ChemicalBook CAS DataBase List 80259-18-3

80259-18-3

Name	JP1302
CAS	80259-18-3
Molecular Formula	C24H24N4
MDL Number	MFCD10565599
Molecular Weight	368.47
MOL File	80259-18-3.mol

Chemical Properties

Boiling point	550.9±50.0 °C(Predicted)
density	1.227±0.06 g/cm3(Predicted)
storage temp.	Desiccate at -20°C
pka	9.03±0.10(Predicted)
Water Solubility	<44.14mg/ml in Water

Hazard Information

Uses

JP 1302 Dihydrochloride is an α2-adrenoceptor blocker and can be used for the treatment or prevention of nephropathy.

Biological Activity

α 2C -adrenoceptor antagonist that displays ~ 50-fold selectivity over other α 2 -adrenoceptor subtypes (K i values are 28, 1470, 1700 and 3150 nM for human α 2C , α 2B , α 2D and α 2A subtypes respectively). Potently antagonizes adrenalin-stimulated 35 GTP γ S binding in vitro (K B = 16 nM) and produces antidepressant and antipsychotic-like effects in vivo .

in vivo

JP1302 (1-10 μmol/kg) decreases immobility time in the FST to a level similar to that seen with 10-30 μmol/kg of the antidepressant Desipramine (HY-B1272A)^[1].
JP1302 (5 μmol/kg, once) is capable of complete reversal of the impairment in PPI induced in Sprague-Dawley rats by the psychotomimetic NMDA receptor antagonist, phencyclidine and similar results are found in Wistar rats^[1].
JP1302 (3 mg/kg, IV, once) significantly ameliorates renal dysfunction^[3].

Animal Model:	Male Sprague Dawley rats (8 weeks old)^[3]
Dosage:	3 mg/kg
Administration:	IV, pre-treatment: administered 5 min before the induction of ischemia, post-treatment: injected 45 min after the initiation of reperfusion
Result:	Significantly ameliorated renal dysfunction in the rats at 24 h after reperfusion. post-ischemic administration of JP-1302 significantly ameliorated renal dysfunction, histological damage and reduced apoptotic cells and pro-inflammatory cytokine mRNA expression.

IC 50

human α2C-adrenoceptor: 28±2 nM (Ki); human α2B-adrenoceptor: 1470±130 nM (Ki); human α2A-adrenoceptor: 3150±50 nM (Ki); rodent α2D-adrenoceptor: 1700±200 nM (Ki)

storage

Desiccate at -20°C

Spectrum Detail

Supplier

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