Biomedical subjects
R Madroñero
Publications and source records attributed to R Madroñero.
Effects of thiophene analogues of chloroamphetamines on central serotonergic mechanisms.
Ring-chlorinated thienylisopropylamines, thiophene analogues of chloroamphetamines, have been synthesized and their effects on serotonergic mechanisms in the rat brain have been evaluated. With 4,5-dichlorothienylisopropylamine (3e), a pharmacological profile similar to that of p-chloroamphetamine, consisting in a marked and long-lasting serotonin depletion and a rather strong and prolonged inhibition of synaptosomal uptake of serotonin, was found. Chloro substitution in position C3 of the thiophene ring did not determine brain serotonin depletion nor serotonin uptake inhibition but enhanced brain MAO inhibitory activity present in all these compounds. 3,5-Dichlorothienylisopropylamine (3g) was the only compound of the series in which the inhibition of serotonin uptake was more marked than the serotonin depleting property.
beta-Adrenoceptor blocking activity of halogenated thienylethanolamine derivatives.
The synthesis of a number of ring-halogenated N-isopropyl- and N-tert-butyl-2-amino-1-(2-thienyl)ethanols has been carried out in order to ascertain the influence of chloro or bromo substitution at the thiophene moiety on their blocking beta-adrenoceptor activity. It was found that chloro- and bromo-substituted compounds exhibited a similar activity. Monohalo substitution at positions C4 or C5 of the thiophene ring resulted in comparable blocking potency, whereas C3 halo-substituted compounds were practically devoid of activity. The highest activity in these series was observed with compounds dihalogenated at C4 and C5, their effect on myocardial beta-receptors being comparable to that of propranolol.
Pharmacological properties of 6,7-tetramethylene-5-phenyl-1,2-dihydro-3H-thieno[2,3-e](1,4)-diazepin-2-one (QM-6008, thiadipone), a new psychotropic drug.
The pharmacological actions of 6,7-tetramethylene-5-phenyl-1,2,-dihydro-3H-thieno]2,3-e](1,4)-diazepin-2-one (QM-6008, thiadiapone), a new psychotropic drug, have been studied. QM-6008 shares many of the psychosedative effects in rodents of benzodiazepines. The electroencephalographic actions in rats and rabbits of QM-6008 and chlordiazepoxide are also rather similar. This new compounds is endowed with clear conflict attenuating properties in an approach-avoidance schedule and can be considered, in consequence, as a new potentially useful anxiolytic drug. In other operant conditioning procedures in rats--Variable Interval and Discriminated Avoidance--QM-6008 induces an increase in response rate which is not generally shared by chlordiazepoxide. The psychopharmacological data collected in the present work leal to classify this new thienodiazepine derviative within the fram of tranquilizers of the benxodaizapine type. The sedative effects of QM-6008 appear howerer to be less potent and the psychostimulatn effects more markde than those ofchlordiazeposide.
Beta-adrenoreceptor blocking properties of new thienylethanolamine derivatives.
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N-substituted 2-amino-1-(2-thienyl)ethanols as beta-adrenergic blocking agents.
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Heterocyclic N-glycosyl derivatives. 15. Synthesis of unsaturated 6-methylthiopurine nucleosides.
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2,5-dihydro-1,2,4-benzothiadiazepine 1,1-dioxides. Synthesis and pharmacological evaluation.
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