Drug intelligence / Profile preview

penehyclidine

Development stage
Phase 4
Lead developer
Beijing Institute of Pharmacology and Toxicology
Modality
Small Molecules
Administration
Intravenous, Intramuscular, Inhalation
01

Overview

Penehyclidine is a synthetic anticholinergic small molecule drug developed in China. It acts as a selective antagonist of muscarinic acetylcholine receptors (mAChRs), with higher selectivity for the M1 and M3 subtypes and minimal activity on M2 and M4 subtypes. This selectivity results in fewer side effects such as tachycardia or blurred vision compared to non-selective agents like atropine. Penehyclidine is used primarily for anesthesia adjunct therapy and as an antidote for organophosphate or carbamate insecticide poisoning. It also has applications in treating gastrointestinal disorders such as peptic ulcers and irritable bowel syndrome due to its ability to reduce smooth muscle spasm and glandular secretion. The drug can activate NF-kB in lung tissue, suppress inflammatory cytokines, and alleviate pulmonary inflammation during mechanical ventilation or chronic obstructive pulmonary disease (COPD). Its clinical advantages include strong anticholinergic effects with prolonged duration of action and reduced toxicity profile[1][2][5][6].

Brand names
长托宁
Other names
penehyclidine hydrochloride盐酸戊乙奎醚Penequinine hydrochloride
02

Targets

M1 (Muscarinic acetylcholine receptor M1)CHRM3 (M3)CHRM5 (M5)CHRM2 (M2)CHRM4 (M4)

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