The dopaminergic stabilizer ASP2314/ACR16 selectively interacts with D2High receptors

Synapse

Volumn 63, Issue 10, 2009, Pages 930-934

  Seeman, Philip ^a   Tokita, Kenichi ^b   Matsumoto, Mitsuyuki ^c   Matsuo, Ayako ^b   Sasamata, Masao ^b   Miyata, Keiji ^b  

^a Clera Inc   (Canada)

^b ASTELLAS PHARMA INC   (Japan)

^c ASTELLAS PHARMA GLOBAL DEVELOPMENT   (United States)

Author keywords

ACR16; Antipsychotic; D2High receptor; DA partial agonist; Schizophrenia

Indexed keywords

4 PROPYL 3,4,4A,5,6,10B HEXAHYDRO 2H NAPHTHO[1,2 B][1,4]OXAZIN 9 OL; ASP 2314; DOMPERIDONE H 3; DOPAMINE 2 RECEPTOR; GUANOSINE 5' O (3 THIOTRIPHOSPHATE) S 35; LIGAND; NEUROLEPTIC AGENT; UNCLASSIFIED DRUG;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; CLONE; CONTROLLED STUDY; DISSOCIATION CONSTANT; DRUG MECHANISM; DRUG RECEPTOR BINDING; LABELING INDEX; LIGAND BINDING; MALE; NERVE CELL MEMBRANE; NONHUMAN; PRIORITY JOURNAL; RAT; STRIATE CORTEX;

ANIMALS; BINDING, COMPETITIVE; BRAIN; CHO CELLS; CLONING, MOLECULAR; CRICETINAE; CRICETULUS; DOPAMINE; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG INTERACTIONS; GUANOSINE 5'-O-(3-THIOTRIPHOSPHATE); MALE; PIPERIDINES; PROTEIN BINDING; RADIOISOTOPES; RATS; RATS, SPRAGUE-DAWLEY; RECEPTORS, DOPAMINE D2; TRANSFECTION; VITAMIN K 1;

EID: 70349112311     PISSN: 08874476     EISSN: 10982396     Source Type: Journal    
DOI: 10.1002/syn.20663     Document Type: Article

References (32)

1. Baumeister AA, Francis JL. 2002. Historical development of the dopamine hypothesis of schizophrenia. J History Neurosci 11:265-277.
2. Carlsson ML, Carlsson A, Nilsson M. 2004. "Schizophrenia: From dopamine to glutamate and back." Curr Med Chem 11:267-277.
3. Cheng Y, Prusoff WH. 1973. Relationship between the inhibition constant (K1) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reaction. Biochem Pharmacol 22:3099-3108.
4. 11C]raclopride binding in primate brains. Neuropharmacology 38:331-338.
5. George SR,Watanabe M, Di Paolo T, Falardeau P, Labrie F, Seeman P. 1985. The functional state of the dopamine receptor in the anterior pituitary is in the high-affinity form. Endocrinology 117:690-697. (Pubitemid 15237891)
6. Gilchrist A. 2007. Modulating G-protein-coupled receptors: From traditional pharmacology to allosterics. Trends Pharmacol Sci 28:431-437. (Pubitemid 47087973)
7. Longer receptor has a high-affinity state and inhibits adenylyl cyclase. Brain Res Mol Brain Res 77:281-284.
8. McDonald WM, Sibley DR, Kilpatrick BF, Caron MG. 1984. Dopaminergic inhibition of adenylate cyclase correlates with high affinity agonist binding to anterior pituitary D2 dopamine receptors. Mol Cell Endocrinol 36:201-209.
9. Natesan S, Svensson KA, Reckless GE, Nobrega JN, Barlow KB, Johansson AM, Kapur S. 2006. The dopamine stabilizers (S)-(-)-(3-methanesulfonyl-phenyl)-1- propyl-piperidine [(-2)-OSU6162] and 4-(3-methanesulfonylphenyl)-1-propyl- piperidine (ACR16) show high in vivo D2 receptor occupancy, antipsychotic-like efficacy, and low potential for motor side effects in the rat. J Pharmacol Exp Ther 318:810-818. (Pubitemid 44061255)
10. NeuroSearch. 2006. http://www.neurosearch.com/Files/Filer/Presentations/ 20061121-DDF-Biotechseminar.pdf
11. Nyberg S, Lyssarides E, Nord M, Tedroff J, Lindström L, Hagström P, Persson P, Stenseth A, Carlsson A, Sonesson C, Waters N, Waters S, Gefvert O. 2004. Efficacy and tolerability of the new dopamine stabiliser ACR16. A randomised placebo-controlled addon study in patients with schizophrenia. In 12th Biennial Winter Workshop on Schizophrenia, 7-13 February, Davos, Switzerland.
12. Pettersson F, Waters N, Waters ES, Carlsson A, Sonesson C. 2002. The developement of a new class of dopamine stabilizers. Program No. 894.11. 2002 Abstract Viewer/Itinerary Planner. Washington, DC: Society for Neuroscience.
13. Pounds S, Seguin RJ, Filer CN. 2005. Tritium labelling of dopaminergic ligands domperidone and (±)-7-hydroxy DPAT. Appl Radiat Isot 62:49-53. (Pubitemid 39446101)
14. Rung JP, Rung E, Helgeson L, Johansson AM, Svensson K, Carlsson A, Carlsson ML. 2008. Effects of (-)-OSU6162 and ACR16 on motor activity in rats, indicating a unique mechanism of dopaminergic stabilization. J Neural Transm 115:899-908.
15. Seeman P. 1992. Dopamine receptor sequences. Therapeutic levels of neuroleptics occupy D2, clozapine occupies D4. Neuropsychopharmacology 7:261-284.
16. Seeman P. 2006. Targeting the dopamine D2 receptor in schizophrenia. Expert Opin Ther Targets 10:515-531.
17. High receptors moderately elevated by bifeprunox and aripiprazole. Synapse 62:902-908.
18. Seeman P, Van Tol HHM. 1995. Deriving the therapeutic concentrations for clozapine and haloperidol: The apparent dissociation constant of a neuroleptic at the dopamine D2 or D4 receptor varies with the affinity of the competing radioligand. Eur J Pharmacol Mol Pharmacol 291:59-66.
19. Seeman P, Guan H-C. 2007. Dopamine partial agonist action of (-)OSU6162 is consistent with dopamine hyperactivity in psychosis. Eur J Pharmacol 557:151-153. (Pubitemid 46188631)
20. High receptors: D2 basis for schizophrenia. Synapse 62:819-828.
21. Seeman P, Chau-Wong M, Tedesco J, Wong K. 1975. Receptors for antipsychotic drugs and dopamine: Direct binding assays. Proc Natl Acad Sci USA 72:4376-4380.
22. 3H]spiperone depend on tissue concentration: Analysis and examples. J Neurochem 43:221-235.
23. Seeman P, Ulpian C, Larsen RD, Anderson PS. 1993. Dopamine receptors labeled by PHNO. Synapse 14:254-262.
24. 3H]spiperone in isotonic medium: Implications for human positron emission tomography. Synapse 49:209-215.
25. Seeman P, Ko F, Tallerico T. 2005. Dopamine receptor contribution to the action of PCP. LSD and ketamine psychotomimetics. Mol Psychiatry 10:877-883.
26. High dopamine receptors. Synapse 60:319-346.
27. 3H](+)PHNO. Synapse 61:263-267.
28. Sonesson C, Lin CH, Hansson L, Waters N, Svensson K, Carlsson A, Smith MW, Wikström H. 1994. Substituted (S)-phenylpiperidines and rigid congeners as preferential dopamine autoreceptor antagonists: Synthesis and structure-activity relationships. J Med Chem 37:2735-2753. (Pubitemid 24273465)
29. Tadori Y, Kitagawa H, Forbes RA, McQuade RD, Stark A, Kikuchi T. 2007. Differences in agonist/antagonist properties at human dopamine D(2) receptors between aripiprazole, bifeprunox and SDZ 208-912. Eur J Pharmacol 574:103-111. (Pubitemid 47575529)
30. Van Rossum JM. 1966. The significance of dopamine-receptor blockade for the mechanism of action of neuroleptic drugs. Arch int Pharmacodyn Ther 160:492-494.
31. Van Rossum JM. 1967. The significance of dopamine-receptor blockade for the action of neuroleptic drugs. In: Brill H, Cole JO, Deniker P, Hippius H, Bradley PB, eds. Neuro-psycho-pharmacology, Proceedings of the Fifth International Congress of the Collegium Internationale Neuro-Psycho- pharmacologicum, March 1966, Excerpta Medica Foundation, Amsterdam. p 321-329.
32. Waters N, Carlsson A, Carlsson M, Martin P, Tedroff J, Kullingsjö J, Petterson F, Sonesson S, Waters ES. 2002. Pharmacology of ACR16, a dopamine stabilizer. Program No. 894.13. 2002 Abstract Viewer/Itinerary Planner. Washington, DC: Society for Neuroscience.