NEDOCROMIL SODIUM

Names

[ Name ]:
NEDOCROMIL SODIUM

[Synonym ]:
Nedocromil sodium (USAN)
Tilarin
disodium 9-ethyl-6,9-dihydro-4,6-dioxo-10-propyl-4H-pyrano[3,2-g]-quinoline-2,8-dicarboxylate
dissodium 9-ethyl-6,9-dihydro-4,6-dioxo-10-propyl-4H-pyrano<3,2-g>quinoline-2,8-dicarboxylate
9-ethyl-6,9-dihydro-4,6-dioxo-10-propyl-4H-pyrano[3,2-g]quinoline-2,8-dicarboxylic acid disodium salt
Alocril
disodium,9-ethyl-4,6-dioxo-10-propylpyrano[3,2-g]quinoline-2,8-dicarboxylate
Nedocromil sodium
UNII-ET8IF4KS1T
disodium 9-ethyl-4,6-dioxo-10-propyl-4H,6H pyrano[3,2-g]quinoline-2,8-dicarboxylate
di-sodium 9-ethyl-4,6-dioxo-10-propyl-4H,6H-pyrano[3,2-g]quinoline-2,8-dicarboxylic trihydrate
Tilade

Biological Activity

[Description]:

Nedocromil sodium suppresses the action or formation of multiple mediators, including histamine, leukotriene C4 (LTC4), and prostaglandin D2 (PGD2).

[Related Catalog]:

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

Signaling Pathways >> Immunology/Inflammation >> Histamine Receptor

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

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

Research Areas >> Inflammation/Immunology

[Target]

Histamine

LTC4

PGD2

[In Vitro]

Nedocromil inhibits the release of histamine, LTC4, and PGD2 from mast cells challenged with antigen (with IC30 values of 2.1 μM, 2.3 μM, and 1.9 μM, respectively) and with anti-human IgE (IC30 values of 4.7 μM, 1.3 μM, and 1.3 μM, respectively)[1].

[In Vivo]

Nedocromil-treated diabetic mice show significantly improved heart function compared with controls. The contractility and relaxation forces show similar improvements. However, the cardiac function of Nedocromil-treated diabetic mice remains significantly impaired when compared with normal mice. Nedocromil can significantly improve cardiac function in mice with diabetic cardiomyopathy, but the treatment cannot restore normal function[2].

[Animal admin]

Mice[2] 8-12 weeks old C57/BL6 male mice between 23-25 g receive intraperitoneal (i.p.) injections of 50 mg/kg Streptozotocin (STZ), dissolved in 100 mM citrate buffer pH 4.5, for five consecutive days. Diabetic mice (13-week-old) are randomly divided into three groups: 1) untreated group; 2) Nedocromil group, with Nedocromil released at the rate of 30 mg/kg per day from a subcutaneous (s.c.) pellet implantation; and vehicle group, with an inactive pellet implanted. Normal mice (non-diabetic) and normal mice that receive Nedocromil (30 mg/kg per day) are also included in this study for comparison. All sample groups included 15 mice (n=15)[2].

[References]

[1]. Wells E, et al. Characterization of primate bronchoalveolar mast cells. II. Inhibition of histamine, LTC4, and PGD2 release from primate bronchoalveolar mast cells and a comparison with rat peritoneal mastcells. J Immunol. 1986 Dec 15;137(12):3941-5.

[2]. Myocardial remodeling in diabetic cardiomyopathy associated with cardiac mast cell activation. Huang ZG, et al. PLoS One. 2013;8(3):e60827.

[Related Small Molecules]

Chemical & Physical Properties

[ Boiling Point ]:
645.5ºC at 760 mmHg

[ Molecular Formula ]:
C₁₉H₁₅NNa₂O₇

[ Molecular Weight ]:
415.30400

[ Flash Point ]:
344.2ºC

[ Exact Mass ]:
415.06400

[ PSA ]:
132.47000

[ Storage condition ]:
2-8°C

Safety Information

[ RIDADR ]:
NONH for all modes of transport

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Articles

The role of the Annexin-A1/FPR2 system in the regulation of mast cell degranulation provoked by compound 48/80 and in the inhibitory action of nedocromil.

Int. Immunopharmacol. 32 , 87-95, (2016)

1.We investigated the role of Annexin (ANX)-A1 and its receptor, ALX/FPR2, in the regulation of mast cell degranulation produced by compound 48/80. 2.Both human cord-blood derived mast cells (CBDMCs) ...