Histamine, antihistamines, and the central nervous system
Related Experiment Video
Updated: Jun 19, 2026

Basophil Activation Test for Allergy Diagnosis
Published on: May 31, 2021
1Departments of Medicine and Pediatrics, University of Tennessee, Memphis, Tennessee, USA. aac@allergymemphis.com
Abstract:
Histamine is a central nervous system (CNS) neurotransmitter. It acts in the brain via three receptors, H(1), H(2), and H(3). It is a mediator of "wakefulness" and its activity is necessary to maintain wakefulness, alertness, and reaction time. These activities can be impaired by H(1)-antagonists (reverse agonists) capable of penetrating the blood-brain barrier. By blocking the homeostatic effects of histamine in the CNS, drowsiness and functional impairment with or without drowsiness can occur. Several tests have been designed to assess the effects of antihistamines on the CNS. These include subjective measurements of drowsiness and more objective measurements of impairment. Second-generation antihistamines have been designed to minimize blood-brain barrier penetration by reducing lipophilicity and increasing the affinity for P-aminnoglycoprotein.
Related Concept Videos
Upper Respiratory Drugs: First and Second-Generation Antihistamines
Histamine binds to specific receptor sites, known as H1 receptors, on tissue cells, triggering inflammation and swelling. Antihistamines combat these effects by competing with histamine for these receptor sites. By...
Cholinergic Antagonists: Pharmacological Actions
Gastrointestinal Effects: Antimuscarinics reduce gut contractions, increase gastric emptying, and slow intestinal transit. They partly inhibit gastric acid secretion...
Drugs Affecting Neurotransmitter Release or Uptake
Indirect-Acting Cholinergic Agonists: Pharmacological Actions
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...
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...
Pathophysiology of Vomiting
