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Wonder what substances contain this stuff


#1

Quinolines Ligand Pharmaceuticals Inc was one of the first companies devoted to the development of steroid receptor modulators. In the mid 1990s it established a series of patents on bi-, tri- and tetracyclic quinoline-based scaffolds as the basis for the developmentof SARMs [101-108]. For example,tetrahydropyridinoquinolines (5; Figure 3) and several related derivatives exhibited potent AR agonist activity. The tetrahydropyridinoquinoline LG-121071 had a Ki value for AR binding of 13 nM and an AR agonist EC50value of 7 nM that was 74% as efficient as DHT. The in vivo activity of LG-121071 was tested in the Hershberger assay with castrated rats [58]. Following castration, luteinizing hormone (LH) levels increased dramatically and restoration of androgenic activity with testosterone suppressed LHlevels by negative feedback at the level of thehypothalamus/pituitary. The administration of LG-121071 (20 mg/kg, po) daily for 2 weeks restored normal levels of LH in castrated rats [59]. By comparison, subcutaneoustestosterone propionate suppressed castration-inducedelevation of LH levels in male rats at a dose of 1 mg/kg.Pfizer subsequently claimed this chemical preparation and reported a much higher AR binding affinity for the (-)-enantiomer of LG-121071 (IC50= 5 nM) than the (+)-enantiomer (IC50= 112 nM) [109]. The AR antagonistic activity of this class of compounds wasdetermined in vivo. An AR antagonist and testosterone propionate (1 mg/kg) were co-administered daily for 3 daysto immature rats or for 2 weeks to adult rats. Serum LH levels and weights of the androgen-dependent, ventralprostate and seminal vesicles were determined as endpoints.In this assay, the LG-121071-related compounds with R1 = CH3, R2,3 = CH3and R1= H, R2,3= [b]CH3caused significantinhibition of ventral prostate and seminal vesicle growth at 20 and 40 mg/kg, when given orally [60]. These effects were comparable to the effects of the prototypic AR antagonists flutamide and bicalutamide. However, in contrast to these known antagonists, neither test compound caused significant changes in serum LH or testosterone levels


#2

dude that s not even english, i couldnt even tell what s the name of the substance in that artcile