| 词条 | Piromelatine |
| 释义 |
| drug_name = | IUPAC_name = N-[2-(5-Methoxy-1H-indol-3-yl)ethyl]-4-oxopyran-2-carboxamide | image = Piromelatine.svg | alt = | caption = | tradename = | Drugs.com = | MedlinePlus = | pregnancy_AU = | pregnancy_US = | pregnancy_category= | legal_AU = | legal_CA = | legal_UK = | legal_US = | legal_status = | routes_of_administration = | bioavailability = | protein_bound = | metabolism = | onset = | elimination_half-life = | excretion = | CAS_number = 946846-83-9 | ATCvet = | ATC_prefix = | ATC_suffix = | PubChem = 24815904 | DrugBank = | ChemSpiderID = 32700981 | chemical_formula = | C=17 | H=16 | N=2 | O=4 | molecular_weight = 312.32 g/mol | 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. See also
References1. ^http://www.neurim.com/news/2013-02-18/positive-phase-2-clinical-trial-results-of-piromelatine-for-the-treatment-of-insomnia/ {{Melatonin receptor modulators}}{{Serotonin receptor modulators}}{{nervous-system-drug-stub}}2. ^http://www.neurim.com/news/2011-07-24/positive-results-from-phase-i-and-ib-clinical-trials-with-neu-p11/ 3. ^{{cite journal|last1=Liu|first1=YY|last2=Yin|first2=D|last3=Chen|first3=L|last4=Qu|first4=WM|last5=Chen|first5=CR|last6=Laudon|first6=M|last7=Cheng|first7=NN|last8=Urade|first8=Y|last9=Huang|first9=ZL|title=Piromelatine exerts antinociceptive effect via melatonin, opioid, and 5HT1A receptors and hypnotic effect via melatonin receptors in a mouse model of neuropathic pain|journal=Psychopharmacology|date=October 2014|volume=231|issue=20|pages=3973–85|pmid=24700387|doi=10.1007/s00213-014-3530-5}} 4. ^{{cite journal|last1=Huang|first1=L|last2=Zhang|first2=C|last3=Hou|first3=Y|last4=Laudon|first4=M|last5=She|first5=M|last6=Yang|first6=S|last7=Ding|first7=L|last8=Wang|first8=H|last9=Wang|first9=Z|last10=He|first10=P|last11=Yin|first11=W|title=Blood pressure reducing effects of piromelatine and melatonin in spontaneously hypertensive rats.|journal=European Review for Medical and Pharmacological Sciences|date= September 2013|volume=17|issue=18|pages=2449–56|pmid=24089222}} 5. ^{{cite journal | pmid=23651610| year=2013| author1=He| first1=P| title=A novel melatonin agonist Neu-P11 facilitates memory performance and improves cognitive impairment in a rat model of Alzheimer' disease| journal=Hormones and Behavior| volume=64| issue=1| pages=1–7| last2=Ouyang| first2=X| last3=Zhou| first3=S| last4=Yin| first4=W| last5=Tang| first5=C| last6=Laudon| first6=M| last7=Tian| first7=S| doi=10.1016/j.yhbeh.2013.04.009}} 6 : 5-HT1A agonists|5-HT1D agonists|Melatonin receptor agonists|Hypnotics|Indoles|4-Pyrones |
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