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Cholinergic Receptors: Muscarinic

Cholinergic Receptors: Muscarinic

The pharmacological actions of acetylcholine are elicited via its binding to two families of cholinergic receptors or cholinoceptors, namely, muscarinic and nicotinic receptors. Muscarinic receptors are G protein-coupled receptors and have five subtypes, M1–M5. All mAChR subtypes are activated by acetylcholine and blocked by the antagonist, atropine.
The subtypes M1, M3, and M5 couple with the Gq subunit and activate the phospholipase C (PLC) activity, mobilizing intracellular Ca2+. Activation...

Direct-Acting Cholinergic Agonists: Pharmacological Actions

Direct-Acting Cholinergic Agonists: Pharmacological Actions

Direct-acting cholinergic agonists exert their pharmacological actions by mimicking the effects of acetylcholine on postsynaptic muscarinic receptors to generate parasympathetic responses. These agents elicit a range of physiological responses, including cardiovascular effects. For example, activation of muscarinic receptors induces bradycardia, decreased cardiac output, reduced peripheral resistance, and consequent hypotension. In the eye, stimulation of M3 receptors leads to smooth muscle...

Indirect-Acting Cholinergic Agonists: Pharmacological Actions

Indirect-Acting Cholinergic Agonists: Pharmacological Actions

Indirect-acting cholinergic agonists, also known as anticholinesterases, exert their pharmacological effects by enhancing cholinergic transmission in various body parts, including the neuromuscular junction, autonomic cholinergic synapses, and the brain.
At the neuromuscular junction, these agents work by inhibiting the breakdown of acetylcholine, allowing it to remain bound to the receptor and bind to nearby receptors. This process leads to repetitive firing of the endplate, causing muscle...

Cholinergic Antagonists: Pharmacological Actions

Cholinergic Antagonists: Pharmacological Actions

Antimuscarinic drugs block muscarinic receptors in multiple systems, including the gut, eye, smooth muscles, respiratory tract, cardiovascular, and central nervous systems. They produce similar effects with varying selectivity depending on the specific agent and tissue. Here are the key pharmacological actions of antimuscarinics:
Gastrointestinal Effects: Antimuscarinics reduce gut contractions, increase gastric emptying, and slow intestinal transit. They partly inhibit gastric acid secretion...

Cholinergic Antagonists: Therapeutic Uses

Cholinergic Antagonists: Therapeutic Uses

Antimuscarinic drugs have various therapeutic applications by inhibiting parasympathetic stimulation in different systems. Here are the key therapeutic uses of antimuscarinics:
Respiratory Tract: Ipratropium, aclidinium, and tiotropium treat asthma, chronic bronchitis, and chronic obstructive pulmonary disease (COPD). They protect against bronchoconstriction caused by irritants like cigarette smoke, sulfur dioxide, and ozone. They also help reduce nasopharyngeal secretions in common...

Gastric Motility

Gastric Motility

Gastric motility is the coordinated contraction and relaxation of stomach muscles that convert ingested food into chyme, a semi-liquid substance ready for further digestion in the intestines. The process begins with the vagus nerve inducing the relaxation of the smooth muscles in the fundus and body of the stomach, allowing these regions to expand and accommodate up to approximately 1.5 liters of food and liquid.
Peristaltic Waves and Chyme Formation
Upon food entry, the stomach initiates...

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Related Experiment Video

Updated: Jul 13, 2026

Gastrointestinal Motility Monitor (GIMM)

Gastrointestinal Motility Monitor (GIMM)

Published on: December 1, 2010

Cholinergic effects on human gastric motility.

H P Parkman¹, D M Trate, L C Knight

¹Gastroenterology Section, Department of Medicine, Temple University Hospital, Philadelphia, Pennsylvania, USA.

|August 14, 1999

Summary

Cholinergic antagonism with atropine reduces antral contractility and slows gastric emptying. Cholinergic stimulation with bethanechol increases contractility but does not significantly alter gastric emptying.

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Published on: August 18, 2014

Area of Science:

Gastroenterology
Physiology
Pharmacology

Background:

Cholinergic regulation of gastric motility and emptying is not fully understood.
Investigating the impact of cholinergic agents on antral contractility is crucial.

Purpose of the Study:

To determine the effects of cholinergic stimulation and inhibition on gastric motility.
To assess impacts on myoelectric activity, antral contractility, and gastric emptying.

Main Methods:

Simultaneous electrogastrography (EGG), antroduodenal manometry, and dynamic antral scintigraphy (DAS) were used in 10 healthy subjects.
Subjects received intravenous atropine (cholinergic antagonist) or subcutaneous bethanechol (cholinergic agonist).
Gastric emptying was assessed after a radiolabeled solid meal.

Main Results:

Atropine decreased antral contractility and slowed gastric emptying.
Bethanechol increased antral contractility amplitude but decreased contraction frequency.
Neither atropine nor bethanechol significantly altered the overall antral motility index or gastric emptying time.

Conclusions:

Cholinergic antagonism with atropine impairs antral contractility and delays gastric emptying.
Cholinergic stimulation with bethanechol enhances antral contractility but does not improve gastric emptying.