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Related Concept Videos

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.
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...
Cholinergic Antagonists: Pharmacokinetics01:24

Cholinergic Antagonists: Pharmacokinetics

Cholinergic antagonists—such as antimuscarinics—are available in oral, topical, ocular, parenteral, and inhalational formulations. Most antimuscarinics are oral formulations,  while scopolamine is available as a topical patch, and ipratropium and tiotropium are available as inhalation aerosols or powders. Atropine, tropicamide, and cyclopentolate are topically instilled in the eye. Most antimuscarinics are lipid-soluble and readily absorbed from the gastrointestinal tract and the conjunctiva.
Cholinergic Antagonists: Chemistry and Structure-Activity Relationship01:29

Cholinergic Antagonists: Chemistry and Structure-Activity Relationship

Cholinergic antagonists bind to cholinergic receptors and limit the effects of acetylcholine and other cholinergic agonists. Based on the specific cholinergic receptor affinity, these antagonists are classified as muscarinic or nicotinic. Anticholinergics interrupt parasympathetic innervations while sympathetic innervations remain uninterrupted. Muscarinic antagonists are also called 'muscarinic antagonists', 'antimuscarinics', or 'parasympatholytics'. Nicotinic antagonists are called...
Indirect-Acting Cholinergic Agonists: Chemistry and Structure-Activity Relationship01:29

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

Indirect-acting cholinergic agonists are agents that interact with the acetylcholinesterase enzyme in the synaptic cleft, preventing the breakdown of acetylcholine into choline and acetate. Consequently, the concentration of acetylcholine in the synaptic cleft increases. These agonists can be classified into reversible and irreversible inhibitors based on their duration of action.
Reversible inhibitors display short to medium durations of action. Short-acting agents include simple alcohols with...
Cholinergic Antagonists: Therapeutic Uses01:26

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...

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Updated: Jun 25, 2026

Color Spot Test As a Presumptive Tool for the Rapid Detection of Synthetic Cathinones
06:06

Color Spot Test As a Presumptive Tool for the Rapid Detection of Synthetic Cathinones

Published on: February 5, 2018

Morpholine containing CB2 selective agonists.

Renée Zindell1, Doris Riether, Todd Bosanac

  • 1Department of Medicinal Chemistry, Boehringer Ingelheim Pharmaceuticals, Inc., 900 Ridgebury Road, PO Box 368, Ridgefield, CT 06877-0368, USA.

Bioorganic & Medicinal Chemistry Letters
|February 27, 2009
PubMed
Summary
This summary is machine-generated.

Researchers identified and optimized two types of selective cannabinoid receptor 2 (CB2) agonists. These compounds demonstrated efficacy comparable to prednisolone in a mouse model of inflammation, offering potential new therapeutic avenues.

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Area of Science:

  • Pharmacology
  • Medicinal Chemistry
  • Immunology

Background:

  • Cannabinoid receptor 2 (CB2) agonists are explored for therapeutic potential.
  • Inflammation is a complex biological response with significant unmet medical needs.
  • Selective CB2 agonists offer targeted anti-inflammatory effects with potentially fewer side effects.

Purpose of the Study:

  • To identify and optimize novel selective CB2 agonists.
  • To evaluate the anti-inflammatory efficacy of these compounds in a preclinical model.

Main Methods:

  • Drug discovery and optimization of two distinct chemical classes of CB2 agonists.
  • In vivo testing of lead compounds in a murine model of inflammation.
  • Comparative efficacy assessment against a known anti-inflammatory drug, prednisolone.

Main Results:

  • Successful identification and optimization of two novel classes of selective CB2 agonists.
  • Representative compounds from each class exhibited significant anti-inflammatory activity.
  • Oral administration of the CB2 agonists showed comparable efficacy to prednisolone in the inflammation model.

Conclusions:

  • The developed selective CB2 agonists represent promising candidates for treating inflammatory conditions.
  • These findings support further investigation of CB2 agonists as anti-inflammatory agents.
  • The compounds offer a potential alternative to existing therapies like prednisolone.