Brain histamine receptors as targets for antidepressant drugs

Kanof, Philip D.; Greengard, Paul

doi:10.1038/272329a0

Cited by 262 publications

(91 citation statements)

References 59 publications

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“…Angus & Black (1980) argued that amitriptyline might express phosphodiesterase inhibition concomitantly with histamine H2-receptor antagonism. This possibility was considered to account for the apparently low affinity expressed by amitriptyline for the histamine H2-receptors in tissue bioassays compared with that expressed in adenylate cyclase assays (Kanof & Greengard, 1979). The known, leftward-shifting effect of phosphodiesterase inhibition on histamine concentration-effect curves (Reinhardt et al, 1977: Broadley & Wilson, 1980 would account for this discrepancy and indeed amitriptyline was later found to inhibit this enzyme (Reynolds & Claxton, 1982).…”

Section: Introductionmentioning

confidence: 99%

Analysis of competitive antagonism when this property occurs as part of a pharmacological resultant

Black¹,

Vp²,

Leff

et al. 1986

British J Pharmacology

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I In this paper, pharmacological resultant is defined as the net effect of a single compound resulting from the simultaneous expression of two or more specific actions. 2 The principles of concentration-ratio analysis are extended to develop a method for detecting and quantifying competitive antagonism when this property is a component of a pharmacological resultant. The method is general to the extent that it allows analysis of competitive antagonism in combination with all types of post-receptor intervention. Essentially it depends on the altered expression of competition by a reference antagonist. It incorporates tests for validating its application and it is independent of agonist concentration-effect curve shape: in these respects the method is analogous to Schild plot-analysis of simple competition. 3 The methodology for the practical application of the analysis is exemplified by studying the net effect of a combination of a phosphodiesterase inhibitor (isobutylmethylxanthine) and histamine H2-receptor antagonist (metiamide) on histamine-stimulated tachycardia in guinea-pig, isolated, right atrium. Cimetidine was used as the reference antagonist. 4 The equation used in this analysis is similar in form to one recently described by to elucidate the situation when competitive antagonism occurs in combination with functional interactions. The relation between their method and the present analysis is discussed.

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Section: Introductionmentioning

confidence: 99%

Analysis of competitive antagonism when this property occurs as part of a pharmacological resultant

Black¹,

Vp²,

Leff

et al. 1986

British J Pharmacology

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“…The biogenic amine histamine (HA) was among the first compounds recognized as a messenger molecule in intercellular communication (Kanof and Greengard 1978). In vertebrates, it functions as a transmitter in the brain as well as a transmitter, hormone and mediator in peripheral systems.…”

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confidence: 99%

Putative histamine‐gated chloride channel subunits of the insect visual system and thoracic ganglion

Witte¹,

Kreienkamp

Gewecke³

et al. 2002

Journal of Neurochemistry

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Histamine-gated chloride channels, members of the ligandgated ion channel superfamily, are thought to be peculiar for arthropods. Their cognate ligand, histamine, is the transmitter of all arthropod photoreceptors and of thoracic mechanoreceptors. To identify putative histamine-gated chloride channel subunits we scanned the Drosophila genome for putative ligand-gated chloride channel subunits and found 12 candidate genes. We found four groups of transcripts based on their expression pattern. Only members of the last group show an expression pattern that is consistent with our knowledge about histamine-gated chloride channels in insects. In the brain these transcripts (Dm HA-Cl I and II) are exclusively present in interneurones postsynaptic to photoreceptors.Within the lamina (the first visual ganglion) only the L1-L3 neurones are labelled. The lack of non-photoreceptor dependent staining in the brain indicates that mechanosensory transmission differs between the head and the thorax/abdomen, and that the receptors responding to brain-intrinsic histaminergic cells use different signalling pathways. The putative histamine-gated chloride channels show the greatest homology mammalian glycine receptors. These ion-channels are the first specific molecular markers for postsynaptic cells in the insect visual system, thus representing ideal tools to study its physiology and development.

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“…In clinical trials in man, the anticholinergic effects of mianserin have been found to be absent or negligible (Brogden et al, 1978) so that anticholinergic effects are unlikely to be responsible for the gastric secretory inhibition. Mianserin also blocks the histamine-sensitive adenyl cyclase of mammalian brain (Kanof & Greengard, 1978) and it seems possible that an analogous effect on gastric cellular adenyl cyclase activity could be functionally important, since this enzyme is activated when histamine stimulates gastric secretion (Soll et al, 1981).…”

Section: Discussionmentioning

confidence: 99%

Inhibition of pentagastrin‐stimulated and overnight gastric secretion by mianserin.

Wilson¹,

Read²,

Boyd³

et al. 1983

Brit J Clinical Pharma

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1 The effects of mianserin (60 mg) have been studied on nocturnal and pentagastrin‐stimulated gastric secretion. 2 Mianserin reduced pentagastrin‐stimulated gastric acid secretion by 38%, pepsin by 40% and secretory volume by 45% during a 1 h test. 3 Twelve‐hour overnight secretion of acid was reduced by 37%, while secretion of pepsin was reduced by 43% and secretory volume by 51%. 4 No adverse effects were noted. 5 These findings, which achieve statistical significance, suggest the need for further study to evaluate the possible role of mianserin in the therapy of duodenal ulcer disease.

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Brain histamine receptors as targets for antidepressant drugs

Cited by 262 publications

References 59 publications

Analysis of competitive antagonism when this property occurs as part of a pharmacological resultant

Analysis of competitive antagonism when this property occurs as part of a pharmacological resultant

Putative histamine‐gated chloride channel subunits of the insect visual system and thoracic ganglion

Inhibition of pentagastrin‐stimulated and overnight gastric secretion by mianserin.

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