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Milnacipran

С Википедије, слободне енциклопедије
Milnacipran
Klinički podaci
Prodajno imeDalcipran, Ixel, Savella, Toledomin
Drugs.comMonografija
Način primeneOralno
Farmakokinetičkipodaci
Poluvreme eliminacije6-8 sati
IzlučivanjeUrinom (50%- 60%, 24% kao l-milnacipran i 31% kao d-milnacipran)
Identifikatori
CAS broj92623-85-3ДаY
ATC kodN06AX17(WHO)
PubChemCID65833
DrugBankDB04896ДаY
ChemSpider59245ДаY
ChEMBLCHEMBL252923ДаY
Hemijski podaci
FormulaC15H22N2O
Molarna masa246,348
  • CCN(CC)C(=O)[C@@]1(C[C@@H]1CN)C1=CC=CC=C1
  • InChI=1S/C15H22N2O/c1-3-17(4-2)14(18)15(10-13(15)11-16)12-8-6-5-7-9-12/h5-9,13H,3-4,10-11,16H2,1-2H3/t13-,15+/m1/s1ДаY
  • Key:GJJFMKBJSRMPLA-HIFRSBDPSA-NДаY
Fizički podaci
Tačka topljenja179 °C (354 °F)

Milnacipranjeorgansko jedinjenje,koje sadrži 15atomaugljenikai imamolekulsku masuod 246,348Da.[1][2][3][4][5][6][7][8][9][10][11][12][13][14][15]

Osobina Vrednost
Broj akceptora vodonika 2
Broj donora vodonika 1
Broj rotacionih veza 5
Particioni koeficijent[16](ALogP) 1,3
Rastvorljivost[17](logS,log(mol/L)) -3,0
Polarna površina[18](PSA,Å2) 46,3
  1. ^Leo RJ, Brooks VL: Clinical potential of milnacipran, a serotonin and norepinephrine reuptake inhibitor, in pain. Curr Opin Investig Drugs. 2006 Jul;7(7):637-42.PMID16869117
  2. ^Sato S, Yamakawa Y, Terashima Y, Ohta H, Asada T: Efficacy of milnacipran on cognitive dysfunction with post-stroke depression: preliminary open-label study. Psychiatry Clin Neurosci. 2006 Oct;60(5):584-9.PMID16958942
  3. ^Simon LS: Is milnacipran effective in treating pain in patients with fibromyalgia? Nat Clin Pract Rheumatol. 2006 Mar;2(3):126-7.PMID16932669
  4. ^Soya A, Terao T, Nakajima M, Kojima H, Okamoto T, Inoue Y, Iwakawa M, Shinkai K, Yoshimura R, Ueta Y, Nakamura J: Effects of repeated milnacipran administration on brain serotonergic and noradrenergic functions in healthy volunteers. Psychopharmacology (Berl). 2006 Sep;187(4):526-7. Epub 2006 Jul 8.PMID16830129
  5. ^King T, Rao S, Vanderah T, Chen Q, Vardanyan A, Porreca F: Differential blockade of nerve injury-induced shift in weight bearing and thermal and tactile hypersensitivity by milnacipran. J Pain. 2006 Jul;7(7):513-20.PMID16814690
  6. ^Moojen VK, Martins MR, Reinke A, Feier G, Agostinho FR, Cechin EM, Quevedo J: Effects of milnacipran in animal models of anxiety and memory. Neurochem Res. 2006 Apr;31(4):571-7. Epub 2006 May 9.PMID16758367
  7. ^Moret C, Charveron M, Finberg JP, Couzinier JP, Briley M: Biochemical profile of midalcipran (F 2207), 1-phenyl-1-diethyl-aminocarbonyl-2-aminomethyl-cyclopropane (Z) hydrochloride, a potential fourth generation antidepressant drug. Neuropharmacology. 1985 Dec;24(12):1211-9.PMID3005901
  8. ^Briley M, Prost JF, Moret C: Preclinical pharmacology of milnacipran. Int Clin Psychopharmacol. 1996 Sep;11 Suppl 4:9-14.PMID8923122
  9. ^Puozzo C, Panconi E, Deprez D: Pharmacology and pharmacokinetics of milnacipran. Int Clin Psychopharmacol. 2002 Jun;17 Suppl 1:S25-35.PMID12369608
  10. ^Leinonen E, Lepola U, Koponen H, Mehtonen OP, Rimon R: Long-term efficacy and safety of milnacipran compared to clomipramine in patients with major depression. Acta Psychiatr Scand. 1997 Dec;96(6):497-504.PMID9421348
  11. ^Papakostas GI, Fava M: A meta-analysis of clinical trials comparing milnacipran, a serotonin--norepinephrine reuptake inhibitor, with a selective serotonin reuptake inhibitor for the treatment of major depressive disorder. Eur Neuropsychopharmacol. 2007 Jan;17(1):32-6. Epub 2006 Jun 8.PMID16762534
  12. ^Kako Y, Niwa Y, Toyomaki A, Yamanaka H, Kitagawa N, Denda K, Koyama T: A case of adult attention-deficit/hyperactivity disorder alleviated by milnacipran. Prog Neuropsychopharmacol Biol Psychiatry. 2007 Apr 13;31(3):772-5. Epub 2007 Jan 12.PMID17300859
  13. ^Bernstein CD, Albrecht KL, Marcus DA: Milnacipran for fibromyalgia: a useful addition to the treatment armamentarium. Expert Opin Pharmacother. 2013 Mar 19.PMID23506481
  14. ^Knox C, Law V, Jewison T, Liu P, Ly S, Frolkis A, Pon A, Banco K, Mak C, Neveu V, Djoumbou Y, Eisner R, Guo AC, Wishart DS (2011).„DrugBank 3.0: a comprehensive resource for omics research on drugs”.Nucleic Acids Res.39(Database issue): D1035—41.PMC3013709Слободан приступ.PMID21059682.doi:10.1093/nar/gkq1126.уреди
  15. ^David S. Wishart; Craig Knox; An Chi Guo; Dean Cheng; Savita Shrivastava; Dan Tzur; Bijaya Gautam; Murtaza Hassanali (2008).„DrugBank: a knowledgebase for drugs, drug actions and drug targets”.Nucleic acids research.36(Database issue): D901—6.PMC2238889Слободан приступ.PMID18048412.doi:10.1093/nar/gkm958.уреди
  16. ^Ghose, A.K.; Viswanadhan V.N. & Wendoloski, J.J. (1998).„Prediction of Hydrophobic (Lipophilic) Properties of Small Organic Molecules Using Fragment Methods: An Analysis of AlogP and CLogP Methods”.J. Phys. Chem. A.102:3762—3772.doi:10.1021/jp980230o.
  17. ^Tetko IV, Tanchuk VY, Kasheva TN, Villa AE (2001).„Estimation of Aqueous Solubility of Chemical Compounds Using E-State Indices”.Chem Inf. Comput. Sci.41:1488—1493.PMID11749573.doi:10.1021/ci000392t.уреди
  18. ^Ertl P.; Rohde B.; Selzer P. (2000).„Fast calculation of molecular polar surface area as a sum of fragment based contributions and its application to the prediction of drug transport properties”.J. Med. Chem.43:3714—3717.PMID11020286.doi:10.1021/jm000942e.уреди


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