Piromelatine Explained

Drug Name:Piromelatine
Iupac Name:N-[2-(5-Methoxy-1''H''-indol-3-yl)ethyl]-4-oxopyran-2-carboxamide
Width:250px
Cas Number:946846-83-9
Unii:S3UN2146K9
Pubchem:24815904
Chemspiderid:32700981
Chembl:4297523
C:17
H:16
N:2
O:4
Stdinchi: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)
Stdinchikey:PNTNBIHOAPJYDB-UHFFFAOYSA-N
Smiles:COC1=CC2=C(C=C1)NC=C2CCNC(=O)C3=CC(=O)C=CO3

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

Notes and References

  1. Web site: Neurim Pharmaceuticals Announces Positive Phase 2 Clinical Trial Results of Piromelatine for the Treatment of Insomnia . 18 February 2013 . Neurim Pharmaceuticals .
  2. Web site: Neurim Pharmaceuticals Announces Positive Results From Phase I and Ib Clinical Trials With Neu-p11, a Sleep Maintenance Drug . 24 July 2011 . Neurim Pharmaceuticals .
  3. Liu YY, Yin D, Chen L, Qu WM, Chen CR, Laudon M, Cheng NN, Urade Y, Huang ZL . 815868 . 6 . 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 . 24700387 . 10.1007/s00213-014-3530-5 .
  4. Huang L, Zhang C, Hou Y, Laudon M, She M, Yang S, Ding L, Wang H, Wang Z, He P, Yin W . 6 . 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 . 24089222 .
  5. He P, Ouyang X, Zhou S, Yin W, Tang C, Laudon M, Tian S . 205806140 . 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 . 23651610 . 10.1016/j.yhbeh.2013.04.009 .
  6. Tian SW, Laudon M, Han L, Gao J, Huang FL, Yang YF, Deng HF . Antidepressant- and anxiolytic effects of the novel melatonin agonist Neu-P11 in rodent models . Acta Pharmacologica Sinica . 31 . 7 . 775–783 . July 2010 . 20581849 . 4007730 . 10.1038/aps.2010.80 .

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