/sup 3/H-cimetidine and the H/sub 2/-receptor
The H/sub 2/-antagonist cimetidine is widely employed in biochemical and pharmacological studies of the H/sub 2/-receptor. These studies include the use of /sup 3/H-cimetidine in radioligand binding experiments. Confirming our previous finding as to the unsuitability of this ligand in these types of investigations, we now report data showing the lack of correlation between the displacement of specific /sup 3/H-cimetidine binding and histamine stimulated adenylate cyclase activity, and the displacement of specific binding by imidazoles devoid of H/sub 2/-receptor activity. Results are also presented which question the use of copper ions in /sup 3/H-cimetidine binding studies. Our conclusions are discussed in relation to the work carried out by a number of laboratories where /sup 3/H-cimetidine is reported to label the H/sub 2/-receptor. 30 references, 2 figures, 2 tables.
- Research Organization:
- Hoechst Pharmaceutical Research Laboratories, Milton Keynes, England
- OSTI ID:
- 6101232
- Journal Information:
- Life Sci.; (United States), Journal Name: Life Sci.; (United States) Vol. 33:12; ISSN LIFSA
- Country of Publication:
- United States
- Language:
- English
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59 BASIC BIOLOGICAL SCIENCES
AMINES
AZOLES
BIOCHEMISTRY
CARBONIC ACID DERIVATIVES
CHEMICAL BONDS
CHEMISTRY
COPPER
CYCLASES
DATA
ELEMENTS
ENZYME ACTIVITY
ENZYMES
EXPERIMENTAL DATA
GUANIDINES
HETEROCYCLIC COMPOUNDS
HISTAMINE
IMIDAZOLES
INFORMATION
INTERLABORATORY COMPARISONS
ISOTOPE APPLICATIONS
LABELLED COMPOUNDS
LIGANDS
LYASES
METALS
NUMERICAL DATA
ORGANIC COMPOUNDS
ORGANIC NITROGEN COMPOUNDS
PHARMACOLOGY
RADIOASSAY
RECEPTORS
TRACER TECHNIQUES
TRANSITION ELEMENTS
TRITIUM COMPOUNDS