Some aspects of the NMR-spectra of aporphine and phenanthrene alkaloids

Summary The C-11 proton of an aprophine possessing a C-1,2 methylenedioxy group falls relatively upfield between 7.47 and 7.86. Additionally, the i.c.s. for the two protons of the methylenedioxy group is large (4–12 Hz). The presence of a methylenedioxy at C-3,4 in a phenanthrene alkaloid also results in an upfield shift ( 8.95–9.00) of the C-5 proton.This project was supported by NIH research grant No. HL-12971, awarded by the National Heart and Lung Institute, PHS/DHEW.     

Effect of heat treatment on the ATPase activity of various sarcoplasmic reticulum preparations.

Ca2+-stimulated ATPase activity of sarcoplasmic reticulum (SR) preparations is activated after a short period of preincubation at temperatures between 40 and 45 degrees C, but for temperatures higher than 48 degrees C pronounced denaturation is observed. Heat denaturation is decreased if Mg2+ or K+ are present during heat treatment.     

Pyrogen fever in rabbits pretreated with p-chlorophenylalanine or 5, 6-dihydroxytryptamine.

The hyperthermic effect of a bacterial pyrogen has been studied in rabbits pretreated or not with p-chlorophenylalanine or 5, 6-dihydroxytryptamine. The results obtained indicate that a selective reduction of cerebral 5-hydroxytryptamine levels by these drugs do not significantly affect pyrogen hypertermia.     

Beta-adrenergic receptors in rat myocardium: Direct detection by a new fluorescent beta-blocker

Summary A new fluorescent -blocker, 9-amino-acridin propranolol (9-AAP), was administered i.v. to rats. Multiple fluorescent 9-AAP binding sites were observed on cardiac muscle cells in frozen sections. Intensity and density of cardiac 9-AAP fluorescence were markedly reduced following pretreatment with (±)- and (–)-propranolol but not with (+)-propranolol. Our findings suggest that 9-AAP may label -adrenergic receptor sites in rat myocardium.D. A. is supported by a fellowship from the Lady Davis Fellowship Trust and by a Research Grant from the Bat-Sheva de Rothschild Fund for The Advancement of Science and Technology. The technical assistance ofA. Itzhak is gratefully acknowledged.     

Alpha-receptor subsensitivity of isolated atria from rats following repeated injections of phenylephrine or isoprenaline

Summary Daily injections of phenylephrine or isoprenaline for 4 or 7 days lowered the chronotropic sensitivity of -adrenoreceptors in isolated rat atria.This study was supported by grants from the National Science Council of Finland.     

Effect of X-537A on the phosphorylated protein in sarcoplasmic reticulum vesicles

Summary The effect of the antibiotic X-537A on the phosphorylated ATPase (EP) was investigated. The results show that X-537A depresses the level of EP which is dependent on the Ca²⁺ gradient, while the Ca²⁺-independent EP is not affected. Acknowledgments. This work was supported by grants from the Instituto de Alta Cultura of the Portuguese Ministry of Education (No. CB/2) and the Calouste Gulbenkian Foundation.     

Regulation of enzymes of ethanol metabolism in yeast (Rhodotorula gracilis)

Summary The three enzymes of ethanol metabolism alcohol dehydrogenase, aldehyde dehydrogenase and acetyl-CoA synthetase in the obligate aerobic yeastRhodotorula gracilis are repressed by glucose and induced by C₂ metabolic fuels with a regulatory pattern indicating a correlation in the control mechanisms. To try an identification of the molecular signals involved in the transmission of the inducing stimulus, experiments were carried out by blocking with 2 mM pyrazole the ethanol acetaldehyde metabolic step. Results indicate that ethanol is not specifically required as a molecular signal for induction.This work was supported by a grant from the Italian Consiglio Nazionale delle Ricerche.     

DDT: The degradation of ring-labeled14C-DDT to14CO2 in the rat

Summary Ring fission ofp, p-DDT was studied in the rat following a single oral dose of 0.74 mg/kg (1.04 Ci) of uniformly ring-labeled¹⁴C-DDT. Expired air was passed through a solution of ethanolamine-ethylene glycol monomethyl ether (12) to trap¹⁴CO₂. A total of 1.6% of the radioactivity administered was recovered in the expired air collected continually for 10 days, indicating that while degradation of the phenyl moiety is not a major route pfp, p-DDT metabolism in the rat, it is equal to the urinary excretion. Nevertheless, these results represent the most radical change accomplished in vivo of a residual insecticide yet reported in mammals.Acknowledgment. We acknowledge the secretarial work of Ms.Elaine Smolko. This study was supported by NIH fellowship No. 1 F22 ES01723-01 and No. HL16264.     

Struktur-Wirkungsbeziehungen beim menschlichen Calcitonin. III. Die biologische Aktivität verkürzter oder an den Kettenenden modifizierter,synthetischer analoger

Summary Assays of 8 synthetic analogues of human calcitonin in rats showed that their hypocalcaemic activity was drastically reduced by deletion of the C-terminal amide group, chain-shortening or opening of the disulphide ring, but unaffected or enhanced by modification of the N-terminal amino group.

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II. vgl.R. Maier, B. Kamber, B. Riniker andW. Rittel, Hormon. Metab. Res.7, 511 (1975).

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Die hier verwendete, abgekürzte Schreibweise für Peptide folgt den Empfehlungen der IUPAC-IUB Kommission für Biochemische Nomenklatur, J.B.C.247, 977 (1972). Weitere Abkürzungen: HCT, Human-Calcitonin; PCT, Schweinecalcitonin; Bmp, -Mercaptopropionsäure (Desaminocystein); NMet, Normethionin (S-Methylcystein); -OMe, Methylester.