(±)-Tazifylline

Modify Date: 2024-01-02 18:08:20

(±)-Tazifylline Structure
(±)-Tazifylline structure
Common Name (±)-Tazifylline
CAS Number 79712-55-3 Molecular Weight 472.60400
Density 1.34g/cm3 Boiling Point 705.1ºC at 760 mmHg
Molecular Formula C23H32N6O3S Melting Point N/A
MSDS N/A Flash Point 380.2ºC

 Use of (±)-Tazifylline


(±)-Tazifylline is a potent, selective and long-acting histamine H1 receptor antagonist.

 Names

Name 7-[2-hydroxy-3-[4-(3-phenylsulfanylpropyl)piperazin-1-yl]propyl]-1,3-dimethylpurine-2,6-dione
Synonym More Synonyms

 (±)-Tazifylline Biological Activity

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

[1]. Poizot A, et al. Animal pharmacology of the selective histamine H1-receptor antagonist tazifylline. Arzneimittelforschung. 1986 Apr;36(4):695-702.

 Chemical & Physical Properties

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

 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
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