors (mAChRs), M1, M2, M3, M4, and M5 (Kis= 0.1, 0.14, 0.14, 0.21, and 0.16 nM, respectively).{34049} It has a fast onset of action and dissociates more slowly from M3 receptors, which are located on bronchial smooth muscle and submucosal glands, than from M2 receptors (t1/2 = 29 and 4.7 hours, respectively) in guinea pigs. It had an improved cardiovascular safety profile compared with tiotropium (Item No. 15773) in Beagle dogs. Inhalant formulations containing aclidinium (bromide) are used in maintenance therapy to reduce bronchospasm in patients with chronic obstructive pulmonary disease.  

 

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Description

A muscarinic antagonist at the mAChRs, M1, M2, M3, M4, and M5 (Kis= 0.1, 0.14, 0.14, 0.21, and 0.16 nM, respectively); longer t1/2, on M3 receptors than on M2 receptors (t1/2 = 29 and 4.7 hours, respectively)

Formal name: (3R)-3-[(2-hydroxy-2,2-di-2-thienylacetyl)oxy]-1-(3-phenoxypropyl)-1-azoniabicyclo[2.2.2]octane, monobromide

Synonyms:  LAS 34273|LAS-W 330

Molecular weight: 564.6

CAS: 320345-99-1

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Immunology & Inflammation|Pulmonary Diseases|COPD/Emphysema

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