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Cholinergic Antagonists
Published in Sahab Uddin, Rashid Mamunur, Advances in Neuropharmacology, 2020
Vishal S. Gulecha, Manoj S. Mahajan, Aman Upaganlawar, Abdulla Sherikar, Chandrashekhar Upasani
Telenzepine, a pirenzepine analog, possesses higher potency for M1 receptor. Like pirenzepine, telenzepine is selective for M1 receptor. It also binds to M3 receptors without affecting their organizational structure (Pediani et al., 2017). This drug is mainly prescribed for acid-peptic disease in different parts of the world, but not in the United States (Brunton et al., 2011).
Antagonists at Muscarinic Cholinergic Receptors
Published in Kenneth J. Broadley, Autonomic Pharmacology, 2017
The M1-selective antagonist, pirenzepine (GastrozepinR), shows selectivity for inhibition of gastric acid secretion with a lower incidence of muscarinic side-effects than the non-selective antimuscarinics. It has been shown to be as effective as the H2 receptor antagonist, cimetidine, at promoting wound healing in patients with duodenal ulcers. The dose required is approximately one-tenth that of cimetidine. The patients experience reduced day and night pain and antacid consumption. Pirenzepine also performs equally with cimetidine in benign gastric ulceration. The addition of pirenzepine to the H2 receptor antagonists inhibits gastric acid secretion to a greater extent than do the individual drugs alone, and their combined use appears to be more effective in treatment of gastric and duodenal ulceration. Muscarinic side-effects are minimal and are only the cause of withdrawing the treatment in -2% of patients. Pirenzepine is not a quaternary compound but is hydrophilic with low lipid solubility and therefore does not penetrate into the CNS. It therefore has no central side-effects at the normal twice daily therapeutic dosing. The site of action of pirenzepine has already been discussed. The M1 receptor selectivity of pirenzepine is clearly not targeted at parietal cell secretion, which is M2 receptor-mediated. It appears to be due to inhibition of ganglionic M1 receptors in the myenteric plexus of the gut. Telenzepine is structurally related to pirenzepine (Table 9.6) and has a similar profile of action, being 4–10 times more potent as an antisecretory agent (Eltze et al. 1985).
Updated review on the link between cortical spreading depression and headache disorders
Published in Expert Review of Neurotherapeutics, 2021
Doga Vuralli, Hulya Karatas, Muge Yemisci, Hayrunnisa Bolay
Recently, the effect of cholinergic activation with the cholinomimetic agonist carbachol on CSD in mouse neocortical brain slices was investigated and an inhibitory effect of cholinergic activation on the initiation and the propagation of CSD, through the action of muscarinic receptors, was shown [189]. Muscarinic modulation both increased the threshold of CSD induction and resulted in inhibition of its propagation. CSD inhibition induced by carbachol was blocked by both atropine and the preferential M1 muscarinic antagonist telenzepine. McN-A-343, a muscarinic agonist with preferential action at M1 receptors, also inhibited CSD similar to carbachol. The inhibitory effect of McN-A-343 on CSD was blocked when McN-A-343 was applied with telenzepine. The inhibitory action of muscarinic agonists on CSD may be targeted for new treatment options in migraine.
Central muscarinic receptor subtypes (M1 and M3) involved in carbacol-induced hypophagia in neonatal broiler chicken
Published in International Journal of Neuroscience, 2020
Morteza Zendehdel, Leila Lankarani Mohajer, Shahin Hassanpour
Drugs include carbacol (a cholinergic agonist), Telenzepine (M1 muscarinic receptor antagonist), F-DX 116 (M2 muscarinic receptor antagonist), 4-DAMP (M3 muscarinic receptor antagonist), PD102807 (M4 muscarinic receptor antagonist) from Tocris Co. (Bristol, UK) and Evans blue from Sigma Co. (Ronkonkoma, NY, USA) purchased. Drugs at first dissolved in absolute dimethyl sulfoxide (DMSO) then diluted with 0.85% saline containing Evans blue at a ratio of 1/250. DMSO with this ratio does not have a cytotoxic effect [16,17].