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. 1989 Feb;27(2):139–145. doi: 10.1111/j.1365-2125.1989.tb05344.x

Pharmacological characterization of histamine receptors in the human temporal artery.

A Ottosson 1, I Jansen 1, L Edvinsson 1
PMCID: PMC1379773  PMID: 2523719

Abstract

1. The subtypes of histamine-receptors which mediate dilatation of small human temporal arteries have been characterized in vitro using 'selective' agonists and antagonists. 2. Dilatory responses were studied after preconstriction with prostaglandin F2 alpha since contraction was not seen at histamine concentrations up to 10(-4) M. Histamine caused a concentration-related relaxation of cerebral vessels with an IC50 value of 2.8 +/- 0.6 X 10(-7) M. 3. Cimetidine caused a parallel shift to the right of the histamine concentration-response curve whereas mepyramine was without observable effect. This suggests the presence of histamine H2-receptors only. However, combined treatment with mepyramine and cimetidine caused a more marked displacement of the concentration-response curve to the right. Schild analysis indicated that in situations of near complete blockade of the histamine H1-receptor subtypes, simple competitive antagonism at H2-receptors can be revealed with a pA2 value of 6.58 for cimetidine. The apparent pA2 value for mepyramine was 8.58. 4. The 'selective' H1-receptor agonists pyridylethylamine, 2-methylhistamine and thiazolylethylamine, and the H2-receptor agonists dimaprit, impromidine and 4-methylhistamine all mimicked the histamine response, but all except impromidine were less potent than histamine. The order of potency was impromidine greater than thiazolylamine greater than 4-Me-histamine greater than 2-Me-histamine greater than dimaprit greater than pyridylethylamine greater than tele-Me-histamine. 5. These results indicate that the histamine-induced dilatation in small human temporal arteries is mediated by both H1- and H2-receptors and that the latter subtype of histamine receptors predominates.

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Selected References

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  1. ARIENS E. J., SIMONIS A. M., VAN ROSSUM J. M. A theoretical basis of molecular pharmacology. III. Interaction of one or two compounds with two independent receptor systems. Arzneimittelforschung. 1956 Dec;6(12):737–746. [PubMed] [Google Scholar]
  2. Anthony M., Lance J. W. Histamine and serotonin in cluster headache. Arch Neurol. 1971 Sep;25(3):225–231. doi: 10.1001/archneur.1971.00490030051005. [DOI] [PubMed] [Google Scholar]
  3. Black J. W., Owen D. A., Parsons M. E. An analysis of the depressor responses to histamine in the cat and dog: involvement of both H1- and H2-receptors. Br J Pharmacol. 1975 Jul;54(3):319–324. doi: 10.1111/j.1476-5381.1975.tb07571.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  4. Duckworth J. W., Lance J. W., Lord G. D., Mylecharane E. J., Raper C. Histamine receptors in the cranial circulation of the monkey [proceedings]. Br J Pharmacol. 1976 Nov;58(3):444P–444P. [PMC free article] [PubMed] [Google Scholar]
  5. Edvinsson L., Owman C. A pharmacologic comparison of histamine receptors in isolated extracranial and intracranial arteries in vitro. Neurology. 1975 Mar;25(3):271–276. doi: 10.1212/wnl.25.3.271. [DOI] [PubMed] [Google Scholar]
  6. Ercan Z. S., Türker R. K. Histamine receptors in the vasculature of the rabbit ear. Naunyn Schmiedebergs Arch Pharmacol. 1975;291(1):23–29. doi: 10.1007/BF00510818. [DOI] [PubMed] [Google Scholar]
  7. FURUKAWA T. EFFECT OF HISTAMINE ON MICROCIRCULATION AND INFLUENCE OF DIPHENHYDRAMINE ON THAT. Jpn J Pharmacol. 1964 Dec;14:474–475. doi: 10.1254/jjp.14.474. [DOI] [PubMed] [Google Scholar]
  8. Flynn S. B., Owen D. A. Histamine receptors in peripheral vascular beds in the cat. Br J Pharmacol. 1975 Oct;55(2):181–188. doi: 10.1111/j.1476-5381.1975.tb07627.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  9. Gross P. M. Cerebral histamine: indications for neuronal and vascular regulation. J Cereb Blood Flow Metab. 1982;2(1):3–23. doi: 10.1038/jcbfm.1982.2. [DOI] [PubMed] [Google Scholar]
  10. Hardebo J. E., Krabbe A. A., Gjerris F. Enhanced dilatory response to histamine in large extracranial vessels in chronic cluster headache. Headache. 1980 Nov;20(6):316–320. doi: 10.1111/j.1526-4610.1980.hed2006316.x. [DOI] [PubMed] [Google Scholar]
  11. Högestätt E. D., Andersson K. E., Edvinsson L. Mechanical properties of rat cerebral arteries as studied by a sensitive device for recording of mechanical activity in isolated small blood vessels. Acta Physiol Scand. 1983 Jan;117(1):49–61. doi: 10.1111/j.1748-1716.1983.tb07178.x. [DOI] [PubMed] [Google Scholar]
  12. Medina J. L., Diamond S., Fareed J. The nature of cluster headache. Headache. 1979 Sep;19(6):309–322. doi: 10.1111/j.1526-4610.1979.hed1906309.x. [DOI] [PubMed] [Google Scholar]
  13. Ottosson A., Jansen I., Edvinsson L. Characterization of histamine receptors in isolated human cerebral arteries. Br J Pharmacol. 1988 Jul;94(3):901–907. doi: 10.1111/j.1476-5381.1988.tb11602.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  14. Owen D. A., Harvey C. A., Gristwood R. W. Cardiovascular studies with impromidine (SK&F 92676), a new very potent and specific histamine H2-receptor agonist. J Pharm Pharmacol. 1979 Sep;31(9):577–582. doi: 10.1111/j.2042-7158.1979.tb13595.x. [DOI] [PubMed] [Google Scholar]
  15. Owen D. A. Histamine receptors in the cardiovascular. Gen Pharmacol. 1977;8(3):141–156. doi: 10.1016/0306-3623(77)90043-x. [DOI] [PubMed] [Google Scholar]
  16. Russell D. Cluster headache: trial of a combined histamine H1 and H2 antagonist treatment. J Neurol Neurosurg Psychiatry. 1979 Jul;42(7):668–669. doi: 10.1136/jnnp.42.7.668. [DOI] [PMC free article] [PubMed] [Google Scholar]
  17. Saxena P. R. The significance of histamine H1 and H2 receptors on the carotid vascular bed in the dog. Neurology. 1975 Jul;25(7):681–687. doi: 10.1212/wnl.25.7.681. [DOI] [PubMed] [Google Scholar]
  18. Sjaastad O., Sjaastad O. V. The histaminuria in vascular headache. Acta Neurol Scand. 1970;46(3):331–342. doi: 10.1111/j.1600-0404.1970.tb05797.x. [DOI] [PubMed] [Google Scholar]
  19. Wahl M., Kuschinsky W. The dilating effect of histamine on pial arteries of cats and its mediation by H2 receptors. Circ Res. 1979 Feb;44(2):161–165. doi: 10.1161/01.res.44.2.161. [DOI] [PubMed] [Google Scholar]

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