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Evidence for histamine H1 and H2 receptors in guinea-pig oxyntic cells.
J Pharmacol Exp Ther. 1983 Oct; 227(1):115-21.JP

Abstract

We have previously shown that histamine in the dose range of 1.0 X 10(-16) to 1.0 X 10(-14) M caused a linear increase in oxyntic cell carbonic anhydrase (CA) activity. A maximal dose of the H2 antagonist, cimetidine, reduced the action of histamine by only 74 +/- 7.8% suggesting a possible H1 component of histamine action on oxyntic cells. Using quantitative cytochemistry of CA activity in guinea-pig oxyntic cells, we compared the dose-response relationships (1.0 X 10(-17)-1.0 X 10(-9) M) of specific H2 (dimaprit, 4-methylhistamine, impromidine) and H1 (2-pyridylethylamine) agonists with histamine (H1 and H2). In addition, we studied the effects of the specific H2 antagonist, cimetidine, and H1 antagonist, mepyramine, on histamine, dimaprit and 2-pyridylethylamine-stimulated CA activity. We found that guinea-pig oxyntic cells respond to both H1 and H2 agonists. H1 agonists were more potent but less efficacious than H2 agonists. H2 agonists were more efficacious, but less potent than H1 agonists. Cimetidine (10(-10)-10(-8) M) was a competitive antagonist of dimaprit-stimulated CA activity. However, at higher doses (10(-5) M), cimetidine antagonism of histamine-stimulated CA activity was of a mixed noncompetitive and competitive type. Cimetidine and mepyramine exhibited both H2 and H1 antagonism, but their affinities for their respective agonists were greater. The data suggests that the oxyntic cell has receptors for both H1 and H2 agonists. H1 agonism is important at low concentrations of agonists. The H1 and H2 receptor components appear to be functionally linked.

Authors

No affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't
Research Support, U.S. Gov't, P.H.S.

Language

eng

PubMed ID

6137553

Citation

Vinik, A I., et al. "Evidence for Histamine H1 and H2 Receptors in Guinea-pig Oxyntic Cells." The Journal of Pharmacology and Experimental Therapeutics, vol. 227, no. 1, 1983, pp. 115-21.
Vinik AI, Heldsinger AA, Skoglund ML. Evidence for histamine H1 and H2 receptors in guinea-pig oxyntic cells. J Pharmacol Exp Ther. 1983;227(1):115-21.
Vinik, A. I., Heldsinger, A. A., & Skoglund, M. L. (1983). Evidence for histamine H1 and H2 receptors in guinea-pig oxyntic cells. The Journal of Pharmacology and Experimental Therapeutics, 227(1), 115-21.
Vinik AI, Heldsinger AA, Skoglund ML. Evidence for Histamine H1 and H2 Receptors in Guinea-pig Oxyntic Cells. J Pharmacol Exp Ther. 1983;227(1):115-21. PubMed PMID: 6137553.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Evidence for histamine H1 and H2 receptors in guinea-pig oxyntic cells. AU - Vinik,A I, AU - Heldsinger,A A, AU - Skoglund,M L, PY - 1983/10/1/pubmed PY - 1983/10/1/medline PY - 1983/10/1/entrez SP - 115 EP - 21 JF - The Journal of pharmacology and experimental therapeutics JO - J. Pharmacol. Exp. Ther. VL - 227 IS - 1 N2 - We have previously shown that histamine in the dose range of 1.0 X 10(-16) to 1.0 X 10(-14) M caused a linear increase in oxyntic cell carbonic anhydrase (CA) activity. A maximal dose of the H2 antagonist, cimetidine, reduced the action of histamine by only 74 +/- 7.8% suggesting a possible H1 component of histamine action on oxyntic cells. Using quantitative cytochemistry of CA activity in guinea-pig oxyntic cells, we compared the dose-response relationships (1.0 X 10(-17)-1.0 X 10(-9) M) of specific H2 (dimaprit, 4-methylhistamine, impromidine) and H1 (2-pyridylethylamine) agonists with histamine (H1 and H2). In addition, we studied the effects of the specific H2 antagonist, cimetidine, and H1 antagonist, mepyramine, on histamine, dimaprit and 2-pyridylethylamine-stimulated CA activity. We found that guinea-pig oxyntic cells respond to both H1 and H2 agonists. H1 agonists were more potent but less efficacious than H2 agonists. H2 agonists were more efficacious, but less potent than H1 agonists. Cimetidine (10(-10)-10(-8) M) was a competitive antagonist of dimaprit-stimulated CA activity. However, at higher doses (10(-5) M), cimetidine antagonism of histamine-stimulated CA activity was of a mixed noncompetitive and competitive type. Cimetidine and mepyramine exhibited both H2 and H1 antagonism, but their affinities for their respective agonists were greater. The data suggests that the oxyntic cell has receptors for both H1 and H2 agonists. H1 agonism is important at low concentrations of agonists. The H1 and H2 receptor components appear to be functionally linked. SN - 0022-3565 UR - https://www.unboundmedicine.com/medline/citation/6137553/Evidence_for_histamine_H1_and_H2_receptors_in_guinea_pig_oxyntic_cells_ L2 - http://jpet.aspetjournals.org/cgi/pmidlookup?view=long&pmid=6137553 DB - PRIME DP - Unbound Medicine ER -