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Related Concept Videos

Drugs Acting on Autonomic Ganglia: Stimulants01:23

Drugs Acting on Autonomic Ganglia: Stimulants


Ganglionic stimulants activate NM nicotinic receptors in autonomic ganglia, falling into two categories: nicotine mimetics [e.g., lobeline, dimethylpiperazine, tetramethylammonium] and muscarinic receptor agonists [e.g., muscarine, methacholine]. The first category's action is rapid and blocked by nicotinic receptor antagonists, while the second category's action is delayed and blocked by atropine-like agents. Nicotine, an alkaloid, affects the heart rate by stimulating sympathetic or...
Drug Abuse and Addiction: Pharmacological Phenomena01:15

Drug Abuse and Addiction: Pharmacological Phenomena

Drug dependence, abuse, and addiction are complex phenomena that can precipitate various abnormal states. Physical dependence refers to a state of pharmacological adaptation to a drug. This adaptation often results in tolerance—a reduced response to the drug after repeated administrations. When the drug use is abruptly stopped, withdrawal symptoms occur due to the body's need to readjust from the pharmacologically induced imbalance. However, tolerance and withdrawal symptoms do not necessarily...
Indirect-Acting Cholinergic Agonists: Pharmacological Actions01:30

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...
Direct-Acting Cholinergic Agonists: Chemistry and Structure-Activity Relationship01:22

Direct-Acting Cholinergic Agonists: Chemistry and Structure-Activity Relationship

Cholinergic agonists or cholinomimetics mimic the action of acetylcholine to stimulate the parasympathetic nervous system. They are categorized into direct-acting and indirect-acting agents. The direct-acting cholinergic drugs induce the parasympathetic response by directly binding to the muscarinic or nicotine receptors. In comparison, the indirect-acting cholinergic drugs prevent acetylcholine hydrolysis, indirectly contributing to the extended parasympathetic response.
The direct-acting...
Direct-Acting Cholinergic Agonists: Pharmacokinetics01:31

Direct-Acting Cholinergic Agonists: Pharmacokinetics

Direct-acting cholinergic agonists, such as synthetic choline esters and naturally occurring alkaloids, exert their effects by enhancing the actions of acetylcholine and stimulating the parasympathetic nervous system. Synthetic choline esters share structural similarities with acetylcholine. For example, they have a positively charged quaternary ammonium or onium group, contributing to their hydrophilic characteristics. As a result, they are poorly absorbed in the body through oral...
Direct-Acting Cholinergic Agonists: Therapeutic Uses01:11

Direct-Acting Cholinergic Agonists: Therapeutic Uses

Direct-acting cholinergic agonists have many therapeutic uses in various medical fields. Choline esters, including acetylcholine, have limited clinical utility due to their non-selectivity and short duration of action. Still, acetylcholine and carbachol are applied topically during ophthalmologic surgery to induce miosis. Pilocarpine, a muscarinic and ganglionic stimulator, effectively treats open-angle glaucoma and alleviates xerostomia and dry mouth caused by radiotherapy or Sjögren syndrome.

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Related Experiment Video

Updated: Jun 19, 2026

A Computerized Test Battery to Study Pharmacodynamic Effects on the Central Nervous System of Cholinergic Drugs in Early Phase Drug Development
07:02

A Computerized Test Battery to Study Pharmacodynamic Effects on the Central Nervous System of Cholinergic Drugs in Early Phase Drug Development

Published on: February 11, 2019

Cholinergic functioning in stimulant addiction: implications for medications development.

Mehmet Sofuoglu1, Marc Mooney

  • 1Yale University, School of Medicine, Department of Psychiatry and VA Connecticut Healthcare System, West Haven, Connecticut 06516, USA. Mehmet.Sofuoglu@yale.edu

CNS Drugs
|October 23, 2009
PubMed
Summary

Acetylcholine, a key neurotransmitter, shows promise for treating stimulant addiction by interacting with the brain's reward system. Targeting cholinergic receptors may offer new therapeutic strategies for addiction.

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Area of Science:

  • Neuroscience
  • Pharmacology
  • Addiction Research

Background:

  • Acetylcholine (ACh) is a neurotransmitter involved in numerous central nervous system (CNS) functions.
  • Cholinergic effects are mediated by nicotinic (nAChR) and muscarinic (mAChR) receptors.
  • The interaction between acetylcholine and the dopaminergic reward system is crucial for understanding addiction.

Purpose of the Study:

  • To review the literature on acetylcholine as a potential treatment target for stimulant addiction.
  • To explore the role of cholinergic systems in the brain's reward pathways.
  • To synthesize evidence from preclinical and human studies regarding cholinergic interventions for addiction.

Main Methods:

  • Literature review synthesizing preclinical and human studies.
  • Analysis of acetylcholine's interaction with the dopaminergic system in key brain regions (VTA, NAc, PFC).
  • Evaluation of the effects of nicotinic and muscarinic receptor agonists and acetylcholinesterase inhibitors.

Main Results:

  • Nicotinic receptor agonists may facilitate stimulant addiction development.
  • Muscarinic receptor agonists appear to inhibit stimulant addiction.
  • Acetylcholinesterase inhibitors show promise in human studies for treating stimulant addiction.

Conclusions:

  • The cholinergic system, particularly acetylcholine, represents a viable therapeutic target for stimulant addiction.
  • Further clinical trials are needed to confirm the efficacy of cholinergic medications for stimulant addiction treatment.
  • Understanding cholinergic mechanisms offers novel avenues for addiction pharmacotherapy.