Characterization and tissue distribution of H3 histamine receptors in guinea pigs by Nα-methylhistamine

Korte, Alexandra; Myers, Joyce; Shih, Neng‐Yang; Egan, Robert W.; Clark, Mike A.

doi:10.1016/0006-291x(90)91125-c

Cited by 92 publications

(38 citation statements)

References 12 publications

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“…Specific binding was defined as the radioactivity bound after subtraction of nonspecific binding, determined in the presence of 10 Table 1.…”

Section: Bindings Of [3hjsmt and [3hj(r)amhmentioning

confidence: 99%

“…The tritium-labeled agonists [3H]Na-methylhistamine (10,11) and [3H](R)aMH (12) Measurement of histamine content of mouse brain ICR mice were injected intraperitoneally with S-methyl thioperamide dihydrochloride (10 and 20 mg/kg) and thioperamide maleate (20 mg/kg) 1 hr before sacrifice. Their brains were homogenized in 5 10 volumes of 3 % perchloric acid containing 5 mM EDTA-2 Na in a Poly tron, and the homogenate was centrifuged at 12,000 x g for 20 min.…”

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confidence: 99%

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Binding Characteristics of a Histamine H3-Receptor Antagonist, (3H)S-Methylthioperamide: Comparison with (3H)(R).ALPHA.-Methylhistamine Binding to Rat Tissues.

et al. 1994

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“…Specific binding was defined as the radioactivity bound after subtraction of nonspecific binding, determined in the presence of 10 Table 1.…”

Section: Bindings Of [3hjsmt and [3hj(r)amhmentioning

confidence: 99%

mentioning

confidence: 99%

Binding Characteristics of a Histamine H3-Receptor Antagonist, (3H)S-Methylthioperamide: Comparison with (3H)(R).ALPHA.-Methylhistamine Binding to Rat Tissues.

et al. 1994

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“…Radioligand binding studies with the high affinity H3-agonists [3H]-R-methylhistamine (Arrang et al, 1990; Kilpatrick & Michel, 1991) and [3H]-Na-methylhistamine (West et al, 1990;Korte et al, 1990) have successfully identified binding sites with the characteristics of H3-receptors in both rat and guinea-pig tissues. The binding of 3H-agonists to these sites has been shown to be regulated by guanine nucleotides (implying a G-protein linkage) and several cations (Arrang et al, 1987a;1990;Zweig et al, 1992).…”

Section: Introductionmentioning

confidence: 99%

Differential effect of sodium ions and guanine nucleotides on the binding of thioperamide and clobenpropit to histamine H₃‐receptors in rat cerebral cortical membranes

Clark

Hill

1995

British J Pharmacology

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1 Conflicting reports in the literature over heterogeneity (West et al., 1990) or homogeneity (Arrang et al., 1990) of histamine H3-receptor binding sites may be attributed to the use of different incubation conditions. In the present study we have investigated the extent to which the binding of H3-receptor ligands to rat cerebral cortical membranes can be modified by both sodium ions and guanine nucleotides. 2 The H3-selective antagonist, thioperamide, discriminated between two specific binding sites for[3H]-Nm-methylhistamine (IC5o I = 2.75 ± 0.87 nM, IC50 2 = 101.6 ± 12.0 nM, % site 1 = 24 ± 2%) in 50 mM Tris HCI buffer, but showed homogeneity of binding in 50 mM Na/K phosphate buffer. 3 Sodium ions markedly altered the binding characteristics of thioperamide (i.e. heterogeneity was lost and IC50 value shifted towards the high affinity site). The competition curves for a second H3-antagonist, clobenpropit and the H3-agonist N-methylhistamine however, were unaltered in the presence of sodium ions. 4 Guanylnucleotides displaced only 60% of specific [3H]-N-methylhistamine binding and modulated thioperamide binding in the same way as sodium ions. 5 These data suggest that the H3-receptor can exist in different conformations for which thioperamide, but not N-methylhistamine and clobenpropit, show differential affinity. 6 The potential nature of these sites, and the implications of this apparent receptor heterogeneity for H3-receptor antagonism by thioperamide, are discussed.

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“…Histamine H3-receptors are involved in the feedback control of histamine synthesis and release in histaminergic pathways in the central nervous system in animals and humans (1,(16)(17)(18). H3-receptors have also been identifed in peripheral tissues including the small intestine (13,15,17). We previously demonstrated that intraperitoneal injection of H3-receptor antagonist (thioperamide) increased histamine output into the mesenteric lymph, indicating that synthesis and release of histamine in the rat small intestine increased following engagement of histamine H3-receptors (22).…”

Section: Discussionmentioning

confidence: 99%

Histaminergic Control of Mucosal Repair in the Small Intestine

Fujimoto¹,

Gotoh²,

Ogata³

et al. 1995

Obesity Research

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ICHI OGATA, SEIJI TSUNADA, TAKASHI OHYAMA, AKIFUMI OOTANI, KAZUYO OKAMOTO AND TOSHIIE SAKATA. Histaminergic control of mucosal repair in the small intestine. Obes Res. 1995;3(Suppl5):795S-799S. The aim of the present paper was to summarize histamine-mediated repair of rat intestinal mucosa. To evaluate intestinal repair, we examined lipid transport (an index of intestinal mucosal function) after 15 minutes occlusion of the superior mesenteric artery. Rats were pretreated with a-fluoromethylhistidine (a suicide inhibitor of histidine decarboxylase, a synthesizing enzyme of histamine), HI-receptor antagonist (chlorpheniramine maleate), H2-antagonist (cimetidine), or H3-antagonist (thioperamide) before ischemia-reperfusion (VR). Lipid transport to rat mesenteric lymph decreased significantly 24 hours after YR in all groups tested compared to sham-treated rats. Lipid transport was restored 48 hours after VR in the vehicle-pretreated control group. Lipid transport was not restored to the control level 48 hours after VR in rats pretreated with HI-antagonist and a suicide inhibitor of histidine decarboxylase. In contrast, intestinal function was restored to the control level 48 hours after UR in rats pretreated with H2-and H3-antagonists. These results support our previous findings that newly formed histamine after I/R plays an important role in mucosal recovery through HI-receptors. FUJIMOTO, KAZUMA, YUDAI GOTOH, SHIN-

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Characterization and tissue distribution of H3 histamine receptors in guinea pigs by Nα-methylhistamine

Cited by 92 publications

References 12 publications

Binding Characteristics of a Histamine H3-Receptor Antagonist, (3H)S-Methylthioperamide: Comparison with (3H)(R).ALPHA.-Methylhistamine Binding to Rat Tissues.

Binding Characteristics of a Histamine H3-Receptor Antagonist, (3H)S-Methylthioperamide: Comparison with (3H)(R).ALPHA.-Methylhistamine Binding to Rat Tissues.

Differential effect of sodium ions and guanine nucleotides on the binding of thioperamide and clobenpropit to histamine H₃‐receptors in rat cerebral cortical membranes

Histaminergic Control of Mucosal Repair in the Small Intestine

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Characterization and tissue distribution of H3 histamine receptors in guinea pigs by Nα-methylhistamine

Cited by 92 publications

References 12 publications

Binding Characteristics of a Histamine H3-Receptor Antagonist, (3H)S-Methylthioperamide: Comparison with (3H)(R).ALPHA.-Methylhistamine Binding to Rat Tissues.

Binding Characteristics of a Histamine H3-Receptor Antagonist, (3H)S-Methylthioperamide: Comparison with (3H)(R).ALPHA.-Methylhistamine Binding to Rat Tissues.

Differential effect of sodium ions and guanine nucleotides on the binding of thioperamide and clobenpropit to histamine H3‐receptors in rat cerebral cortical membranes

Histaminergic Control of Mucosal Repair in the Small Intestine

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Differential effect of sodium ions and guanine nucleotides on the binding of thioperamide and clobenpropit to histamine H₃‐receptors in rat cerebral cortical membranes