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Biomedical subjects

J B Taylor

Publications and source records attributed to J B Taylor.

At least 91 records · Page 5Linked to original sources
PubMed1978

The physiological disposition of the anti-tussive agent, 1,2,3,4a,9b-hexahydro-8,9b-dimethyl-4-[3-(4-methylpiperazin-1-yl)propionamido]dibenzofuran-3-one dihydrochloride Azipranone, in man, rat, dog and baboon.

1. The absorption, tissue distrigution, elimination and biotransformation of the anti-tussive agent Azipranone labelled with 14C have been investigated after oral dosing to rat, dog, baboon and man and parenteral administration to rat and baboon. 2. Levels of radioactivity in plasma were maximal within 20 min of dosing in the rat and after 1-2 h in the remaining species. The concn. declined thereafter with a half-life estimated at 1, 3-4 and 18-24 h for rat, dog, and baboon and man respectively. 3. Three human volunteers excreted 53, 62 and 70% of the radioactivity in the urine in 96 h while the remaining species excreted 50-70% of the dose in the faeces in the same period. 4. Radioactivity was rapidly and extensively eliminated in the bile of both rat and baboon after administration of [14C]Azipranone. 5. The 24 h urine samples from all species contained ten major and a similar number of minor radioactive components. 6. In hepatic microsomal preparations, biotransformations of Azipranone are catalysed by enzymes requiring both NADPH2 and cytochrome-P450.

Administration, Oral↗
PubMed1977

Synthesis and antitussive activity of aminotetra- (and -hexa-) hydrodibenzofurans.

The synthesis of a novel series of antitussive agents is described. Two series of amino-substituted tetra- and hexahydrodibenzofurans were prepared and examined for antitussive activity in the guinea pig after cough elicited by electrical stimulation of the vagus nerve. A significant level of activity, comparable with that of codeine, was found in the 4alpha-amino series. The 4-methylpiperazin-1-ylpropionamide (28) was found to be the most active of the compounds synthesized and was equipment with codeine. The effects of structural modification upon antitussive activity were investigated in numerous analogues but no enhancement of activity was achieved over that of 28.

Animals↗
PubMed1977

Synthesis and central nervous system activity of quinazolones related to 2-methyl-3-(o-tolyl)-4(3H)-quinazolone (methaqualone).

A number of derivatives of 2-methyl-3-(o-tolyl)-4(3H)-quinazolone bearing new substituents on the 2-methyl group have been synthesized. It was established that most substitutions at this position reduce or remove the CNS depressant activity of methaqualone. From the series prepared only the 2-fluoromethyl derivative or certain isothiouronium salts, which could be hydrolyzed in vivo to the 2-mercaptomethyl derivative, showed activity of the same magnitude as methaqualone.

Animals↗
PubMed1977

Central nervous system activity of a novel class of annelated 1,4-benzodiazepines, aminomethylene-2,4-dihydro-1H-imidazo[1,2-a][1,4]benzodiazepin-1-ones.

The synthesis and CNS activity of a noval class of annelated 1,4-benzodiazepines, the aminomethylene-2,4-dihydro-1H-imidazo[1,2-a][1,4]benzodiazepines, are described. An investigation of the structure--activity relationships in the series derived from 8-chloro-2,4-dihydro-2-dimethylaminomethylene-6-phenyl-1H-imidazo[1,2-a][1,4]-benzodiazepin-1-one (10) led to the synthesis of a group of compounds with potent minor tranquillizer activity.

Aggression↗
PubMed1977

Biochemical characterization of some additional mycelial cultures of basidiomycetes.

Twenty-six biochemical tests were used to study cultures of basidiomycetes isolated from roots of fruit-trees and other plants. The results enabled isolates to be placed into one of sixteen groups. Three of these groups were identified as Collybia drucei, Corticium utriculicum and Heteroporus biennis by matching their biochemical reactions with those of isolates from fruiting bodies of these fungi. This suggests that the other groups might also correspond to species. The three named fungi are indigenous, the first two not having been recorded elsewhere. Thus, root infections by these fungi may have originated from the indigenous fungal flora. Isolates of C. utriculicum and Stereum purpureum which were indistinguishable in culture were also separated using biochemical tests.

Agaricales↗
PubMed1977

Bleeding intestinal varices associated with portal hypertension and previous abdominal surgery.

Patients with portal hypertension may develop portasystemic communication in adhesions formed after earlier surgery. This condition causes localized mesenteric and intestinal varices which may lead to significant gastrointestinal hemorrhage. Two patients with this disease spectrum are discussed. The recommended treatment was resection of the involved intestine and formation of a portacaval shunt to eliminate recurrence of the varices and subsequent hemorrhage.

Abdomen↗
PubMed1976

New hepato-protective agents. I. Maleopimaric acid-4alpha-carboxamides.

A number of amide derivatives of maleopimaric acid were synthesised and preliminary results on their protective activity against galactosamine-induced liver damage in the rat are described. The compounds (2, 6, 9 and 15) were found to display the highest level of protective activity producing significant lowering of serum GOT and GPT levels at a daily dose of 250-300 mg/kg. The LD50 of these compounds was typically in excess of 2000 mg/kg.

Animals↗
PubMed1976

New hepato-protective agents. II. Maleopimaridyl morpholides.

A further series of derivatives of maleopimaric acid, the maleopimaridyl morpholides, has been prepared and results on their protection against galactosamine-inducted liver damage in the rat are described. The compounds (3, 4, 8 and 10) were found to display the highest levels of hepato-protective activity in the series. Compound 8 (LD50 greater than 10 g/kg) which exhibited significant, dose-related protection at a daily dose in the range of 50-400 mg/kg, was selected for detailed investigation.

Chemical and Drug Induced Liver Injury↗
PubMed1976

Preliminary studies on the absorption, distribution and excretion of N-(2-hydroxyethyl)-maleopimarimidyl morpholide (3H-RU 18492) in the female rat and dog.

Following the oral administration of 3H-labelled N-(2-hydroxyethyl)-maleopimarimidyl morpholide (3H-RU 18 492) to rats and dogs, radioactivity was detected in plasma and the various tissues examined. However, the major fraction of the dose remained unabsorbed and the highest concentrations of radioactivity were found in the liver. In both species the major route of excretion of radioactivity was via the bile.

Animals↗