JP1302

JP1302 is a potent, selective, high affinity antagonist of the α2C-adrenoceptor, with a Kb of 16 nM and a Ki of 28 nM for the human α2C-receptor. JP1302 shows antidepressant and antipsychotic-like effects. JP1302 can be used for neuropsychiatric disorders and renal dysfunction research[1][2][3].

Signaling Pathways >> GPCR/G Protein >> Adrenergic Receptor

Research Areas >> Neurological Disease

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)

JP1302 shows about 100-fold higher affinity than for α2A or α2B[1].

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.

[1]. Tricklebank MD, et al. JP-1302: a new tool to shed light on the roles of alpha2C-adrenoceptors in brain. Br J Pharmacol. 2007 Feb;150(4):381-2.  

[2]. Sallinen J, et al. Pharmacological characterization and CNS effects of a novel highly selective alpha2C-adrenoceptor antagonist JP-1302. Br J Pharmacol. 2007 Feb;150(4):391-402.  

[3]. Shimokawa T, et al. Post-treatment with JP-1302 protects against renal ischemia/reperfusion-induced acute kidney injury in rats. J Pharmacol Sci. 2019 Mar;139(3):137-142.  

MOLECULAR FORMULA :

C24-H24-N4

MOLECULAR WEIGHT :

368.52

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Oral

SPECIES OBSERVED :

Rodent - mouse

DOSE/DURATION :

1500 mg/kg

TOXIC EFFECTS :

Details of toxic effects not reported other than lethal dose value

REFERENCE :

MPPBAB Meditsinskaya Parazitologiya i Parazitarnye Bolezni. Medical Parasitology and Parasitic Diseases. (V/O Mezhdunarodnaya Kniga, 113095 Moscow, USSR) V.1- 1932- Volume(issue)/page/year: 61(5),55,1991