5α-Androst-16-en-3α-ol (Synonyms: Androstenol, E 281, NSC 71076)

5α-Androst-16-en-3α-ol is a steroid pheromone that has been found in boar testes and human male axillary sweat and has diverse biological activities.^1,2 It enhances GABA-activated currents in primary mouse cerebellar granule cells (EC₅₀ = 0.4 µM).² 5α-Androst-16-en-3α-ol (0.1-1 µM) increases the amplitude of GABA-activated currents in HEK293 cells expressing human α₁β₂γ₂ and α₂β₂γ₂ subunit-containing GABA_A receptors. In vivo, 5α-androst-16-en-3α-ol (5-10 mg/kg) decreases immobility time in the forced swim test in mice. It increases time spent in the open arms of the elevated plus maze in mice, indicating anxiolytic-like activity, when administered at doses ranging from 30 to 50 mg/kg. 5α-Androst-16-en-3α-ol protects against seizures induced by pentylenetetrazole or electroshock in mice (ED₅₀s = 48.9 and 21.9 mg/kg, respectively).

1.Brooksbank, B.W., Brown, R., and Gustafsson, J.A.The detection of 5α-androst-16-en-3α-ol in human male axillary sweatExperientia30(8)864-865(1974) 2.Kaminski, R.M., Marini, H., Ortinski, P.I., et al.The pheromone androstenol (5α-androst-16-en-3α-ol) is a neurosteroid positive modulator of GABAA receptorsJ. Pharmacol. Exp. Ther.317(2)694-703(2006)