4-NEMD

Из Википедије, слободне енциклопедије
4-NEMD
4-NEMD.png
IUPAC ime
4-(1-naftalen- 1-iletil)- 1H-imidazol
Identifikatori
CAS broj 137967-81-8 ДаY
ATC kod none
PubChem CID 132110
ChemSpider 24531958 ДаY
Hemijski podaci
Formula C15H14N2
Molarna masa 222,285 g/mol
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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.[1] 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,[2][3] koji mogu da budu selektivni za različite podtipove alfa-2 receptora.[4] On ima dva izomera, od kojih je (S) izomer potentniji, što je slučaj i sa medetomidinom.[5]

Reference[уреди]

  1. 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. PMID 7914537. doi:10.1021/jm00041a011. 
  2. Zhang, X; Yao, XT; Dalton, JT; Shams, G; Lei, L; Patil, PN; Feller, DR; Hsu, FL; George, C (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. PMID 8709134. doi:10.1021/jm9506074. 
  3. Zhang, X; De Los Angeles, JE; He, MY; Dalton, JT; Shams, G; Lei, L; Patil, PN; Feller, DR; Miller, DD (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. PMID 9301663. doi:10.1021/jm960642q. 
  4. 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. PMID 14667931. doi:10.1016/j.bcp.2003.08.043. 
  5. 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. PMID 1361151. doi:10.1002/chir.530040706.