216 products were found matching "K04149"!

An analytical reference standard categorized as an antihistamine and a sedative, intended for research and forensic applications. SMILES: CC(C=C1)=CC=C1/C(C2=CC=CC=N2)=C\CN3CCCC3.Cl. InChi Code:...

Recombinant HEK293 cells stably overexpress human histamine receptor 1 (H1) on the surface and contain high levels of G protein Galphaq to couple with the receptor in downstream signaling pathways.

Tripelennamine is a histamine H1 receptor antagonist (Ki = 7. nM). It is selective for the histamine H1 receptor over muscarinic acetylcholine receptors (mAChRs, Ki = 1,300 nM). Tripelennamine also selectively inhibits histamine- over acetylcholine-induced contractions in isolated guinea pig ileum segments (EC50s =...

A histamine H1 receptor antagonist (Ki = 15 nM), selective for the histamine H1 receptor over mAChRs (Ki = 263 nM) but also inhibits 5-HT2 (Ki = 7 nM), inhibits histamine release induced by an anti-IgE antibody in isolated human lung fragments (IC50 = 4.5 nM), inhibits A23187-induced degranulation of RBL-2H3 mast...

Cetirizine N-oxide is an oxidative degradation product of the histamine H1 receptor antagonist cetirizine (Cay-19686).. Solulibility: Acetonitrile: Slightly Soluble: 0.1-1 mg/ml: DMSO: Slightly Soluble: 0.1-1 mg/ml, Water: Slightly Soluble: 0.1-1 mg/ml.

Terfenadine is a selective histamine H1-receptor antagonist with anti-allergic effects that lacks central nervous system depressant activity. It is a prodrug that undergoes extensive first-pass hepatic metabolism by the cytochrome P450 enzyme CYP3A4 to its pharmacologically active metabolite fexofenadine...

A non-sedating H1-receptor agonist, free from antimuscarinic/anticholinergic effects. It has novel antiallergic and anti-inflammatory effects.

Promethazine is a first-generation histamine H1 receptor antagonist (Ki = 0.98 nM for the human receptor). It is selective for histamine H1 over H3 and H4 receptors (Kis = >100 and 77.6 µM, respectively, for the human receptors). Promethazine also binds muscarinic acetylcholine receptors (mAChRs, Ki = 22 nM). It...

Levocabastine is a histamine H1 receptor antagonist (Ki = 62.5 nM). It is selective for histamine H1 over H2 and H3 receptors (Kis = 23.5 and 1.94 µM, respectively). Levocabastine also binds to the rat neurotensin-2 receptor (IC50 = 10 nM). Ocular application of levocabastine (0.025%) alone or in combination with...

Loratadine is a non-sedating antihistamine that acts as a selective inverse agonist of peripheral histamine H1 receptors (Ki = 35 nM). It has been shown to inhibit the release of leukotriene C4 (IC50 = 8 µM) and histamine (IC50 = 11 µM) from rodent mast cells and to inhibit allergic bronchospasm in guinea pigs with...

Cetirizine is a bioactive carboxylated metabolite of hydroxyzine (Cay-24039) that acts as a selective histamine H1 receptor antagonist (Ki = 10 nM). As a second generation antihistamine, it is non-sedating due to low lipophilicity, which prevents blood-brain barrier transit. Cetirizine is a racemic mixture composed...

Dexchlorpheniramine is a histamine H1 receptor antagonist with a pA2 value of 9.36 in guinea pig ileal tissue in vitro. It inhibits the proliferation of previously sensitized, allergen-challenged peripheral blood mononuclear cells by 92% at a concentration of 4.8 µM. Dexchlorpheniramine reduces noradrenaline uptake...