Characteristics of the antihistamine effect of TAK-427, a novel imidazopyridazine derivative

Fukuda, Shoko; Midoro, Katsuo; Yamasaki, Masashi; Gyoten, Michiyo; Kawano, Yukio; Fukui, Hirokazu; Ashida, Yuzuru; Nagaya, Hideaki

doi:10.1007/s000110300073

Cited by 10 publications

(3 citation statements)

References 10 publications

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“…Woodward et al [17] in the same year also demonstrated that a conjunctival itch-scratch response (ISR) was produced by topical instillation of various pruritogenic agents in guinea pigs. It is currently accepted that these models will permit convenient, systematic characterization of the pharmacology of itch; additionally, antipruritic effects of various drugs were examined utilizing these models [18][19][20] .…”

Section: Introductionmentioning

confidence: 99%

Itch-Scratch Responses Induced by Lysophosphatidic Acid in Mice

Hashimoto¹,

Ohata²,

Momose³

2004

Pharmacology

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The present investigation was conducted in order to determine whether lysophosphatidic acid (LPA) induces itch-scratch responses (ISRs) in mice. Intradermal administration of LPA induces ISRs; furthermore, the time course for LPA-induced ISRs was similar to that for histamine-induced responses. Comparative study of the pruritogenic activity revealed that histamine possessed a potent effect characterized by a dose-response relationship; however, prostaglandin D₂ failed to induce this response. Pretreatment with ketotifen, a histamine H₁ receptor antagonist, and capsaicin inhibited LPA-induced ISRs. Additionally, LPA-induced ISRs were abolished by Y-27632, an inhibitor of Rho-associated protein kinase (ROCK). These findings suggest that LPA-induced ISRs are attributable to histamine- and substance-P-mediated pathways. Moreover, the Rho/ROCK-mediated pathway may be involved.

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Section: Introductionmentioning

confidence: 99%

Itch-Scratch Responses Induced by Lysophosphatidic Acid in Mice

Hashimoto¹,

Ohata²,

Momose³

2004

Pharmacology

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“…45 In the following year, the same research group reported the antihistamine effect of the new imidazopyridazine derivative 46 to treat allergic disorders. 46,47 The in vitro binding prole of 46 against recombinant human histamine H 1 receptors (rhH 1 R) demonstrated that it inhibited ligand binding to rhH 1 R with an IC 50 value of 17.3 nM. Compound 46 displayed increased selectivity toward peripheral H 1 receptors similar to that of the control and also subdued histamine-induced skin reactions in guinea pigs and mice.…”

Section: Imidazopyridazines As Other Pharmacological Agentsmentioning

confidence: 99%

Exploring the untapped pharmacological potential of imidazopyridazines

Malik,

Alshareef,

Alfaidi

et al. 2024

RSC Adv.

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“…While all the typical antihistamines listed in Table 2 are inverse agonists [ 35 ], neutral antagonists have been synthesised and characterised [ 208 , 209 ]. For instance, mepyramine is an inverse agonist.…”

Section: Agonists and Antagonistsmentioning

confidence: 99%

Function and Role of Histamine H1 Receptor in the Mammalian Heart

et al. 2023

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Histamine can change the force of cardiac contraction and alter the beating rate in mammals, including humans. However, striking species and regional differences have been observed. Depending on the species and the cardiac region (atrium versus ventricle) studied, the contractile, chronotropic, dromotropic, and bathmotropic effects of histamine vary. Histamine is present and is produced in the mammalian heart. Thus, histamine may exert autocrine or paracrine effects in the mammalian heart. Histamine uses at least four heptahelical receptors: H1, H2, H3 and H4. Depending on the species and region studied, cardiomyocytes express only histamine H1 or only histamine H2 receptors or both. These receptors are not necessarily functional concerning contractility. We have considerable knowledge of the cardiac expression and function of histamine H2 receptors. In contrast, we have a poor understanding of the cardiac role of the histamine H1 receptor. Therefore, we address the structure, signal transduction, and expressional regulation of the histamine H1 receptor with an eye on its cardiac role. We point out signal transduction and the role of the histamine H1 receptor in various animal species. This review aims to identify gaps in our knowledge of cardiac histamine H1 receptors. We highlight where the published research shows disagreements and requires a new approach. Moreover, we show that diseases alter the expression and functional effects of histamine H1 receptors in the heart. We found that antidepressive drugs and neuroleptic drugs might act as antagonists of cardiac histamine H1 receptors, and believe that histamine H1 receptors in the heart might be attractive targets for drug therapy. The authors believe that a better understanding of the role of histamine H1 receptors in the human heart might be clinically relevant for improving drug therapy.

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Characteristics of the antihistamine effect of TAK-427, a novel imidazopyridazine derivative

Abstract: These results suggest that TAK-427 may have a long-lasting antihistamine activity with minimum sedative side effect and suppress acute phase allergic reactions.

Cited by 10 publications

References 10 publications

Itch-Scratch Responses Induced by Lysophosphatidic Acid in Mice

Itch-Scratch Responses Induced by Lysophosphatidic Acid in Mice

Exploring the untapped pharmacological potential of imidazopyridazines

Function and Role of Histamine H1 Receptor in the Mammalian Heart

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