Reference

Pancreatic secretion in the rat influenced by the low molecular weight serine proteinase inhibitor Gabexate mesilate

Pancreatic secretion in the rat influenced by the low molecular weight serine proteinase inhibitor Gabexate mesilate. Keim, V.; Goeke, B. (Inst. Appl. Physiol., Univ. Marburg, Fed. Rep. Ger.). Eur. J. Clin. Invest., 16(6), 519-25 (English) 1986. CODEN: EJCIB8. ISSN: 0014-2972. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) The effect of i.v. or intragastric administration of the synthetic proteinase inhibitor Gabexate mesilate (GM) [56974-61-9] on the pancreas of rats was investigated. Infused i.v. at 4 mg kg-1 h-1, GM inhibited both basal or caerulein (0.2 mg kg-1 h-1)-simulated pancreatic protein secretion. Intracellular transport and secretion of newly synthesized pancreatic enzymes was not influenced by i.v. infusion of GM. Intragastric administration of GM (400 mg kg-1) on 4 consecutive days increased pancreatic wet wt., protein and enzyme content of the gland. A preferential increase of proteinases above glucosidases was obsd. Pancreatic lobules from inhibitor-treated rats released 30% less amylase in response to caerulein or carbachol when the rate of discharge was expressed in percent of initial content. The secretion rate expressed in ku amylase/mg DNA was 2-fold higher than in controls. In pancreatic duct cannulated rats GM (400 mg kg-1 h-1), introduced intragastrically on 5 consecutive days, stimulated vol.-bicarbonate and protein secretion rate, the secretory response on the 5th day being higher than on the 1st day. Enzyme pattern in pancreatic juice changed characteristically: mainly the amt. of acidic proteinases increases, whereas the amt. of the basic isoforms was altered only slightly.

Influence of the anti-inflammatory serine esterase inhibitor gabexate mesilate (Foy) on aggregation, locomotion and adhesion of polymorphonuclear leukocytes

Influence of the anti-inflammatory serine esterase inhibitor gabexate mesilate (Foy) on aggregation, locomotion and adhesion of polymorphonuclear leukocytes. Damerau, B.; Wuestefeld, H.; Fricke, D.; Kunze, H. (Dep. Biochem. Pharmacol., Max-Planck-Inst. Exp. Med., Goettingen D-3400, Fed. Rep. Ger.). Agents Actions, 15(5-6), 594-9 (English) 1984. CODEN: AGACBH. ISSN: 0065-4299. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) The effects of the anti-inflammatory serine esterase inhibitor, gabexate mesilate (Foy) [56974-61-9] were studied, on locomotion, autoaggregation and adhesion of polymorphonuclear leukocytes stimulated with the complement peptide C5a-desArg1. The drug inhibited aggregation as well as spontaneous and directed migration of human leukocytes at concns. of about 10-3 M. Adhesion of peritoneal guinea pig leukocytes to autologous aortic strips was reduced at about 20 times lower drug concns. The inhibitory drug effects were highly time- and temp.-dependent. Expts. with the 3 major drug metabolites, pHB and eGC, indicate that gabexate mesilate is not active by itself but rather by its hydrolytic arom. metabolite, pHB. The results further suggest that the inhibitory effects on leukocyte activities obsd. are not related to the anti-inflammatory effects of gabexate mesilate.