JP1302

Modify Date: 2024-01-03 16:18:52

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

 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