The local anaesthetic activity of metiamide a histamine H2-receptor antagonist

Hind, Jonathan; Sutton, T. J.

doi:10.1111/j.2042-7158.1977.tb11299.x

Cited by 7 publications

(5 citation statements)

References 2 publications

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“…and H2 type. However, it must be borne in mind that PYR has some local anaesthetic and anticholinergic activity (Douglas, 1975) which MET does not share (Hind & Sutton, 1977). Therefore, it seems possible that the local anaesthetic effect of PYR could affect the central afférents to the POA-AHA and in this way reduce the magnitude of the prolactin response induced by ether.…”

Section: Discussionmentioning

confidence: 92%

Role of histamine in the increased secretion of prolactin induced by ether in adult male rats

Alvarez¹

1982

Journal of Endocrinology

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The purpose of the present work was to determine the possible role of the histamine receptors located in the rostral zone of the hypothalamus in the control of the prolactin surge induced by ether stress. Cannulae were implanted into the preoptic anterior hypothalamic area or the third ventricle of several groups of adult male rats under ether anaesthesia. On the following day the rats wee cannulated in the jugular vein so that they could be bled frequently. Twenty-four hours later saline, metiamide (an antagonist of H2 histamine) or pyrilamine (an antagonist of H1 histamine) were injected into the brain. Fifteen minutes after the injection all rats were subjected to an ether stress. Blood samples were taken at regular times after the stress and prolactin levels determined by radioimmunoassay. A prolactin surge was observed in rats injected with saline which extended up to 15-30 min after the stress. When the histamine antagonists were administered directly in the rostral hypothalamus both pyrilamine and metiamide inhibited the prolactin surge. When the histamine antagonists were administered into the third ventricle only metiamide was able to block the prolactin response completely. The present results suggest that histamine receptors in the rostral hypothalamus of the rat are involved in the control of prolactin secretion induced by stress.

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Section: Discussionmentioning

confidence: 92%

Role of histamine in the increased secretion of prolactin induced by ether in adult male rats

Alvarez¹

1982

Journal of Endocrinology

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“…However, preliminary experiments showed that the antagonism as observed over a period of 20 to 60 min after a single injection of diphenhydramine has no local anaesthetic action (Hind & Sutton, 1977).…”

Section: Resultsmentioning

confidence: 98%

“…Effects of diphenihydraminie and metiamide on tracheal vasodilatation and tracheal constriction in response to histaminie Diphenhydramine is known to have a local anaesthetic action about 3 times that of procaine (Dutta, 1949). However, preliminary experiments showed that the antagonism as observed over a period of 20 to 60 min after a single injection of diphenhydramine has no local anaesthetic action (Hind & Sutton, 1977).…”

Section: Dose Of Histamine (Ug)mentioning

confidence: 99%

“…Therefore, the antagonism of histamine-induced responses by diphenhydramine as the histamine H ,-receptor antagonist was determined within this definite period. Unlike diphenhydramine, metiamide, the highly specific histamine H 2-receptor antagonist (Black, Duncan, Emmett, Ganellin, Hesselbo, Parsons & Wyllie, 1973), has no local anaesthetic action (Hind & Sutton, 1977).…”

Section: Dose Of Histamine (Ug)mentioning

confidence: 99%

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PHARMACOLOGICAL ANALYSIS OF HISTAMINE RECEPTORS IN MUSCULATURE AND VASCULATURE OF THE DOG TRACHEA in situ

Himori

Taira

1978

British J Pharmacology

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1 The role of histamine H1-and H2-receptors in the musculature and vasculature of the dog trachea was investigated in the blood-perfused trachea in situ. 2 Histamine and acetylcholine caused increases in blood flow (tracheal vasodilatation) and in intraluminal pressure (tracheal constriction) in a dose-dependent manner. Histamine was almost equipotent to acetylcholine in causing tracheal vasodilatation but was about 30 times less potent in causing tracheal constriction. 3 The histamine H2-receptor agonist, dimaprit, caused a dose-dependent increase in tracheal blood flow but failed to cause tracheal constriction. 4 The tracheal constriction produced by histamine was inhibited strongly by diphenhydramine but not modified by metiamide. The tracheal vasodilatation produced by histamine was antagonized by both diphenhydramine and metiamide; diphenhydramine was more effective than metiamide. 5 It is concluded that in the tracheal musculature, histamine receptors are exclusively of the H1-type and mediate constriction, whereas in the tracheal vasculature, both histamine H1-and H2-receptors mediate vasodilatation but histamine Hl-receptors are predominant.

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“…A final problem in using antagonists to characterize the effects of histamine on sympathetic neurotransmission is that many HI-receptor antagonists are potent local anaesthetics (Dutta, 1949). This property is not shared by metiamide and cimetidine (Hind & Sutton, 1977).…”

Section: Histamine Receptors and Sympathetic Neurotransmission (A) Chmentioning

confidence: 99%

Histamine Modulation of Neurotransmission in the Sympathetic Nervous System

Marshall

1981

Journal of Autonomic Pharmacology

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The local anaesthetic activity of metiamide a histamine H2-receptor antagonist

Cited by 7 publications

References 2 publications

Role of histamine in the increased secretion of prolactin induced by ether in adult male rats

Role of histamine in the increased secretion of prolactin induced by ether in adult male rats

PHARMACOLOGICAL ANALYSIS OF HISTAMINE RECEPTORS IN MUSCULATURE AND VASCULATURE OF THE DOG TRACHEA in situ

Histamine Modulation of Neurotransmission in the Sympathetic Nervous System

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