In vitro and in vivo pharmacological profile of 5-{2-[4-(6-fluoro-1H-indole-3-yl)piperidin-1-yl]ethyl}-4-(4-fluorophenyl) thiazole-2-carboxylic acid amide (NRA0562), a novel and putative atypical antipsychotic

Life Sciences

Volumn 71, Issue 12, 2002, Pages 1371-1384

  Funakoshi, Takeo ^a   Chaki, Shigeyuki ^a   Kawashima, Naoya ^a   Suzuki, Yoshiko ^a   Yoshikawa, Ryoko ^a   Kumagai, Toshihito ^a   Nakazato, Atsuro ^a   Kameo, Kazuya ^a   Goto, Makoto ^b   Okuyama, Shigeru ^a  

^a TAISHO PHARMACEUTICAL CO LTD   (Japan)

^b NIHON NOHYAKU CO LTD   (Japan)

Author keywords

Antipsychotic; Clozapine; In vivo occupancy; Risperidone

Indexed keywords

5 [2 [4 (6 FLUORO 1H INDOL 3 YL)PIPERIDIN 1 YL]ETHYL] 4 (4 FLUOROPHENYL)THIAZOLE 2 CARBOXYLIC ACID AMIDE; ALPHA 1 ADRENERGIC RECEPTOR; CARBOXYLIC ACID DERIVATIVE; CLOZAPINE; DOPAMINE 1 RECEPTOR; DOPAMINE 2 RECEPTOR; DOPAMINE 3 RECEPTOR; DOPAMINE 4 RECEPTOR; HISTAMINE H1 RECEPTOR; METHAMPHETAMINE; NEUROLEPTIC AGENT; NRA 0562; OLANZAPINE; PRAZOSIN; RISPERIDONE; SEROTONIN 2A RECEPTOR; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; CATALEPSY; CONTROLLED STUDY; DOSE RESPONSE; DRUG ACTIVITY; DRUG POTENCY; DRUG RECEPTOR BINDING; EXTRAPYRAMIDAL SYMPTOM; HYPERACTIVITY; IN VITRO STUDY; IN VIVO STUDY; LOCOMOTION; MALE; NONHUMAN; PROTEIN BINDING; RAT; RECEPTOR AFFINITY; RECEPTOR OCCUPANCY; STEREOTYPY;

ANIMALS; ANTIPSYCHOTIC AGENTS; BEHAVIOR, ANIMAL; CATALEPSY; CENTRAL NERVOUS SYSTEM STIMULANTS; CLOZAPINE; HUMANS; MALE; METHAMPHETAMINE; MOTOR ACTIVITY; PIPERIDINES; RATS; RECEPTOR, SEROTONIN, 5-HT2A; RECEPTORS, ADRENERGIC, ALPHA-1; RECEPTORS, DOPAMINE; RECEPTORS, DRUG; RECEPTORS, SEROTONIN; RISPERIDONE; STEREOTYPED BEHAVIOR; THIAZOLES;

EID: 18444398659     PISSN: 00243205     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0024-3205(02)01863-5     Document Type: Article

References (48)

1. Positive and negative symptoms in schizophrenia: A critical reappraisal
2. The significance of dopamine receptor blockade for the mechanism of action of neuroleptic drugs
3. Dopamine receptor binding predicts clinical and pharmacological potencies of antischizophrenic drugs
4. Antipsychotic drug doses and neuroleptic/dopamine receptors
5. Brain dopamine receptors
6. Treatment of schizophrenia: A clinical and preclinical evaluation of neuroleptic drugs
7. The risk and benefits of clozapine versus chlorpromazine
8. Clozapine: A novel antipsychotic agent
9. Improvement in cognitive functions and psychiatric symptoms in treatment of refractory schizophrenic patients receiving clozapine
10. 4
11. 3) as a target for neuroleptics
12. 1C sites
13. Neuroleptic affinities for human brain receptors and their use in predicting adverse effects
14. 4 receptor with high affinity for the antipsychotic clozapine
15. 4 receptor selective antagonist
16. 4 receptor antagonist, does not exhibit a neuroleptic-like profile in rodent behavioral tests
17. Pilot clinical investigation of risperidone in the treatment of psychotic patients
18. 2A receptors in antipsychotic activity
19. Thymostenic effects of ritanserin (R55667), a centrally acting serotonin-S2 receptor blocker
20. An open clinical and biochemical study of ritanserin in acute patients with schizophrenia
21. 2A antagonist with a favorable CNS safety profile
22. 2 receptor and alpha 1-adrenoceptor antagonism
23. Phencyclidine-induced deficits in prepulse inhibition of startle are blocked by prazosin, an alpha-1 noeadrenergic antagonist
24. 2A receptor and alpha-1 adrenoceptor antagonist (R)-(+)-2-amino-4-(4-fluorophenyl)-5-[1-[4-(4-fluorophenyl)-4-oxobutyl] pyrrolidin-3-yl]thiazole (NRA0045)
25. 2A receptor antagonist, in rats
26. 4 receptor antagonist, NRA0160: A preclinical neuropharmacological profile
27. In vivo receptor occupancy of NRA0045, a putative atypical antipsychotic, in rats
28. In vitro and in vivo receptor binding and effects on monoamine turnover in rat brain regions of the novel antipsychotics risperidone and ocaperidone
29. 2 receptor occupancy
30. Identical antagonist selectivity of central and peripheral alpha1-adrenoceptors
31. Risperidone compared with new and reference antipsychotic drugs: In vitro and in vivo receptor binding
32. NE-100, a novel sigma receptor ligand: In vivo test
33. Adverse effects of clozapine
34. The relationship of pharmacology to side effects
35. Seizure associated with olanzapine
36. A comparison of the effects of clozapine and olanzapine on the EEG in patients with schizophrenia
37. Review and management of clozapine side effects
38. 2 antagonist MDL100,907 as a putative atypical antipsychotic: Behavioral, electrophysiological, and neurochemical studies
39. Behavioral responses to psychomotor stimulant drugs: Localization in the central nervous system
40. Catalepsy as a rodent model for detecting antipsychotic drugs with extrapyramidal side effect liability
41. Effect of desipramine on dopamine receptor binding in vivo
42. The receptor occupation and plasma concentration of NKY-722, a water soluble dihydropyridine-type calcium antagonist, in spontaneously hypertensive rats
43. Prazosin modulates the changes in firing pattern and transmitter release induced by raclopride in the mesolimbic, but not in the nigrostriatal dopaminergic system
44. 2 receptor and alpha 1-adrenoceptor antagonism
45. 4 receptor antagonists reverse apomorphine-induced blockade of prepulse inhibition
46. 4 receptor antagonist reversal of subchronic phencyclidine-induced object retrieval/detour deficits in monkeys
47. 3 receptor agonist, (PD128,907)
48. 2 dopamine receptor agonists and antagonists on prepulse inhibition of acoustic startle in the rat