Classification and biological distribution of histamine receptor sub-types

Abstract

The distribution and classification of histamine receptors in mammalian and avian tissues have been summarized in Tables 1-4. It is evident that histamine receptors are present on a number of morphologically distinct cell types and the proportion of cells bearing H1- and H2-receptors varies not only with the species but also with the cell source. The pharmacological receptors mediating mepyramine-sensitive histamine responses have been defined as H1-receptors. Receptors mediating mepyramine-resistant, but burimamide or metiamide-sensitive histamine responses have been classified as H2-receptors. Histamine responses mediated via H2-receptors seem to involve the adenylcyclase system resulting in elevation of intracellular cyclic-AMP level, which is susceptible to burimamide blockade but insensitive to beta-adrenergic blocking agents. This mode of action of histamine involving H2-receptors and the adenyl cyclase system has been shown to stimulate the mammalian heart; promote gastric acid secretion; inhibit antigen-induced histamine release from leucocytes and inhibit lymphocyte-mediated cytotoxicity. It can further be concluded that both H1- and H2-receptors are widely distributed throughout the animal body in the gastro-intestinal, reproductive, respiratory and cardiovascular systems, nervous system and on mast cells and blood leucocytes. In these tissues, histamine receptors play an important role in physiological, immunological and immunopathological processes. Interaction of histamine with both H1- and H2-receptors in varying proportions modulates the overall manifestation of cardiovascular and respiratory syndromes during certain immunopathological conditions (e.g. inflammation, allergy and anaphylaxis). Histamine receptors also appear to play and important role in the development of immuno-competence and immunity.

Actions of second messengers synthesized by various spasmogenic agents and their relation to mechanical responses in dog tracheal smooth muscle

“…For example, in the rabbit airway, the potassium (128 mm K)-and histamine (10pM)-induced contractions in the trachea are much smaller than the acetylcholine (ACh, 10 M)-induced contraction, but in the third branch of the right middle bronchial tree, these same three stimulants generate much the same amplitude of contraction and, moreover, the amplitude of the ACh-induced contraction is larger than that observed in the trachea (Fujiwara et al, 1988). In the guinea-pig, dog, bovine and rabbit tracheal and bronchial tissues, histamine produces contraction by stimulation of the Hl-receptor, though H2-receptors are also present (Chand & Eyre, 1975;Kirkpatrick, 1975;Kotlikoff et al, 1987). Ito & Tajima (1982) demonstrated that in the dog trachea, isoprenaline produces hyperpolarization of the membrane, reduces the resting tone and relaxes tissues precontracted by ACh.…”

Relaxant Response of Goat Trachea to 5‐hydroxytryptamine Mediated by D‐tryptamine Receptors

“…As opposed to the goat trachea (this study), several well-known D-and M-tryptamine receptor antagonists have been reported to be ineffective in antagonizing 5-HT-induced contractions of cat trachea (Statkov, 1969) and relaxations of sheep pulmonary vein (Eyre, 1975).…”

“…After HI-receptor blockade, 4-methylhistamine and dimaprit (relatively selective H2-agonists) (Chand & Eyre, 1975; Owen, Ganellin & Durant, 1977) relaxed goat trachea. Cimetidine and metiamide (H2-antagonists) (Chand & Eyre, 1975) weakly enhanced histamine-induced contractions.…”

“…Surprisingly, 5-HT has also been reported to antagonize acetylcholine-induced contractions on rhesus monkey bronchioles, and to relax human bronchioles (Brocklehurst, 1958), and bronchus (Mathe, Astrom & Persson, 1971) and sheep pulmonary vein (Eyre, 1975).…”

Comparison Of Airway Responses In Sheep Of Different Age In Precision-cut Lung Slices (PCLS)

“…Since no analysis of the different histamine receptor expression was performed in lung tissue in the present study the discussion about H 3 and H 4 remains speculative and is a clear limitation of this study. Normally, in the lungs histamine acts on H 1 -and H 2 -receptors and its effect is therefore balanced by the H 1 -mediated contraction and the H 2 -mediated relaxation of airway smooth muscles [42][43][44][45]. The observation that histamine contracts tracheal and bronchial airways, but relaxes smaller bronchi and bronchioles [46], indicates that there is a shift towards predominance of H 2 2receptors towards the peripheral airways.…”