Piromelatine

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.

Piromelatine
Identifiers
CAS Number
PubChem CID
ChemSpider
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC17H16N2O4
Molar mass312.32 g/mol g·mol−1
3D model (JSmol)

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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