Trapidil

Bezeichnung:Trapidil

CAS-Nr15421-84-8

Englisch Name:7-(DIETHYLAMINO)-5-METHYL-S-TRIAZOLO[1,5-A]PYRIMIDINE

CBNumberCB0487317

SummenformelC10H15N5

Molgewicht205.26

MOL-Datei15421-84-8.mol

Synonyma

Trapidil

Trapidil physikalisch-chemischer Eigenschaften

Schmelzpunkt	98-99.4° (Pfeifer); 102-104° from heptane (Tenor)
Dichte	1.20±0.1 g/cm3(Predicted)
storage temp.	Inert atmosphere,Room Temperature
Löslichkeit	H2O: ≥15mg/mL
pka	pKs = 2.79(at 25℃)
Aggregatzustand	powder
Farbe	white to tan
CAS Datenbank	15421-84-8

Sicherheit

Kennzeichnung gefährlicher	Xi
R-Sätze:	36/37/38
S-Sätze:	26
WGK Germany	3
Toxizität	LD50 in mice, rats (mg/kg): 115, 76 i.v.; 380, 235 orally; 155, 100 i.p.; 132, 100 s.c. (Fuller)

Gefahreninformationscode (GHS)

7-(DIETHYLAMINO)-5-METHYL-S-TRIAZOLO[1,5-A]PYRIMIDINE Chemische Eigenschaften,Einsatz,Produktion Methoden

Chemische Eigenschaften
White or almost white, crystalline powder
Originator
Rocornal,Mochida,Japan,1978
Verwenden
Vasodilator;PDGF antagonist
Definition
ChEBI: Trapidil is a member of triazolopyrimidines.
Manufacturing Process
8.4 g of 5-methyl-7-chloro-s-triazolo-(1,5-a)-pyrimidine were suspended in 30 cc of water and 7.3 g of diethylamine added. After 2 hours heating with stirring, the mixture was concentrated under vacuum. The residue was recrystallized from n-heptane. This process yielded 8.1 g of the 5-methyl-7- diethylamino-s-triazolo-(1,5-a)-pyrimidine having a melting point of 103°C to 104°C. The hydrochloride produced in the usual manner had a melting point of 212°C.
Therapeutic Function
Coronary vasodilator
Biologische Aktivität
Trapidil is an antiplatelet agent th at acts in part as a phosphodiesterase inhibitor and as a competitive inhibitor of the platelet-derived growth factor (PDGF) receptor. Trapidil, with its vasodilator and NO releasing effect may have some potential to diminish the tissue injury. Trapidil suppresses platelet-derived growth factor (PDGF)-induced vascular smooth muscle cell (VSMC) proliferation by inhibiting Raf-1/extracellular signal-regulated kinase (ERK) via cAMP/protein kinase A (PKA). In addn. to cAMP/PKA activation, trapidil inhibits RhoA/ROCK activation.
Sicherheitsprofil
Poison by ingestion, intraperitoneal, subcutaneous, and intravenous routes. An experimental teratogen. Other experimental reproductive effects. A coronary vasodilator. When heated to decomposition it emits toxic fumes of NOx. See also MINES.

7-(DIETHYLAMINO)-5-METHYL-S-TRIAZOLO[1,5-A]PYRIMIDINE Upstream-Materialien And Downstream Produkte

Trapidil Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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