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Related Concept Videos

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...
Cholinergic Antagonists: Pharmacological Actions01:28

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...
Adrenergic Agonists: Chemistry and Structure-Activity Relationship01:16

Adrenergic Agonists: Chemistry and Structure-Activity Relationship

Adrenergic agonists' structure-activity relationship (SAR) determines their selectivity and efficacy. These agonists comprise a phenylethylamine moiety with an aromatic ring and an ethylamine side chain.
Aromatic ring substitutions: Substituting the aromatic ring with –OH groups at positions 3 and 4 yields catecholamines (e.g., epinephrine), which have a high affinity for adrenoceptors. Hydrogen bonding between –OH groups and receptors enhances adrenergic activity.
Separation of the aromatic...
Adrenergic Antagonists: Chemistry and Classification of ɑ-Receptor Blockers01:17

Adrenergic Antagonists: Chemistry and Classification of ɑ-Receptor Blockers

Adrenergic antagonists, or sympatholytics, inhibit adrenoceptor activation driven by catecholamines or agonists. Based on their adrenoceptor specificity, adrenergic blockers can be categorized into two primary groups: α-adrenergic blockers (α-blockers) and β-adrenergic blockers (β-blockers). α-blockers interact with α1 and α2 subtypes of α-adrenoceptors.
Nonselective α-blockers: Nonselective α-blockers contain haloalkylamine or imidazoline moieties. Phenoxybenzamine, with a haloalkylamine...
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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Related Experiment Video

Updated: Jun 28, 2026

Operant Protocols for Assessing the Cost-benefit Analysis During Reinforced Decision Making by Rodents
07:05

Operant Protocols for Assessing the Cost-benefit Analysis During Reinforced Decision Making by Rodents

Published on: September 10, 2018

2-Aryloxymethylmorpholine histamine H(3) antagonists.

Michael A Letavic1, John M Keith, Kiev S Ly

  • 1Johnson & Johnson Pharmaceutical Research & Development L.L.C., San Diego, CA 92121-1126, USA. mletavic@its.jnj.com

Bioorganic & Medicinal Chemistry Letters
|October 17, 2008
PubMed
Summary
This summary is machine-generated.

Researchers synthesized novel 2-aryloxymethylmorpholine compounds that act as potent histamine H(3) antagonists. These compounds effectively cross the blood-brain barrier to target histamine H(3) receptors in the rat brain.

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Subcutaneous Administration of Muscarinic Antagonists and Triple-Immunostaining of the Levator Auris Longus Muscle in Mice
07:09

Subcutaneous Administration of Muscarinic Antagonists and Triple-Immunostaining of the Levator Auris Longus Muscle in Mice

Published on: September 8, 2011

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Subcutaneous Administration of Muscarinic Antagonists and Triple-Immunostaining of the Levator Auris Longus Muscle in Mice
07:09

Subcutaneous Administration of Muscarinic Antagonists and Triple-Immunostaining of the Levator Auris Longus Muscle in Mice

Published on: September 8, 2011

Area of Science:

  • Medicinal Chemistry
  • Neuroscience
  • Pharmacology

Background:

  • Histamine H(3) receptors are implicated in various neurological functions.
  • Developing selective histamine H(3) receptor antagonists is a therapeutic goal for CNS disorders.

Purpose of the Study:

  • To synthesize and evaluate a new series of 2-aryloxymethylmorpholine derivatives.
  • To assess the biological activity and CNS penetration of these novel compounds as histamine H(3) antagonists.

Main Methods:

  • Chemical synthesis of 2-aryloxymethylmorpholine analogs.
  • In vitro and in vivo assays to determine histamine H(3) receptor binding affinity.
  • Assessment of central nervous system (CNS) penetration.

Main Results:

  • A novel series of 2-aryloxymethylmorpholine compounds were successfully synthesized.
  • These compounds demonstrated high affinity for the histamine H(3) receptor.
  • The synthesized antagonists were shown to penetrate the CNS and occupy the target receptor in rat brain tissue.

Conclusions:

  • The described 2-aryloxymethylmorpholine derivatives represent promising histamine H(3) receptor ligands.
  • Their ability to cross the blood-brain barrier and bind to CNS targets warrants further investigation for potential therapeutic applications.