Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
. 1990 Nov;101(3):587-90.
doi: 10.1111/j.1476-5381.1990.tb14125.x.

Alterations in histamine receptors of guinea-pig ileal smooth muscle produced during agonist-induced desensitization

Affiliations

Alterations in histamine receptors of guinea-pig ileal smooth muscle produced during agonist-induced desensitization

S Horio et al. Br J Pharmacol. 1990 Nov.

Abstract

1. The effects of prolonged treatment with histamine (10(-4) M, 30 min) on desensitization at histamine H1-receptors of guinea-pig ileal longitudinal muscle were investigated. 2. This treatment did not change either the maximum amount or dissociation constant (Kd) of [3H]-mepyramine binding to membranes of guinea-pig ileal muscle. 3. In contrast, this treatment shifted the histamine inhibition curves of [3H]-mepyramine binding to the right both in the presence and absence of 0.5 mM guanosine-5'-triphosphate (GTP). This rightward shift of the curves occurred rapidly in the first 10 min of exposure to histamine. 4. The histamine inhibition curves were analyzed with a two binding sites model. It was shown that the histamine-induced affinity change of the receptor for the agonist occurred with the high affinity binding component (which comprise about 80% of the total), whereas no significant change occurred with the low affinity component. The GTP-dependent decrease in the affinity of the receptor for the agonist also occurred with the high affinity component both in control and histamine-treated preparations. 5. These studies suggest that histamine-induced desensitization was caused by alteration in the affinity of the receptor for the agonist rather than reduction in the number of the receptors and that the interaction of the receptor with a guanine nucleotide regulatory protein was retained in the desensitized state.

PubMed Disclaimer

Similar articles

Cited by

References

    1. J Pharmacol Exp Ther. 1973 Feb;184(2):494-505 - PubMed
    1. Br J Pharmacol Chemother. 1964 Apr;22:356-65 - PubMed
    1. J Neurochem. 1980 Apr;34(4):916-22 - PubMed
    1. Mol Pharmacol. 1980 May;17(3):309-13 - PubMed
    1. J Biol Chem. 1980 Oct 25;255(20):9571-9 - PubMed

Publication types

LinkOut - more resources