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

Jordan, D. C.; Ponsin, Gabriel; Mornex, R; Fevre, Michelle; Poncet, C; Rostagnat, Anne

doi:10.1016/0014-2999(77)90370-3

Cited by 7 publications

(2 citation statements)

References 13 publications

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“…It has been previously shown that adiphenine hydrochloride (%-diethylaminoethyl diphenylacetate hydrochloride), known for its atropinic properties, can also stirnralate the TSH release from rat anterior pituitaries in viero in a dose-related manner from 0.5 to 4 mM (Mornex et al 1973;Jordan et al 1977) without histological evidence of necrosis or nnembrane alteration of anterior pituitary cells. The possibility of a plurality of action of this drug at adenolaypofiysis level led us to test the action of adiphenine on other anterior pituitary gly coprotein A~13ar.va.4~1o~s: LH-RH, luteinizing hornlone releasing hormone; KRBgBu, Krebs-Ringer bicarbonate rnediuwa with glucose (0.01 M ) ; 2,4-DNP, %,4-dinitrophenol; r-1-H.I.3, purified rat luteinizing hormone; EH-RP-I, luteinizing hormone reference preparation I.…”

Section: Intoduetionmentioning

confidence: 98%

Comparison of pharmacological effect of adiphenine and physiological stimulation by luteinizing hormone releasing hormone on luteinizing hormone release by rat anterior pituitaries in vitro

Fevre¹,

Jordan²,

Tourniaire³

et al. 1979

Can. J. Physiol. Pharmacol.

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FEVRE, M., JORDAN, I?., TOURN~AIRE, J., and MORNEX, R. 1979. eotnparison of pharrnacological erect of adiphenine and physiological stim~llation by luteinizing hormone releasing hormone on lbnteinizing hormone release by rat anterior pituitaries in vitro. Can. J. Physiol. Pharmacol. 57, 1388-1392 The mechanism of action of adiphenine on ĩm vitro rat anterior pituitary LH release was studied and compared with that of the physiological stimulator luteiniring hormone releasing hormone (LH-KM) on LH release. The comparative study showed that adipheniale and LH-RM were able to increase medium LH concentration in a dose-dependent manner and had similar time courses of action between I and 4 h incubation. However, there were several main differences between the effects of adipheiline and LM-WH. The adiphenine: action was not calcium dependent, was inhibited in a high K+ medium concentration, and was substituted after energy depression. It is concluded that adipheninse probably acts near the ultimate steps of the LH release pathway and could be a useful pharniacological tool for studying the mechanism of LH release. FEVRE, M., JORDAN, D., TOUWNIAIRE, J., et MORNEX, W. 1979. Comparison s f pharmacological efTect of adiphenine and physiological stitnulation by luteiniaing hormone releasing hormone on luteiniring hormone release by rat anterior pituitaries in vitro. Can. J. Physiol. Pharmacol. 57, 1388-1392. On a 6tudiC i~t vitro c h e~ Ie rat, le mecanisme d9action de l'adiphgnine sur la liberation de LH par l'hypophyse antericurc. Ceci a it& compare au m6canrsme du stirnulatetar physiologique LH-RH de la libkation de LH. Cette Ctude comparative a montr6 que I'adiphknine et LH-RH son% capakles d'augmenter la concentration du milieu en EH de faqon dose-dkpendante et yue ceci implique des durCes d'action conaparables avec une incubation de 1 A 4 k. I1 existe cependant pluslieurs differences importantes entre les effets de i'adiphktaine et ccux de LH-RM. L9action de l'adinephine n9est pas calcium-dependante, est inhibke par Len milieu riche en Kt et est remplacie suite h une diminution en Cnergie. On conclut que l'adinCphine agit probablement pr$s de 15extr6mitC dia trajet de lilkration ale L H et pourrallt constituer un outil pharmacologique pratique dans 15itude du ~~Pcanisme de la libbation de LH. [Tradmit par le journal] IntoduetionIt has been previously shown that adiphenine hydrochloride (%-diethylaminoethyl diphenylacetate hydrochloride), known for its atropinic properties, can also stirnralate the TSH release from rat anterior pituitaries in viero in a dose-related manner from 0.5 to 4 mM (Mornex et al. 1973;Jordan et al. 1977) without histological evidence of necrosis or nnembrane alteration of anterior pituitary cells. The possibility of a plurality of action of this drug at adenolaypofiysis level led us to test the action of adiphenine on other anterior pituitary gly coprotein A~13ar.va.4~1o~s: LH-RH, luteinizing hornlone releasing hormone; KRBgBu, Krebs-Ringer bicarbonate rnediuwa with glucose (0.01 M ) ; 2,4-DNP,...

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Section: Intoduetionmentioning

confidence: 98%

Comparison of pharmacological effect of adiphenine and physiological stimulation by luteinizing hormone releasing hormone on luteinizing hormone release by rat anterior pituitaries in vitro

Fevre¹,

Jordan²,

Tourniaire³

et al. 1979

Can. J. Physiol. Pharmacol.

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“…More recently, its therapeutic effectiveness in treating various disorders of the nervous system has been evaluated. While the atropinic properties of the drug have been extensively investigated, the finding that adiphenine can stimulate thyrotropin (TSH) and luteinizing hormone (LH) release from rat anterior pituitaries has not yet been explained (2,3,4).…”

Section: Introductionmentioning

confidence: 99%

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

Michelot

Moreau

Veyre

et al. 1985

European Journal of Drug Metabolism and Pharmacokinetics

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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.

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Brain uptake of labelled adiphenine in rats

Michelot

Moreau

Veyre

et al. 1986

Biopharm & Drug Disp

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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.

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

Cited by 7 publications

References 13 publications

Comparison of pharmacological effect of adiphenine and physiological stimulation by luteinizing hormone releasing hormone on luteinizing hormone release by rat anterior pituitaries in vitro

Comparison of pharmacological effect of adiphenine and physiological stimulation by luteinizing hormone releasing hormone on luteinizing hormone release by rat anterior pituitaries in vitro

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

Brain uptake of labelled adiphenine in rats

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