Effect of exogenous pyruvate on acrylamide neuropathy in rats.

The protective effect of exogenous sodium pyruvate on the distal-proximal progression of experimental acrylamide neuropathy in rats was examined. Incorporation of 2% (w/w) sodium pyruvate powder in the diet of rats receiving subcutaneous injections of an aqueous solution of acrylamide (35 mg/kg/day, 5 days/week) retarded the onset and development of functional, morphological, and biochemical measures of acrylamide neuropathy. Pyruvate supplementation did not alter hexobarbital sleep time or zoxazolamine paralysis time, two in vivo measures of microsomal mixed-function oxidase activity, and the disposition of radioactivity in plasma or sciatic nerve following subcutaneous injection of [14C]acrylamide.

Synthesis of a potent enkephalin analog, Tyr-D-Thr-Gly-Phe-delta 3 Pro-NH2, and some of its biological activities.

The enkephalin analog, H-Tyr-D-Thr-Gly-Phe-delta 3 Pro-NH2 X HCl (VI) ([D-Thr2, delta 3 Pro5]-enkephalinamide), has been synthesized by conventional methods in solution and purified to homogeneity by reversed phase HPLC. The analog is a potent analgesic agent. For evaluation of some of its biological activity a related compound [D-Thr2, Thz5]-enkephalinamide (XI) was also synthesized in solution.

(--)-threo-Chlorocitric acid: a novel anorectic agent.

A new class of peripherally acting anorectics is described in these studies. The four stereoisomers of chlorocitric acid which are structurally similar to the known anorectic, (--)-threo-hydroxycitric acid, all suppressed food intake when administered at high doses to rats. Only one of these isomers, (--)-threo-chlorocitric acid, retained its anorectic activity at lower doses.