79712-55-3
79712-55-3 structure
- Name: (±)-Tazifylline
- Chemical Name: 7-[2-hydroxy-3-[4-(3-phenylsulfanylpropyl)piperazin-1-yl]propyl]-1,3-dimethylpurine-2,6-dione
- CAS Number: 79712-55-3
- Molecular Formula: C23H32N6O3S
- Molecular Weight: 472.60400
- Catalog: Signaling Pathways GPCR/G Protein Histamine Receptor
- Create Date: 2018-06-26 19:09:05
- Modify Date: 2024-01-02 18:08:20
-
(±)-Tazifylline is a potent, selective and long-acting histamine H1 receptor antagonist.
| Name | 7-[2-hydroxy-3-[4-(3-phenylsulfanylpropyl)piperazin-1-yl]propyl]-1,3-dimethylpurine-2,6-dione |
|---|---|
| Synonyms |
Tazifyllinum
Tazifilina [Spanish] tazifylline Tazifylline [INN] 7-[3-[4-(3-phenylthiopropyl)-1-piperazinyl]-2-hydroxypropyl]-theophylline 3,7-dihydro-1,3-dimethyl-7-<3-<4-<3-(phenylthio)propyl>piperazin-1-yl>-2-hydroxypropyl>-1H-purine-2,6-dione Tazifyllinum [Latin] UNII-F45OX6FZWP Tazifilina (±)-Tazifylline |
| Description | (±)-Tazifylline is a potent, selective and long-acting histamine H1 receptor antagonist. |
|---|---|
| Related Catalog | |
| Target |
H1-receptor[1] |
| In Vitro | Tazifylline potently inhibits contractions evoked by stimulation of histamine H1-receptors in isolated guinea pig ilea and exhibits high affinity for these receptors in radioligand binding studies in vitro Tazifylline has much lower affinity for histamine H2-receptors, alpha- and beta-adrenoceptors, 5-hydroxytryptamine and muscarinic receptor subtypes. Tazifylline poorly inhibits the release of histamine from rat peritoneal mast cells[1]. |
| In Vivo | In rats, guinea pigs and dogs the antihistaminic effect of Tazifylline is rapid in onset and long-lived. In anesthetized guinea pigs, Tazifylline markedly inhibits histamine-induced bronchoconstriction and protects conscious animals from the lethal effect of large doses of the amine. In conscious rats, Tazifylline is more potent in reducing the inflammatory effects of intradermal histamine than that evoked by anaphylactic reaction. In conscious dogs, orally administered Tazifylline inhibits 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 does not reduce spontaneous locomotor activity in mice, nor do they produce overt symptoms of behavioral depression in conscious rats[1]. |
| References |
| Density | 1.34g/cm3 |
|---|---|
| Boiling Point | 705.1ºC at 760 mmHg |
| Molecular Formula | C23H32N6O3S |
| Molecular Weight | 472.60400 |
| Flash Point | 380.2ºC |
| Exact Mass | 472.22600 |
| PSA | 113.83000 |
| LogP | 0.47040 |
| Index of Refraction | 1.668 |
