A facile one-step synthesis of cysteinyldopas using mushroom tyrosinase

Summary A convenient one-step procedure, based upon the tyrosinase co-oxidation of dopa and cysteine, is reported for the synthesis of 5-S-cysteinyldopa (I) in 74% yield. Secondary products of the reaction turned out to be 2-S-cysteinyldopa (II, 14%), 2,5-S, S-dicysteinyldopa (IV, 5%), and the hitherto unknown 6-S-cysteinyldopa (III, 1%).The generic term cysteinyldopa is proposed to designate the various cotechol amino-acids arising from addition of cysteine to dopaquinone.This work was supported in part by a grant from Consiglio Nazionale delle Ricerche, Roma.     

N-(5′-Phosphopyridoxyl)-4-aminobutyric acid: a stable bisubstrate adduct inhibitor of rat brain 4-aminobutyric acid aminotransferase

Summary N-(5-Phosphopyridoxyl)-4-aminobutyric acid, a stable adduct of pyridoxal phosphate and 4-aminobutyric acid, has been shown to be a potent inhibitor of rat brain 4-aminobutyric acid aminotransferase (GABA-T) with a K_i of 1.4 M.Acknowledgments. This work was supported in part by the United Parkinson Foundation, l'Association Canadienne l'Ataxie de Friedreich, and the Medical Research Council of Canada.     

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".     

An electrophoretic investigation of the binding of 3-14C coumarin to rat serum proteins

Summary The binding of coumarin to serum proteins of the rat has been demonstrated. Of the total bound coumarin (37% of injected dose), 36% was bound to the slow and fast ₁ globulins, 11% to the post albumins, 10% to globulin and 9% to albumin.     

The metabolism of the male antifertility agent 1-amino-3-chloropropan-2-ol in the rat

Summary The male antifertility agent 1-amino-3-chloropropan-2-ol (ACP,I) has been shown to be metabolized to-chlorohydrin (III) and metabolites of-chlorohydrin. This accounts for the similar antifertility and renal toxicity effects of both compounds.     

A tissue-selective prostaglandin E2 analog with potent antifertility effects

Summary N-methanesulfonyl 16-phenoxy--tetranor PGE₂ is a prostaglandin analog which is markedly more tissue selective than PGE₂. This compound is 10–30 times more potent than PGE₂ in animal models which are considered relevant to antifertility effects in humans. In pharmacological tests which are believed to be predictive for side effects in humans, the compound has potency either equal to or less than that of PGE₂.     

Effects of cerebral lateral,ventricular infusions of phloridzin on feeding and body weight in Gallus domesticus (L.)

Summary Contrary to earlier findings in rats, cerebral lateral ventricular infusions of 1×10^–3 M or 2×10^–3 M solutions of phloridzin at a rate of 2.5 l/min for 90 min had no significant stimulating effects on food intake and weight gain in hens and cocks. These different responses to intraventricular phloridzin might reflect a difference of sensitivity to the inhibitory action of phloridzin on glucose transport in cerebral cells or certain peculiarities of mechanisms controlling food intake in chickens.     

Transposable genetic elements as agents of gene instability and chromosomal rearrangements.

Transposable genetic elements in prokaryotes and eukaryotes, when inserted at a given locus, can control expression of the locus and cause large scale rearrangements of adjacent DNA sequences. Striking similarities in genetic behaviour between the two groups of elements have led to the proposal of a molecular model of eukaryotic controlling elements, and to suggestions about the part such elements may play in evolution and differentiation.