80259-18-3

80259-18-3 structure

Name: JP1302
Chemical Name: N-[4-(4-methylpiperazin-1-yl)phenyl]acridin-9-amine
CAS Number: 80259-18-3
Molecular Formula: C₂₄H₂₄N₄
Molecular Weight: 368.47
Catalog: Signaling Pathways GPCR/G Protein Adrenergic Receptor
Create Date: 2016-08-07 19:58:16
Modify Date: 2024-01-03 16:18:52
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].

Name	N-[4-(4-methylpiperazin-1-yl)phenyl]acridin-9-amine
Synonyms	gnf-pf-3427

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	Signaling Pathways >> GPCR/G Protein >> Adrenergic Receptor Research Areas >> Neurological Disease
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.

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

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

1207-69-8

16153-81-4

~12%

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 2
1207-69-8 16153-81-4
DownStream 0

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