New Nonsteroidal Molecules as Blockers of the Steroidogenic Pathway

    January 2022 in “ Current Enzyme Inhibition ”
    Jhoan Piermattey, Maicol Ahumedo, Yvonne Heuze, Juan Rodríguez Soriano, Marisa Cabeza
    Image of study
    TLDR New nonsteroidal molecules can potentially increase dihydrotestosterone in neurons by blocking certain enzymes, without affecting prostate and seminal vesicle weight.
    The research examined the biological activity of new nonsteroidal derivatives of 2-aminonaphthalene-1,4-dione as inhibitors of the aldo-keto reductase 1 enzymes (AKR1C1, AKR1C2). The synthesized derivatives, 2-amino-3-iodonaphthalene-1,4-dione and 2-(iodoamino)-3-methylnaphthalene-1,4-dione, inhibited AKR1C1 and AKR1C2 enzyme activity with IC50 values of 420 nM and 1.95 μM, and 300 nM and 1.52 μM, respectively. They also prevented the formation of 3α and 3β-androstanediols but did not bind to androgen receptors or reduce prostate and seminal vesicle weight. The study concluded that these derivatives could potentially be used therapeutically via direct nasal administration in aged patients to increase dihydrotestosterone in neurons by inhibiting AKR1C1 and AKR1C2 enzyme activity, leading to the accumulation of dihydrotestosterone in androgen-dependent glands.
    Discuss this study in the Community →

    Research cited in this study

    3 / 3 results

    Related Community Posts Join

    6 / 48 results

      community KX-826 Pyrilutamide1% coming soon

      in Update  152 upvotes 3 months ago
      KX-826 Pyrilutamide 1% is launching soon, and users are discussing its potential benefits and drawbacks compared to other treatments like Minoxidil and finasteride. Some users are skeptical about its effectiveness, while others are hopeful it will be a safer alternative.

      community Topical finasteride now the safest possible path?

      in Finasteride/Dutasteride  72 upvotes 4 months ago
      Topical finasteride is considered a safer option for hair regrowth with fewer systemic side effects compared to oral finasteride. Some users report similar efficacy and side effects between topical and oral treatments, while others prefer topical due to reduced systemic exposure.

      community Anyone else crying themselves to sleep because of the pyrilutamide fail?

      in Technology  43 upvotes 11 months ago
      The conversation is about disappointment with pyrilutamide's performance as a hair loss treatment, with some users expressing interest in other treatments like Verteporfin, GT20029, and RU58841, while others suggest sticking with established treatments like finasteride or dutasteride.

      community Binding affinity of pyrilutamide!

      in Update  168 upvotes 2 years ago
      Pyrilutamide, a nonsteroidal antiandrogen drug under development for the potential treatment of androgenic alopecia. The conversation discusses its binding affinity to the androgen receptor and the timeline for possible availability after trials are completed in the United States and China.

    Related Research

    1 / 1 results