Opposite effects ofβ-adrenoceptor stimulation and 8-bromo-cyclic AMP on potassium efflux in mammalian heart muscle

Summary -adrenoceptor stimulation by isoprenaline increases the potassium efflux in beating guinea-pig atria. This effect is not mimicked by 8-bromo-cyclic AMP, a cyclic AMP analogue which exerts a positive inotropic effect in this preparation.     

The effect ofβ-adrenergic stimulation and blockade on the efflux of PGE1-like material from the isolated perfused rabbit heart

Summary Prostaglandin (PG) release was measured from the isolated perfused rabbit heart. The effects of -adrenergic stimulation and blockade suggest that PG synthesis is regulated in part by adrenergic mechanisms.     

An investigation of the interaction between isoniazid and the contraceptive steroid norethindrone in vivo

Summary Isonicotinic acid hydrazide (isoniazid) was shown to react readily with 17-ethinyl-17-hydroxyestr-4-en-3-one (norethindrone) to form the isonicotinyl hydrazone of the steroid under conditions likely to exist in the stomach. The hydrazone was detected in guinea-pig, but not rat, plasma following its oral administration. Rat liver tissue metabolized the compound more rapidly than guinea-pig liver in vitro which probably accounts for the failure to detect the hydrazone in rat plasma.     

Inhibition of rat liver glutamine synthetase by phosphonic analogues of glutamic acid

Summary Analogues of glutamic acid, -methylglutamic acid and glutamine in which the -or -COOH groups are replaced by PO₃H₂ or P(O)(OH₃)OH functions competitively inhibit rat liver glutamine synthetase. The K₁ values are comparable to or lower than K_M for L-glutamate.This study was supported by grant R.1.9.     

Failure of somatostatin to influence experimental tumor cell growth in vivo and in vitro

Summary The influence of somatostatin on tumor cell growth was studied in vivo in mice (sarcoma 180 ascites tumor and Lewis lung tumor) and in vitro on nontransformed and polyoma-transformed cell lines. 4 or 20 g/100 g of cyclic somatostatin and 4 g/100 g of linear protamin Zn-bound somatostatin were injected s.c. twice daily in the in vivo study. Cyclic somatostatin (1, 4 or 10 g/ml) was added twice daily to the cell cultures. Somatostatin administration influenced neither the survival of animals nor the growth rate of cultured cell lines. *** DIRECT SUPPORT *** A2025117 00011     

Inhibitory tripeptide,Lys-Phe-Tyr,as a fragment of physalaemin

Summary Several peptides were separated from-chymotrypsin-treated physalaemin by high voltage paper electrophoresis, and inhibition of the excitability of a molluscan giant neurone (tonically autoactive neurone) by the tripeptide, Lys-Phe-Tyr, was demonstrated.We thank Dr Sadaaki Iwanaga of Osaka University and Dr Atsuo Inoue of Daiichi Pharmaceutical CO for their helpful advice and the donation of the tripeptide (Lys-Phe-Tyr).     

Synthetic identification as a hexapeptide of alpha substance-IB inducing sexual agglutination in Saccharomyces cerevisiae.

For the identification of a peptidyl principle inducing sexual agglutination in the yeast, 2 supposed hexapeptides (1a, b) were synthesized by the conventional method. The 1a (H-Arg-Gly-Pro-Phe-Pro-Ile-OH) revealed complete identity with the natural peptide in TLC, MS and biological property on agglutination. The 1b showed the sexual agglutinability in the same degree as 1a, though distinct differences were observed in the chemical data. Both 1a and 1b had a strong bitter taste.     

In vivo effects of Escherichia coli endotoxin on sulfobromophthalein clearance in the guinea-pig.

In vivo studies indicated that the primary effects of E. coli endotoxin on hepatic clearance of sulfobromophthalein were at the excretory level. Newborns were more sensitive to the LPS than older animals.     

The effect of dehydration on the neurohypophyseal blood flow in rats with hereditary diabetes insipidus

Summary Neurohypophyseal blood flow increases in water-deprived rats. This increase is independent of vasopressin release, since it occurs even in rats with hereditary defect of hypothalamic vasopressin synthesis.Acknowledgment. The technical assistance of D. Vilimovská is acknowledged.     

Model of the effect of 4-aminopyridine at the level of potassium channels of the giant axon of the squid, Logigo forbesi L.]

Most of the effects of 4-aminopyridine on the potassium conductance of the giant axon of the Squid can be explained in terms of a simple model based on the physicochemical properties of the molecule and what is known about the structure of the potassium "channels".