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Biomedical subjects

U Jahn

Publications and source records attributed to U Jahn.

At least 37 records · Page 2Linked to original sources
PubMed1983

Pharmacological studies with beclobrate, a new hypolipidemic agent.

A new diphenylmethane derivative with potent hypolipidemic activity, ethyl-(+/-)-2-[[alpha-(p-chlorophenyl)-p-tolyl]-oxy]-2-methylbutyrate (Sgd 24774, beclobrate) has been investigated in animals. From a comparison of the ED25 values of beclobrate and clofibrate, the new drug is 11 times more potent with respect to its hypocholesterolemic activity and 36 times more hypotriglyceridemic in normally fed rats, and lowers fructose-induced hypertriglyceridemia in rats 20 times as effectively as does clofibrate. On a similar basis of comparison, the hepatomegalic effect of beclobrate in rats is 22 times that of clofibrate. High doses of beclobrate did not reveal any other peripheral or central effects in a wide range of pharmacological tests, indicating a high specificity of the action of the drug on blood lipids. On the basis of the results of interaction studies performed with beclobrate in animals, administration of the substance in man should be largely free from risk.

Animals↗
PubMed1982

The existence of a new subtype of alpha-adrenoceptor on the rat anococcygeus is revealed by SGD 101/75 and phenoxybenzamine.

1 Noradrenaline and Sgd 101/75 (4(2-imidazoline-amino)-2-methylindazol-chlorhydrate) acted as full agonists in contracting the rat anococcygeus. 2 Very low concentrations of phenoxybenzamine (0.3 nM for 2-30 min) reduced preferentially the effects of Sgd 101/75. Preparations made insensitive to Sgd 101/75 by phenoxybenzamine still contracted to noradrenaline, this contraction occurring in the presence of high concentrations (400 microM) of Sgd 101/75. 3 It is concluded therefore that the alpha 1-adrenoceptor in this preparation is not a homogeneous entity and must be subdivided into at least two subtypes.

Adrenergic alpha-Agonists↗
PubMed1979

[Beclobrate and eniclobrate hydrochloride, new diphenylmethane derivatives as agents for lowering cholesterol and triglyceride levels. Part I: Synthesis and consideration of structure-activity relationships (author's transl)].

Within the course of a research project for finding new lipid-lowering substances with better therapeutic indices than the standard agent in use, various diphenylmethane derivatives were synthesized and tested with respect to their activity and toxicity. On the basis of these results Sgd 24774 (beclobrate) and Sgd 33374 (eniclobrate-hydrochloride) were selected for further investigation and clinical studies.

Animals↗
PubMed1976

[Wet dog shake behavior in normal rates, elicited by benzylideneaminooxycarbonic acid derivatives].

Wet dog shake (WDS) behavior in rats, well known as morphine-withdrawal syndrome, could be elicited without concomitant symptoms for the first time chemically in non-morphine-addicted animals. The capability to produce WDS was correlated with a specific chemical structure among the title-compounds. The threshold-dose of the most effective agents was 25-50 mg/kg, rather independent of the mode of application. Maximal response of 10-20 WDS per min and animal were reached after application of 100-200 mg/kg. WDS behavior appeared within the first minutes after dose and lasted up to several hours. Detailed information is given on WDS-action of the substance Sgd 8473 = alpha [(4chlorobenzylideneamino)-oxy]-isobutyric acid and the influence by different pharmacologie agents thereon. Inhibition of WDS was produced by: narcotic analgesics, narcotic antagonists, psychosedativ drugs, yohimbine, dl-amphetamine, cocaine, apomorphine and clonidine. Without influence on WDS were: physostigmine, atropine, ganglionic- or adrenergic-blocking drugs, Dopa, MAO-inhibitors, serotonin- and histamin-antagonists and nonnarcotic analgesics. To some extent chemically induced WDS seemed to be susceptible like precipitated WDS. So Sgd 8473 could be qualified for differentiating narctic analgesics, for a "quasiabstinence" agent in research of dependence mechanisms and for a tool in neuroanatomical studies of the CNS.

Analgesics, Opioid↗