4-Androstadienol

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4-Androstadienol
4,16-Androstadien-3β-ol.svg
Clinical data
Other names3β-Androsta-4,16-dien-3-ol, androsta-4,16-dien-3β-ol, androstadienol
Routes of
administration
Intranasal
ATC code
  • None
Identifiers
CAS Number
PubChem CID
DrugBank
ChemSpider
Chemical and physical data
FormulaC19H28O
Molar mass272.432 g·mol−1
3D model (JSmol)

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 for the acute (p.r.n.) treatment of social anxiety disorder[3].[4][5][6][7][8][9][10][11] It is also being investigated by VistaGen Therapeutics for the treatment of generalized anxiety disorder (GAD) and post-traumatic stress disorder (PTSD)[12][13] The pherine is a positional isomer of the endogenous pheromone andr"First Aid for Mental Health: 8 New and Investigational Drugs"ostadienol (5-androstadienol or 5,16-androstadien-3β-ol). As of 2019, it is in phase III clinical trials for social anxiety disorder.[14]

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.[15] It produces anxiolytic-like effects in animals.[15] 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.[15] 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.[15]

See also[edit]

References[edit]

  1. ^ "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)". VistaGen Therapeutics, Inc. Retrieved 2019-12-19.
  2. ^ "VistaGen nabs phase 3-ready social anxiety drug from Pherin". FierceBiotech. Retrieved 2019-12-19.
  3. ^ "FDA Grants Fast Track Designation to PH94B for Treatment of Social Anxiety Disorder". Pharmacy Times. Retrieved 2019-12-19.
  4. ^ Laird Harrison (11 April 2014). "Could a New Nasal Spray Help Combat Social Anxiety?". Healthline. Retrieved 23 May 2015.
  5. ^ Griebel, Guy; Holmes, Andrew (2013). "50 years of hurdles and hope in anxiolytic drug discovery" (PDF). Nature Reviews Drug Discovery. 12 (9): 667–687. doi:10.1038/nrd4075. ISSN 1474-1776. PMC 4176700. PMID 23989795.
  6. ^ Monti-Bloch, L.; Jennings-White, C.; Dolberg, D.S.; Berliner, D.L. (1994). "The human vomeronasal system". Psychoneuroendocrinology. 19 (5–7): 673–686. doi:10.1016/0306-4530(94)90049-3. ISSN 0306-4530. PMID 7938363.
  7. ^ Edmund T. Rolls (November 2013). Emotion and Decision Making Explained. Oxford University Press. pp. 356–. ISBN 978-0-19-965989-0.
  8. ^ BioScan. Oryx Press. 2009.
  9. ^ a b Liebowitz, Michael R.; Salman, Ester; Nicolini, Humberto; Rosenthal, Norman; Hanover, Rita; Monti, Louis (2014). "Effect of an Acute Intranasal Aerosol Dose of PH94B on Social and Performance Anxiety in Women With Social Anxiety Disorder" (PDF). American Journal of Psychiatry. 171 (6): 675–682. doi:10.1176/appi.ajp.2014.12101342. ISSN 0002-953X. PMID 24700254.
  10. ^ http://ascpmeeting.org/wp-content/uploads/2014/05/ASCP-Poster-Abstract-Book-Online.pdf
  11. ^ US patent 8722652, Louis Monti-Bloch, "Acute Treatment of Social Phobia", published 13 November 2012, assigned to Pherin Pharmaceuticals, Inc. 
  12. ^ "Generalized Anxiety Disorder :: VistaGen Therapeutics, Inc. (VTGN)". VistaGen Therapeutics, Inc. Retrieved 2019-12-19.
  13. ^ "Post-traumatic Stress Disorder :: VistaGen Therapeutics, Inc. (VTGN)". VistaGen Therapeutics, Inc. Retrieved 2019-12-19.
  14. ^ "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)". VistaGen Therapeutics, Inc. Retrieved 2019-12-19.
  15. ^ a b c d Kaminski, R. M. (2006). "The Pheromone Androstenol (5 -Androst-16-en-3 -ol) Is a Neurosteroid Positive Modulator of GABAA Receptors". Journal of Pharmacology and Experimental Therapeutics. 317 (2): 694–703. doi:10.1124/jpet.105.098319. ISSN 0022-3565. PMID 16415088.

External links[edit]