Википедија

L-741,626

L-741,626 je lek koji deluje kao potentan i selektivan antagonist za dopaminki receptor D2. On ima znatnu selektivnost u odnosu na srodne D3 i D4 podtipove i druge receptore. L-741,626 se koristi za laboratorijska istraživanja moždane funkcije. On se pokazao posebno korisnim u razlikovanju D2 posredovanih responsa od onih koji proizvode blisko srodni D3 podtipovi, kao i u studiranju uloga tih podtipova u dejstvu kokaina i amfetamina u mozgu.[1][2][3][4][5][6][7][8][9][10]

L-741,626
IUPAC ime
3-[4-(4-Hlorofenil)-4-hidroksipiperidin-l-il]metil-1H-indol
Identifikatori
CAS broj81226-60-0 ДаY
ATC kodnone
PubChemCID 133633
Hemijski podaci
FormulaC20H21ClN2O
Molarna masa340,134 g/mol
  • OC(CC1)(C2=CC=C(Cl)C=C2)CCN1CC3=CNC4=CC=CC=C43

Reference

уреди
  1. ^ Bowery BJ, Razzaque Z, Emms F, Patel S, Freedman S, Bristow L, Kulagowski J, Seabrook GR (1996). „Antagonism of the effects of (+)-PD 128907 on midbrain dopamine neurones in rat brain slices by a selective D2 receptor antagonist L-741,626”. British Journal of Pharmacology. 119 (7): 1491—7. PMC 1915834  . PMID 8968560. 
  2. ^ Canales JJ, Iversen SD (2000). „Psychomotor-activating effects mediated by dopamine D(2) and D(3) receptors in the nucleus accumbens”. Pharmacology, Biochemistry, and Behavior. 67 (1): 161—8. PMID 11113496. doi:10.1016/S0091-3057(00)00311-7. 
  3. ^ Costanza RM, Barber DJ, Terry P (2001). „Antagonism of the discriminative stimulus effects of cocaine at two training doses by dopamine D2-like receptor antagonists”. Psychopharmacology. 158 (2): 146—53. PMID 11702088. doi:10.1007/s002130100872. 
  4. ^ Chaperon F, Tricklebank MD, Unger L, Neijt HC (2003). „Evidence for regulation of body temperature in rats by dopamine D2 receptor and possible influence of D1 but not D3 and D4 receptors”. Neuropharmacology. 44 (8): 1047—53. PMID 12763098. doi:10.1016/S0028-3908(03)00113-8. 
  5. ^ Grundt P, Husband SL, Luedtke RR, Taylor M, Newman AH (2007). „Analogues of the dopamine D2 receptor antagonist L741,626: Binding, function, and SAR”. Bioorganic & Medicinal Chemistry Letters. 17 (3): 745—9. PMC 1851912  . PMID 17095222. doi:10.1016/j.bmcl.2006.10.076. 
  6. ^ Koffarnus MN, Greedy B, Husbands SM, Grundt P, Newman AH, Woods JH (2009). „The discriminative stimulus effects of dopamine D2- and D3-preferring agonists in rats”. Psychopharmacology. 203 (2): 317—27. PMC 3065021  . PMID 18807248. doi:10.1007/s00213-008-1323-4. 
  7. ^ Depoortère R, Bardin L, Rodrigues M, Abrial E, Aliaga M, Newman-Tancredi A (2009). „Penile erection and yawning induced by dopamine D2-like receptor agonists in rats: influence of strain and contribution of dopamine D2, but not D3 and D4 receptors”. Behavioural Pharmacology. 20 (4): 303—11. PMID 19584712. doi:10.1097/FBP.0b013e32832ec5aa. 
  8. ^ Fan X, Xu M, Hess EJ (2010). „D2 dopamine receptor subtype-mediated hyperactivity and amphetamine responses in a model of ADHD”. Neurobiology of Disease. 37 (1): 228—36. PMC 2839459  . PMID 19840852. doi:10.1016/j.nbd.2009.10.009. 
  9. ^ Achat-Mendes C, Grundt P, Cao J, Platt DM, Newman AH, Spealman RD (2010). „Dopamine D3 and D2 receptor mechanisms in the abuse-related behavioral effects of cocaine: studies with preferential antagonists in squirrel monkeys”. The Journal of Pharmacology and Experimental Therapeutics. 334 (2): 556—65. PMID 20494958. doi:10.1124/jpet.110.167619. 
  10. ^ Watson DJ, Marsden CA, Millan MJ, Fone KC (2011). „Blockade of dopamine D3 but not D2 receptors reverses the novel object discrimination impairment produced by post-weaning social isolation: implications for schizophrenia and its treatment”. The International Journal of Neuropsychopharmacology / Official Scientific Journal of the Collegium Internationale Neuropsychopharmacologicum (CINP): 1—14. PMID 21414250. doi:10.1017/S1461145711000435. 

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уреди
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