Molecular cloning of a gene encoding the histamine H2 receptor

Journal Article · Mon Jan 14 23:00:00 EST 1991 · Proceedings of the National Academy of Sciences of the United States of America; (United States)

DOI:https://doi.org/10.1073/pnas.88.2.429· OSTI ID:5016568

Gantz, I; Schaeffer, M; DelValle, J; Logsdon, C; Campbell, V; Uhler, M; Yamada, Tadataka ^[1]

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1. Univ. of Michigan Medical Center, Ann Arbor (United States)

The H2 subclass of histamine receptors mediates gastric acid secretion, and antagonists for this receptor have proven to be effective therapy for acid peptic disorders of the gastrointestinal tract. The physiological action of histamine has been shown to be mediated via a guanine nucleotide-binding protein linked to adenylate cyclase activation and cellular cAMP generation. The authors capitalized on the technique of polymerase chain reaction, using degenerate oligonucleotide primers based on the known homology between cellular receptors linked to guanine nucleotide-binding proteins to obtain a partial-length clone from canine gastric parietal cell cDNA. This clone was used to obtain a full-length receptor gene from a canine genomic library. Histamine increased in a dose-dependent manner cellular cAMP content in L cells permanently transfected with this gene, and preincubation of the cells with the H2-selective antagonist cimetidine shifted the dose-response curve to the right. Cimetidine inhibited the binding of the radiolabeled H2 receptor-selective ligand (methyl-{sup 3}H)tiotidine to the transfected cells in a dose-dependent fashion, but the H1-selective antagonist diphenhydramine did not. These data indicate that they have cloned a gene that encodes the H2 subclass of histamine receptors.

• OSTI ID: 5016568
• Journal Information: Proceedings of the National Academy of Sciences of the United States of America; (United States), Journal Name: Proceedings of the National Academy of Sciences of the United States of America; (United States) Vol. 88:2; ISSN 0027-8424; ISSN PNASA
• Country of Publication: United States
• Language: English

Related Subjects

550201* -- Biochemistry-- Tracer Techniques
59 BASIC BIOLOGICAL SCIENCES
AMINES
AMINO ACID SEQUENCE
AZOLES
BIOLOGICAL MATERIALS
BODY FLUIDS
CLONING
DNA HYBRIDIZATION
DNA SEQUENCING
DNA-CLONING
DOSE-RESPONSE RELATIONSHIPS
GASTRIC ACID
GENES
HETEROCYCLIC COMPOUNDS
HISTAMINE
HYBRIDIZATION
HYDROGEN COMPOUNDS
IMIDAZOLES
MATERIALS
MEMBRANE PROTEINS
MOLECULAR STRUCTURE
NUCLEIC ACIDS
OLIGONUCLEOTIDES
ORGANIC COMPOUNDS
ORGANIC NITROGEN COMPOUNDS
PROTEINS
RECEPTORS
STRUCTURAL CHEMICAL ANALYSIS
TRITIUM COMPOUNDS