Agonists

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H128 (R)(−)-α-Methylhistamine dihydrochloride solid, ≥98% (HPLC) Potent, selective H3 histamine receptor agonist which crosses the blood-brain barrier; inhibits histamine synthesis and release.
M4910 1-Methylhistamine dihydrochloride ≥98% (TLC), powder Major metabolite of histamine by histamine N-methyltransferase.
T4951 2-((3-Trifluoromethyl)phenyl)histamine dimaleate ≥98% (HPLC), powder 2-((3-Trifluoromethyl)phe
A4730 Amthamine dihydrobromide ≥98% (HPLC), solid Amthamine dihydrobromide is a H2 histamine receptor agonist. Amthamine dihydrobromide, similar to histamine, inhibits H2 receptor-mediated eosinophil peroxidase (EPO) release with IC50 = 0.4 μM; a weak antagonist at H3 and shows no activity at H1 receptors.
D1069 Desloratadine powder, ≥98% (HPLC) Desloratadine is a selective and nonsedating histamine H1 receptor antagonist, an active metabolite of loratadine (Claritin), used to relieve hay fever and allergy symptoms with less drowsiness than other antihistamines; does not significantly inhibits cardiac K+ channels at clinically achievable blood levels. Free from antimuscarinic/anticholinergic effects.
H7375 Histamine bisphosphate monohydrate  
H7250 Histamine dihydrochloride ≥99% (TLC), powder  
H7125 Histamine ≥97.0% Endogenous H1 and H2 histamine receptor agonist; H1 activation mobilizes Ca2+; H2 activation stimulates adenylate cyclase activity in neurons; activates nitric oxide synthetase; potent vasodilator.
I135 Imetit dihydrobromide ≥98% (HPLC) Potent and selective H3 histamine receptor agonist.
I4034 Immepip dihydrobromide ≥97% (HPLC), powder Immepip is a H3 and H4 histamine receptor agonist. Immepip is a selective H3 agonist equipotent to (R)-α-methylhistamine and also effective in vitro and in vivo. It is devoid of side activities elicited at H1 and α2 receptors and 5-HT3 receptors.
H5914 Nα-Methylhistamine dihydrochloride solid Production of N-alpha-methyl-histamine (NAMH), a histamine H(3) receptor (H3R) agonist, is promoted in Helicobacter pylori infected human gastric mucosa. NAMH acts directly on histamine H(2) receptors (H2Rs) in animals to stimulate acid secretion and to be a H2R agonist. NAMH dose dependently stimulated cAMP productions in CHO-H2R cells. This production was inhibited by famotidine but not by thioperamide. Control CHO cells were unresponsive to either histamine or NAMH. In addition, the effect of NAMH, in terms of cAMP production in CHO-H2R cells, was more potent than that of histamine-that is, with a lower EC50 concentration and higher maximal cAMP production. Both NAMH and histamine, but not R-alpha-methyl-histamine, effectively inhibited [(3)H] tiotidine binding to CHO-H2R cells. These results confirm that NAMH, which is produced in the gastric mucosa by H pylori, is a potent H2R agonist as well as a H3R agonist.
S5321 S15535 ≥98% (HPLC), solid Potent, orally active, partial 5-HT1A receptor agonist
S15535, a benzodioxane, is a selective but partial agonist of histamine 5-HT1A receptor. It activates presynaptic 5-HT1A receptors and suppresses the release of hippocampal 5-HT. It acts as anxiolytic agent and modulates the cholinergic and cognitive function in rodents.3,4
V4390 VUF 8430 dihydrobromide ≥97% (NMR) VUF 8430 dihydrobromide is a potent histamine H4 receptor agonist, with a 33-fold selectivity over the histamine H3 receptor and negligible affinity for the other histamine receptor.