Novel 3-(4-piperidinylthio)-1H-indoles as potent nonopioid orally active central analgesics.

A series of 3-(4-piperidinylthio)-1H-indoles was synthesized and evaluated in mice in the phenylbenzoquinone(PBQ)-induced writhing and hot plate tests. Most of these compounds are good analgesics with activities comparable to that of morphine. Among them compound 1i (UP 237-61), which has a strong serotonin binding profile, has an interesting antinociceptive activity which is not reversed by naloxone.

N6-substituted adenosine receptor agonists. Synthesis and pharmacological activity as potent antinociceptive agents.

Novel N6-(indol-3-yl)alkyl derivatives of adenosine were synthesized. The adenosine receptor affinity and the antinociceptive activity of these compounds were assessed in binding studies and the phenylbenzoquinone-induced writhing test. Most of these analogues exhibited a potent analgesic activity without side effects.

A simple device for the optimized isolation of fat cells.

We describe a simple cell isolation device that allows the separation and sequential collection of fat cells as they are released from adipose tissue fragments exposed to a collagenase preparation. This is done without interrupting the digestion process. Use of the device allows for appreciable lowering of the degree of cell damage and the extent to which larger cells are ruptured during the isolation process.

Lipoprotein lipase in rat heart--III. Effects of sex steroid hormones on tri-, di- and monoacylglycerol lipase activities in post-heparin effluents.

The in vivo administration of ethinylestradiol to female rats causes dose-dependent decreases in tri-, di- and monoacylglycerol lipase activities in post-heparin heart effluents; monoacylglycerol lipase is less sensitive to estrogen than the other two.

Lipoprotein lipase in rat heart--II. Influence of apolipoproteins and nutritional factors on tri-, di- and monoacylglycerol lipase activities in post-heparin effluents.

1. The in vitro effects of serum and apolipoproteins (apo), and the influence of the nutritional state of the animals were compared on triacylglycerol lipase (TAGL), diacylglycerol lipase (DAGL) and monoacylglycerol lipase (MAGL) activities in post-heparin effluent from rat heart. 2.

Lipoprotein lipase in rat heart--I. Characterization of tri-, di- and monoacylglycerol lipase activities in post-heparin effluents.

1. The lipolytic activities that sequentially hydrolyze tri-, di- and monoacylglycerol in rat post-heparin heart effluents were examined. 2.

Nutritional dependence of the effect of estrogen on fat cell lipoprotein lipase.

We investigated the effects of ethynylestradiol (EE) at low dose (1.2 micrograms/day) injected s.c.

Effects of 2-fluoroestradiol on lipid metabolism in the ovariectomized rat.

Biological activities of estrogen molecules are altered by fluorination of ring A, and the resulting impairment to form catechols. 2-fluoroestradiol (2-F-E2) has been found to be devoid of carcinogenic action despite its high estrogenic potency; its metabolic effects are so far unknown. This study was designed to investigate the effects of 2-F-E2 on lipid metabolism, as compared to those of estradiol-17 beta(E2).

[Comparative study of adrenaline-induced lipolysis of human deltoid and trochanter adipose tissue].

In vitro lipolysis by adrenaline, adrenaline + phentolamine (alpha-blocker) and isoprenalin (beta-agonist) was studied in deltoid and trochanter adipose tissues of sixteen obese females (10 android and 6 gynoid). Lipolysis differs in the upper and lower parts of the body. The more the obesity predominates in the upper part of the body, the more this difference is significant.

Pharmacological comparison of the potential antidepressant UP 614-04 with viloxazine and imipramine; behavioral studies.

1. Several behavioral tests were used to compare the pharmacological activity of the potential antidepressant UP 614-04 with those of viloxazine and imipramine. 2.