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Interactions of Histamine H1-Receptor Agonists and Antagonists with the Human Histamine H4-Receptor
Molecular Pharmacology, 2009The human histamine H(4)-receptor (hH(4)R) possesses high constitutive activity and, like the human H(1)-receptor (hH(1)R), is involved in the pathogenesis of type-I allergic reactions. The study aims were to explore the value of dual H(1)/H(4)R antagonists as antiallergy drugs and to address the question of whether H(1)R ligands bind to hH(4)R.
Karl-Friedrich, Deml +4 more
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Chemistry of Anti-H1 Histamine Antagonists
1978In this Chapter a survey and discussion of the chemistry of compounds which antagonize the effects of histamine at H1 receptors are presented. Ellis (1969) has compiled an extensive list of reviews on histamine, 5-hydroxytryptamine, and their antagonists, several of which include some account of the chemical aspects of antihistaminics.
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Inhibition by Cations of Antagonist Binding to Histamine H1-Receptors
1991The binding of the quaternary radioligand [3H] QMDP to the histamine H1-receptor was inhibited by a series of mono- and di-valent cations. The order of potency was Hg2+ greater than Cd2+ greater than Zn2+ greater than Ni2+ greater than Co2+ greater than Mn2+ greater than Ca2+ greater than Mg2+ greater than Li+ = Na+ greater than K+ greater than Cs ...
J M, Treherne +3 more
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In silico binding characteristics between human histamine H1 receptor and antagonists
Journal of Molecular Modeling, 2010It is widely acknowledged that the H(1) receptor antagonists have important therapeutic significance in the treatment of various allergic disorders, but little was known about the binding mode between the receptor and antagonists since the crystal structure of G-protein coupling receptors (GPCRs) were hard to obtain.
Xiaojian, Wang +4 more
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Pharmacological properties of α-mangostin, a novel histamine H1 receptor antagonist
European Journal of Pharmacology, 1996In the isolated rabbit thoracic aorta and guinea-pig trachea, alpha-mangostin inhibited histamine-induced contractions in a concentration-dependent manner in the presence or absence of cimetidine, a histamine H2 receptor antagonist. But KCl-, phenylephrine- or carbachol-induced contractions were not affected by alpha-mangostin.
N, Chairungsrilerd +4 more
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Antagonists of H1 Receptors of Histamine: Recent Developments
1991In the previous handbook of this series on this topic (Casy 1978), attention was drawn to the fact that most compounds known at that time which effectively antagonized histamine at H1-receptor sites could be described by the general structure (1) Open image in new window (1)
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Histamine and histamine H1- and H2-receptor antagonists in acute inflammation
Biochemical Society Transactions, 1980D A, Owen, D F, Woodward
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