I. in vivo evidence for partial agonist effects of (2)-OSU6162 and (+)-OSU6162 on 5-HT2A serotonin receptors

Journal of Neural Transmission

Volumn 118, Issue 11, 2011, Pages 1511-1522

  Carlsson, Maria L ^a   Burstein, Ethan S ^b   Kloberg, Angélica ^c   Hansson, Sarah ^c   Schedwin, Arja ^c   Nilsson, Marie ^a   Rung, Johan P ^c   Carlsson, Arvid ^a  

^a UNIVERSITY OF GOTHENBURG   (Sweden)

^b Pharmaceuticals Inc   (United States)

^c A Carlsson Research AB   (Sweden)

Author keywords

5 HT2A receptor; Dopamine stabilizer; Head twitch; OSU6162; Serotonin

Indexed keywords

3 [3 (METHYLSULFONYL)PHENYL] 1 PROPYLPIPERIDINE; 8 CHLORO 2,3,4,5 TETRAHYDRO 3 METHYL 5 PHENYL 1H 3 BENZAZEPIN 7 OL HYDROGEN MALEATE; DOPAMINE 2 RECEPTOR; HALOPERIDOL; RACLOPRIDE; SEROTONIN 2A RECEPTOR; VOLINANSERIN;

ANIMAL EXPERIMENT; ARTICLE; CONTROLLED STUDY; DOPAMINERGIC SYSTEM; DRUG EFFECT; DRUG MECHANISM; DRUG MEGADOSE; DRUG POTENCY; ENANTIOMER; HEAD TWITCH; IN VIVO STUDY; LOCOMOTION; MALE; MOUSE; NEUROTRANSMISSION; NONHUMAN; PARTIAL AGONISM; PHARMACOLOGICAL BLOCKING; PHARMACOLOGICAL STIMULATION; PRIORITY JOURNAL; RAT; SEROTONINERGIC SYSTEM;

ANIMALS; BRAIN CHEMISTRY; MALE; MICE; MICE, INBRED STRAINS; MOTOR ACTIVITY; PIPERIDINES; RATS; RATS, SPRAGUE-DAWLEY; RECEPTOR, SEROTONIN, 5-HT2A; SEROTONIN 5-HT2 RECEPTOR AGONISTS; STEREOISOMERISM;

EID: 84855212618     PISSN: 03009564     EISSN: 14351463     Source Type: Journal    
DOI: 10.1007/s00702-011-0704-8     Document Type: Article

References (19)

1. Carlsson ML, Carlsson A, Nilsson M (2004) Schizophrenia: from dopamine to glutamate and back. Curr Med Chem 11(3): 267-277 (Pubitemid 38240207)
2. Dyhring T, Nielsen EO, Sonesson C, Pettersson F, Karlsson J, Svensson P, Christophersen P, Waters N (2010) The dopaminergic stabilizers pridopidine (ACR16) and (-)-OSU6162 display dopamine D(2) receptor antagonism and fast receptor dissociation properties. Eur J Pharmacol 628(1-3):19-26
3. Ekesbo A, Andrén PE, Gunne LM, Tedroff J (1997) (-)-OSU 6162 inhibits levodopa-induced dyskinesias in a monkey model ofParkinson's disease. Neuroreport 8(11):2567-2570 (Pubitemid 27308462)
4. Ekesbo A, Torstenson R, Hartvig P, Carlsson A, Sonesson C, Waters N, Tedroff J, Långström B (1999) Effects of the substituted (S) 3-phenylpiperidine (-)-OSU6162 on PET measurements of [11C]SCH23390 and [11C]raclopride binding in primate brains. Neuropharmacology 38(3):331-338 (Pubitemid 29097716)
5. Gefvert O, Lindström LH, Dahlbäck O, Sonesson C, Waters N, Carlsson A, Tedroff J (2000) (-)-OSU6162 induces a rapid onset of antipsychotic effect after a single dose. A double-blind placebo-controlled pilot study. Scandinavian Society for Psychopharmacology 41st annual meeting, Copenhagen, Denmark. Nord J Psychiatry 54:93-94
6. Grubbs FE (1969) Procedures for detecting outlying observations in samples. Technometrics 11(1):1-21
7. Kara E, Lin H, Svensson K, Johansson AM, Strange PG (2010) Analysis of the actions of the novel dopamine receptor-directed compounds (S)-OSU6162 and ACR16 at the D2 dopamine receptor. Br J Pharmacol 161(6):1343-1350
8. Lahti RA, Tamminga CA, Carlsson A (2007) Stimulating and inhibitory effects of the dopamine ''stabilizer'' (-)-OSU6162 on dopamine D(2) receptor function in vitro. J Neural Transm 114(9):1143-1146 (Pubitemid 47313178)
9. Lundberg T, Tedroff J, Waters N, Sonesson C, Carlsson A, Hagström P, Lindström LH, Gefvert O (2002) Safety of early clinical experience with (-)-OSU6162, a dopaminergic stabilizer with antipsychotic properties. In: SCNP 43rd Annual and 2nd Mediterranean Meeting, Juan-les-Pins, France. Nord J Psychiatry 56:24
10. Moreno FA, Wiegand CB, Taitano EK, Delgado PL (2006) Safety, tolerability, and efficacy of psilocybin in 9 patients with obsessive-compulsive disorder. J Clin Psychiatry 67(11): 1735-1740 (Pubitemid 44955154)
11. 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 [(-)-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(2):810-818 (Pubitemid 44061255)
12. Rodriguez CA, Azie NE, Adams G et al (2004) Single oral dose safety, tolerability, and pharmacokinetics of PNU-96391 inhealthy volunteers. J Clin Pharmacol 44:276-283 (Pubitemid 38233824)
13. 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(6):899-908
14. Rung JP, Rung E, Johansson AM, Svensson K, Carlsson A, Carlsson ML (2011) Effects of the dopamine stabilizers (S)-(-)-OSU6162 and ACR16 on prolactin secretion in drug-naive and monoamine- depleted rats. Naunyn Schmiedebergs Arch Pharmacol 384:39-45
15. Seeman P, Guan HC (2007) Dopamine partial agonist action of (-) OSU6162 is consistent with dopamine hyperactivity in psychosis. Eur J Pharmacol 557(2-3):151-153 (Pubitemid 46188631)
16. 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(17):2735-2753 (Pubitemid 24273465)
17. Sonesson C (1995) Arylpiperidine and arylpyrrolidine derivatives with potential antipsychotic efficacy. Thesis, ISBN 91-554- 3453-3
18. Svensson KA, Falcone JF, Johansson AM, Perry KW et al (2009) heactions of the dopamine stabilizer ACR16, but not (-)- OSU6162, in behavioral and neurochemical assays are not dependent on the presence of functional dopamine D2 receptors. Presented at the 39th Annual Meeting, Society for Neuroscience. Chicago, October
19. Tedroff J, Ekesbo A, Sonesson C, Waters N, Carlsson A (1999) Longlasting improvement following (-)-OSU6162 in a patient with Huntington's disease. Neurology 53(7):1605-1606 (Pubitemid 29491967)