Histamine dependent cyclic AMP generating system in rabbit CNS: Interaction with neuroregulators and forskolin

Sek, B.; Sebastjanska, A.; Nowak, Jerzy Z.

doi:10.1007/bf02142551

Cited by 5 publications

(5 citation statements)

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“…Comparison of the HA action in the chick pineal, cerebral cortex, and retina revealed that the cyclic AMP-generating system of the pineal is much more sensitive to HA than these systems in the brain and retinal tissues (Nowak andSek, 1991, 1992;authors' unpublished data) . Like in guinea pig or rabbit brain (Daly, 1977 ;Daly et al ., 1982;Sek et al ., 1988 ;Nowak, 1993), the action of HA was strongly potentiated by forskolin, a direct activator of adenylyl cyclase (Seamon and Daly, 1986), suggesting a likely 134 3 receptor-type mode of action for HA. Furthermore, addition to the incubation medium of a phosphodiesterase inhibitor, IBMX, significantly increased the effect of HA, indicating that the HA action is related to the activation of cyclic AMP production rather than inhibition of the nucleotide breakdown .…”

Section: Discussionmentioning

confidence: 99%

“…(c) It may suggest that the pineal HA receptors do not represent an H2 -type receptor ; the latter possibility, however, is in contrast to guinea pig hippocampus, where cyclic AMP production is linked to the activation of H2 receptors, and dimaprit, as expected, was active in this tissue (present study ; Palacios et al ., 1978). However, it must be noted that dimaprit (in contrast to HA) has been reported to be ineffective in enhancing cyclic AMP accumulation in chick cerebral cortex (Brine et al, 1983) and, surprisingly, in the CNS of rabbits (Al-Gadi and Hill, 1985), a species whose brain, similar to guinea pig brain (see, e.g., Daly, 1977;Palacios et al, 1978 ;Nowak et al, 1983), is known to possess HA HZ receptors linked to the cyclic AMPgenerating system (Al-Gadi and Hill, 1985 ;Sek et al, 1987Sek et al, , 1988Hill, 1990) . Thus, dimaprit, owing to its inconsistent, and thus unclarified, mode of action in at least some tissues/species (see Al-Gadi and Hill, 1985; see also Van der Goot et al, 1991), does not seem to be the drug of choice (as a pharmacological tool) in studying HA HZ receptors in the CNS .…”

Section: Discussionmentioning

confidence: 99%

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Stimulatory Effect of Histamine on Cyclic AMP Formation in Chick Pineal Gland

Nowak

Sek

1994

Journal of Neurochemistry

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Histamine (HA) potently stimulated cyclic AMP accumulation in intact pineal glands taken from light‐exposed chicks. The action of HA was stronger in the presence of forskolin and the phosphodiesterase inhibitor 3‐isobutyl‐1‐methylxanthine (IBMX). The effect of HA was mimicked by HA H1‐ and H2‐receptor‐selective agonists in the following order of potency: HA > 4‐methylhistamine (H2) > 2‐methylhistamine (H1) > 2‐thiazolylethylamine (H1) ≫ dimaprit (H2). The HA H3‐receptor‐selective agonist (R)α‐methylhistamine was poorly active. The effect of HA was antagonized by selective H2‐receptor blockers (tiotidine > oxmetidine > cimetidine = ranitidine) and was not significantly affected by the selective H1‐ and H3‐receptor blockers mepyramine and thioperamide. A detailed analysis of an antagonistic action of ranitidine (versus HA) revealed a noncompetitive mode of action of the H2 blocker. The stimulatory action of the H1 agonist 2‐thiazolylethylamine (both under basal conditions and in the presence of forskolin or IBMX) was not significantly influenced by three H1‐receptor‐selective blockers (mepyramine, triprolidine, and diphenhydramine), but it was totally counteracted by ranitidine. Using accepted selective agonists and antagonists of the HA H1, H2, and H3 receptor we were unable to identify clearly the receptor subtype mediating the HA action on the cyclic AMP‐generating system of the chick pineal. It is suggested that the receptor under consideration may represent either an H2‐like (in terms of mammalian criteria) or avian‐specific HA receptor. The data suggest that HA may be considered a modulator of the pineal activity in chicks.

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Section: Discussionmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

Stimulatory Effect of Histamine on Cyclic AMP Formation in Chick Pineal Gland

Nowak

Sek

1994

Journal of Neurochemistry

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“…1995a,b). Although the ineffectiveness of dimaprit could be attributed to its possible lack of intrinsic activity in some CNS tissues (as previously demonstrated for the rabbit brain and avian pineal gland; Al‐Gadi and Hill 1985; Sek et al . 1988; Nowak and Sek 1994; Nowak et al .…”

Section: Discussionmentioning

confidence: 75%

“…As in the rodent brain and the avian pineal gland (Daly et al . 1982; Sek et al . 1988; Nowak 1993; Nowak and Sek 1994), the action of HA was strongly potentiated by forskolin, a direct activator of adenylyl cyclase (Seamon and Daly 1986), suggesting a likely receptor‐related mode of action for HA.…”

Section: Discussionmentioning

confidence: 99%

“…For example, dimaprit increased the nucleotide production in guinea pig hippocampal slices (Palacios et al . 1978; Nowak and Sek 1994) but had no action in rabbit cerebral cortical slices (despite the fact that the latter tissue possesses the H 2 receptor system positively linked to cAMP production) (Al‐Gadi and Hill 1985; Sek et al . 1988).…”

Section: Discussionmentioning

confidence: 99%

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Histamine H₂‐like receptors in chick cerebral cortex: effects on cyclic AMP synthesis and characterization by [³H]tiotidine binding

Zawilska

Woldan-Tambor

Nowak

2002

Journal of Neurochemistry

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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 [(3) H]tiotidine, a selective H(2) 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 microm) potently and concentration dependently stimulated cAMP production in [(3) H]adenine pre-labelled slices of chick cerebral cortex, displaying an EC(50) value (concentration that produces 50% of maximum response) of 2.65 microm. The effect of HA was mimicked by agonists of HA receptors with the following rank order of potency: HA >or= 4-methylHA (H(2)) >or= N alpha,N alpha-dimethylHA (H(3) >> H(2) = H(1)) >> 2-methylHA (H(1)) >> 2-thiazolylethylamine (H(1)) >or= R alpha-methylHA (H(3)) >> amthamine, dimaprit (H(2)), immepip (H(3), H(4)). The HA-evoked increase in cAMP production in chick cerebral cortex was antagonized by selective H(2) receptor blockers (aminopotentidine >or= tiotidine > ranitidine >> zolantidine), and not significantly affected by mepyramine and thioperamide, selective H(1) and H(3) /H(4) receptor blockers, respectively. A detailed analysis of the antagonistic action of aminopotentidine (vs. HA) revealed a non-competitive mode of action. The binding of [(3) H]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 (K (d)) = 4.42 nm] and high capacity [maximum number of binding sites (B (max) ) = 362 fmol/mg protein]. The relative rank order of HA-ergic drugs to inhibit [(3) H]tiotidine binding to chick cerebrum was: antagonists - tiotidine >> aminopotentidine = ranitidine >or= zolantadine >> thioperamide - triprolidine; agonists - HA >or= 4-methylHA >> 2-methylHA >or=R alpha-methylHA - dimaprit. In conclusion, chick cerebral cortex contains H(2) -like HA receptors that are linked to the cAMP-generating system and are labelled with [(3) H]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 H(2) -like HA receptors or a novel subtype of HA receptors.

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Histamine-mediated regulation of cAMP levels and inositol phosphate metabolism in isolated rabbit retina

1989

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In pieces of the rabbit retina, histamine (HI) had no significant effect on cAMP accumulation; however, HI inhibited forskolin-evoked accumulation of the nucleotide. Mepyramine (H1-antagonist) was without effect, while cimetidine (H2-antagonist) antagonized the HI action. Dimaprit (H2-agonist) mimicked the HI action, however its action was not significantly affected by H2-antagonists. Since phosphodiesterase (PDE) inhibitors prevented the HI action it is suggested that HI-induced inhibition of the forskolin effect results from HI-induced activation of cAMP breakdown. The muscarinic agonist carbachol, and to a lesser extent HI, both increased [3H]inositol incorporation and intensified accumulation of [3H]inositol phosphates in the rabbit retina.

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Histamine dependent cyclic AMP generating system in rabbit CNS: Interaction with neuroregulators and forskolin

Cited by 5 publications

References 6 publications

Stimulatory Effect of Histamine on Cyclic AMP Formation in Chick Pineal Gland

Stimulatory Effect of Histamine on Cyclic AMP Formation in Chick Pineal Gland

Histamine H₂‐like receptors in chick cerebral cortex: effects on cyclic AMP synthesis and characterization by [³H]tiotidine binding

Histamine-mediated regulation of cAMP levels and inositol phosphate metabolism in isolated rabbit retina

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Histamine dependent cyclic AMP generating system in rabbit CNS: Interaction with neuroregulators and forskolin

Cited by 5 publications

References 6 publications

Stimulatory Effect of Histamine on Cyclic AMP Formation in Chick Pineal Gland

Stimulatory Effect of Histamine on Cyclic AMP Formation in Chick Pineal Gland

Histamine H2‐like receptors in chick cerebral cortex: effects on cyclic AMP synthesis and characterization by [3H]tiotidine binding

Histamine-mediated regulation of cAMP levels and inositol phosphate metabolism in isolated rabbit retina

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Histamine H₂‐like receptors in chick cerebral cortex: effects on cyclic AMP synthesis and characterization by [³H]tiotidine binding