4-NEMD

4-NEMD
(IUPAC) ime
4-(1-naftalen- 1-iletil)- 1H-imidazol
Klinički podaci
Identifikatori
CAS broj 137967-81-8
ATC kod nije dodeljen
PubChem[1][2] 132110
ChemSpider[3] 24531958
Hemijski podaci
Formula C15H14N2 
Mol. masa 222,285 g/mol
SMILES eMolekuli & PubHem
Farmakoinformacioni podaci
Trudnoća ?
Pravni status

4-NEMD je potentan sedativni lek koji deluje kao selektivni alfa-2 adrenergički agonist. On je blisko srodan sa deksmedetomidinom, ali je nekoliko puta potentniji.[4] Poput drugih alfa-2 agonista, on proizvodi sedativne i mišićno relaksantne efekte, ali ne uzrokuje respiratornu depresiju. On trenutno nema medicinsku primenu, ali je istraživan kao baza za potencijalno novu generaciju alfa-2 agonistnih lekova,[5][6] koji mogu da budu selektivni za različite podtipove alfa-2 receptora.[7] On ima dva izomera, od kojih je (S) izomer potentniji, što je slučaj i sa medetomidinom.[8]

Reference

  1. ↑ Li Q, Cheng T, Wang Y, Bryant SH (2010). „PubChem as a public resource for drug discovery.”. Drug Discov Today 15 (23-24): 1052-7. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519.  edit
  2. ↑ Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). „Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities”. Annual Reports in Computational Chemistry 4: 217-241. DOI:10.1016/S1574-1400(08)00012-1. 
  3. ↑ Hettne KM, Williams AJ, van Mulligen EM, Kleinjans J, Tkachenko V, Kors JA. (2010). „Automatic vs. manual curation of a multi-source chemical dictionary: the impact on text mining”. J Cheminform 2 (1): 3. DOI:10.1186/1758-2946-2-3. PMID 20331846.  edit
  4. ↑ Hong, SS; Romstedt, KJ; Feller, DR; Hsu, FL; Cupps, TL; Lyon, RA; Miller, DD (1994). „A structure-activity relationship study of benzylic modifications of 4-1-(1-naphthyl)ethyl-1H-imidazoles on alpha 1- and alpha 2-adrenergic receptors”. Journal of Medical Chemistry 37 (15): 2328–33. DOI:10.1021/jm00041a011. PMID 7914537. 
  5. ↑ Zhang, X; Yao, XT; Dalton, JT; Shams, G; Lei, L; Patil, PN; Feller, DR; Hsu, FL i dr.. (1996). „Medetomidine analogs as alpha 2-adrenergic ligands. 2. Design, synthesis, and biological activity of conformationally restricted naphthalene derivatives of medetomidine”. Journal of Medical Chemistry 39 (15): 3001–13. DOI:10.1021/jm9506074. PMID 8709134. 
  6. ↑ Zhang, X; De Los Angeles, JE; He, MY; Dalton, JT; Shams, G; Lei, L; Patil, PN; Feller, DR i dr.. (1997). „Medetomidine analogs as alpha 2-adrenergic ligands. 3. Synthesis and biological evaluation of a new series of medetomidine analogs and their potential binding interactions with alpha 2-adrenoceptors involving a "methyl pocket"”. Journal of Medical Chemistry 40 (19): 3014–24. DOI:10.1021/jm960642q. PMID 9301663. 
  7. ↑ Lalchandani, SG; Zhang, X; Hong, SS; Liggett, SB; Li, W; Moore Bm, 2nd; Miller, DD; Feller, DR (2004). „Medetomidine analogs as selective agonists for the human alpha2-adrenoceptors”. Biochemical pharmacology 67 (1): 87–96. DOI:10.1016/j.bcp.2003.08.043. PMID 14667931. 
  8. ↑ Hong, SS; Romstedt, KJ; Feller, DR; Hsu, FL; George, C; Cupps, TL; Lyon, RA; Miller, DD (1992). „Resolution and adrenergic activities of the optical isomers of 4-1-(1-naphthyl)ethyl-1H-imidazole”. Chirality 4 (7): 432–8. DOI:10.1002/chir.530040706. PMID 1361151.