Behavioural effects of histamine and its antagonists: a review

  title={Behavioural effects of histamine and its antagonists: a review},
  author={Jason M. White and Greg Rumbold},
This review focusses on the behavioural effects of histamine and drugs which affect histaminergic function, particularly the H1- and H2-receptors antagonists. Research in this area has assumed considerable importance with increasing interest in the role of brain histamine, the clinical use of both H1 and H2 antagonists and evidence of nonmedical use of H1 antagonists. Results from a number of studies show that H1 and H2 antagonists have clear, but distinct subjective effects and that H1… 

Histamine H1-receptor blockade in humans affects psychomotor performance but not memory

Results show that dexchlorpheniramine and scopolamine clearly impaired performance on psychomotor and attention tasks but do not suggest a specific role of the histaminergic system in learning and memory in humans.

Pitolisant and Other Histamine-3 Receptor Antagonists—An Update on Therapeutic Potentials and Clinical Prospects

Although limited clinical studies have been conducted on this new class of drugs, the reviewed literature showed promising results for future additions to the clinical indications of pitolisant, and the expansion of the list of approved drugs in this class for a variety of indications.

Histamine receptors in the central nervous system

Several aspects of the pharmacology of histamine in the central nervous system are still a matter of empirism and speculations, but the recent publications on the brain-penetrating H2 antagonist zolantidine and the selective H3 agonists and antagonists are expected to contribute to the knowledge of the histaminergic pathways in the brain.

Histamine and the striatum

Comparison of the effects of eleven histamine H1-receptor antagonists on monoamine turnover in the mouse brain

The results suggest that (1) the degree of inhibition of the uptake of DA and 5-HT by histamine H1-receptor antagonists is considerably different, (2) most Ht-antagonists have little influence on NA uptake and some compounds enhance NA release, and (3) carbinoxamine, clemastine, triprolidine, and meclizine have comparatively weak influences on monoamine metabolism.

Punishing and cardiovascular effects of intravenous histamine in rats: pharmacological selectivity.

The present findings extend the general hypothesis that activation of histamine H1 -receptors mediates the punishing effects of histamines and introduce methods for rapidly assessing pharmacological mechanisms underlying drug-induced punishment.

Histamine H3 receptor as a drug discovery target.

The current medicinal chemistry programs are based on the monumental amount of research effort that has gone into establishing various aspects of H3 receptor biology, and suggest an abundance of therapeutic applications for small-molecule receptor modulators.

Induction of prolonged, continuous slow‐wave sleep by blocking cerebral H1 histamine receptors in rats

The effect of classic and modern antihistamines on rats' sleep using continuous i.c.v. infusions is analysed to characterize both histaminergic sleep regulation and the central actions of antihistamine.



Effects of antidepressant drugs on histamine-H1 receptors in the brain.

Peripheral antihistamine and central sedative effects of three H1-receptor antagonists

The independence of peripheral and CNS effects was suggested by correlation analysis and should encourage development of new and more specific antihistamine compounds.

Effects of a histamine synthesis inhibitor and antihistamines on the sexual behavior of female rats

It is concluded that treatments which either deplete histamine or block their receptors can alter female copulatory responsiveness, and antihistamine-injected rats showed no soliciting behavior.

Central effects of histamine and H1 and H2 receptors agonists and antagonists after intraventricular infusion in fowls.

Pharmacological evidence is provided for the existence of H1 and H2 histamine receptors in avian brain and an involvement of histamine H2 and H1 receptors in the control of arousal-sleep and thermoregulatory mechanisms is suggested.

Relative potencies of histamine H1 antagonists as behavioral stimulants in the squirrel monkey

A report from this laboratory showed that several drugs with H 1 antagonist actions produce marked increases in responding of squirrel monkeys studied under fixed-interval (FI) schedules of food delivery or of stimulus-shock termination.

Effects of centrally administered H2 antagonists in the behavioral despair test

The results suggest that H1 and H2 receptors in the brain may mediate opposing behavioral effects in mice and that cimetidine and chlorpheniramine alone have no effect on swimming.