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TAN-67

TAN-67
IUPAC ime
3-[(4aS,12aR)-11-amino-2-methyl-1,3,4,5,12,12a-hexahydropyrido[3,4-b]acridin-4a(2H)-yl]phenol
Identifikatori
CAS broj148545-09-9 ДаY
PubChemCID 9798940
Hemijski podaci
FormulaC23H25N3O
Molarna masa359.464 g/mol
  • CN1CC[C@@]2(CC3=NC4=CC=CC=C4C(=C3C[C@H]2C1)N)C5=CC(=CC=C5)O

TAN-67 (SB-205,607) je lek koji se koristi u naučnim istraživanjima. On je potentan i selektivan δ-opioidni agonist,[1] selektivan za δ1 tip receptora.[2] Ovaj materijal ima analgetska svojstva[3][4] i indukuje oslobađanje dopamina u mozgu.[5] On takođe štiti srčano i moždano tkivo od oštećenja tokom hipoksije putem više mehanizama među kojima je interakcija δ receptora i mitohondrijskih K(ATP) kanala.[6][7][8][9][10]

  1. ^ Fujii, H.; Kawai, K.; Kawamura, K.; Mizusuna, A.; Onoda, Y.; Murachi, M.; Tanaka, T.; Endoh, T.; Nagase, H. (2001). „Synthesis of optically active TAN-67, a highly selective delta opioid receptor agonist, and investigation of its pharmacological properties”. Drug Design and Discovery. 11765135 (4): 325—330. PMID 11765135. 
  2. ^ Nagase, H.; Kawai, K.; Hayakawa, J.; Wakita, H.; Mizusuna, A.; Matsuura, H.; Tajima, C.; Takezawa, Y.; Endoh, T. (1998). „Rational drug design and synthesis of a highly selective nonpeptide delta-opioid agonist, (4aS*,12aR*)-4a-(3-hydroxyphenyl)-2-methyl- 1,2,3,4,4a,5,12,12a-octahydropyrido3,4-bacridine (TAN-67)”. Chemical & Pharmaceutical Bulletin. 9845952 (11): 1695—2302. PMID 9845952. doi:10.1248/cpb.46.1695. 
  3. ^ Yajima, Y.; Narita, M.; Tsuda, M.; Imai, S.; Kamei, J.; Nagase, H.; Suzuki, T. (2000). „Modulation of NMDA- and (+)TAN-67-induced nociception by GABA(B) receptors in the mouse spinal cord”. Life Sciences. 11205886 (6): 719—725. PMID 11205886. doi:10.1016/s0024-3205(00)00975-9. 
  4. ^ Nagase, H.; Yajima, Y.; Fujii, H.; Kawamura, K.; Narita, M.; Kamei, J.; Suzuki, T. (2001). „The pharmacological profile of delta opioid receptor ligands, (+) and (-) TAN-67 on pain modulation”. Life Sciences. 11358331 (19–20): 2227—2231. PMID 11358331. doi:10.1016/s0024-3205(01)01010-4. 
  5. ^ Fusa, K.; Takahashi, I.; Watanabe, S.; Aono, Y.; Ikeda, H.; Saigusa, T.; Nagase, H.; Suzuki, T.; Koshikawa, N.; Cools, A. R. (2005). „The non-peptidic delta opioid receptor agonist TAN-67 enhances dopamine efflux in the nucleus accumbens of freely moving rats via a mechanism that involves both glutamate and free radicals”. Neuroscience. 15590157 (3): 745—755. PMID 15590157. S2CID 42710264. doi:10.1016/j.neuroscience.2004.10.016. 
  6. ^ Fryer, R. M.; Hsu, A. K.; Nagase, H.; Gross, G. J. (2000). „Opioid-induced cardioprotection against myocardial infarction and arrhythmias: Mitochondrial versus sarcolemmal ATP-sensitive potassium channels”. The Journal of Pharmacology and Experimental Therapeutics. 10900218 (2): 451—457. PMID 10900218. 
  7. ^ Huh, J.; Gross, G. J.; Nagase, H.; Liang, B. T. (2001). „Protection of cardiac myocytes via delta(1)-opioid receptors, protein kinase C, and mitochondrial K(ATP) channels”. American Journal of Physiology. Heart and Circulatory Physiology. 11123254 (1): H377—83. PMID 11123254. S2CID 86775469. doi:10.1152/ajpheart.2001.280.1.H377. 
  8. ^ Patel, H. H.; Ludwig, L. M.; Fryer, R. M.; Hsu, A. K.; Warltier, D. C.; Gross, G. J. (2002). „Delta opioid agonists and volatile anesthetics facilitate cardioprotection via potentiation of K(ATP) channel opening”. FASEB Journal : Official Publication of the Federation of American Societies for Experimental Biology. 12205051 (11): 1468—1470. PMID 12205051. S2CID 22952889. doi:10.1096/fj.02-0170fje. 
  9. ^ Maslov, L. N.; Platonov, A. A.; Lasukova, T. V.; Lishmanov, IuB; Oeltgen, P.; Nagase, H.; Podoksenov, IuK; Podoksenov, A. Iu. (2006). „Delta-opioid receptor activation prevents appearance of irreversible damages of cardiomyocytes and exacerbates myocardial contractility dysfunction during ischemia and reperfusion”. Patologicheskaia Fiziologiia I Eksperimental'naia Terapiia. 17300082 (4): 13—17. PMID 17300082. 
  10. ^ Tian, X. S.; Zhou, F.; Yang, R.; Xia, Y.; Wu, G. C.; Guo, J. C. (2008). „Effects of intracerebroventricular injection of delta-opioid receptor agonist TAN-67 or antagonist naltrindole on acute cerebral ischemia in rat”. Sheng Li Xue Bao : [Acta Physiologica Sinica]. 18690389 (4): 475—484. PMID 18690389. 

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TAN-67
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