Effects of 1-alkyl-1,2,3,4-tetrahydrocarbazole-1-ethanamines and related compounds,potential antidepressants,on biogenic amine uptake mechanisms

Summary A new series of compounds structurally related to the potential antidepressant tandamine, i.e., the 1-alkyl-1,2,3,4-tetrahydrocarbazole-1-ethanamines, inhibit the noradrenaline uptake mechanism and are relatively ineffective in inhibiting the serotonin uptake mechanism in vivo. The potency of the most effective compound (9-ethyl-N,N, 1-trimethyl-1,2,3,4-tetrahydrocarbazole is similar to that of desimipramine and is of potential use in the treatment of endogenously depressed patients.The authors acknowledge the technical assistance of Mrs J. Farnsworth, Mrs B. Gut and Mr J. Lacasse.     

The in vitro effect of adrenergic agents and related compounds on triglyceride levels of guinea-pig lymphoid cells.

Isoproterenol, epinephrine and norepinephrine were highly potent in decreasing the triglyceride levels of the splenic lymphoid cells from guinea-pigs in vitro, while they were quite inert upon the inguinal lymph node cells.     

l-DOPA administration to neonate chicks: Effects on behavior and levels of brain biogenic amines

Zusammenfassung Nachweis, dass bei Küken die i.v. Injektion vonl-Dopa (100 mg/kg) eine sofortige Überaktivität herbeiführt. Nach 10 min wurde im Gehirn eine Verminderung des Serotoningehaltes (14%) und eine Erhöhung des Dopamingehaltes (12fach) festgestellt, während Adrenalin, Noradrenalin und Histamin unverändert blieben.

---

---

The author (JPH) was supported in part by a National Science Foundation Predoctoral Traineeship.     

Effects of TA [4-ethoxy-1-(p-tolyl)-s-triazine-2,6-(1H, 3H)-dione] on growth,antheridium differentiation and gibberellin uptake of gametophytes ofAnemia phyllitidis L. Sw.

Summary Synergistic effects of TA on gibberellin-dependent reactions in spermatophytes are not detectable in gametophytes of the fernAnemia phyllitidis where gibberellin substitutes for antheridiogens with regard to induction of male sexual organs and dark germination. In this archegoniate TA caused a significant reduction in growth rate and morphogenesis of the gametophytes, inhibitions that were not abolished by simultaneous application of gibberellin.     

Antigastric secretory activity of 4-chloro-α,α-dimethylphenethylaminopropan-2-one and related compounds

Zusammenfassung AY-14,948 [4-Chlor-,-Dimethylphenethylaminopropan-2-on] setzt die basale Ausscheidung von Magensäure in der Ratte herab. Die Prüfung der strukturverwandten Verbindungen ergab, dass AY-18,672 [,-Dimethylphenethylaminopropan-2-on] in dieser Hinischt wirksamer ist als AY-14,948, indem es auch die reserpinbedingte Erregung der Magensäureausscheidung blockiert.     

The effect of the phytoalexins,lubimin, (−)-maackiain,pinosylvin, and the related compounds dehydroloroglossol and hordatine M on human lymphoblastoid cell lines

Summary We have tested the effect of the phytoalexins lubimin, (–)-maackiain and pinosylvin and the related compounds dehydroloroglossol and hordatine M on the growth of the human lymphoblastoid cell lines Molt and Raji. (–)-maackiain, pinosylvin and dehydroloroglossol showed significant growth inhibitory action on the cells. Suppression of [³H] thymidine and [³H] leucine uptake was tested and noted in pinosylvin and dehydroloroglossol. The phytoalexins and related compounds are widespread in plants and provide a potential source of antineoplastic substances.We would like to acknowledge the assistance of J. Hux in preparing the phytoalexins and related compounds. This work was supported by a grant from National Health and Welfare Canada. Correspondence to Dr. L. Skinnider, Department of Pathology, University of Saskatchewan, Saskatoon, Saskatchewan, Canada S7M OWO.     

The influence of inhibitors of amine metabolism on the effects of serotonin and its metabolites on photic evoked potential in rabbits

Resumen El estudio de la curva dosis-respuesta demuestra que el 5-hidroxi-triptofol y el acido 5-hidroxi-indolacético son tan potentes como la serotonina en modificar las respuestas corticales ópticas en el conejo. Pretratamiento con pargilina o con disulfiram, dos inhibidores distintos del metabolismo de las neuroaminas, influenció marcadamente los efectos de la serotonina sin cambiar los efectos de sus metabolitos.     

Inhibition of brain enolases by acrylamide and its related compounds in vitro,and the structure-activity relationship

Summary Acrylamide and its related compounds inhibited brain enolases in vitro independently of their neurotoxicity. The inhibitory potency was a function of the binding constants of the compounds for phenylalanine. The binding constant for tryptophan was higher in neurotoxic compounds than in non-neurotoxic ones.     

Inhibition of brain enolases by acrylamide and its related compounds in vitro, and the structure-activity relationship

Acrylamide and its related compounds inhibited brain enolases in vitro independently of their neurotoxicity. The inhibitory potency was a function of the binding constants of the compounds for phenylalanine. The binding constant for tryptophan was higher in neurotoxic compounds than in non-neurotoxic ones.     

Effects of levophacetoperane, pemoline, fenozolone, and centrophenoxine on catecholamines and serotonin uptake in various parts of the rat brain]

These drugs, except centrophenoxine, inhibit in vitro in a competitive manner, norepinephrin uptake in Rat hypothalamus and cortex, and dopamine uptake in corpus striatum and cortex, at higher concentrations than d.l. amphetamine; this alone inhibits serotonin uptake in hypothalamus.     

Effects of some membrane-active and other compounds on thrombin-induced platelet aggregation

Zusammenfassung Substanzen, welche die thrombin-induzierte Plättchenaggregation hemmen, lassen sich in drei Hauptgruppen aufteilen: 1. membranstabilisierende Steroide, 2. Substanzen, welche die elektrischen Eigenschaften der Membran oder die Permeabilität oder beide beeinflussen, und 3. Substanzen, die eine Erhöhung des intrazellulären cAMP-Spiegels bewirken sollen. Eine Hypothese über die Hemmung der Plättchenaggregation durch Thrombin wird vorgeschlagen.

---

---

Supported in part by Grants No. HE-01648 and No. HE-06350 from the National Heart and Lung Institute. Dr.Mason is a Markle Scholar in Academic Medicine and an N.I.H. Career Development Awardee.     

The effect of the phytoalexins, lubimin, (-)-maackiain, pinosylvin, and the related compounds dehydroloroglossol and hordatine M on human lymphoblastoid cell lines

We have tested the effect of the phytoalexins lubimin, (-)-maackiain and pinosylvin and the related compounds dehydroloroglossol and hordatine M on the growth of the human lymphoblastoid cell lines Molt and Raji. (-)-maackiain, pinosylvin and dehydroloroglossol showed significant growth inhibitory action on the cells. Suppression of [3H] thymidine and [3H] leucine uptake was tested and noted in pinosylvin and dehydroloroglossol. The phytoalexins and related compounds are widespread in plants and provide a potential source of antineoplastic substances.     

Cellular uptake of amelogenin,and its localization to CD63, and Lamp1-positive vesicles

Proteins of the developing enamel matrix include amelogenin, ameloblastin and enamelin. Of these three proteins amelogenin predominates. Protein-protein interactions are likely to occur at the ameloblast Tomes’ processes between membrane-bound proteins and secreted enamel matrix proteins. Such protein-protein interactions could be associated with cell signaling or endocytosis. CD63 and Lamp1 are ubiquitously expressed, are lysosomal integral membrane proteins, and localize to the plasma membrane. CD63 and Lamp1 interact with amelogenin in vitro. In this study our objective was to study the molecular events of intercellular trafficking of an exogenous source of amelogenin, and related this movement to the spatiotemporal expression of CD63 and Lamp1 using various cell lineages. Exogenously added amelogenin moves rapidly into the cell into established Lamp1-positive vesicles that subsequently localize to the perinuclear region. These data indicate a possible mechanism by which amelogenin, or degraded amelogenin peptides, are removed from the extracellular matrix during enamel formation and maturation. Received 27 September 2006; received after revision 24 November 2006; accepted 5 December 2006     

Influence in vitro of high-energy adenosine phosphates and related compounds on anaphylaxis of isolated smooth muscle

Zusammenfassung Im Schultz-Dale'schen Versuch wird festgestellt, dass Adenosin-Triphosphat und Adenosin-Diphosphat die anaphylaktische Reaktion verstärken.d-Glukose-6-Phosphat wirkt abschwächend, während Kreatin-Phosphat keinen Einfluss auf die Reaktion hat.     

Effects of tryptophan and other amino acids on glucose uptake and carbon dioxide output by the insulin-stimulated adipose tissue.

Tryptophan (4-10 mM) reduces the stimulating effect of insulin on glucose uptake, CO2 output and lactate production by adipose tissue. Similar but lesser effects were also obtained with high concentrations of other amino acids.     

Testing of LSD-25 and related compounds for possible effects on egg-laying capacity and egg-to-adult viability inDrosophila

Résumé On a injecté du LSD-25, de l'acide bromolysergique-diéthylamide et de l'acided-lysergique à desDrosophila pseudoobscura au troisième stade larvaire. Le LSD-25 n'affecte ni leur capacité de ponte, lorsqu'elles sont adultes, ni la viabilité (rapport numérique adultes/ufs) de leur progéniture. En revanche, la capacité de ponte est réduite tant par l'acide lysergique que par l'acide bromolysergique-diéthylamide, et ce dernier altère en outre la viabilité.