The Binding of [3H]-tiotidine to Homogenates of Guinea-pig Lung Parenchyma

Overview

Journal Br J Pharmacol

Publisher Wiley

Specialty Pharmacology

Date 1985 Oct 1

PMID 2864974

Citations 6

Authors

J C Foreman

D B Norris

T J Rising

S E Webber

Affiliations

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Abstract

By use of a rapid filtration assay, the binding of [3H]-tiotidine to homogenates of guinea-pig lung parenchyma was found to be saturable and of a high affinity. Mean values for the KD and Bmax were calculated as 8.5 +/- 1.5 nM and 28 +/- 5 fmol mg-1 protein respectively. The association and dissociation rate constants for [3H]-tiotidine binding at 4 degrees C were calculated to be 0.81 +/- 0.06 microM min-1 and 0.063 +/- 0.005 min-1 respectively, yielding a kinetically derived KD of 7.8 nM. A wide range of H2-receptor agonist and antagonists displaced [3H]-tiotidine binding from lung parenchyma homogenates in a biphasic manner. Examination of the first phase of the displacement of [3H]-tiotidine yielded Ki values for the antagonists tested similar to those found in other binding studies using this ligand and similar to KB values calculated for the antagonists in pharmacological studies.

Citing Articles

3H-tiotidine binding to guinea-pig cortical and striatal membranes.

Smith I, Leigh B, Mylek M Agents Actions. 1986; 19(3-4):169-73.

PMID: 3825739 DOI: 10.1007/BF01966202.

A study of the histamine H2-receptor mediating relaxation of the parenchymal lung strip preparation of the guinea-pig.

Foreman J, Rising T, Webber S Br J Pharmacol. 1985; 86(2):465-73.

PMID: 2932195 PMC: 1916698. DOI: 10.1111/j.1476-5381.1985.tb08916.x.

A study of the H2-receptor for histamine stimulating adenylate cyclase in homogenates of guinea-pig lung parenchyma.

Foreman J, Norris D, Rising T, Webber S Br J Pharmacol. 1986; 87(1):37-44.

PMID: 2869813 PMC: 1916899. DOI: 10.1111/j.1476-5381.1986.tb10154.x.

Responses to histamine and selective H2-receptor agonists in lung parenchymal strips from normal and sensitized guinea-pigs.

Cortijo J, Sanz C, Perpina M, Ortiz J, Oron J, ESPLUGUES J Agents Actions. 1989; 28(1-2):45-52.

PMID: 2571243 DOI: 10.1007/BF02022979.

Airway receptors.

Barnes P Postgrad Med J. 1989; 65(766):532-42.

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