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Piromelatine

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Piromelatine
Identifiers
  • N-[2-(5-Methoxy-1H-indol-3-yl)ethyl]-4-oxopyran-2-carboxamide
CAS Number
PubChem CID
ChemSpider
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC17H16N2O4
Molar mass312.32 g/mol g·mol−1
3D model (JSmol)
  • COC1=CC2=C(C=C1)NC=C2CCNC(=O)C3=CC(=O)C=CO3
  • InChI=1S/C17H16N2O4/c1-22-13-2-3-15-14(9-13)11(10-19-15)4-6-18-17(21)16-8-12(20)5-7-23-16/h2-3,5,7-10,19H,4,6H2,1H3,(H,18,21)
  • Key:PNTNBIHOAPJYDB-UHFFFAOYSA-N

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.

See also

References

  1. ^ http://www.neurim.com/news/2013-02-18/positive-phase-2-clinical-trial-results-of-piromelatine-for-the-treatment-of-insomnia/
  2. ^ http://www.neurim.com/news/2011-07-24/positive-results-from-phase-i-and-ib-clinical-trials-with-neu-p11/
  3. ^ Liu, YY; Yin, D; Chen, L; Qu, WM; Chen, CR; Laudon, M; Cheng, NN; Urade, Y; Huang, ZL (October 2014). "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. doi:10.1007/s00213-014-3530-5. PMID 24700387.
  4. ^ Huang, L; Zhang, C; Hou, Y; Laudon, M; She, M; Yang, S; Ding, L; Wang, H; Wang, Z; He, P; Yin, W (September 2013). "Blood pressure reducing effects of piromelatine and melatonin in spontaneously hypertensive rats". European review for medical and pharmacological sciences. 17 (18): 2449–56. PMID 24089222.
  5. ^ He, P; Ouyang, X; Zhou, S; Yin, W; Tang, C; Laudon, M; Tian, S (2013). "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. doi:10.1016/j.yhbeh.2013.04.009. PMID 23651610.


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