[2-(Octahydro-1-azocinyl)-ethyl]-guanidine sulfate (CIBA 5864-SU), a new synthetic antihypertensive agent

Résumé On décrit la chimie et la pharmacologie d'un nouvel agent antihypertenseur.     

1-(5-Methyl-1-phenyl-4-pyrazolyl)-3-[4-(o-tolyl)-piperazinyl]-1-propanone,a new synthetic antihypertensive agent

Zusammenfassung 1-(5-Methyl-1-phenyl-4-pyrazolyl)-3-[4-(o-tolyl)-piperazinyl]-1-propanone (I; CIBA 1002-Go), senkt an normotonischen und hypertonischen Tieren den Blutdruck. Die Drucksenkung kann auf eine periphere Vasodilatation und eine Hemmung hypothalamischer oder medullärer Vasomotorenzentren bezogen werden. Ausserdem wirkt CIBA 1002-Go adrenolytisch.

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Hydrochloride = CIBA 1002-Go.     

Oral anti-ulcer activity of a synthetic prostaglandin analogue (9-oxoprostanoic acid: AY-22,469)

Résumé AY-22,469, un analogue synthétique de la prostaglandine, inhibe les différents types d'ulcère développé chez le rat lorsqu'il est administré par voie orale.     

Effects of [N-(2-oxo-3,5,7-cycloheptatrien-1-yl)] aminooxoacetic acid ethyl ester (AY-25,674) on cyclic 3′,5′-nucleotide formation and phosphodiesterase activity

Summary The orally-effective antiallergic compound [N-(2-oxo-3,5,7-cycloheptatrien-1-yl)] aminooxoacetic acid ethyl ester (AY-25,674) exhibited a potency equivalent to or 3 times less than theophylline in inhibiting guinea-pig lung and beef heart PDE, respectively. AY-25,674 did not affect the basal activity of guinea-pig lung adenyl cyclase. Although part of the antiallergic activity of AY-25,674 may be due to the ability to elevate cyclic AMP levels by PDE inhibition, other modes of action appear to be of greater relevance.The authors acknowledge the excellent technical assistance of Ms M.T. Silvestre.     

Effects of [N-(2-oxo-3,5,7-cycloheptatrien-1-yl)] aminooxoacetic acid ethyl ester (AY-25,674) on cyclic 3',5'-nucleotide formation and phosphodiesterase activity.

The orally-effective antiallergic compound [N-(2-oxo-3,5,7-cycloheptatrien-1-yl)] aminooxoacetic acid ethyl ester (AY-25,674) exhibited a potency equivalent to or 3 times less than theophylline in inhibiting guinea-pig lung and beef heart PDE, respectively, AY-25,674 did not affect the basal activity of guinea-pig lung adenyl cyclase. Although part of the antiallergic activity of AY-25,674 may be due to the ability to elevate cyclic AMP levels by PDE inhibition, other modes of action appear to be of greater relevance.     

Evolution of vasopressins in marsupials: a new hormone, phenypressin (Phe2-Arg8-vasopressin), present in the Macropodidae

A duplication of the pressor hormone has been found in some marsupials, either American species belonging to the family Didelphidae or Australian species belonging to the family Macropodidae. Two pressor peptides, lysine vasopressin and phenypressin (Phe2-Arg8-vasopressin) have been chemically identified in the red Kangaroo (Macropus rufus) and the Tammar (Macropus eugenii). In contrast, the brush-tailed Possum (Trichosurus vulpecula), a species belonging to the family Phalangeridae, has a single pressor hormone, arginine vasopressin. Because this latter hormone was also found in a prototherian species, the Echidna, it might be assumed that it is the product of a primitive gene and that a duplication and subsequent mutations led to lysine vasopressin and phenypressin in Macropodidae.     

Synthesis of O1.5-(beta-D-galactopyranosyl) [DMet2, Hyp5] enkephalin amide, a new highly potent analgesic enkephalin-related glycosyl peptide

A new series of O-glycosyl enkephalins has been prepared, following a convergent strategy, with high chemical yields. The galactosyl analogue, O1.5-(beta-D-galactopyranosyl) [DMet2, Hyp5] enkephalin amide proved to be one of the most potent in vivo opioid agonists synthesized up to now.     

Effect of N-6 2'-O-dibutyryl adenosine 3'-5'monophosphate (dibutyryl cyclic AMP) on the condenstion of the X chromosome into the form of a Barr body]

Addition of exogen DB-c AMP in medium of human fibroblasts culture, with 46 XX karyotypes, enables us to observe a high frequency of Barr bodies, about 80 or 85%. This observation suggests that the condensation of the X chromosome in the form of Barr bodies depends on the level of endogen cyclic AMP.