Brain adenylate cyclase activation in the jaundiced rat.

Adenylate cyclase responses of brain cortex and neostriatum to noradrenaline and dopamine are increased in rats with jaundice in proportion to its severity. In comparing the situation with uraemia, the relevance of phenols has to be considered.     

Brain adenylate cyclase activation in the jaundiced rat

Summary Adenylate cyclase responses of brain cortex and neostriatum to noradrenaline and dopamine are increased in rats with jaundice in proportion to its severity. In comparing the situation with uraemia, the relevance of phenols has to be considered.     

Pentagastrin activation of adenylate cyclase in human gastric biopsy specimens.

Adenylate cyclase activity of human fundic mucosa is log-normally distributed and equally stimulated by pentagastrin and histamine. Cimetidine inhibits the histamine, but not the pentagastrin effect, which is even intensified by H2-receptor blockade. The results indicate that pentagastrin and histamine activate adenylate cyclase via distinct receptors.     

Pentagastrin activation of adenylate cyclase in human gastric biopsy specimens

Summary Adenylate cyclase activity of human fundic mucosa is log-normally distributed and equally stimulated by pentagastrin and histamine. Cimetidine inhibits the histamine, but not the pentagastrin effect, which is even intensified by H₂-receptor blockade. The results indicate that pentagastrin and histamine activate adenylate cyclase via distinct receptors.Acknowledgments. This study was supported by a grant from the Deutsche Forschungsgemeinschaft. The helpfull technical assistence of Mr W. Beer is gratefully acknowledged.     

Effects of penfluridol of dopamine-sensitive adenylate cyclase in corpus striatum and substantia nigra of rats.

Penfluridol, a neuroleptic with diphenylbutyl piperidine structure, blocked the dopamine-sensitive adenylate cyclase in homogenates of corpus striatum and substantia nigra of rats, probably by a competitive antagonism versus dopamine.     

Actions ofl-glutamate,acetylcholine and dopamine on single neurones in the nuclei cuneatus and gracilis of the cat

Zusammenfassung Von 250 Neuronen im Gebiet des Nucleus cuneatus und des Nucleus gracilis der Katze wurden 132 durch periphere physiologische Reizung aktiviert und 6 gehemmt. Mit Hilfe der Mikroelektrophorese wurden die folgenden Substanzen in die unmittelbare Nähe dieser Neurone gebracht:l-Glutaminsäure aktivierte 50 % der Neurone. Acetylcholin war nur an wenigen Zellen im Kerngebiet wirksam, von diesen wurden 2 gehemmt und 3 aktiviert. Dopamin hemmte die Mehrzahl der durch periphere Reizung becinflussbaren Neurone.     

Catecholamine-sensitive adenylate cyclase of human fat cell ghosts. Inhibition of catecholamine stimulation by phenylephrine

Summary The alpha-adrenergic agonist phenylephrine (up to 1 mM) did not affect basal and NaF-stimulated adenylate cyclase activities of human fat cell ghosts, but caused a dose-dependent inhibition of cAMP formation in the presence of catecholamines.     

Competitive inhibitors of neurohypophyseal hormones on adenylate cyclase from the toad urinary bladder

Zusammenfassung Adenylat-Cyclase in plasmamembranreichen Präparationen des Epitheliums von der Harnblase der Kröte wird durch Arginine-Vasopressin aktiviert. Diese Aktivierung wird durch mehre Oxytocinanaloge, die alle eine Substitution des Glutaminrestes in Position 4 des Hormones durch Leucin oder Isoleucin gemeinsam haben, kompetitiv gehemmt. Der stärkste Antagonist der Serie ist [2,4-diisoleucin]-Oxytocin und die antagonistische Aktivität nimmt in der Reihenfolge [4-Leucin]-, [2-Isoleucin-4-leucin]-, [2,4-Dileucin]- und [2-Phenylalanin-4-leucin]-Oxytocin ab. Die Resultate werden an Hand der Oxytocinkonformation diskutiert.

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Supported by United States Public Health Service grants No. AM-13567 (RW), by the Life Sciences Foundation, Inc., and by the National Science Foundation No. GB-30716X (VJH).

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Neurohypophyseal hormone analogs are denoted in accordance with the IUPAC-IUB [Tentative Rules (Biochemistry6, 362, 1967)].     

The smooth endoplasmic reticulum as a possible storage site for dendritic dopamine in substantia nigra neurones.

In dendrites of the substantia nigra neurones the monoamine marker 5-hydroxydopamine injected intracerebrally was localized inside of smooth endoplasmic reticulum cisterns. This observation opens the possibility of the existence of an alternative site for dopamine storage in dendrites as opposed to the well-known vesicular storage.     

Effects of penfluridol on dopamine-sensitive adenylate cyclase in corpus striatum and substantia nigra of rats

Summary Penfluridol, a neuroleptic with diphenylbutyl piperidine structure, blocked the dopamine-sensitive adenylate cyclase in homogenates of corpus striatum and substantia nigra of rats, probably by a competitive antagonism versus dopamine.Acknowledgment. We thank Dr P. Janssen (Beerse, Belgium) for a generous gift of penfluridol.     

Cyclic nucleotides vs. adenosine analogs as inhibitors of adenylate cyclase activity: Nonidentity of sites of action

Zusammenfassung Substitution einerN ⁶-Aminogruppe eines zyklischen Nukleotids führt zu einer erh?hten Hemmwirkung des Nukleotids gegenüber Adenyl-Cyclase von Meerschweinchenlungen, w?hrend dieN ⁶-Amino-Substition von Adenosin-Analogen eine herabgesetzte Inhibitionswirksamkeit gegenüber demselben Enzym zur Folge hat. Die experimentellen Daten führen zu dem Schluss, dass der Inhibitionsmechanismus gegenüber Cyclase für beide Verbindungstypen verschieden ist.      

Chemical synthesis of a hexadecapeptide segment of ubiquitin that activates adenylate cyclase and induces lymphocytes to differentiate.

A hexadecapeptide corresponding to positions 59--74 of ubiquitin was synthesized and purified. The peptide was characterized by its mobility in TLC and electrophoresis, amino acid sequence and composition, and molar rotation. The peptide possessed approximately 40% activity compared with native ubiquitin in each of 3 biological assays in vitro: a) thymocyte induction, b) B cell induction and c) elevation of intracellular cyclic AMP levels in sarcoma 180 cells.     

Endotoxin inhibits the fluoride-stimulated adenylate cyclase activity of rat liver plasma membranes enriched with bile canaliculi

Summary Escherichia coli endotoxin inhibited the fluoride-stimulated adenylate cyclase activity of liver plasma membranes enriched with bile canaliculi. Inhibition was of a mixed competitive and uncompetitive type. This effect, which may result from changes of membrane organization, may have relevance in the understanding of endotoxin-cell membrane interactions.     

Effects of adrenergic and cholinergic agonists on adenylate and guanylate cyclase activity of isolated guinea-pig seminal vesicle epithelium.

Isolated seminal vesicle epithelium of the guinea-pig contained increased amounts of cAMP and cGMP after treatment with PGE1 and carbachol, respectively. Adrenergic agents had no influence. Possible physiological implications of these results are discussed.     

Effects of the adenylate cyclase activator forskolin and its inactive derivative 1,9-dideoxyforskolin on insect cytochrome P-450 dependent steroid hydroxylase activity.

The adenylate cyclase activator forskolin and its pharmacologically inactive derivative 1,9-dideoxyforskolin were found to inhibit in a dose-dependent fashion the ecdysone 20-monooxygenase activity associated with wandering stage larvae of Drosophila melanogaster and fat body and midgut from last instar larvae of the tobacco hornworm, Manduca sexta. The concentrations of these labdane diterpenes required to elicit a 50% inhibition of the cytochrome P-450 dependent steroid hydroxylase activity in the insect tissues ranged from approximately 5 x 10(-6) to 5 x 10(-4) M.     

A rapid,sensitive method for the determination of follicle-stimulating activity

Riassunto Gli Autori riportano un nuovo metodo di saggio sul topo di piccole quantità di ormone follicolo stimolante (FSH), basato sulla riduzione intravaginale del cloruro di 2,3,5-trifeniltetrazolio cloruro (TTC). È cosi possibile determinare quantitativamente in sole 30 h dosi di FSH almeno 50 volte inferiori a quelle valutabili con i metodi fino ad oggi proposti.     

The relation between cell proliferation and adenylate cyclase activity in grafts of 3-methylcholanthrene induced mouse uterine cervical tumors

Summary In transplanted uterine cervical tumors, induced by 3-methylcholanthrene, a significant negative correlation was obtained between adenylate cyclase activity and cell proliferation.