4,16-Androstadien-3β-ol

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4,16-Androstadien-3β-ol (developmental code name PH94B; tentative commercial name Aloradine or Aloradine IN) is a pherine which is under development by Pherin Pharmaceuticals, Inc. in a nasal spray formulation for the acute (p.r.n.) treatment of social anxiety disorder in women.[1][2][3][4][5][6][7][8] It is also being investigated by Pherin Pharmaceuticals for the treatment of generalized anxiety disorder in women.[2] As of 2015, it is in phase III clinical trials.[9]

The compound 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).[6]

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.[10] It produces anxiolytic-like effects in animals.[10] 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.[10] As 4,16-androstadien-3β-ol is very closely related structurally to androstadienol (which is 5,16-androstadien-3β-ol), being a positional isomer of the steroid, the mechanism of action of 4,16-androstadien-3β-ol could similarly be potentiation of the GABAA receptor.[10]

See also

References

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External links


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  1. ↑ Lua error in package.lua at line 80: module 'strict' not found.
  2. ↑ 2.0 2.1 Lua error in package.lua at line 80: module 'strict' not found.
  3. ↑ Lua error in package.lua at line 80: module 'strict' not found.
  4. ↑ Lua error in package.lua at line 80: module 'strict' not found.
  5. ↑ Lua error in package.lua at line 80: module 'strict' not found.
  6. ↑ 6.0 6.1 Lua error in package.lua at line 80: module 'strict' not found.
  7. ↑ http://ascpmeeting.org/wp-content/uploads/2014/05/ASCP-Poster-Abstract-Book-Online.pdf
  8. ↑ US patent 8722652, Louis Monti-Bloch, "Acute Treatment of Social Phobia", published 13 November 2012, assigned to Pherin Pharmaceuticals, Inc. 
  9. ↑ http://www.pherin.com/products.html
  10. ↑ 10.0 10.1 10.2 10.3 Lua error in package.lua at line 80: module 'strict' not found.
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