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Bioorg Med Chem Lett. 2001 Apr 9;11(7):951-4.

Different antagonist binding properties of human and rat histamine H3 receptors.

Author information

1
Freie Universität Berlin, Institut für Pharmazie, Berlin, Germany. h.stark@pharmchem.uni-frankfurt.de

Abstract

Different histamine H3-receptor antagonists have been tested in displacement studies at human and rat H3 receptors in stably transfected cells. Based on an actual rhodopsin structure, models for receptor antagonist interaction were developed for receptors of both species. Similarities and discrepancies in binding profiles can be explained, but not quantified by hydrophilic interactions with Asp114 and an important lipophilic binding pocket modified by two nearby amino acids.

PMID:
11294398
DOI:
10.1016/s0960-894x(01)00090-7
[Indexed for MEDLINE]

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