Chemistry:Piromelatine

From HandWiki
Short description: Chemical compound
Piromelatine
Chemical structure of Piromelatine
Identifiers
CAS Number
PubChem CID
ChemSpider
UNII
ChEMBL
Chemical and physical data
FormulaC17H16N2O4
Molar mass312.325 g·mol−1
3D model (JSmol)

Piromelatine (Neu-P11) is a multimodal sleep drug under development by Neurim Pharmaceuticals. It is an agonist at melatonin MT1/MT2 and serotonin 5-HT1A/5-HT1D receptors. Neurim is conducting a phase II randomized, placebo controlled trial of cognitive and sleep effects in Alzheimer's disease.

Results of a phase II trial on insomnia in 120 adults were announced in 2013, finding piromelatine 20/50 mg improved sleep over 4 weeks vs placebo.[1] Phase 1A/1B studies in 2011, showed safe dose-dependent improvement in sleep.[2] Pre-clinical studies showed antinociceptive[3] antihypertensive[4] and cognitive benefits[5] in rat disease models of pain, hypertension, and Alzheimer's disease.

Antidepressant and anti-anxiety effects were also demonstrated in animal models.[6]

See also

References

  1. ↑ "Neurim Pharmaceuticals Announces Positive Phase 2 Clinical Trial Results of Piromelatine for the Treatment of Insomnia". Neurim Pharmaceuticals. 18 February 2013. http://www.neurim.com/news/2013-02-18/positive-phase-2-clinical-trial-results-of-piromelatine-for-the-treatment-of-insomnia/. 
  2. ↑ "Neurim Pharmaceuticals Announces Positive Results From Phase I and Ib Clinical Trials With Neu-p11, a Sleep Maintenance Drug". Neurim Pharmaceuticals. 24 July 2011. http://www.neurim.com/news/2011-07-24/positive-results-from-phase-i-and-ib-clinical-trials-with-neu-p11/. 
  3. ↑ "Piromelatine exerts antinociceptive effect via melatonin, opioid, and 5HT1A receptors and hypnotic effect via melatonin receptors in a mouse model of neuropathic pain". Psychopharmacology 231 (20): 3973–85. October 2014. doi:10.1007/s00213-014-3530-5. PMID 24700387. 
  4. ↑ "Blood pressure reducing effects of piromelatine and melatonin in spontaneously hypertensive rats". European Review for Medical and Pharmacological Sciences 17 (18): 2449–56. September 2013. PMID 24089222. 
  5. ↑ "A novel melatonin agonist Neu-P11 facilitates memory performance and improves cognitive impairment in a rat model of Alzheimer' disease". Hormones and Behavior 64 (1): 1–7. June 2013. doi:10.1016/j.yhbeh.2013.04.009. PMID 23651610. 
  6. ↑ "Antidepressant- and anxiolytic effects of the novel melatonin agonist Neu-P11 in rodent models". Acta Pharmacologica Sinica 31 (7): 775–783. July 2010. doi:10.1038/aps.2010.80. PMID 20581849. 



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