4-(Phenylsulfonyl)piperidines: Novel, selective, and bioavailable 5-HT2A receptor antagonists

Journal of Medicinal Chemistry

Volumn 45, Issue 2, 2002, Pages 492-503

  Fletcher, Stephen R ^a   Burkamp, Frank ^a   Blurton, Peter ^a   Cheng, Susan K F ^a   Clarkson, Robert ^a   O'Connor, Desmond ^a   Spinks, Daniel ^a   Tudge, Matthew ^a   Van Niel, Monique B ^a   Patel, Smita ^a   Chapman, Kerry ^a   Marwood, Rose ^a   Shepheard, Sara ^a   Bentley, Graham ^a   Cook, Gina P ^a   Bristow, Linda J ^a   Castro, Jose L ^a   Hutson, Peter H ^a   MacLeod, Angus M ^a  

^a NEUROSCIENCE RESEARCH CENTRE   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

ALPHA (2,3 DIMETHOXYPHENYL) 1 [2 (4 FLUOROPHENYL)ETHYL] 4 PIPERIDINEMETHANOL; EPLIVANSERIN; FANANSERIN; MIRTAZAPINE; NEFAZODONE; OLANZAPINE; PIPERIDINE DERIVATIVE; RISPERIDONE; SEROTONIN ANTAGONIST;

ANIMAL CELL; ARTICLE; BINDING AFFINITY; BIOAVAILABILITY; DRUG EFFICACY; DRUG PENETRATION; LIVER MICROSOME; NONHUMAN; RECEPTOR BLOCKING; RECEPTOR OCCUPANCY; SCREENING;

ADMINISTRATION, ORAL; ANIMALS; BENZAMIDES; BIOLOGICAL AVAILABILITY; BRAIN; CATION TRANSPORT PROTEINS; CELL LINE; CRICETINAE; DNA-BINDING PROTEINS; DRUG EVALUATION, PRECLINICAL; ELECTROCARDIOGRAPHY; ETHER-A-GO-GO POTASSIUM CHANNELS; FERRETS; HUMANS; MALE; MICROSOMES, LIVER; NITRILES; PIPERIDINES; POTASSIUM CHANNELS; POTASSIUM CHANNELS, VOLTAGE-GATED; RADIOLIGAND ASSAY; RATS; RATS, SPRAGUE-DAWLEY; RECEPTOR, SEROTONIN, 5-HT2A; RECEPTORS, SEROTONIN; SEROTONIN AGONISTS; SEROTONIN ANTAGONISTS; SPIRO COMPOUNDS; STRUCTURE-ACTIVITY RELATIONSHIP; SULFONES; TRANS-ACTIVATORS;

EID: 0037122751     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm011030v     Document Type: Article

References (32)

1. 2C receptors
2. 2C receptors expressed in the human neuroblastoma cell line SH-SY5Y: Comparative stimulation by hallucinogenic drugs
3. A novel approach to the identification of psychiatric drugs: Serotonin-glutamate interactions in the prefrontal cortex
4. The pharmacologic profile of mirtazepine
5. Evaluation of nefazodone as a serotonin uptake inhibitor and a serotonin antagonist in vivo
6. 2A and muscarinic receptors
7. 2C antagonistic properties of newer antipsychotics
8. 2 Antagonists: A concept for the treatment of schizophrenia
9. 4 receptor
10. 2A antagonist with a favorable CNS safety profile
11. 2 receptor antagonist
12. 2A antagonist fananserin in the treatment of schizophrenia
13. Current and novel approaches to the drug treatment of schizophrenia
14. 2A receptor occupancy in M 100907-treated schizophrenic patients
15. 2A receptor antagonists
16. Piperidinylteralin σ ligands
17. Drugs that prolong QT interval as an unwanted effect: Assessing their likelihood of inducing hazardous cardiac dysrhythmias
18. Lipophilicity and related molecular properties as determinants of pharmacokinetic behavior
19. Potent 3-spiropiperidine growth hormone secretagogues
20. Synthesis of 5′-alkylthio-5′-deoxynucleosides from nucleosides in a one-pot reaction
21. Selective oxidation of phenyl sulphides to sulphoxides or sulphones using oxone and wet alumina
22. Signal transduction differences between 5-hydroxytryptamine type 2A and type 2C receptor systems
23. 4 receptor
24. 3H] prazosin binding
25. Relative affinities of drugs acting at cholinoceptors in displacing agonist and antagonist radioligands: The NMS/Oxo-M ratio as an index of efficacy at cortical muscarinic receptors
26. The synthesis of antineoplastic agents XXXII. N-nitrosoureas
27. Preparation and characterisation of microsomal fractions for studies on xenobiotic metabolism