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• W1554083932 abstract "In this study, histamine (HA) receptors in chick cerebral cortex were characterized using two approaches: (1) analysis of the effects of HA-ergic drugs on the cAMP-generating system, and (2) radioreceptor binding of [3H]tiotidine, a selective H2 antagonist. HA was a weak activator of adenylyl cyclase in a crude membrane preparation of chick cerebrum. On the other hand, HA (0.1–1000 μm) potently and concentration dependently stimulated cAMP production in [3H]adenine pre-labelled slices of chick cerebral cortex, displaying an EC50 value (concentration that produces 50% of maximum response) of 2.65 μm. The effect of HA was mimicked by agonists of HA receptors with the following rank order of potency: HA ≥ 4-methylHA (H2) ≥ Nα,Nα-dimethylHA (H3 ≫ H2 = H1) ≫ 2-methylHA (H1) ≫ 2-thiazolylethylamine (H1) ≥ Rα-methylHA (H3) ≫ amthamine, dimaprit (H2), immepip (H3, H4). The HA-evoked increase in cAMP production in chick cerebral cortex was antagonized by selective H2 receptor blockers (aminopotentidine ≥ tiotidine > ranitidine ≫ zolantidine), and not significantly affected by mepyramine and thioperamide, selective H1 and H3/H4 receptor blockers, respectively. A detailed analysis of the antagonistic action of aminopotentidine (vs. HA) revealed a non-competitive mode of action. The binding of [3H]tiotidine to chick cortical membranes was rapid, stable and reversible. Saturation analysis resulted in a linear Scatchard plot, suggesting binding to a single class of receptor binding site with high affinity [equilibrium dissociation constant (Kd) = 4.42 nm] and high capacity [maximum number of binding sites (Bmax) = 362 fmol/mg protein]. The relative rank order of HA-ergic drugs to inhibit [3H]tiotidine binding to chick cerebrum was: antagonists – tiotidine ≫ aminopotentidine = ranitidine ≥ zolantadine ≫ thioperamide ≈ triprolidine; agonists – HA ≥ 4-methylHA ≫ 2-methylHA ≥Rα-methylHA ≈ dimaprit. In conclusion, chick cerebral cortex contains H2-like HA receptors that are linked to the cAMP-generating system and are labelled with [3H]tiotidine. The pharmacological profile of these receptors is different from that described for their mammalian counterpart. It is suggested that the studied receptors represent either an avian-specific H2-like HA receptors or a novel subtype of HA receptors." @default.
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• W1554083932 date "2002-05-21" @default.
• W1554083932 modified "2023-09-27" @default.
• W1554083932 title "Histamine H2-like receptors in chick cerebral cortex: effects on cyclic AMP synthesis and characterization by [3H]tiotidine binding" @default.
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• W1554083932 doi "https://doi.org/10.1046/j.1471-4159.2002.00870.x" @default.
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