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.

Organophosphate ester derivatives of heterocyclic compounds and process

Abstract: An organophosphate ester having the formula ##SPC1## substituted Wherein A represents a divalent radical selected from the group consisting of alkylene having three to five carbon atoms, aza substitued alkylene having three to five carbon atoms in the chain and thia substituted alkylene having three to five carbon atoms in the chain, Y' represents a member selected from the group consisting of hydrogen, alkyl having one to six carbon atoms, cyano, halo and alkylthio having one to six carbon atoms, X represents a member selected from the group consisting of sulfur and oxygen, R1 " represents an alkyl having one to four carbon atoms, R2 " represents a member selected from the group consisting of alkyl having one to four carbon atoms, alkoxy having one to four carbon atoms, alkoxyalkoxy having one to four carbon atoms in each alk, and ##SPC2## Where R1 ' and R2 ' are members selected from the group consisting of hydrogen and alkyl having one to three carbon atoms; as well as the process of producing said organophosphate esters. The compounds have insecticidal and acaricidal properties.

The antiandrogen anandron potentiates the castrating effect of the LH-RH agonist buserelin in the rat.

Abstract: When buserelin (0.04-25 micrograms/kg/day), a potent LH-RH agonist, was administered s.c. daily for 15 days to male rats, prostate weight decreased after a transient increase in the first days of treatment but never as much as after orchidectomy, since testosterone secretion was never totally suppressed. The combination of the pure nonsteroid antiandrogen Anandron (20 mg/kg/day) with even low doses of buserelin led to an immediate decrease in prostate weight that was complete at 15 days. This could be explained (a) by an additivity of effects: inhibition by Anandron of the action of residual testosterone unsuppressed by buserelin on the prostate and prevention by buserelin of the rebound testosterone increase induced by Anandron: (b) by a potentiation by Anadron of the direct castrating effect of buserelin on the testis since testis weight and testosterone secretion were lowered to a greater extent by the combination than by buserelin alone. Anandron might increase the sensitivity of LH-RH receptors to LH-RH agonist in the testes, as has been shown in the pituitary. In contrast, the combination of the antiandrogenic steroid progestin, cyproterone acetate, with buserelin never potentiated the castrating effect of buserelin on testis weight and testosterone and only partially potentiated prostate atrophy. If such actions also exist in the human, the addition of Anandron to LH-RH agonist treatment would not only counter flare-up and adrenal androgen effects on the prostate but would also lower the doses of peptide or the time required for chemical castration.