The binding of [<sup>3</sup>H]‐tiotidine to homogenates of guinea‐pig lung parenchyma

Foreman, J. C.; Norris, David B.; Rising, Trevor J.; Webber, Stephanie

doi:10.1111/j.1476-5381.1985.tb08917.x

Cited by 35 publications

(13 citation statements)

References 22 publications

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“…In radioligand binding studies of H2-receptors, [3H]-tiotidine has been reported to be a valuable tool as a radiolabel (Gajtkowski et al, 1983 (Gajtkowski et al, 1983;Foreman et al, 1985). These results suggest that the specific [3H]-tiotidine binding in this study represents binding to H2-receptors, that is, H2-receptors are present in guinea-pig left atria.…”

Section: Drugsmentioning

confidence: 50%

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Identification and characterization of histamine H₁‐ and H₂‐receptors in guinea‐pig left atrial membranes by [³H]‐mepyramine and [³H]‐tiotidine binding

Hattori

Endou

Gando

et al. 1991

British J Pharmacology

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8 It is concluded that both Hj-and H2-receptors exist in guinea-pig left atria. H1-receptors probably couple to intracellular effector(s) through a guanine nucleotide-dependent transducing mechanism. On the other hand, H2-receptors seem unlikely to be linked to guanine nucleotide regulatory proteins in guineapig left atria, which may explain the failure of histamine to cause an increase in cyclic AMP in spite of the presence of H2-receptors.

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Section: Drugsmentioning

confidence: 50%

“…In contrast, unlabelled mepyramine inhibited [3H]-mepyramine binding with a monophasic displacement curve ( Figure 4) (0) (Gajtkowski et al, 1983) and guinea-pig lung parenchyma (Foreman et al, 1985). Scatchard analysis of the specific binding (Figure 5c) (Figure 6).…”

Section: Drugsmentioning

confidence: 98%

Identification and characterization of histamine H₁‐ and H₂‐receptors in guinea‐pig left atrial membranes by [³H]‐mepyramine and [³H]‐tiotidine binding

Hattori

Endou

Gando

et al. 1991

British J Pharmacology

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“…The specific binding for [3H]tiotidine accounted routinely for 20% or less in both species. The relatively large por tion of the nonspecific component for this ligand has been reported in previous studies on guinea pig cerebral cortex (25) and guinea pig lung parenchyma (26). The equilib rium dissociation constant (KD) and the maximal binding capacity (Borax) were calculated from plots according to the method of Scatchard (27).…”

Section: Adenylate Cyclase Assaymentioning

confidence: 99%

Histamine Receptors Mediating a Positive Inotropic Effect in Guinea Pig and Rabbit Ventricular Myocardium: Distribution of the Receptors and Their Possible Intracellular Coupling Processes

Hattori

Gando

Nagashima

et al. 1994

Japanese Journal of Pharmacology

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ABSTRACT-The difference in histamine receptor subtypes that are involved in the positive inotropic effect of histamine in guinea pig and rabbit ventricular myocardium was analytically characterized. In guinea pig papillary muscles, the positive inotropic effect of histamine was antagonized by cimetidine but not by mepyramine. The converse was true in rabbit papillary muscles. However, histamine evoked a positive iso tropic effect through H1 and H2-receptors after blockade of H2 and HI-receptors in guinea pig and rabbit papillary muscles, respectively. Adenylate cyclase was significantly activated by histamine via H2-receptors in guinea pig but not in rabbit myocardial ventricular membranes. tiotidine showed an increased number of H1-receptors and a decreased number of H2-receptors in guinea pig compared with rabbit ventricular myocardium. These results suggest that the positive inotropic effects of histamine are dominated by an H1-receptor-mediated effect in rabbits and by an H2-receptor-mediated one in guinea pig ventricular myocardium, and the positive inotropic effect manifested by one subtype apparently restricts the expression of the positive inotropic effect mediated by the other subtype. This species difference is not due to a difference in densities of the receptor subtypes, but may be partly related to a difference in the extents of coupling of H2-receptors to adenylate cyclase. Histamine exerts widespread effects on a variety of tis sues physiologically and pharmacologically.In the heart, histamine produces a slowing of atrioventricular conduc tion, an acceleration of sinus rate and an increase in force of contraction. The negative dromotropic effect and the positive chronotropic effect are mediated exclusively by H1 and H2-receptors, respectively. However, the sub types of histamine receptors mediating the positive iso tropic effect have been shown to vary among mamma lian species and among the heart sections being studied (1).In guinea pig ventricular myocardium, histamine elicits a positive inotropic effect predominantly mediated by H2 receptors (2). Although it remains controversial whether H1-receptors can also contribute to the positive inotropic effect of histamine in this tissue (2-4), radioligand bind ing studies with the H1-antagonist [3H]mepyramine have confirmed the presence of H1-receptors in guinea pig ven tricular membranes (5, 6). In contrast, the predominant involvement of H1-receptors in the positive inotropic effect has been found in rabbit ventricular myocardium (7). In this tissue, however, histamine causes a decrease in action potential duration that is unquestionably mediated by H2-receptors (8). Furthermore, a H2-receptor-mediat ed positive inotropic component has become detectable in the presence of the H1-antagonist chlorpheniramine or by the use of the selective H2-agonist impromidine as a stimulant (7,8). Thus, in spite of the fact that H1 and H2 receptors coexist in both guinea pig and rabbit ventricular myocardium, the subtype of histamine receptors that is predominantly i...

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“…To date, the distribution of histamine receptors in different mammalian tissues has been studied with selective radioligands for each receptor subtype. Yet, these studies have been hampered by high nonspecific binding and/or significant binding to secondary nonhistamine-receptor sites (Chang et al, 1979;Hill and Young, 1980;Foreman et al, 1985;Rising and Norris, 1985;Liu et al, 1992). Thus, many of the radioligands used to label H 1 and H 2 receptors seem to be of limited value for an accurate estimate of the distribution and molecular characteristics of cardiac histamine receptors (Hattori et al, 1991(Hattori et al, , 1994.…”

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confidence: 99%

Histamine H₁and H₂Receptor Gene and Protein Levels Are Differentially Expressed in the Hearts of Rodents and Humans

Matsuda¹,

Jesmin²,

Takahashi³

et al. 2004

J Pharmacol Exp Ther

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Histamine is highly concentrated in the heart of animals and humans. Excessive release in pathophysiological conditions, such as immediate hypersensitivity and septic shock, causes cardiac dysfunction and arrhythmias. Previous pharmacological studies revealed that H 1 and H 2 receptors mediate these effects. Yet, an accurate estimate of the distribution and molecular characteristics of cardiac histamine receptors is missing. Recently, the genes encoding H 1 and H 2 receptors have been cloned, and the amino acid sequence and protein structure have been elucidated. Accordingly, we analyzed gene and protein expression levels of H 1 and H 2 receptors in atria and ventricles of guinea pig, rabbit, rat, and human hearts. With immunocytochemical techniques, we examined the regional expression of H 1 and H 2 receptor proteins in the sinoatrial and atrioventricular nodes and surrounding myocardium of the guinea pig heart. Northern and Western blot studies revealed that cardiac histamine H 1 and H 2 receptors are variably distributed among different mammalian species and different regions of the heart, whereas H 2 receptors are abundantly expressed in human atrial and ventricular myocardium. These findings agree with those of previous pharmacological studies, clearly demonstrating that the responses of the heart to histamine depend on the expression level of H 1 and H 2 receptors. The highly abundant expression of H 2 receptors in the human heart substantiates histamine arrhythmogenicity in various disease states. The new knowledge of a differential distribution of histamine receptor subtypes in the human heart will foster a better understanding of histamine roles in cardiovascular pathophysiology and may contribute to new therapeutic approaches to histamine-induced cardiac dysfunctions.The actions of histamine as a cardiac stimulant have been appreciated for more than 90 years since the seminal work of Dale and Laidlaw (1910). The primary and direct actions of histamine in the heart are characterized by an increase in sinus rate and ventricular automaticity, a decrease in AV conduction velocity, and an increase in force of contraction (Levi et al., 1991;Hattori, 1999). Because histamine is present in high concentrations in cardiac tissues in most animal species, including humans (Bristow et al., 1982;Wolff and Levi, 1986), its release from cardiac stores and its subsequent actions on the heart may be of importance in pathological conditions associated with histamine release (Levi, 1988). In this context, we recently reported that superinduction of histamine receptor gene products and histamine overproduction contribute to the hemodynamic derangement characteristic of septic shock (Matsuda et al., 2002).The negative dromotropic and positive chronotropic effects of histamine invariably result from the activation of H 1 and H 2 receptors, respectively (Levi et al., 1991;Hattori, 1999). In contrast, there is a marked species difference in the subtype of histamine receptors mediating the positive inotropic effect. Mor...

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The binding of [³H]‐tiotidine to homogenates of guinea‐pig lung parenchyma

Cited by 35 publications

References 22 publications

Identification and characterization of histamine H₁‐ and H₂‐receptors in guinea‐pig left atrial membranes by [³H]‐mepyramine and [³H]‐tiotidine binding

Identification and characterization of histamine H₁‐ and H₂‐receptors in guinea‐pig left atrial membranes by [³H]‐mepyramine and [³H]‐tiotidine binding

Histamine Receptors Mediating a Positive Inotropic Effect in Guinea Pig and Rabbit Ventricular Myocardium: Distribution of the Receptors and Their Possible Intracellular Coupling Processes

Histamine H₁and H₂Receptor Gene and Protein Levels Are Differentially Expressed in the Hearts of Rodents and Humans

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The binding of [3H]‐tiotidine to homogenates of guinea‐pig lung parenchyma

Cited by 35 publications

References 22 publications

Identification and characterization of histamine H1‐ and H2‐receptors in guinea‐pig left atrial membranes by [3H]‐mepyramine and [3H]‐tiotidine binding

Identification and characterization of histamine H1‐ and H2‐receptors in guinea‐pig left atrial membranes by [3H]‐mepyramine and [3H]‐tiotidine binding

Histamine Receptors Mediating a Positive Inotropic Effect in Guinea Pig and Rabbit Ventricular Myocardium: Distribution of the Receptors and Their Possible Intracellular Coupling Processes

Histamine H1and H2Receptor Gene and Protein Levels Are Differentially Expressed in the Hearts of Rodents and Humans

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The binding of [³H]‐tiotidine to homogenates of guinea‐pig lung parenchyma

Identification and characterization of histamine H₁‐ and H₂‐receptors in guinea‐pig left atrial membranes by [³H]‐mepyramine and [³H]‐tiotidine binding

Identification and characterization of histamine H₁‐ and H₂‐receptors in guinea‐pig left atrial membranes by [³H]‐mepyramine and [³H]‐tiotidine binding

Histamine H₁and H₂Receptor Gene and Protein Levels Are Differentially Expressed in the Hearts of Rodents and Humans