Further observations on the action of β‐iminazolylethylamine

Dale, H. H.; Laidlaw, P. P.

doi:10.1113/jphysiol.1911.sp001464

Cited by 126 publications

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“…Histamine was first shown to cause hypothermia in 1911 (Dale and Laidlaw, 1911). More recent experiments suggested a brain site of action and the involvement of H 1 R (Shaw, 1971;Bugajski and Zacny, 1981;Haas et al, 2008).…”

Section: Discussionmentioning

confidence: 99%

Peripheral Adenosine A3 Receptor Activation Causes Regulated Hypothermia in Mice That Is Dependent on Central Histamine H1 Receptors

Carlin

Tosh

Xiao

et al. 2015

Journal of Pharmacology and Experimental Therapeutics

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Adenosine can induce hypothermia, as previously demonstrated for adenosine A 1 receptor (A 1 AR) agonists. Here we use the potent, specific A 3 AR agonists MRS5698, MRS5841, and MRS5980 to show that adenosine also induces hypothermia via the A 3 AR. The hypothermic effect of A 3 AR agonists is independent of A 1 AR activation, as the effect was fully intact in mice lacking A 1 AR but abolished in mice lacking A 3 AR. A 3 AR agonist-induced hypothermia was attenuated by mast cell granule depletion, demonstrating that the A 3 AR hypothermia is mediated, at least in part, via mast cells. Central agonist dosing had no clear hypothermic effect, whereas peripheral dosing of a non-brainpenetrant agonist caused hypothermia, suggesting that peripheral A 3 AR-expressing cells drive the hypothermia. Mast cells release histamine, and blocking central histamine H 1 (but not H 2 or H 4 ) receptors prevented the hypothermia. The hypothermia was preceded by hypometabolism and mice with hypothermia preferred a cooler environmental temperature, demonstrating that the hypothermic state is a coordinated physiologic response with a reduced body temperature set point. Importantly, hypothermia is not required for the analgesic effects of A 3 AR agonists, which occur with lower agonist doses. These results support a mechanistic model for hypothermia in which A 3 AR agonists act on peripheral mast cells, causing histamine release, which stimulates central histamine H 1 receptors to induce hypothermia. This mechanism suggests that A 3 AR agonists will probably not be useful for clinical induction of hypothermia.

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Section: Discussionmentioning

confidence: 99%

Peripheral Adenosine A3 Receptor Activation Causes Regulated Hypothermia in Mice That Is Dependent on Central Histamine H1 Receptors

Carlin

Tosh

Xiao

et al. 2015

Journal of Pharmacology and Experimental Therapeutics

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“…The vasodepressor action of histamine has been known for 70 years (Dale & Laidlaw, 1910;1911) but it was not until the discovery of anti-histamine drugs (HI-receptor antagonists) that the fall in blood pressure following small doses of histamine could be blocked. However, antagonists of this type could not prevent the fall in blood pressure resulting from the administration of higher doses of histamine.…”

Section: Discussionmentioning

confidence: 99%

ANTAGONISM OF VASODEPRESSOR AND GASTRIC SECRETORY RESPONSES TO HISTAMINE BY THE H₂‐RECEPTOR ANTAGONISTS, RANITIDINE AND CIMETIDINE, IN THE ANAESTHETIZED DOG

Daly

Humphray

Stables

1981

British J Pharmacology

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1 The new H2-receptor antagonist, ranitidine, has been compared with cimetidine as an inhibitor of gastric acid secretion in the anaesthetized dog. 2 Both ranitidine and cimetidine given intravenously inhibited histamine-induced gastric secretion in a dose-related manner. Ranitidine was 4.2 times more potent than cimetidine when given as an intravenous infusion and 9.6 times more potent as an intravenous bolus dose. 3 In a separate series of experiments, ranitidine was compared with cimetidine as an antagonist of vasodepressor responses to histamine. Mepyramine alone displaced the histamine dose-response curve to the right. After a maximally effective dose of mepyramine, further displacement could be achieved with ranitidine and cimetidine, ranitidine being 19.2 times more potent than cimetidine. 4 Ranitidine alone had no effect on vasodepressor response curves to histamine, acetylcholine or (-)-isoprenaline or on vasopressor response curves to phenylephrine. 5 These results indicate that displacement of the histamine dose-response curve after mepyramine blockade by ranitidine and cimetidine is due to selective H2-receptor antagonism.

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“…This results from direct action on the musculature of the vessels, and is independent of innervation (Dale & Laidlaw, 1910, 1911. FIG.…”

Section: Effect Of Extract On Cardiovascular Systemmentioning

confidence: 99%

The effects of histamine in malaria

Maegraith¹,

Onabanjo²

1970

British J Pharmacology

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Summary1. Extracts of the blood of monkeys (Macaca mulatta) infected with Plasmodium knowlesi contain histamine. A mean total concentration of 0-15 jug/ml was present in the circulating blood. 2. No histamine was detected in the blood of healthy monkeys. 3. Vasodilatation and increased vascular permeability was observed at the site of injection of the extract into the skin and brain of guinea-pigs. 4. Infiltration of the dermal layer by leucocytes was observed after intradermal injection of the histamine extract. A similar response was obtained in the brain. 5. The extract of the blood from the infected animal produced hypotension in rabbits when administered intravenously. 6. The pathophysiological significance of histamine in malaria is discussed.

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Further observations on the action of β‐iminazolylethylamine

Abstract: IN a previous communication' we described the general features of the action of 8-Iminazolylethylamine. We have now to describe and discuss certain additional and supplementary observations.

Cited by 126 publications

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Peripheral Adenosine A3 Receptor Activation Causes Regulated Hypothermia in Mice That Is Dependent on Central Histamine H1 Receptors

Peripheral Adenosine A3 Receptor Activation Causes Regulated Hypothermia in Mice That Is Dependent on Central Histamine H1 Receptors

ANTAGONISM OF VASODEPRESSOR AND GASTRIC SECRETORY RESPONSES TO HISTAMINE BY THE H₂‐RECEPTOR ANTAGONISTS, RANITIDINE AND CIMETIDINE, IN THE ANAESTHETIZED DOG

The effects of histamine in malaria

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Further observations on the action of β‐iminazolylethylamine

Abstract: IN a previous communication' we described the general features of the action of 8-Iminazolylethylamine. We have now to describe and discuss certain additional and supplementary observations.

Cited by 126 publications

References 0 publications

Peripheral Adenosine A3 Receptor Activation Causes Regulated Hypothermia in Mice That Is Dependent on Central Histamine H1 Receptors

Peripheral Adenosine A3 Receptor Activation Causes Regulated Hypothermia in Mice That Is Dependent on Central Histamine H1 Receptors

ANTAGONISM OF VASODEPRESSOR AND GASTRIC SECRETORY RESPONSES TO HISTAMINE BY THE H2‐RECEPTOR ANTAGONISTS, RANITIDINE AND CIMETIDINE, IN THE ANAESTHETIZED DOG

The effects of histamine in malaria

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ANTAGONISM OF VASODEPRESSOR AND GASTRIC SECRETORY RESPONSES TO HISTAMINE BY THE H₂‐RECEPTOR ANTAGONISTS, RANITIDINE AND CIMETIDINE, IN THE ANAESTHETIZED DOG