Ostwald solubility coefficients, L, have been determined for 37 gases and vapours in methylene iodide at 298 K, and have been correlated through equation (i). where the solute explanatory log L = -0.74 + 0.32R2 + 1.34~: + 0.83@ + 1.1 9 B + 0.87 log L"variables are R, an excess molar refraction, . n: the solute dipolarity/polarisability, a: and fl the solute hydrogen-bond acidity and basicity, and log L16 where L" is the solute Ostwald solubility coefficient on hexadecane at 298 K. Similar equations have been constructed for solvation of solutes in tetrachloromethane, trichloromethane and 1.2-dichloroethane using literature data. It is shown that polarisability effects favour solvation in methylene iodide, through the R, term, but that such effects enhance the solubility of polarisable solutes only moderately: thus the R, term contributes 0.4 log units more in methylene iodide than in trichloromethane for the solute benzene.

Selective androgen receptor modulators (SARMs) are an emerging class of therapeutics targeted to cachexia, sarcopenia, and hypogonadism treatment. LGD-4033 is a SARM which has been included on the Prohibited List annually released by the World Anti-Doping Agency (WADA). The aim of the present work was the investigation of the metabolism of LGD-4033 in a human excretion study after administration of an LGD-4033 supplement, the determination of the metabolites' excretion profiles with special interest in the determination of its long-term metabolites, and the comparison of the excretion time of the phase I and phase II metabolites. The results were also compared to those derived from previous LGD-4033 studies concerning both in vitro and in vivo experiments. Supplement containing LGD-4033 was administered to one human male volunteer and urine samples were collected up to almost 21 days. Analysis of the hydrolyzed (with β-glucuronidase) as well as of the non-hydrolyzed samples was performed using liquid chromatography-high resolution mass spectrometry (LC-HRMS) in negative ionization mode and revealed that, in both cases, the two isomers of the dihydroxylated metabolite (M5) were preferred target metabolites. The glucoconjugated parent LGD-4033 and its gluco-conjugated metabolites M1 and M2 can be also considered as useful target analytes in non-hydrolyzed samples. The study also presents two trihydroxylated metabolites (M6) identified for the first time in human urine; one of them was recently reported in an LGD-4033 metabolism study in horse urine and plasma. KEYWORDS human doping, LGD-4033, liquid chromatography-mass spectrometry, SARM, selective androgen receptor modulator

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