2-Pyridylethylamine dihydrochloride - CAS 3343-39-3
Category: Inhibitor
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Molecular Weight:
Histamine Receptor
2-Pyridylethylamine dihydrochloride is a histamine H1 receptor agonist that produces vasoconstriction.
≥99% by HPLC
2-Pyridineethanamine dihydrochloride
Store in a cool and dry place (or refer to the Certificate of Analysis).
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1.Inhibition of histamine-induced Ca2+ efflux in cultured vascular smooth muscle cells by an antihypertensive drug, cicletanine.
Lonchampt MO;Goulin J;Chabrier PE;Braquet P Drugs Exp Clin Res. 1988;14(2-3):155-8.
The effect of cicletanine, a new antihypertensive drug, on histamine-induced Ca2+ release in cultured vascular smooth muscle cells from guinea-pig aorta was examined. In 45Ca2+ labelled cells, histamine increased in a dose-dependent manner the Ca2+ efflux (EC50 = 8 x 10(-6) M). This stimulation of 45Ca2+ efflux was also observed with an H1-agonist [2-pyridylethylamine dihydrochloride (2-PEA)] but not with an H2-agonist (dimaprit). Histamine- or 2-PEA-induced 45Ca2+ efflux was inhibited by an H1-antagonist (mepyramine), whereas an H2-antagonist (cimetidine) had no effect. Cicletanine was as effective as the H1-antagonist in inhibiting histamine- or 2-PEA-stimulated 45Ca2+ efflux in a dose-dependent manner (IC50 = 10(-6) M). Only the racemic form and the R(-) enantiomer of cicletanine behaved as histaminergic antagonists, the S(+) enantiomer having no effect. These results suggest that the direct effect of cicletanine on the mobilization of Ca2+ by blocking H1-receptors may participate in an antihypertensive mechanism by producing relaxation of blood vessels.
2.The role of histamine in the regulation of the viability, proliferation and transforming growth factor β1 secretion of rat wound fibroblasts.
Wolak M;Bojanowska E;Staszewska T;Ciosek J;Juszczak M;Drobnik J Pharmacol Rep. 2017 Apr;69(2):314-321. doi: 10.1016/j.pharep.2016.11.006. Epub 2016 Nov 15.
BACKGROUND: ;Inflammation mediators play a regulatory role in repair processes. The study will examine the influence of histamine on wound fibroblast metabolic activity, viability, proliferation, and TGFβ1 secretion. The study also will identify the histamine receptor involved in regulation of the tested repair processes.;METHODS: ;Fibroblasts were obtained from the granulation tissue of wounds or intact dermis of rats. The MTT and BrdU assays were used to examine the effect of histamine (10;-8;M-10;-4;M) on the viability and metabolic activity of fibroblasts, and on their proliferative capacity. The influence of histamine receptor antagonists (i.e., ketotifen, ranitidine, ciproxifan and JNJ7777120) and agonists (2-pyridylethlamine dihydrochloride, amthamine dihydrobromide) was also investigated. The TGFβ1 and histamine receptors H1 were evaluated by enzyme-linked immunosorbent assay.;RESULTS: ;Histamine significantly increased granulation tissue fibroblast viability and metabolic activity at 10;-8; and 10;-6;M but did not change their proliferative activity. Only the blockade of the H1 receptor removed this effect of histamine. H1 receptor agonist (2-pyridylethlamine dihydrochloride) increased cell viability, thereby mimicking histamine action.
3.Histamine H1-receptors mediate phosphoinositide and calcium response in cultured smooth muscle cells--interaction with cicletanine (CIC).
Lonchampt MO;Marche P;Demerle C;Girard A;Cabanie M;Esanu A;Chabrier PE;Braquet P Agents Actions. 1988 Jul;24(3-4):255-60.
Smooth muscle cells were cultured from guinea-pig aorta and labelled with 45Ca++ and 32Pi to investigate the possible effect of cicletanine, a new antihypertensive drug, on the release of intracellular Ca++ and the metabolism of phosphoinositide induced by histamine. In 45Ca++ labelled cells, histamine increased in a dose-dependent manner the 45Ca++ efflux in the first two minutes. Stimulation of 45Ca++ release was observed with H1-agonist [2-pyridylethylamine dihydrochloride (2-PEA)] but not with H2-agonist (dimaprit). In addition, histamine- or 2-PEA- induced 45Ca++ efflux was inhibited by the H1-antagonists (mepyramine and terfenadine) whereas the H2-antagonist (cimetidine) was without effect. Similar results were obtained in 32Pi labelled cells; both H1-agonists (histamine and 2-PEA) increased the labelling of phosphoinositides. This effect was completely blocked by mepyramine. These results demonstrate that the histamine-induced stimulation of 45Ca++ efflux and phosphoinositide metabolism are mediated through H1-receptors. In the above systems, cicletanine was as effective as the H1-antagonist (mepyramine) with an IC50 of 10(-6) M for both 45Ca++ efflux and phosphoinositide metabolism.
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CAS 3343-39-3 2-Pyridylethylamine dihydrochloride

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