Roussel Uclaf

About: Roussel Uclaf is a based out in . It is known for research contribution in the topics: Alkyl & Alkoxy group. The organization has 1888 authors who have published 2338 publications receiving 36508 citations.

Interactions between hydralazine, propildazine and purines on arterial smooth muscle

Abstract: 1 The interaction of hydralazine (Hyd) and propildazine (Pyd) with purine compounds was studied in the isolated tail artery from normotensive Wistar (NW) rats. 2 Exogenously added purines inhibit non competitively the antispasmogenic response to Hyd in denervated NW segments. The order of potency is 2-Cl-adenosine > adenosine > adenosine 5′-triphosphate (ATP) > inosine. Pyd action is modified only by the most active purine 2-Cl-adenosine, which displaces the dose-response curves to the right. Hyd and Pyd seem to act on the same site, since their maximal effects are not additive. 3 Theophylline (Theo) 50 μM induces the appearance of the antispasmogenic effect of Hyd in the usually poorly responsive innervated proximal NW arterial segments. The potentiating action of Theo is identical to the enhancement of the Hyd response observed after 6-hydroxydopamine denervation. This result suggests that the release of endogenous purines from sympathetic nerves is sufficient to block the smooth muscle responses to Hyd, under our experimental conditions. A similar potentiating effect is obtained with propranolol (5 μM). 4 The spontaneous release of 3H, after loading with [3H]-noradrenaline, was considered as an indirect indication of purine leakage from nerve terminals. There is an inverse relationship between the rate of 3H release, under these conditions, and the magnitude of the relaxant response to Hyd, i.e., 3H leakage is higher in proximal NW segments. 5 The most satisfactory explanation for the interaction of Hyd and Pyd with exogenous purines, and for the modulating actions of sympathetic nerve terminals, is that both antihypertensives act on a common receptor, sensitive to endogenous ATP and adenosine.

Monoclonal antibodies to human interleukin-1 beta and their use in a sensitive two-site enzyme linked immunosorbent assay.

Abstract: Five Monoclonal Antibodies (MAbs) coded respectively #111, 122, 206, 209 and 609 were produced against human recombinant Interleukin-1 beta (rIL-1 beta, amino acids 117-269). Four of these MAbs (#111, 122, 206 and 609) have been identified able to inhibit the biological activity of recombinant and natural Interleukin-1 beta. Competition studies suggested that three non-overlapping epitopes of the molecule were recognized by the MAbs. MAbs #609 and 206 have been selected on the basis of high affinity and used together in a two-site ELISA to detect IL-1 beta. The sensitivity of this ELISA was 1 pg/well (10-20 pg/ml). The assay did not detect rHuIL-1 alpha, rHuIL-2, rHuTNF-alpha, rHuIFN-gamma, rHuIL-6, and natural a- and b-FGF. The immunoassay was then compared to current assay such as co-mitogenic effect on murine thymocytes for detection of IL-1 beta in the intra- and extracellular compartments of IFN-gamma and/or LPS-stimulated human blood monocytes. We confirm that IFN-gamma potentiates IL-1 beta secretion in response to LPS (even with high dose 1 microgram/ml) but not the intracellular precursor of IL-1 beta. This immunoassay could be used also to detect IL-1 beta in plasma, sera and synovial fluids.

Derivatives of 3-amino-pregn-5-ene

Abstract: A compound selected from the group consisting of: 3-amino-Δ5 -pregnenes of the formula I: ##STR1## wherein X is selected from the group of ##STR2## the wavy lines indicate that the group may be in the α-or β-position, R1 is selected from the group consisting of hydrogen and hydroxyalkyl or 2 to 5 carbon atoms, R2 is selected from the group consisting of hydrogen, hydroxyalkyl of 2 to 5 carbon atoms, acyl of an aliphatic carboxylic acid of 3 to 8 carbon atoms, alkoxycarbonyl of 2 to 8 carbon atoms, acyl of an α-amino-carboxylic acid or from a peptide of 2 to 3 amino acids of which amines may be either unsubstituted or mono-or disubstituted with alkyl of 1 to 5 carbon atoms with the proviso that R1 and R2 are not both hydrogen and that if the 3-amino group is in the β-position, (i) when X is ##STR3## R1 and R2 are not both hydroxyethyl or (ii) when X is ##STR4## and R1 is hydrogen, R2 is not ethoxycarbonyl, the compound of the formula I wherein X is ##STR5## R1 is hydrogen and R2 is methyl, the 3-amino group is in the α-position and their non-toxic, pharmaceutically acceptable acid addition salts which are useful as stimulants of the mammalian immune system.