2. LDG-3303 effect and application prospects
As a latest SARM, LGD-3303 has potent activity against the levator ani muscle in a castrated rat model of androgen deficiency, but only partial agonist activity in the foreskin and ventral prostate. Although the plasma concentration of the compound increased, LGD-3303 never stimulated the ventral prostate beyond intact levels. When LGD-3303 was administered orally or by continuous infusion, tissue selective activity was maintained and the time of the two routes of administration was significantly different from the profile of exposure. Although the local tissue concentration of LGD-3303 is higher in the prostate than in the levator muscle, compared to greater muscle activity in the prostate. LGD-3303 has SARM properties that are independent of its pharmacokinetic characteristics, suggesting that the main mechanism of tissue-selective activity is the result of molecular interactions that change at androgen receptor levels.
Experimental materials and methods:
The selected compound was LGD-3303. LGD-3303 is a non-steroidal androgen receptor agonist that efficiently binds the androgen receptor and activates gene transcription. LGD-3303 has minimal binding or transcriptional activity on relevant nuclear receptors (Vajda , 2008). LGD-3303 was synthesized at Ligand Pharmaceuticals (San Diego, CA).