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Direct-Acting Cholinergic Agonists: Pharmacological Actions

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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...

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Indirect-Acting Cholinergic Agonists: Pharmacological Actions

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Parasympathetic Signaling

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Parasympathetic signaling plays a crucial role in regulating various physiological processes. It involves the release of acetylcholine (ACh) by parasympathetic neurons, which can have localized and short-lived effects. The majority of ACh released is rapidly inactivated at the synapse by the enzyme acetylcholinesterase (AChE), which hydrolyzes Ach into choline and acetate. Additionally, the tissue cholinesterase deactivates any ACh diffusing into the surrounding tissues.
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Related Experiment Video

Updated: Oct 30, 2025

In Vivo Functional Assessment of Rat Masseter Muscle Following Surgical Creation of a Volumetric Muscle Loss (VML) Injury

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Age-related decrease of cholinergic parasympathetic reflex vasodilation in the rat masseter muscle.

Kohei Mito¹, Toshiya Sato¹, Rina Ishikawa¹

¹Division of Physiology, Department of Oral Biology, School of Dentistry, Health Sciences University of Hokkaido, Ishikari-Tobetsu, Hokkaido, Japan.

Microvascular Research

|July 4, 2021

Summary

This summary is machine-generated.

Aging significantly reduces parasympathetic vasodilation in jaw muscles. This decline in masseter muscle blood flow (MBF) is linked to decreased muscarinic acetylcholine receptor expression in older rats.

Keywords:

Aging Atropine Hexamethonium Lingual nerve Muscarinic acetylcholine receptors

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Published on: September 22, 2011

Area of Science:

Physiology
Neuroscience
Aging Research

Background:

Skeletal muscle hemodynamics are crucial for function and are influenced by aging.
Parasympathetic vasodilation may significantly impact masseter muscle blood flow (MBF), but its age-related changes are not well understood.

Purpose of the Study:

To investigate the effect of aging on parasympathetic vasodilation in the masseter muscle.
To elucidate the mechanisms underlying age-related changes in trigeminal nerve-mediated vasodilation.

Main Methods:

Examined MBF during lingual nerve (LN) stimulation in young and old rats.
Utilized pharmacological agents (hexamethonium, atropine) and exogenous acetylcholine to assess pathways.
Quantified muscarinic acetylcholine receptor (MR1 and MR3) mRNA expression in the masseter muscle.

Main Results:

LN stimulation induced intensity- and frequency-dependent increases in MBF in young rats, significantly reduced in old rats.
Cholinergic pathway involvement was confirmed by blockade with hexamethonium and atropine in young rats.
Acetylcholine administration increased MBF in young rats but not in old rats, correlating with reduced MR1 and MR3 mRNA in aged muscle.

Conclusions:

Aging diminishes cholinergic parasympathetic reflex vasodilation in the masseter muscle.
This reduction is associated with decreased expression of muscarinic acetylcholine receptors (MR1 and MR3) in the masseter muscle with age.