Chemistry:4-Androstadienol
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| Other names | 3β-Androsta-4,16-dien-3-ol, androsta-4,16-dien-3β-ol, androstadienol |
| Routes of administration | Intranasal |
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| Formula | C19H28O |
| Molar mass | 272.432 g·mol−1 |
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4-Androstadienol (developmental code name PH94B; tentative commercial name Aloradine or Aloradine IN), also known as 4,16-androstadien-3β-ol, is a pherine which is under development by VistaGen Therapeutics,[1][2] Inc. in a nasal spray formulation (PRN) for the acute treatment of social anxiety disorder.[3][4][5][6][7][8][9][10] It is also being investigated by VistaGen Therapeutics for the treatment of generalized anxiety disorder (GAD) and post-traumatic stress disorder (PTSD).[11][12] The pherine is a positional isomer of the endogenous pheromone androstadienol (5-androstadienol or 5,16-androstadien-3β-ol). As of 2020, it is in phase III clinical trials for social anxiety disorder.[13]
4-Androstadienol lacks affinity for steroid hormone receptors and has instead been found to directly activate isolated human vomeronasal receptor cells at nanomolar concentrations (EC50 = 200 nM).[9]
The pheromone androstenol has been found to act as a potent positive allosteric modulator of the GABAA receptor, and it has been proposed that this action may mediate its pheromone effects.[14] It produces anxiolytic-like effects in animals.[14] Androstadienol, androstadienone, and androstenone, all of which are also pheromones, have been found to be converted into androstenol, and as such, it may be responsible for their pheromone effects.[14] As 4-androstadienol is very closely related structurally to androstadienol, 4-androstadienol might be converted into androstenol similarly and hence potentiation of the GABAA receptor could contribute to its mechanism of action.[14]
See also
References
- ↑ "VistaGen Therapeutics Acquires Worldwide License of Phase 3-Ready CNS Drug Candidate from Pherin Pharmaceuticals for As-Needed Treatment of Social Anxiety Disorder :: VistaGen Therapeutics, Inc. (VTGN)" (in en). https://www.vistagen.com/news-media/press-releases/detail/96/vistagen-therapeutics-acquires-worldwide-license-of-phase.
- ↑ "VistaGen nabs phase 3-ready social anxiety drug from Pherin" (in en). 13 September 2018. https://www.fiercebiotech.com/biotech/vistagen-nabs-phase-3-ready-social-anxiety-med-from-pherin.
- ↑ "FDA Grants Fast Track Designation to PH94B for Treatment of Social Anxiety Disorder". 10 December 2019. https://www.pharmacytimes.com/news/fda-grants-fast-track-designation-for-ph94b-for-treatment-of-social-anxiety-disorder.
- ↑ Harrison, Laird (11 April 2014). "Could a New Nasal Spray Help Combat Social Anxiety?". Healthline. http://www.healthline.com/health-news/nasal-spray-to-combat-social-anxiety-041114.
- ↑ "50 years of hurdles and hope in anxiolytic drug discovery". Nature Reviews. Drug Discovery 12 (9): 667–87. September 2013. doi:10.1038/nrd4075. PMID 23989795. PMC 4176700. http://ggriebel.chez-alice.fr/Pub127.pdf.
- ↑ "The human vomeronasal system". Psychoneuroendocrinology 19 (5–7): 673–86. 1994. doi:10.1016/0306-4530(94)90049-3. PMID 7938363.
- ↑ Rolls, Edmund T. (November 2013). Emotion and Decision Making Explained. Oxford University Press. pp. 356–. ISBN 978-0-19-965989-0. https://books.google.com/books?id=fZWcAQAAQBAJ&pg=PA356.
- ↑ BioScan. Oryx Press. 2009. https://books.google.com/books?id=L_5PAQAAIAAJ.
- ↑ 9.0 9.1 "Effect of an acute intranasal aerosol dose of PH94B on social and performance anxiety in women with social anxiety disorder". The American Journal of Psychiatry 171 (6): 675–82. June 2014. doi:10.1176/appi.ajp.2014.12101342. PMID 24700254. https://www.researchgate.net/publication/261511611.
- ↑ "Acute Treatment of Social Phobia" US patent 8722652, published 13 November 2012, assigned to Pherin Pharmaceuticals, Inc.
- ↑ "Generalized Anxiety Disorder :: VistaGen Therapeutics, Inc. (VTGN)" (in en). https://www.vistagen.com/pipeline/ph94b/generalized-anxiety-disorder.
- ↑ "Post-traumatic Stress Disorder :: VistaGen Therapeutics, Inc. (VTGN)" (in en). https://www.vistagen.com/pipeline/ph94b/post-traumatic-stress-disorder.
- ↑ "Positive Pilot Phase 3 Data Position VistaGen's PH94B Neuroactive Nasal Spray for Pivotal Phase 3 Development as a Novel, As-Needed Treatment for Social Anxiety Disorder :: VistaGen Therapeutics, Inc. (VTGN)" (in en). https://www.vistagen.com/news-media/press-releases/detail/117/positive-pilot-phase-3-data-position-vistagens-ph94b.
- ↑ 14.0 14.1 14.2 14.3 "The pheromone androstenol (5 alpha-androst-16-en-3 alpha-ol) is a neurosteroid positive modulator of GABAA receptors". The Journal of Pharmacology and Experimental Therapeutics 317 (2): 694–703. May 2006. doi:10.1124/jpet.105.098319. PMID 16415088.
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