AT 1015 Struktur

AT 1015

Bezeichnung:AT 1015

CAS-Nr190508-50-0

Englisch Name:AT 1015

CBNumberCB73037158

SummenformelC29H34ClN3O2

Molgewicht492.06

MOL-Datei190508-50-0.mol

AT 1015 physikalisch-chemischer Eigenschaften

storage temp.	Store at -20°C
Löslichkeit	<49.2mg/ml in H2O; <49.2mg/ml in DMSO
Aggregatzustand	solid
Farbe	White

AT 1015 Chemische Eigenschaften,Einsatz,Produktion Methoden

Verwenden
AT 1015 is a potent 5-HT2A receptor antagonist, which also shows antithrombotic activity in a in rat arterial thrombosis model. AT-1015 is a potent and long-acting oral antithrombotic agent in this model.
Biologische Aktivität
at 1015 is a potent antagonist of 5-ht2a receptor [1].the 5-ht2a receptor is a g protein-coupled receptor and a subtype of the 5-ht2 receptor, which belongs to the serotonin receptor family. the 5-ht2a receptor plays an important role in clathrin mediated endocytosis of jc virus, the human polyoma virus which causes progressive multifocal leukoencephalopathy (pml).at 1015 is a potent 5-ht2a receptor antagonist. at 1015 bound to 5-ht2 receptors in rabbit cerebral cortex membrane with pki value of 7.94 [1].in a photochemically induced rat femoral arterial thrombosis (pit) model, at 1015 (1 mg/kg) significantly inhibited vascular contraction induced by 5-ht and prolonged the time for 24 h that required to occlusion of the artery in a dose-dependent way. while, at 1015 (10 mg/kg) didn’t prolong bleeding time in the tail transection bleeding time test [2]. at 1015 inhibited 5-ht2a receptor-mediated platelet aggregation both in vitro and in rat. in the rat peripheral vascular lesion model, at 1015 (1 mg/kg) significantly inhibited progression of peripheral vascular lesions [3].
Einzelnachweise
[1]. rashid m, watanabe m, nakazawa m, et al. assessment of affinity and dissociation ability of a newly synthesized 5-ht2 antagonist, at-1015: comparison with other 5-ht2 antagonists. jpn j pharmacol, 2001, 87(3): 189-194.
[2]. kihara h, koganei h, hirose k, et al. antithrombotic activity of at-1015, a potent 5-ht(2a) receptor antagonist, in rat arterial thrombosis model and its effect on bleeding time. eur j pharmacol, 2001, 433(2-3): 157-162.
[3]. kihara h, hirose k, koganei h, et al. at-1015, a novel serotonin (5-ht)2 receptor antagonist, blocks vascular and platelet 5-ht2a receptors and prevents the laurate-induced peripheral vascular lesion in rats. j cardiovasc pharmacol, 2000, 35(4): 523-530.

AT 1015 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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