Reference

Comparison of the degree of non-biospecific binding of 125I-insulin to Sepharose CL-6B conjugates prepared with different activating agents

Comparison of the degree of non-biospecific binding of 125I-insulin to Sepharose CL-6B conjugates prepared with different activating agents. Maxwell, J. Gerard; Irvine, G. Brent (Dep. Biochem., Queen's Univ. Belfast, Belfast BT9 7BL, UK). Biochem. Soc. Trans., 12(3), 485-6 (English) 1984. CODEN: BCSTB5. ISSN: 0300-5127. DOCUMENT TYPE: Journal CA Section: 2 (Mammalian Hormones) Section cross-reference(s): 9 Sepharose CL-6B was activated with cyanogen bromide [506-68-3], 1,1'-carbonyldiimidazole (I) [530-62-1], or toluene-p-sulfonyl chloride (II) [98-59-9] and then treated with 1 of the following ligands: glucagon, IgG, or ovine anti-glucagon IgG. The Sepharose-ligand conjugates were then reacted with 125I-labeled insulin [9004-10-8] and the amt. of labeled insulin remaining assocd. with each gel conjugate was detd. after 3 washings. Activation by cyanogen bromide did not alter the adsorption properties of the Sepharose. II activation resulted in a matrix that strongly adsorbed protein. Gels activated with I were only slightly improved over cyanogen bromide-activated gels. Except in the case of II activation, the presence of the protein ligand increased the adsorption of the labeled insulin. The high degree of adsorption on Sepharose activated with II was probably due to hydrophobic interactions between protein and toluene-p-sulfonyl groups remaining on the Sepharose even after incubation in ethanolamine soln.

g-Aminobutyric acid uptake inhibition and anticonvulsant activity of nipecotic acid esters

g-Aminobutyric acid uptake inhibition and anticonvulsant activity of nipecotic acid esters. Crider, A. Michael; Wood, J. D.; Tschappat, Kathryn D.; Hinko, Christine N.; Seibert, Karen (Coll. Pharm., Univ. Toledo, Toledo, OH 43606, USA). J.Several reagents such as 56-12-2 is used here. Pharm. Sci., 73(11), 1612-16 (English) 1984. CODEN: JPMSAE. ISSN: 0022-3549. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) Section cross-reference(s): 27 n-Alkyl esters of nipecotic acid were prepd. by Fischer esterification, and the esters were evaluated against bicuculline-induced seizures in mice. Evaluation of the alkyl esters for inhibition of g-aminobutyric acid [56-12-2] uptake into mouse whole brain mini-slices revealed that the order of potency was proportional to chain length. The octyl ester inhibited g-aminobutyric acid and b-alanine [107-95-9] uptakes by apparently nonspecific mechanisms. A variety of Ph esters of nipecotic acid were also synthesized utilizing either dicyclohexylcarbodiimide or 1,1'-carbonyldiimidazole [530-62-1] as the condensing agent. Most of the Ph esters were potent inhibitors of g-aminobutyric acid uptake. The uptake inhibition appeared to involve specific and nonspecific (detergent-like) mechanisms. The m-nitrophenyl [94528-08-2] and p-nitrophenyl [84358-20-3] esters were particularly potent against bicuculline-induced seizures in mice. .