FRG8701 

FRG-8701 is a new Histamine H₂-receptor antagonist with an IC₅₀ of ranging from 0.25 to 0.43 μM.

IC50: 0.25 to 0.43 μM (Histamine H₂-receptor)^[1]

Positive chronotropic response to histamine at 10^-5 M is dose dependently inhibited by FRG8701 (FRG-8701) famotidine or cimetidine; and the IC₅₀ values of FRG8701, famotidine and cimetidine are 3.3, 3.0 and 108.6 (×10^-7M), respectively.The inhibitory potency of FRG8701 is almost the same as that of famotidine and approximately 33 times greater than that of cimetidine^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In the pylorus-ligated (4 hr) rats, each drug, given intraduodenally, dose-dependently inhibits the total acid output. FRG8701 at 10 or 30 mg/kg, given orally or intraperitoneally, significantly prevent the formation of the gastric mucosal lesions induced by 0.4 N HCI+50% ethanol (HCI•ethanol). Other necrotizing agents-induced gastric lesions are also inhibited by treatment of FRG8701. The oral ED₅₀ values against the lesions range from 1.1 to 9.4 mg/kg. FRG8701, given orally, dose-dependently prevents the development of gastric lesions induced by stress and indomethacin. Duodenal ulcer induced by mepirizole is also inhibited with FRG8701. The ED₅₀ values of FRG8701 for each ulcer model range from 1.7 to 6.9 mg/kg^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

418.55

C₂₂H₃₀N₂O₄S

108498-50-6

O=C(NCCCOC1=CC=CC(CN2CCCCC2)=C1)CS(CC3=CC=CO3)=O

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Shibata M,et al. Effects of FRG-8701 on gastric acid secretion, gastric mucosal lesions by necrotizing agents and experimental gastric or duodenal ulcer in rats. Jpn J Pharmacol. 1990 Nov;54(3):277-85.  [Content Brief]