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At least 19 recordsLinked to original sources
PubMed1977

Comparison of adiphenine and TRH effects on TSH release by rat pituitary in vitro.

The mechanism of action of adiphenine on in vitro rat anterior pituitary TSH release was compared to that of the physiological stimulator TRH. The comparative study showed that adiphenine and TRH were able to increase TSH release in a dose-dependent manner, had similar time courses of action for equipotent stimulating concentrations and produced similar aspects of stimulated TSH cells. However, there were several differences between the effects of adiphenine and TRH. Adiphenine action was inhibited by 20 mM K+; was not calcium dependent; was inhibited by neither thyroid hormones nor somatostatin; was little affected by energy depression. It is concluded that adiphenine probably acts near the ultimate steps of the TSH release pathway and could be a useful pharmacological tool for studying the mechanism of TSH release.

Animals↗
PubMed1981

Metabolism of adiphenine. I. Absorption, distribution and excretion in rats and mice.

1. The disposition of adiphenine labelled with 14C in two positions has been investigated in rats and mice after i.v. administration, and has been compared with that of the [14C]diethylethanolamine HCl and of the [14C]diphenylacetic acid. 2. Radioactivity in the blood declined in a biphasic manner. Biliary elimination depended upon the 14C-labelled compound administered: less than 5% dose for the diethylethanolamine moiety, 100% dose for the carboxylic moiety. Of the radioactivity appearing in rat bile, less than 1% is associated with unchanged adiphenine. 3. In preliminary metabolic studies, three major metabolites have been identified: diphenylacetic acid, diethylethanolamine and a diphenylacetic acid glucuronide. 4. Uptake by the brain of [14C]adiphenine shortly after dosing is 15 times greater than that of blood. Radioactivity is also found in the hypophysis, the adrenals and melanoid pigments, with a concn. up to 30 times greater than that found in the blood.

Absorption↗
PubMed1982

Metabolism of adiphenine. II. Identification of major excretion metabolites in rats.

1. Major metabolites isolated from rat urine after administration of a single dose of [14C]adiphenine or [3H]adiphenine were identified by chromatography and n.m.r. spectrometry, and by comparison with authentic reference compounds chemically synthesized. 2. Adiphenine was extensively metabolized by hydrolysis of the ester bond into diethylaminoethanol, diphenylacetic acid, diphenylacetic acid glucuronide and, in small quantities, the corresponding glycine and glutamine conjugates.

Animals↗
PubMedDate not supplied

Adiphenine plasma levels and blood-brain barrier crossing in the rat.

Adiphenine was administered in 3H-labelled form in doses of 15 mumole/kg intravenously to male Wistar rats. Plasma and brain levels of the unchanged drug were measured. The elimination of the 3H-labelled compound from the plasma was monophasic with a half-life of 13 minutes. The unchanged drug was detectable in the plasma for 30 minutes after the injection. The time course of brain levels of unchanged drug paralleled that found in the plasma with a half-life of 9 to 12 minutes. In all experiments, brain and plasma levels of unchanged adiphenine correlate highly.

Animals↗
PubMedDate not supplied

Brain uptake of labelled adiphenine in rats.

This study describes the behaviour of a dual labelled drug, adiphenine, in the rat brain. Macroautoradiographies show images of the brain at different times after injection. Some of the tissue metabolites are identified at the brain level and the passage of the blood brain barrier is compared with tritiated water. The obtained data give very interesting indications on the blood brain distribution and on the metabolism at the brain level. Different techniques of high pressure liquid chromatography, macro- and histoautoradiographies allowed us to visualize how the drug is fixed on cerebral structures, giving indications on its mechanism of action. This fat soluble compound freely crosses the normal blood brain barrier and if labelled with the appropriate emittor could be very useful in nuclear medicine to obtain imaging of the brain.

Animals↗
PubMed1981

Kinetics of drug decomposition. Part 69: Effect of excipients on the thermal decomposition of the mixture of aminophenazone allobarbital and adiphenine hydrochloride in the solid.

By the method of accelerated testing at elevated temperature, the thermal decomposition rate of the mixture of aminophenazone (AP), allobarbital (AB) and adiphenine hydrochloride (AD) and its individual components in the presence of the excipients starch (potato), agar, talcum, kaolin and magnesium stearate is studied. The individual and joint effect of the excipients on the components of the mixture AP + AB + AD as well as on the mixture as a whole is determined and compared. The theoretically predicted stability of the components is discussed and compared with the results of "self-life" tests in the presence and absence of the excipients.

Aminopyrine↗
PubMedDate not supplied

Kinetics of drug decomposition. Part 60. Thermal decomposition of the mixture of aminophenazone, allobarbital and adiphenine hydrochloride in the solid state.

Kinetics of decomposition of a mixture of aminophenazone, allobarbital and adiphenine hydrochloride has been examined using accelerated testing at elevated temperatures (333-353 K). The reaction order, rate constants and activation parameters (Q10 degrees, EA, delta H#, delta S#, delta G) have been determined and compared for each component, in the presence of each component of the mixture and in the presence of two components of the mixture. The effect of individual components of the mixture on the rate of decomposition of the other components has been observed, the value of this effect has been determined using the rate constants obtained. The rate constants and times t10% for room temperature were calculated. The "shelf-life time" (t10%) was calculated from accelerated testing data at elevated temperature and compared with that obtained for Vegantalgin ragées in the mixture studied at 293 K.

Aminopyrine↗