L-741,626

L-741,626 is a drug which acts as a potent and selective antagonist for the dopamine receptor D2. It has good selectivity over the related D3 and D4 subtypes and other receptors. L-741,626 is used for laboratory research into brain function and has proved particularly useful for distinguishing D2 mediated responses from those produced by the closely related D3 subtype, and for studying the roles of these subtypes in the action of cocaine and amphetamines in the brain.[1][2][3][4][5][6][7][8][9][10]

L-741,626
Clinical data
ATC code
  • none
Identifiers
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC20H21ClN2O
Molar mass340.85 g·mol−1
3D model (JSmol)
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References
  1. Bowery BJ, Razzaque Z, Emms F, Patel S, Freedman S, Bristow L, Kulagowski J, Seabrook GR (December 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. doi:10.1111/j.1476-5381.1996.tb16063.x. PMC 1915834. PMID 8968560.
  2. Canales JJ, Iversen SD (September 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. doi:10.1016/S0091-3057(00)00311-7. PMID 11113496.
  3. Costanza RM, Barber DJ, Terry P (November 2001). "Antagonism of the discriminative stimulus effects of cocaine at two training doses by dopamine D2-like receptor antagonists". Psychopharmacology. 158 (2): 146–53. doi:10.1007/s002130100872. PMID 11702088.
  4. Chaperon F, Tricklebank MD, Unger L, Neijt HC (June 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. doi:10.1016/S0028-3908(03)00113-8. PMID 12763098.
  5. Grundt P, Husband SL, Luedtke RR, Taylor M, Newman AH (February 2007). "Analogues of the dopamine D2 receptor antagonist L741,626: Binding, function, and SAR". Bioorganic & Medicinal Chemistry Letters. 17 (3): 745–9. doi:10.1016/j.bmcl.2006.10.076. PMC 1851912. PMID 17095222.
  6. Koffarnus MN, Greedy B, Husbands SM, Grundt P, Newman AH, Woods JH (April 2009). "The discriminative stimulus effects of dopamine D2- and D3-preferring agonists in rats". Psychopharmacology. 203 (2): 317–27. doi:10.1007/s00213-008-1323-4. PMC 3065021. PMID 18807248.
  7. Depoortère R, Bardin L, Rodrigues M, Abrial E, Aliaga M, Newman-Tancredi A (July 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. doi:10.1097/FBP.0b013e32832ec5aa. PMID 19584712.
  8. Fan X, Xu M, Hess EJ (January 2010). "D2 dopamine receptor subtype-mediated hyperactivity and amphetamine responses in a model of ADHD". Neurobiology of Disease. 37 (1): 228–36. doi:10.1016/j.nbd.2009.10.009. PMC 2839459. PMID 19840852.
  9. Achat-Mendes C, Grundt P, Cao J, Platt DM, Newman AH, Spealman RD (August 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. doi:10.1124/jpet.110.167619. PMC 2913766. PMID 20494958.
  10. Watson DJ, Marsden CA, Millan MJ, Fone KC (March 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. 15 (4): 471–484. doi:10.1017/S1461145711000435. PMID 21414250.


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