JP1302

Modify Date: 2025-08-24 19:43:38

JP1302 Structure
JP1302 structure
Common Name JP1302
CAS Number 80259-18-3 Molecular Weight 368.47
Density 1.227g/cm3 Boiling Point 550.9ºC at 760 mmHg
Molecular Formula C24H24N4 Melting Point N/A
MSDS N/A Flash Point 287ºC

 Use of 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].

 Names

Name N-[4-(4-methylpiperazin-1-yl)phenyl]acridin-9-amine
Synonym More Synonyms

 JP1302 Biological Activity

Description 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].
Related Catalog
Target

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)

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

[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.  

 Chemical & Physical Properties

Density 1.227g/cm3
Boiling Point 550.9ºC at 760 mmHg
Molecular Formula C24H24N4
Molecular Weight 368.47
Flash Point 287ºC
Exact Mass 368.20000
PSA 31.40000
LogP 4.95930
Index of Refraction 1.714
InChIKey QZKGUNQLVFEEBA-UHFFFAOYSA-N
SMILES CN1CCN(c2ccc(Nc3c4ccccc4nc4ccccc34)cc2)CC1

 Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :
AR7147000
CHEMICAL NAME :
9-Acridinamine, N-(4-(4-methyl-1-piperazinyl)phenyl)-
CAS REGISTRY NUMBER :
80259-18-3
LAST UPDATED :
199612
DATA ITEMS CITED :
1
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

 Synthetic Route

~12%

JP1302 Structure

JP1302

CAS#:80259-18-3

Literature: Wurster, Siegfried; Engstrom, Mia; Savola, Juha-Matti; Hoglund, Iisa; Sallinen, Jukka; Haapalinna, Antti; Tauber, Andrei Yurievitch; Hoffren, Anna-Marja Katariina; Salo, Harri Elias Patent: US2001/46991 A1, 2001 ;

 Precursor & DownStream

Precursor  2

DownStream  0

 Synonyms

gnf-pf-3427
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