SB-243213; a selective 5-HT2C receptor inverse agonist with improved anxiolytic profile: Lack of tolerance and withdrawal anxiety

Neuropharmacology

Volumn 41, Issue 2, 2001, Pages 186-199

  Wood, M D ^a   Reavill, C ^a   Trail, B ^a   Wilson, A ^a   Stean, T ^a   Kennett, G A ^a,b   Lightowler, S ^a,b   Blackburn, T P ^a,c   Thomas, D ^a   Gager, T L ^a   Riley, G ^a   Holland, V ^a   Bromidge, S M ^a   Forbes, I T ^a   Middlemiss, D N ^a  

^a GLAXOSMITHKLINE   (United Kingdom)

^b Vernalis PLC   (United Kingdom)

^c H LUNDBECK A S   (Denmark)

Author keywords

5 HT2C receptor; Anxiety; Catalepsy; Feeding; SB 243213; Seizures; Tolerance; Withdrawal

Indexed keywords

(3 CHLOROPHENYL)PIPERAZINE; 1,2,3,5 TETRAHYDRO 5 METHYL 1 (3 PYRIDYLCARBAMOYL)PYRROLO[2,3 F]INDOLE; 5 METHYL 1 [[2 [(2 METHYL 3 PYRIDYL)OXY] 5 PYRIDYL]CARBAMOYL] 6 TRIFLUOROMETHYLINDOLINE; 5 METHYL 1 [[2 [(2 METHYL 3 PYRIDYL)OXYL] 5 PYRIDYL]CARBAMOYL] 6 TRIFLUOROMETHLYINDOLINE HYDROCHLORIDE; 6 CHLORO 5 METHYL 1 [[2 [(2 METHYL 3 PYRIDYL)OXY] 5 PYRIDYL]CARBAMOYL]INDOLINE; 8 AMINO 7 CHLORO 1,4 BENZODIOXAN 5 CARBOXYLIC ACID 1 BUTYL 4 PIPERIDINYLMETHYL ESTER; 8 AMINO 7 CHLORO 1,4 BENZODIOXAN 5 CARBOXYLIC ACID 1 BUTYL 4 PIPERIDINYLMETHYL ESTER 1,2,3,5 TETRAHYDRO 5 METHYL 1 (3 PYRIDYLCARBAMOYL)PYRROLO[2,3 F]INDOLE; 8 AMINO 7 IODO 1,4 BENZODIOXAN 5 CARBOXYLIC ACID 1 BUTYL 4 PIPERIDINYLMETHYL ESTER; AMPHETAMINE; ANXIOLYTIC AGENT; BENZODIAZEPINE DERIVATIVE; DIAZEPAM; DIZOCILPINE; EMONAPRIDE; HALOPERIDOL; ION CHANNEL; PHENCYCLIDINE; POLIDOCANOL; SEROTONIN 2C RECEPTOR; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANXIETY; ARTICLE; BODY WEIGHT; CATALEPSY; CONTROLLED STUDY; DIAGNOSTIC TEST; DOPAMINERGIC TRANSMISSION; DRUG INHIBITION; DRUG POTENTIATION; DRUG SELECTIVITY; DRUG TOLERANCE; HUMAN; HUMAN CELL; HYPERACTIVITY; IN VIVO STUDY; LOCOMOTION; MALE; NEUROTRANSMISSION; NONHUMAN; PRIORITY JOURNAL; RAT; RECEPTOR AFFINITY; RECEPTOR BLOCKING; SEIZURE THRESHOLD; SOCIAL INTERACTION; TRANQUILIZING ACTIVITY; WITHDRAWAL SYNDROME;

ANIMALS; ANTI-ANXIETY AGENTS; ANXIETY; CATALEPSY; DIAZEPAM; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG TOLERANCE; HUMANS; INDOLES; INOSITOL PHOSPHATES; MALE; MOTOR ACTIVITY; PYRIDINES; RATS; RATS, SPRAGUE-DAWLEY; RECEPTOR, SEROTONIN, 5-HT2C; RECEPTORS, SEROTONIN; SOCIAL BEHAVIOR; SUBSTANCE WITHDRAWAL SYNDROME;

EID: 0034903523     PISSN: 00283908     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0028-3908(01)00054-5     Document Type: Article

References (44)

1. 2C receptor protein in human and rat brain using specific antisera
2. Evidence that the median raphe nucleus-dorsal hippocampal pathway mediates diazepam withdrawal induced anxiety
3. An autoradiographic analysis of the differential ascending projections of the dorsal and median raphe nuclei in the rat
4. Effect of drugs influencing central serotonergic mechanisms on haloperidol-induced catalepsy
5. 2C/2B receptor antagonist SB 221284
6. 2 receptor antagonists can attenuate sub-maximal haloperidol-induced catalepsy in rats
7. 2C receptor inverse agonists: Identification of 5-methyl-1-[[2-[(2-methyl-3-pyridyl)oxy]- 5-pyridyl]carbamoyl]-6-trifluoromethylindoline (SB-243213) as a potential antidepressant/anxiolytic agent
8. 2A receptor-mediated phosphoinositide (PI) turnover by clozapine in the rat: A comparison to other antipsychotics
9. Antipsychotic drugs, neurotransmitters and schizophrenia
10. Repeated treatment with imipramine and amitryptiline reduced the immobility of rats in the forced swimming test by enhancing dopamine mechanisms in the nucleus accumbens
11. 4.4 receptors expresses in Chinese hamster ovary cells
12. 2C receptors: A parallel phosphatidylinositol and calcium accumulation comparison with clozapine and haloperidol
13. SB-242084, a selective serotonin2C receptor antagonist, increases dopaminergic transmission in the mesolimbic system
14. 2C receptor antagonist
15. 2C-induced oral dyskinesia
16. The effect of treatment regimen on the development of tolerance to the sedative and anxiolytic effects of diazepam
17. The use of social interaction as a method for detecting anxiolytic activity of chlordiazepoxide-like drugs
18. 2C receptor antagonism in the substantia nigra zona reticulata of the 6-hydroxydopamine-lesioned rat model of Parkinson's Disease
19. Evidence for 5-HT2 involvement in the mechanism of action of hallucinogenic agents
20. VII. International Union of Pharmacology classification of receptors for 5-hydroxytryptamine (serotonin)
21. m-Chlorophenylpiperazine as a probe of serotonin function
22. Cataleptogenic effect of subtype selective 5-HT receptor antagonists in the rat
23. 2A antagonist with a favourable CNS safety profile
24. 1C receptors and their therapeutic relevance
25. 2C/2B receptor antagonist
26. 2C receptor antagonist
27. 2C/2B receptor antagonist
28. Preclinical pharmacology of atypical antipsychotic drugs
29. i values
30. 2C receptor agonists exhibit antidepressant-like properties in the anhedonia model of depression
31. 2 receptor antagonism reduces hyperactivity induced by amphetamine, cocaine, and MK-801 but not D1 agonist C-APB
32. Dose-dependent and time-dependent changes in phencyclidine metabolite covalent binding in rats and the possible role of cyp2D1
33. Distribution and cellular localisation of the serotonin type 2C receptor messenger RNA in human brain
34. Treatment of neuroleptic-induced akathisia with the 5-HT2 antagonist mianserin
35. Serotonergic agents in the treatment of acute neuroleptic-induced akathisia: Open-label study of buspirone and mianserin
36. 4 receptor antagonism does not affect motor and reward mechanisms in the rat
37. 2C receptor antagonist
38. 2C receptor gene inactivation
39. 2C serotonin receptors
40. 2B receptor
41. 2C receptors in functional studies
42. 2C receptor
43. 2A receptor
44. 2 receptor subtype mRNAs in rat brain