Inhibition of Ca2+-induced noradrenaline release from central noradrenergic neurons by morphine

Summary Morphine inhibited the noradrenaline release from slices of rat brain cortex induced by introduction of Ca²⁺ ions after superfusion with Ca²⁺-free, K⁺-rich solution. The degree of inhibition was inversely related to the Ca²⁺ concentration used for stimulation.Acknowledgment. We thank Mrs G. Thielecke and Miss G. Werthmann for technical assistance.     

Inhibition by tetanus and botulinum A toxin of the release of [3H]noradrenaline and [3H]GABA from rat brain homogenate

Summary Rat brain homogenate was preloaded with [³H]noradrenaline or [³H]GABA and stimulated with high K⁺. Tetanus toxin and botulinum A neurotoxin partially prevent the evoked [³H]noradrenaline release in the same range of toxin concentrations starting below 10^–10M. In contrast, release of -amino butyric acid (GABA) is much more sensitive to tetanus than to botulinum A toxin.     

Inhibition by tetanus and botulinum A toxin of the release of [3H]noradrenaline and [3H]GABA from rat brain homogenate

Rat brain homogenate was preloaded with [3H]noradrenaline or [3H]GABA and stimulated with high K+. Tetanus toxin and botulinum A neurotoxin partially prevent the evoked [3H]noradrenaline release in the same range of toxin concentrations starting below 10(-10) M. In contrast, release of gamma-amino butyric acid (GABA) is much more sensitive to tetanus than to botulinum A toxin.     

The metabolism of dibenz[b,f]-1,4-oxazepine (CR): in vivo hydroxylation of 10,11-dihydrodibenz[b,f]-1,4-oxazepin-11-(1OH)-one and the NIH shift

Studies of the in vivo metabolism of 10,11-dihydrodibenz[b,f]-1,4-oxazepin-11-(1OH)-one (2) specifically deuteriated at C7 implicate an arene oxide intermediate during the conversion to 7-hydroxy-2 (4) as evidenced by the observation of the NIH shift.     

The metabolism of dibenz[b,f]-1,4-oxazepine (CR): In vivo hydroxylation of 10,11-dihydrodibenz[b,f]-1,4-oxazepin-11-(1OH)-one and the NIH shift

Summary Studies of the in vivo metabolism of 10,11-dihydrodibenz[b,f]-1,4-oxazepin-11-(1OH)-one (2) specifically deuteriated at C-7 implicate an arene oxide intermediate during the conversion to 7-hydroxy-2 (4) as evidenced by the observation of the NIH shift.     

Inhibition of DNA biosynthesis in human lymphocytes by alpha 1-antitrypsin]

Incorporation of tritiated thymidine into human lymphocytes from tonsils is markedly inhibited by purified alpha1-antitrypsin-preparations. This inhibitory effect is observed in lymphocytes stimulated by a mitogen factor (phytohemagglutinin) as in non stimulated lymphocytes.     

Inhibition of LH-RH induced release of gonadotropins by substance P in cultured rat anterior pituitary cells]

Using anterior pituitary cells cultured for 7 days and then incubated for 4 hrs, substance P, an undecapeptide, inhibited the stimulatory effect of LH-RH on the release of LH-RH on the release of LH and FSH. This inhibitory effect, which was similar for both gonadotropins was only observed when the adenopituitary cells were put in culture at DI and Proestrus stages of the oestrous cycle. Furthermore substance P partly inhibited the basal release of FSH at DI and DII stages but did never affected that of LH.     

Antihypertensive agents III. Synthesis and antihypertensive activity of 3-[4-(p-fluoro-phenyl)-1,2,3,6-tetrahydro-1-pyridyl]-1-[1-(2-hydroxyethyl)-5-methyl-4-pyrazolyl]-1-propanone

Zusammenfassung 3-[4-(p-Fluorphenyl)-1,2,3,6-te-trahydro-1-pyridyl]-1-[1-(2-hydroxyaethyl)-5-methyl-4-pyrazolyl]-1-propanon (I, CIBA 4416/B-Go) senkt bei normotonischen und hypertonischen Tieren den Blutdruck. Die Drucksenkung kann hauptsächlich auf die periphere Vasodilatation sowie auf die Vasomotorenzentren bezogen werden. Ausserdem wirkt CIBA 4416/B-Go adrenolytisch.

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Previous paper:V. P. Arya, R. S. Grewal, C. L. Kaul, S. P. Ghate, D. V. Mehta andT. George, J. Pharm. Sci.58, 432 (1969).Contribution No. 243 from CIBA Research Centre.     

Inhibition of interleukin-1 beta release from cultured human peripheral blood mononuclear cells by prednisolone

Prednisolone, a water-soluble glucocorticoid hormone, suppressed the secretion of interleukin-1 beta from human peripheral blood mononuclear cells in culture. The prednisolone-induced suppression of the monokine release was dose-related and the half maximal response was observed at 0.1 nM.     

Inhibition of noradrenaline release from sympathetic nerves by pentobarbital

Summary Pentobarbital concentrations of 10–100 M selectively inhibited the noradrenaline release evoked by activation of the nicotinic receptors on the terminals sympathetic nerves of the rabbit heart. Higher concentrations also decreased the noradrenaline release induced by KCl or by electrical stimulation of the nerve axons.This paper is dedicated to Professor Dr. G. Malorny on the occasion of his 65th birthday.Acknowledgment: We thank Mrs G. Thielecke for technical assistance.     

Inhibition of noradrenaline release from sympathetic nerves by pentobarbital

Pentobarbital concentrations of 10--100 micrometer selectively inhibited the noradrenaline release evoked by activation of the nicotinic receptors on the terminals sympathetic nerves of the rabbit heart. Higher concentrations also decreased the noradrenaline release induced by KCl or by electrical stimulation of the nerve axons.     

Inhibition of antigenic competition by immunostimulants]

The diminution of immune response against SRBC induced in mice, by a prior injection of HRBC was counteracted by addition of certain immunostimulants to SRBC. The intensity of inhibition of antigenic competition was related to the quantity of immunostimulant added to SRBC. Some immunostimulants (B. abortus, lipopolysaccharide) were more active than others (C. parvum, Poly I : C). To inhibit antigenic competition immunostimulant had to be injected after or in mixture with SRBC never before.     

Inhibition of skin calcification (Calciphylaxis) by polyphosphates

Zusammenfassung Grahamsalz, ein langkettiges Polyphosphat, ist bei subcutaner Verabreichung imstande, eine pathologische Verkalkung der Haut (Calciphylaxe) bei der Ratte zu hemmen. Der Wirkungsmechanismus dieser Hemmung wird kurz diskutiert.     

Inhibition of catalase by (Arylthio)-acetohydroxamic acids

Zusammenfassung Leberkatalase wird durch (Arylthio)-acetohydroxamsäure gehemmt. I₆₀ Werte: 4.5·10^–3 to 1,0·10^–4 M.p-Bromoderivat (pI₅₀=4.0) zeigt die stärkste Hemmung. Substitution in der Para-Stellung des Benzol Ringes verursacht eine zunehmende Hemmung in der Reihenfolge: CH₃OCH₃ClBr. Es wird vermutet, dass sich der Hemmstoff nicht mit dem aktiven Zentrum des Ferments verbindet.