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Biomedical subjects

J Knoll

Publications and source records attributed to J Knoll.

At least 163 records · Page 9Linked to original sources
PubMed1975

The pharmacology of 14-hydroxyazidomorphine.

6-Deoxy-6-dihydroazido-14-hydroxyisomorphine (14-hydroxyazidomorphine) was synthesized, its analgesic potency in mice and rats, its antitussive effect in rats and its dependence liability in mice, rats and monkeys were studied. Azidomorphine the 14-nonhydroxylated parent molecule, morphine, hydromorphone and oxymorphone were used for comparison. 14-Hdroxyazidomorphine proved to be as potent an analgesic as azidomorphine, even more potent as an antitussive, and showed the same low tolerance and dependence capacity. It was 11-6 times less toxic than azidomorphine in mice and 6-5 times less toxic in rats.

Analgesics↗
PubMed1975

Para-substituted amphetamines and brain serotonin.

Among the para-substituted amphetamines was V-111 the most potent inhibiting of examined synaptosomal reuptake of 3H-5-HT. In this respect both optical isomers of V-111 were equally effective while in the inhibition of the uptake of 3H-NA and mainly in that of 3H-DA the (+) form was found to be more potent inhibitor. Concerning the releasing potency of the former amines, in the case of 3H-5-HT both isomers were equally effective releasers. The release of 3H-NA and 3H-DA was influenced more effectively by the (+) form. The stereoselective influence of V-111 on the amine reuptake and release suggests a possibility to reach more selective serotonergic and catecholaminergic effects of amphetamines. For the irreversible inhibition of the uptake in vivo presumably one of the metabolities of V-111 is responsible.

Animals↗
PubMed1975

The metabolism of azidomorphine in the rat.

The metabolism of [7,8-3H]azidomorphine and the in vivo stability of the azidogroup in azidomorphine and 14-hydroxyazidomorphine was studied. Asidomorphine conjugates with glucuronic acid, and is N-demethylated by rat liver microsomes. Detection by means of infrared spectroscopy proved that the azidroup in azidomorphine and 14-hydroxyazidomorphine strongly resists biotransformation in the rat.

Animals↗
PubMed1975

Absorption, distribution and elimination of azidomorphine and related substances.

The absorption, distribution and elimination of 14C- and 3H-azidomorphine, 3H-14-OH-azidomorphine, 14C- and 3H-azidocodeine and 3H-azidoethylmorphine were studied in comparison to 14-C-morphine. Whole body autoradiography of pregnant mice, quantitative estimations of tissue radioactivity in male mice, brain autoradiography, subcellular distribution in rat brain and elimination studies in rats were performed. Azidomorphine and morphine are absorbed from the gastrointestinal tract at the same rate but the absorption of 14-OH-azidomorphine, azidocodeine and azidoethylmorphine exceeds that of the formers. The azidomorphines pass across the blood-brain barrier more readily than does morphine. In rats treated with azidomorphines, 30--50% of the doses given were excreted with the urine the first 4 hours and about 90% within 48 hours; whereas 2--5% were recovered from the collected stools.

Adipose Tissue, Brown↗