Gastrazole

Names

[ Name ]:
Gastrazole

[Synonym ]:
unii-55tzm8f95p

Biological Activity

[Description]:

Gastrazole (JB95008) is potent and selective CCK2/gastrin receptor antagonist. Gastrazole can decrease the level of gastric acid. Gastrazole inhibits the Gastrin-stimulated growth of pancreatic cancer[1][2].

[Related Catalog]:

Research Areas >> Cancer

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

[Target]

CCK2/gastrin receptor[1]

[In Vivo]

Gastrazole (0.15-3 μmol/kg; i.v.) dose-dependently inhibits the Pentagastrin-stimulated gastric acid secretion[2]. Animal Model: Male Sprague-Dawley rats with a gastric fistula[2] Dosage: 0.15, 0.3, 3 mg/kg Administration: Intravenous administration Result: Dose-dependently inhibited Pentagastrin-stimulation acid secretion by maximally 73%.

[References]

[1]. Chau I, et, al. Gastrazole (JB95008), a novel CCK2/gastrin receptor antagonist, in the treatment of advanced pancreatic cancer: results from two randomised controlled trials. Br J Cancer. 2006 Apr 24;94(8):1107-15.

[2]. Rudholm T, et, al. Release of regulatory gut peptides somatostatin, neurotensin and vasoactive intestinal peptide by acid and hyperosmolal solutions in the intestine in conscious rats. Regul Pept. 2009 Jan 8;152(1-3):8-12.

Chemical & Physical Properties

[ Molecular Formula ]:
C₃₄H₃₂FN₅Na₂O₇

[ Molecular Weight ]:
687.62500

[ Exact Mass ]:
687.20800

[ PSA ]:
206.71000

[ LogP ]:
6.32250

Related Compounds

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