Zu "K04149" wurden 221 Artikel gefunden!
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Mequitazine
Artikelnummer: Cay45325-10
A dual histamine H1 and muscarinic acetylcholine receptor antagonist (Kis = 4.4 and 5 nM, respectively), oral or subcutaneous administration increases survival in a rat model of compound 48/80-induced mast cell degranulation (ED50s = 1.02 and 0.26 mg/kg, respectively). SMILES:...
| Schlagworte: | NSC 303612, 10-(1-azabicyclo[2.2.2]oct-3-ylmethyl)-10H-phenothiazine |
| Anwendung: | Dual histamine H1 / muscarinic acetylcholine receptor antagonist |
| CAS | 29216-28-2 |
| MW: | 322.47 D |
ab 91,00 €
Triprolidine (hydrochloride)
Artikelnummer: Cay39376-100
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:...
| Schlagworte: | 2-[(1E)-1-(4-methylphenyl)-3-(1-pyrrolidinyl)-1-propen-1-yl]-pyridine, monohydrochloride |
| Anwendung: | Analytical reference standard, antihistamine, sedative, H1 receptor antagonist |
| CAS | 550-70-9 |
| MW: | 314.86 D |
ab 109,00 €
Tripelennamine (hydrochloride)
Artikelnummer: Cay44223-1
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 =...
| Schlagworte: | NIH 10186, N,N-dimethyl-N-(phenylmethyl)-N-2-pyridinyl-1,2-ethanediamine, monohydrochloride |
| Anwendung: | Histamine H1 receptor antagonist |
| CAS | 154-69-8 |
| MW: | 291.82 D |
ab 116,00 €
Terfenadine
Artikelnummer: Cay20305-500
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...
| Schlagworte: | (±)-Terfenadine, DL-Terfenadine, MDL 9918, NSC 665802,... |
| Anwendung: | Histamine H1 receptor antagonist, CYP3A4 substrate, otassium channel blocker |
| CAS | 50679-08-8 |
| MW: | 471.7 D |
ab 51,00 €
Desloratadine
Artikelnummer: LKT-D1774.100
A non-sedating H1-receptor agonist, free from antimuscarinic/anticholinergic effects. It has novel antiallergic and anti-inflammatory effects.
| Anwendung: | H1-receptor agonist |
| CAS | 100643-71-8 |
| MW: | 310,82 D |
ab 150,00 €
Promethazine (hydrochloride)
Artikelnummer: Cay16478-10
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...
| Schlagworte: | Diprazin, Fellozine, Lergigan, Phenergan, Romergan, N,N,alpha-trimethyl-10H-phenothiazine-10-ethanamine, monohydrochloride |
| Anwendung: | H1-receptor antagonist |
| CAS | 58-33-3 |
| MW: | 320.9 D |
ab 51,00 €
Levocabastine (hydrochloride)
Artikelnummer: Cay21014-5
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...
| Schlagworte: | (3S,4R)-1-[cis-4-cyano-4-(4-fluorophenyl)cyclohexyl]-3-methyl-4-phenyl-4-piperidinecarboxylic acid |
| Anwendung: | Histamine H1 receptor antagonist |
| CAS | 79547-78-7 |
| MW: | 457 D |
ab 51,00 €
Oxatomide
Artikelnummer: Cay42288-10
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...
| Schlagworte: | KW 4354, NSC 309710, R 35443, 1-[3-[4-(diphenylmethyl)-1-piperazinyl]propyl]-1,3-dihydro-2H-benzimidazol-2-one |
| Anwendung: | Histamine H1 receptor antagonist |
| CAS | 60607-34-3 |
| MW: | 426.6 D |
ab 112,00 €
Loratadine
Artikelnummer: Cay15625-10
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...
| Schlagworte: | SCH 29851, 4-(8-chloro-5,6-dihydro-11H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-ylidene)-1-piperidinecarboxylic acid, ethyl... |
| Anwendung: | Histamine H1 receptor antagonist |
| CAS | 79794-75-5 |
| MW: | 382.9 D |
ab 69,00 €
Cetirizine (hydrochloride)
Artikelnummer: Cay19686-1
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...
| Schlagworte: | UCB-P 071, 2-[2-[4-[(4-chlorophenyl)phenylmethyl]-1-piperazinyl]ethoxy]-acetic acid, dihydrochloride |
| Anwendung: | H1-receptor antagonist |
| CAS | 83881-52-1 |
| MW: | 461.8 D |
ab 58,00 €
Dexchlorpheniramine (maleate)
Artikelnummer: Cay24027-500
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...
| Schlagworte: | d-Chlorpheniramine (maleate), Fortamine, S-(+)-Chlorpheniramine (maleate),... |
| Anwendung: | H1 receptor antagonist |
| CAS | 2438-32-6 |
| MW: | 390.9 D |
ab 91,00 €
Astemizole
Artikelnummer: Cay16967-25
Astemizole is a non-sedating antihistamine that antagonizes the histamine H1 receptor with a Ki value of 4.4 nM. It is considerably less potent at muscarinic acetylcholine receptors (Ki = 2.4 µM). Astemizole is also a potent blocker of ether-a-go-go-related gene (ERG) potassium channels (IC50 = ~1 nM) that has been...
| Schlagworte: | NSC 329963, 1-[(4-fluorophenyl)methyl]-N-[1-[2-(4-methoxyphenyl)ethyl]-4-piperidinyl]-1H-benzimidazol-2-amine |
| Anwendung: | Histamine H1 receptor antagonist |
| CAS | 68844-77-9 |
| MW: | 458.6 D |
ab 76,00 €