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The binding of doxepin to histamine H1-receptors in guinea-pig and rat brain.

The binding of doxepin to histamine H1-receptors in guinea-pig and rat brain.
The binding of doxepin to histamine H1-receptors in guinea-pig and rat brain.
The affinity constant for doxepin obtained from inhibition of histamine-induced contraction of guinea-pig intestinal smooth muscle at 30 degrees C was 2.6 +/- 0.18 X 10(10)M-1. The slope of a Schild plot was not significantly different from unity. The affinity constant of doxepin did not vary markedly with temperature. At 37 degrees C it was 3.75 +/- 0.02 X 10(10)M-1 and at 25 degrees C 2.1 X 10(10)M-1. Doxepin was a competitive inhibitor of [3H]-mepyramine binding to guinea-pig cerebellar homogenates. The affinity constant derived for doxepin at 30 degrees C was 1.12 +/- 0.45 X 10(10)M-1. Hill coefficients for curves of doxepin or mepyramine inhibition of [3H]-mepyramine binding in guinea-pig cerebellum, cerebral cortex and hippocampus did not differ significantly from unity. The mean affinity of mepyramine for histamine H1-receptors in rat brain homogenates at 30 degrees C was 3.5 X 10(8)M-1. Hill coefficients for curves of doxepin or mepyramine inhibition of [3H]-mepyramine binding to homogenates of rat cerebral cortex or rat whole brain were near unity. These studies provide no evidence that doxepin binds preferentially to a sub-class of histamine H1-receptors in rat brain.
0007-1188
417-424
Aceves, J.
cb447635-f096-4630-b035-94b4894cd24a
Mariscal, S.
d9419114-b35d-4cf8-b355-872f70499a9a
Morrison, K.E.
f00890f0-2fde-4dbd-a73b-7422e1b0ede8
Young, J.M.
25eaef55-a189-4a05-85a5-ab73f7dca1ec
Aceves, J.
cb447635-f096-4630-b035-94b4894cd24a
Mariscal, S.
d9419114-b35d-4cf8-b355-872f70499a9a
Morrison, K.E.
f00890f0-2fde-4dbd-a73b-7422e1b0ede8
Young, J.M.
25eaef55-a189-4a05-85a5-ab73f7dca1ec

Aceves, J., Mariscal, S., Morrison, K.E. and Young, J.M. (1985) The binding of doxepin to histamine H1-receptors in guinea-pig and rat brain. British Journal of Pharmacology, 84 (2), 417-424. (doi:10.1111/j.1476-5381.1985.tb12925.x). (PMID:3978317)

Record type: Article

Abstract

The affinity constant for doxepin obtained from inhibition of histamine-induced contraction of guinea-pig intestinal smooth muscle at 30 degrees C was 2.6 +/- 0.18 X 10(10)M-1. The slope of a Schild plot was not significantly different from unity. The affinity constant of doxepin did not vary markedly with temperature. At 37 degrees C it was 3.75 +/- 0.02 X 10(10)M-1 and at 25 degrees C 2.1 X 10(10)M-1. Doxepin was a competitive inhibitor of [3H]-mepyramine binding to guinea-pig cerebellar homogenates. The affinity constant derived for doxepin at 30 degrees C was 1.12 +/- 0.45 X 10(10)M-1. Hill coefficients for curves of doxepin or mepyramine inhibition of [3H]-mepyramine binding in guinea-pig cerebellum, cerebral cortex and hippocampus did not differ significantly from unity. The mean affinity of mepyramine for histamine H1-receptors in rat brain homogenates at 30 degrees C was 3.5 X 10(8)M-1. Hill coefficients for curves of doxepin or mepyramine inhibition of [3H]-mepyramine binding to homogenates of rat cerebral cortex or rat whole brain were near unity. These studies provide no evidence that doxepin binds preferentially to a sub-class of histamine H1-receptors in rat brain.

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Published date: February 1985
Organisations: Medical Education

Identifiers

Local EPrints ID: 399576
URI: https://eprints.soton.ac.uk/id/eprint/399576
ISSN: 0007-1188
PURE UUID: ca930d2d-af43-4f02-b09b-f57766d05a21
ORCID for K.E. Morrison: ORCID iD orcid.org/0000-0003-0216-5717

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Date deposited: 18 Aug 2016 14:04
Last modified: 06 Jun 2018 12:19

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