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2 edition of Pharmacological and cooperative properties of histaminic receptors in guinea-pig brain. found in the catalog.

Pharmacological and cooperative properties of histaminic receptors in guinea-pig brain.

William Gregory Sinkins

Pharmacological and cooperative properties of histaminic receptors in guinea-pig brain.

by William Gregory Sinkins

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Published .
Written in English


The Physical Object
Pagination205 leaves.
Number of Pages205
ID Numbers
Open LibraryOL18648414M

It is likely that the binding site labelled by [3H]-clonidine in guinea-pig kidney membranes is an alpha-adrenoceptor similar in some pharmacological aspects to an alpha2-adrenoceptor. Full text Get a printable copy (PDF file) of the complete article (M), or click on a .   Čarman-Kržan M () Heterogeneity of vascular histamine H 1 - and H 2-receptor binding sites in bovine and guinea pig aorta. Can J Physiol Pharmacol 72 [Suppl 1] Google Scholar Čarman-Kržan M, Kržan M, Schunack W () Pharmacological properties of cardiovascular histamine H 1 receptor binding sites: characterisation with 2.

Abstract. Antidepressant drugs of many chemical classes are antagonists of several different types of neurotransmitter receptors. Among the first known of these receptor interactions were the antagonisms of histamine H 1 and muscarinic acetylcholine receptors. In fact, the first antidepressant, imipramine hydrochloride, was originally synthesized for use as an antihistamine (Kuhn, ). Methods to study brain histamine receptors provide additional means of assessing the roles of histamine in brain. A description of these receptors, some of their associated effects, and their response to psychotropic drugs is presented in this review.

General. Histamine is an ubiquitous chemical messenger that can be released from a variety of cells (e.g. mast cells, enterochromaffin-like cells, neurones) to act on one of four histamine receptors: H 1, H 2, H 3 and H classification of histamine receptors has resulted from rigorous pharmacological analysis of the response of different isolated tissues and cells to histamine. MINIREVIEW—A LATIN AMERICAN PERSPECTIVE ON G PROTEIN-COUPLED RECEPTORS The Histamine H 3 Receptor: Structure, Pharmacology, Inactivation of histamine in the brain is due primarily Fig. 2. Alignment of the amino acid sequence of the human, monkey, guinea pig, rat, and mouse H 3Rs. Sequences were obtained from Uniprot.


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Pharmacological and cooperative properties of histaminic receptors in guinea-pig brain by William Gregory Sinkins Download PDF EPUB FB2

Pharmacology of Histamine Receptors presents a summary of the pharmacology of histamine receptors. It discusses the research and developments made in the use of histamine. It addresses the biological actions of the drug in various pathological instances. Pharmacological characterization of histamine receptors mediating the stimulation of cyclic AMP accumulation in slices from guinea-pig hippocampus.

Mol Pharmacol. Nov; 14 (6)– Portaleone P, Pagnini G, Crispino A, Genazzani E. Histamine-sensitive adenylate cyclase in hypothalamus of rat brain: H1 and H2 receptors. J by:   Purchase Pharmacology of Histamine Receptors - 1st Edition. Print Book & E-Book.

ISBNBook Edition: 1. Cell Mol Biol (Noisy-le-grand). May;40(3) Pharmacological properties of histamine receptor subtypes. Arrang JM(1). Author information: (1)Unité de Neurobiologie et Pharmacologie, U de l'INSERM, Centre Paul Broca, Paris, France. Histamine, a ubiquitous cell-to-cell messenger, exerts its numerous actions through interaction with three pharmacologically distinct receptor Cited by:   The distribution and characteristics of histamine H 1-receptors in various regions of guinea-pig airways have been studied using the antagonist [3 H]mepyramine.

A similar density of specific [3 H]mepyramine sites was found in trachea, bronchi and parenchyma and these sites possessed pharmacological properties expected of a histamine H addition, there was a large Cited by: The histamine receptors were characterized on isolated circular segments of trachea and pulmonary arteries from the guinea‐pig.

The motor responses to histamine H 1 ‐, H 2 ‐ and H 3 ‐receptor agonists and antagonists were tested and the responses obtained were analysed in relation to the respiratory epithelium and the vascular endothelium.

The effect of the selective histamine H 3 ‐receptor agonist R ‐(α)‐methylhistamine has been investigated on the contractile responses of the longitudinal smooth muscle of guinea‐pig ileum elicited by electrical field stimulation of acetylcholine release from myenteric nerve endings.

R ‐(α)‐methylhistamine produced a concentration‐dependent (EC 50 = ± × Histamine and histamine analogues were without effect on the isolated longitudinal strip of the rat colon. It is concluded that histamine produced dose‐dependent contractions of the guinea‐pig colon due to direct activation of H 1 ‐histamine receptors.

The effects of prolonged treatment with histamine (10(-4) M, 30 min) on desensitization at histamine H1-receptors of guinea-pig ileal longitudinal muscle were investigated. This treatment did not change either the maximum amount or dissociation constant (Kd) of [3H]-mepyramine binding to membranes of guinea-pig ileal muscle.

THERE is increasing interest in the possibility that histamine may be a neurotransmitter in the mammalian central nervous system (CNS). Electrophysiological evidence supports the existence of histamine receptors in nervous tissue through which neuronal excitability can be regulated. For example, the firing rate of certain neurones in the brain is depressed by histamine and this.

We characterized the histamine H 3 receptors involved in the modulation of electrical field stimulated neurogenic contraction of guinea pig pulmonary artery sympathetic, and guinea pig ileum parasympathetic preparations.

Simultaneous measures of electrical field stimulation-evoked 3 H overflow and tension in [3 H]norepinephrine-loaded pulmonary artery were sensitive to tetrodotoxin.

Histamine H 3 receptor modulation of electrical field stimulation-induced contractile responses in guinea pig ileum. Electrical field stimulation-evoked contractions in isolated guinea pig ileum were dose dependently inhibited by (R)-α-methylhistamine (pD 2 =±, n=13, Fig.

1B).In addition, average pA 2 estimates for the histamine H 3 receptor antagonists thioperamide (, Aminophenpyramine--i.e., N-(5-[2-(4-aminophenyl)ethanamidopentyl])-N'-(4-methoxybenzyl)-N-m ethyl-N'- (2-pyridinyl)-1,2-ethanediamine, a derivative of mepyramine (pyrilamine), a typical antagonist of histamine at its H1 receptor--was synthesized and converted into [I)iodoazidophenpyramine, a potential photoaffinity probe for the H1 receptor.

In the dark, reversible binding of this probe to. Histamine is a developmentally highly conserved autacoid found in most vertebrate tissues. Its physiological functions are mediated by four 7-transmembrane G protein–coupled receptors (H1R, H2R, H3R, H4R) that are all targets of pharmacological intervention.

The receptors display molecular heterogeneity and constitutive activity. H1R antagonists are long known antiallergic and sedating.

Charles A. Rizzo, Salvatore Tozzi, Mary Ellen Monahan, John A. Hey, Pharmacological characterization of histamine H3 receptors in isolated guinea pig pulmonary artery and ileum, European Journal of Pharmacology, /(95),1, (), (). Since the appearance of my review additional relevant reports relating to the subject have been published and are discussed below.

Of major importance was the observation that [3 H]tiotidine specifically labels histamine H2 receptors in the guinea-pig cerebral cortex (Gajtkowski, Norris, Rising and Wood, ).As previously discussed, radioligand binding experiments with [3 H]-cimetidine and.

The histamine receptors were characterized on isolated circular segments of trachea and pulmonary arteries from the guinea-pig. The motor responses to histamine H1- H2- and H3-receptor agonists.

Introduction and Historical Perspective. The classification of histamine receptors has to date been based on rigorous classical pharmacological analysis, and as yet, the classification of the three histamine receptors that have been defined by this process, (i.e., the H 1- H 2- andH 3-receptors) have not been added to because of more recent molecular biological approaches (Schwartz et al.

Over the past few decades, H 3 R receptors in the brain have attracted attention as therapeutic targets to modulate the histamine system. This receptor identified by Arrang et al. in is a Gi/o protein-coupled receptor and negatively regulates histamine release as a presynaptic autoreceptor at nerve end terminals [2,13].H 3 R inverse agonists, which could induce histamine release, were.

Pyrilamine (also known as Mepyramine) is a first generation antihistamine, targeting the H1 receptor. However, it rapidly permeates the brain and so often causes drowsiness as a side effect.

It is used in over-the-counter combination products for colds and menstrual symptoms. Mepyramine is a histamine H1 receptor inverse agonist.

Abstract. We tested several histamine H 1 receptor (H 1 R) and antagonists for their differences in agonists binding affinities between human and guinea pig H 1 Rs transiently expressed in African green monkey kidney (COS-7) cells. Especially, the bivalent agonist histaprodifen-histamine dimer (HP-HA) shows a higher affinity for guinea pig than for human H 1 Rs.1 The aim of this study was to characterize the histamine receptor type mediating relaxation of the vascular bed of the nasal mucosa from the guinea‐pig, and to determine the role of cyclo‐oxygenase products and nitric oxide in this relaxant response to studies were performed in isolated nasal mucosae examined in vitro to obtain potencies of histamine receptor‐type.The estimated KB values were all within a factor of three of those values reported for the histamine H3-receptor mediating inhibition of histamine release in rat cerebral cortex.

5. These data suggest that the histamine receptor mediating inhibition of cholinergic neurotransmission by R-(alpha)-methylhistamine in guinea-pig ileum is the same as.