| Name | (±)-Tazifylline |
| Description | (±)-Tazifylline is a selective and long-acting antagonist of histamine H1 receptor. Tazifylline shows much lower affinity for H2 receptors, α- and β-adrenoceptors, 5-hydroxytryptamine and muscarinic receptor subtypes. |
| In vitro | Tazifylline potently inhibits histamine H1-receptor-induced contractions in isolated guinea pig ilea and demonstrates high affinity in radioligand binding studies[1]. |
| In vivo | In anesthetized guinea pigs, Tazifylline causes an inhibition in histamine-induced bronchoconstriction and protects conscious animals from the lethal effect of large doses of the amine. In conscious rats, Tazifylline reduces the inflammatory effects of intradermal histamine. In conscious dogs, Tazifylline(orally) causes inhibition in histamine-induced skin inflammation for long periods of time, and in anesthetized animals attenuated that portion of the histamine-evoked hypotension attributable to stimulation of H1 receptors. Large oral doses of Tazifylline do not reduce spontaneous locomotor activity in mice, nor do they produce overt symptoms of behavioral depression in conscious rats[1]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 45 mg/mL (95.22 mM), Sonication is recommended.
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| Keywords | Tazifylline | HistamineReceptor | Histamine Receptor | H1-receptor | H1 receptor | (±)Tazifylline | (±) Tazifylline |
| Inhibitors Related | Chlorphenesin | Histamine dihydrochloride | Meclizine dihydrochloride | Mirtazapine | Lidocaine | Famotidine | Mebhydrolin napadisylate | Sodium butanoate | Amitriptyline hydrochloride | Alginic acid | Trazodone hydrochloride | Mianserin hydrochloride |
| Related Compound Libraries | Histamine & Melatonin Receptor-Targeted Compound Library | Pain-Related Compound Library | Bioactive Compound Library | Neuronal Signaling Compound Library | Membrane Protein-targeted Compound Library | ReFRAME Related Library | Neurotransmitter Receptor Compound Library | Inhibitor Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | GPCR Compound Library | Anti-Cancer Compound Library |