Metabolism of a pharmacologically active pyrrolidine derivative (prolintane) by lactam formation

Zusammenfassung Prolintan, N-1-(-Benzylbutyl)-Pyrrolidin, wurde in Kaninchen durch ein Mikrosomensystem der Leber in das entsprechende Laktam, N-1-(-Benzylbutyl)-Pyrrolidin-2-on, umgebaut. Das gleiche Stoffwechselprodukt fand sich auch im Gewebe von Ratten, denen das Medikament gegeben wurde; allenfalls Spuren davon wurden im Urin der Ratten ausgeschieden.

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We thank Dr.D. C. Remy for a sample of syntheticdl-1-(-propylphenethyl)-pyrrolidin-2-one.     

Potentiation of sympathetic effects by a new diphenylpropylamine derivative

Résumé Par le composé 1, 1-bis-(4-amino-phényl)-propyl-(3)-amine (TK174), de même que par la cocaïne, les actions de la noradrénaline sont considérablement augmentées tandis que celles de la tyramine sont bloquées. Les autres effets pharmacodynamiques de la cocaïne ne sont pas produits par TK 174.

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A detailed report will be published in the journal Drug Research (Arzneimittelforschung).     

An adrenergic participation subserving a positive inotropism and chonotropism of prostacyclin on isolated rat atria.

The effects of prostacyclin (PGI2) on the contractile frequency and on the isometric developed tension of spontaneously beating or paced isolated rat atria were explored. PGI2 enhanced frequency and contractile tension, both effects being blocked by the presence of propranolol, or following a pretreatment with 6-OHDopamine.     

Increase of free 5-hydroxytryptamine in blood plasma by reserpine and a benzoquinolizine derivative

Zusammenfassung Nach Vorbehandlung von Kaninchen mit einem Monoaminoxydase-Hemmer des Hydrazin-Typs wurde plättchenreiches Plasma mit Reserpin und einem Benzochinolizin-Derivat inkubiert. Im Plasma kam es dadurch zu einem Anstieg des nicht an Thrombozyten gebundenen 5HT, der dem Abfall des Amins in den Thrombozyten entsprach. Bei Kontrolltieren (ohne Monoaminoxydase-Hemmer) führte die Inkubation von plättchenreichem Plasma mit Reserpin zu keinem Anstieg des freien 5HT im Plasma, obgleich es in den Thrombozyten zu einer starken Senkung des Amins kam.

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Supported by a grant from the Finnish Medical SocietyDuodecim.     

Modification of visual signals by nigral stimulation

Summary Responses of the lateral geniculate neurons to light were modified by stimulation of the substantia nigra. Nigral stimulation often caused enhancement of firing in neurons responding primarily to flash, but it usually had the contrary effect on units inhibited by light.     

Modification by levo-propranolol of tremors induced by harmine in mice

It has been recently reported that the levo isomer of propranolol possesses anti-serotonin properties in animals. Since harmine-induced behavioural changes in mice are reported to be mediated through central serotonergic receptors, an attempt was made to test whether 1-propranolol would also modify harmine-induced responses by virtue of its anti-serotonergic or anti-adrenergic property. The results indicated that l- and dl-propranolol inhibited central serotonin receptor mediated responses to harmine in mice, a finding that is analogous to other recent observations.     

Modification by levo-propranolol of tremors induced by harmine in mice

Summary It has been recently reported that the levo isomer of propranolol possesses anti-serotonin properties in animals. Since harmine-induced behavioural changes in mice are reported to be mediated through central serotonergic receptors, an attempt was made to test whether 1-propranolol would also modify harmine-induced responses by virtue of its antiserotonergic or anti-adrenergic property. The results indicated that 1- and dl-propranolol inhibited central serotonin receptor mediated responses to harmine in mice, a finding that is analogous to other recent observations.     

Modification of visual signals by nigral stimulation.

Responses of the lateral geniculate neurons to light were modified by stimulation of the substantia nigra. Nigral stimulation often caused enhancement of firing in neurons responding primarily to flash, but it usually had the contrary effect on units inhibited by light.     

Demethylation in vivo of natulan,a tumour-inhibiting methylhydrazine derivative

Zusammenfassung Die intraperitoneale Verabreichung von 1-¹⁴CH₃-Natulan bei der Maus und der Ratte hat eine Ausscheidung von¹⁴CO₂ in der Atemluft zur Folge. Die Demethylierungsrate in vivo beträgt bei der Maus 3,1, bei der Ratte 1,7µM/h/100 g Körpergewicht. Sie wird bei der Ratte durch Behandlung mit Phenobarbital mehr als verdoppelt. Über das Substrat der N-Demethylierung lässt sich keine sichere Aussage machen.     

Quantification of digoxin by enzyme immunoassay: synthesis of a maleimide derivative of digoxigenin succinate for enzyme coupling

Summary We synthesized the m-maleimidobenzoyl derivative of digoxigenin-3-0-succinate (through a p-phenylenediamine bridge) as a hapten derivative directed towards coupling to sulfhydryl groups of -galactosidase. Prepared enzyme conjugate had about 97% of the enzyme labeled with the hapten derivative while retaining full enzyme activity. The enzyme immunoassay for digoxin we prepared showed a maximum sensitivity of 30 pg per assay (c.v.=3%) with minimal cross-reaction with digotoxin (3.8%). Our method for hapten conjugation to -galactosidase is highly efficient and is simple and easily replicated.     

Modification of lymphocyte response to phytomitogens by polycations and polyanions

Summary The stimulation effect on mitogen-induced lymphocyte response by polycationic compounds such as polylysine, DEAE dextran protamine and methylated albumin, is studied at different serum-protein concentrations and mitogen concentrations. It is suggested that the polar interaction between polycationic compounds and glycoproteins are of major importance for reactivity of lymphocytes to mitogens.     

A central nervous system effect of a non-hallucinatory lysergic acid derivative

Zusammenfassung Ähnlich wie Serotonin und LSD-25 vermindert BOL-148, ein Lysergsäurederivat, das keine Halluzinationen erzeugt, die durch den Balken fortgeleiteten, postsynaptischen Potentiale. Vorbehandlung mit BOL-148 macht das Versuchstier für ungefähr eine Stunde unempfindlich gegen Serotonin. BOL-148 blockiert anscheinend im Zentralnervensystem wie auch in der Peripherie den Serotonineffekt. Es wird versucht, zu erklären, weshalb diese Droge keine Halluzinationen bewirkt.