The local anesthetic potency of norcocaine,a metabolite of cocaine

Summary The local anesthetic effects of cocaine and one of its main metabolites norcocaine, were investigated comparatively on isolated ganglion cells of the marine gastropod,Aplysia californica. During a 1-hour-period, different action potential parameters such as amplitude, duration, maximum rate of rise were observed, which demonstrated that norcocaine exhibits a higher local anesthetic potency than cocaine.Acknowledgments. The authors are grateful to Dr M. R. Klee and Dr M. R. Park for helpful discussion. The work was partly supported by Österreichischer Fonds zur Förderung der wissenschaftlichen Forschung     

Autoradiographic localization of testosterone-3H in the female rat brain and estradiol-3H in the male rat brain

Zusammenfassung Eine halbe Stunde nach der i.v. Injektion wurde Testosterone-³H von den Nerven- und Glialzellen innerhalb des Gehirns der weiblichen Ratte und Estradiol-³H innerhalb des Gehirns der männlichen Ratte aufgenommen. Zwei Stunden nach der Injektion war die Aufnahme in hohem Masse nur noch in gewissen Teilen des hypothalamisch-limbischen Systems vorhanden.

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This investigation was supported by grants from NASA (No. NsG 496) and the John A. Hartford Foundation to Dr.H.-L. Teuber, and from the U.S. Atomic Energy Commission to Dr.J. Altman, both of the Massachusetts Institute of Technology, and the work was performed while the author was at M.I.T.     

Identification of mucondialdehyde as a novel stress metabolite

In a survey of antifungal stress compounds induced by cupric chloride we found that leaves ofChenopodium album exuded a highly fungitoxic metabolite mucondialdehyde (trans-2,trans-4-hexadienedial), which was associated with 13-oxo-9,11-tridecadienoic acids (cis-9,trans-11 andtrans-9,trans-11 isomers) presumably resulting from -scission of 13-hydroperoxy-octadecadi(tri)enoic acid. The biogenesis and role as a general defensive agent in plants are briefly discussed.     

Identification of calcium antagonist receptor binding sites using (3H)nitrendipine in bovine tracheal smooth muscle membranes

Summary (³H)Nitrendipine binding to the bovine tracheal muscle membrane at 25°C was rapid, saturable (B_max=14.8±3.9fmol/mg protein) and of high affinity (K_d=0.15±0.04 nM). The rank order of Ca²⁺ antagonists competing for airway (³H)nitrendipine binding was nitrendipine nisoldipine nifedipine » verapamil. Cromolyn, however, neither inhibited nor increased the binding.J.B.C. is a visiting associate professor at the NYMMC. We thank Ms. Pang-jang Chang for technical assistance. This work is supported by a grant (NSC 72-0412-BO10-R20) from the National Science Council, ROC. To whom reprint requests should be addressed: Allergic Disease Center, Creighton University School of Medicine, Omaha, Nebraska 68178.     

Identification of calcium antagonist receptor binding sites using (3H)nitrendipine in bovine tracheal smooth muscle membranes

(3H)Nitrendipine binding to the bovine tracheal muscle membrane at 25 degrees C was rapid, saturable (Bmax = 14.8 +/- 3.9 fmol/mg protein) and of high affinity (Kd = 0.15 +/- 0.04 nM). The rank order of Ca2+ antagonists competing for airway (3H)nitrendipine binding was nitrendipine not equal to nisoldipine not equal to nifedipine much greater than verapamil. Cromolyn, however, neither inhibited nor increased the binding.     

Failure of carbon tetrachloride (CCl4) and trichlorobromo-methane (CCl3 Br) to alter polyribosomal profiles in the rat brain

Riassunto La disaggregazione dei polisomi di fegato di ratto trattato con CCl₄ o CCl₃Br non é riproducibile nei polisomi di cervello, neppure in animali pretrattati con fenobarbital.     

Feeding induced by blockade of histamine H1-receptor in rat brain

Histamine antagonists were infused into the third ventricle of the cerebrum in rats. All the H1-, but none of the H2-antagonists tested, induced initial feeding during the early portion of the light phase when histamine level was highest. No periprandial drinking was observed. Ambulation increased during feeding. The effect on feeding was attenuated when brain histamine was normally low during the early portion of the dark phase, or was decreased by alpha-fluoromethylhistidine. Hypothalamic neuronal histamine may suppress food intake through H1-receptors, and diurnal fluctuations of food intake may mirror neuronal histamine levels.     

Feeding induced by blockade of histamine H1-receptor in rat brain

Summary Histamine antagonists were infused into the third ventricle of the cerebrum in rats. All the H₁-, but none of the H₂-antagonists tested, induced initial feeding during the early portion of the light phase when histamine level was highest. No periprandial drinking was observed. Ambulation increased during feeding. The effect on feeding was attenuated when brain histamine was normally low during the early portion of the dark phase, or was decreased by -fluoromethylhistidine. Hypothalamic neuronal histamine may suppress food intake through H₁-receptors, and diurnal fluctuations of food intake may mirror neuronal histamine levels.     

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 structure determination of a novel C17 metabolite from streptomyces X-537 using Eu (DPM)3

Zusammenfassung Die Struktur destrans-6-[2-(1-hydroxybutyl)-4-tolyl]-hex-5-enamids (I), eines neuen mikrobiellen Metaboliten, wurde durch Protonenresonanz-Spektroskopie unter Verwendung des Verschiebungsreagenz Eu (DPM)₃ bestimmt.     

Increase in in vivo (3H) spiperone binding in the rat hippocampal formation and striatum after repeated treatment with haloperidol

Summary An increase in in vivo (³H) spiperone binding was observed in rat hippocampal formation and striatum after repeated treatment with haloperidol. This suggests that in hippocampus as well as in striatum prolonged blockade of dopaminergic transmission by a neuroleptic agent results in the development of a supersensitivity of the dopamine receptors.Acknowledgments. We wish to thank Mrs J. Krauss for skillful technical assistance, Drs Helmut Bittiger and Rainer Ortmann for helpful discussions.     

Binding of [3H]GABA and [3H]muscimol to subcellular particles of a neurone-enriched culture of mouse brain

Summary Binding of [³H]GABA and [³H]muscimol, indicative of GABA-receptors, has been demonstrated in a neurone-enriched culture of embryonic mouse brain using a ligand-binding technique. Evidence is provided for the existence of different populations of GABA-receptors.This study was supported by C.N.R.S., ATP N^o 3356 and by Commissariat à l'Energie Atomique, Departement of Biologie. Thanks are due to Mlle Marie-Anne Frenkel for her excellent technical assistance.