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.

Angiotensin-converting enzyme in rat brain and extraneural tissues visualized by quantitative autoradiography using 3H-trandolaprilate.

Abstract: Tritium-labeled trandolaprilate (RU 44403), the active diacid form of the potent and long-acting angiotensin-converting enzyme (ACE) inhibitor trandolapril, has been evaluated as a new autoradiographic marker for the enzyme. The characteristics of 3H-trandolaprilate binding were first determined autoradiographically in tissue sections from rat brain (caudate-putamen) and kidney. 3H-Trandolaprilate binds saturably to these tissues, and with very high affinity (Kd values, 0.36 and 0.13 nM, respectively), and appears to show good selectivity for the enzyme. Due to its high affinity (approximately 100 times that of captopril), the performance of 3H-trandolaprilate as an autoradiographic marker is comparable to that of the recently described 125I-labeled derivative of lisinopril (125I-351A). Saturation and displacement studies in serial sections from a variety of central and peripheral tissues confirmed that the specificity of labeling was similar throughout. The anatomical distribution of ACE visualized with 3H-trandolaprilate in these tissues was close to that described for 3H-captopril and 125I-351A with some minor differences which might arise from difference in the specificity of the ligands.

Novel 11 β-alkynylphenyl-10-nor-steroids

Abstract: Novel 11β-alkynylphenyl-19-nor-steroids of the formula ##STR1## wherein R 1 is alkynyl of 2 to 8 carbon atoms optionally substituted with at least one member of the group consisting of --OH halogen, trialkylsilyl of 1 to 6 alkyl carbon atoms, alkoxy and alkylthio of 1 to 6 carbon atoms and dialkylamino of 1 to 6 alkyl carbon atoms having remarkably antiprogestomimetic and antiglucocorticoidal activity.

Precursors for cholesterol synthesis (7-dehydrocholesterol, 7-dehydrodesmosterol, and desmosterol): cholesterol/7-dehydrocholesterol ratio as an index of development and aging in PNS but not in CNS.

Abstract: In rat sciatic nerve, the 7-dehydrocholesterol content decreased dramatically during the postnatal period and slowly during adulthood and aging. In contrast, the 7-dehydrodesmosterol content peaked at 14 days and was nearly undetectable after 60 days. The desmosterol content peaked at 21 days and was nearly undetectable after 1 year. The cholesterol content increased up to 21 days and remained nearly constant thereafter. In brain (in contrast to sciatic nerve), 7-dehydrodesmosterol and desmosterol contents decreased dramatically during development and slightly during adulthood and aging; the 7-dehydrocholesterol content peaked at 21 days and remained constant during aging. Only 7-dehydrocholesterol was dramatically more concentrated in PNS than in CNS. In brain, the cholesterol/7-dehydrocholesterol ratio increased during development and remained stable after 6 months. In contrast, in sciatic nerve, this ratio continuously increased during development and aging (950-fold between 5 days and 18 months). Thus, the cholesterol/7-dehydrocholesterol ratio is a useful biochemical index of development and aging in the PNS.