Identification | Back Directory | [Name]
JP1302 | [CAS]
80259-18-3 | [Synonyms]
JP1302 MMV006172 Brn 5117597 JP 1302 dihydrochloride N-(4-(4-Methyl-1-piperazinyl)phenyl)-9-acridinamine 9-Acridinamine, N-(4-(4-methyl-1-piperazinyl)phenyl)- JP1302(9-Acridinamine, N-[4-(4-methyl-1-piperazinyl)phenyl]-) N-[4-(4-Methyl-1-piperazinyl)phenyl]-9-acridinaminedihydrochloride | [Molecular Formula]
C24H24N4 | [MDL Number]
MFCD10565599 | [MOL File]
80259-18-3.mol | [Molecular Weight]
368.47 |
Chemical Properties | Back Directory | [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 | Back Directory | [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.html" class="link-product" target="_blank">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 |
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