Biochemical Journal · 1985 · 20 citations · 14 references
MedicinePharmacologyBiochemical PharmacologyCell SignalingPharmacodynamicsCartilage MetabolismJoint DiseaseAdenylate Cyclase RegulationAdenylate Cyclase SignalingDose-response Curve AnalysisHistamine H2 Receptor AntagonismHistamine Receptor AntagonistsHistamine ReceptorsMast Cell InteractionsSynovial Fibroblasts
Histamine (1-100 microM) induced a concentration-dependent increase in intracellular cyclic AMP in monolayer cultures of human, canine and foetal-bovine articular chondrocytes. The dose-response curve for histamine in each culture was progressively displaced to the right with increasing concentrations of cimetidine, an H2-receptor antagonist. The histamine-induced cyclic AMP elevation in human articular chondrocytes was also significantly decreased by ranitidine, another H2 antagonist, but not by the H1 antagonists mepyramine and chlorpheniramine. These findings indicate that histamine activates chondrocyte adenylate cyclase through an H2 receptor. The cyclic AMP response of human chondrocytes to histamine was many times greater than that measured for synovial fibroblasts under similar conditions. Such findings suggest that mast-cell-chondrocyte interactions in vivo may contribute to changed chondrocyte metabolism in joint disease.
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Definition and Antagonism of Histamine H2-receptors
J. W. Black, W. A. M. Duncan, C. J. DURANT et al. · Nature · 1972 · 2.3K citations