Pirenzepine

• 28797-61-7 ( pirenzepine )
• 29868-97-1 ( pirenzepine · dihydrochloride)

A02BX03

Ulkustherapeutikum

Muscarinic acetylcholine receptor inhibitor

427 mg · kg -1 ( LD50, mouse, ip)

Template: Infobox chemical / molecular formula search available

Pirenzepine (trade name: gastrozepin ®, manufactured by Boehringer Ingelheim ), a substance from the group of parasympatholytics, selectively inhibits Muscarinic acetylcholine receptors, and this case has a particularly high affinity for M1 acetylcholine receptors.

Pirenzepine is used for the reduction of gastric acid secretion, as less histamine is secreted by the inhibition of M1 receptors by enterochromaffinartigen cells and thus the gastric acid secretion is lowered.

In the usual dose for the treatment of 100-150 mg / day pirenzepine inhibits the M3 receptors on the parietal cell, with typical anticholinergic effects such as dry mouth, and tachycardia, so it does not matter in the Ulcustherapie.

The treatment of myopia by pirenzepine is currently under investigation.

Production

A multi-step synthesis for pirenzepine, starting from 2-chloro -3-aminopyridine has been described in the literature.