5-Hydroxytryptamine2A receptor inverse agonists as antipsychotics

Journal of Pharmacology and Experimental Therapeutics

Volumn 299, Issue 1, 2001, Pages 268-276

  Weiner, D M ^a,b,c   Burstein, E S ^a   Nash, N ^a   Croston, G E ^a   Currier, E A ^a   Vanover, K E ^a   Harvey, S C ^a   Donohue, E ^a   Hansen, H C ^a   Andersson, C M ^a   Spalding, T A ^a   Gibson, D F C ^a,d   Krebs Thomson, K ^c   Powell, S B ^c   Geyer, M A ^c   Hacksell, U ^a   Brann, M R ^a,c  

^a ACADIA PHARMACEUTICALS INC   (United States)

^b UNIVERSITY OF CALIFORNIA   (United States)

^c UNIVERSITY OF CALIFORNIA   (United States)

^d Dow Pharmaceutical Sciences Inc   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

AC 90179; ALPHA (2,3 DIMETHOXYPHENYL) 1 [2 (4 FLUOROPHENYL)ETHYL] 4 PIPERIDINEMETHANOL; AMOXAPINE; BUTACLAMOL; CHLORPROMAZINE; CLOROTEPINE; CLOTIAPINE; CLOZAPINE; DOPAMINE 2 RECEPTOR BLOCKING AGENT; FLUPENTIXOL; FLUSPIRILENE; G PROTEIN COUPLED RECEPTOR; HISTAMINE H1 RECEPTOR AGONIST; HISTAMINE H1 RECEPTOR ANTAGONIST; LOXAPINE; NEUROLEPTIC AGENT; OLANZAPINE; PIMOZIDE; RISPERIDONE; SEROTONIN 2A AGONIST; SEROTONIN 2B RECEPTOR; SEROTONIN 2B RECEPTOR BLOCKING AGENT; SEROTONIN 2B RECEPTOR STIMULATING AGENT; SEROTONIN 2C AGONIST; SEROTONIN 2C ANTAGONIST; SERTINDOLE; SPIPERONE; TEFLUDAZINE; TIOSPIRONE; UNCLASSIFIED DRUG; UNINDEXED DRUG; GUANINE NUCLEOTIDE BINDING PROTEIN; SEROTONIN 2A RECEPTOR; SEROTONIN AGONIST; SEROTONIN RECEPTOR;

AGONIST; ANIMAL EXPERIMENT; ARTICLE; BEHAVIOR; BIOASSAY; COMPETITIVE INHIBITION; DRUG EFFECT; DRUG EFFICACY; DRUG POTENCY; DRUG SCREENING; EXTRAPYRAMIDAL SYMPTOM; HEAD TWITCH; LOCOMOTION; MALE; MONOAMINERGIC SYSTEM; MOUSE; NONHUMAN; PRIORITY JOURNAL; PSYCHOPHARMACOLOGY; RAT; STARTLE REFLEX; ANIMAL; ANIMAL BEHAVIOR; GENE AMPLIFICATION; HEAD MOVEMENT; METABOLISM; MOLECULAR CLONING; MOTOR ACTIVITY; QUANTITATIVE STRUCTURE ACTIVITY RELATION; SPRAGUE DAWLEY RAT;

ANIMALS; ANTIPSYCHOTIC AGENTS; BEHAVIOR, ANIMAL; CLONING, MOLECULAR; DRUG EVALUATION, PRECLINICAL; GENE AMPLIFICATION; GTP-BINDING PROTEINS; HEAD MOVEMENTS; MALE; MICE; MOTOR ACTIVITY; QUANTITATIVE STRUCTURE-ACTIVITY RELATIONSHIP; RATS; RATS, SPRAGUE-DAWLEY; RECEPTOR, SEROTONIN, 5-HT2A; RECEPTORS, SEROTONIN; SEROTONIN AGONISTS; STARTLE REACTION;

EID: 0034741106     PISSN: 00223565     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (41)

1. Pharmacogenetic prediction of clozapine response
2. Effects of amperozide in schizophrenia. An open study of a potent 5-HT2 receptor antagonist
3. Clozapine antagonizes phencyclidine-induced deficits in sensorimotor gating of the startle response
4. Mutations and diseases of G protein coupled receptors
5. Molecular physiology of norepinephrine and serotonin transporters
6. Physiological effects of inverse agonists in transgenic mice with myocardial overexpression of the beta 2-adrenoceptor
7. Identification of a family of muscarinic acetylcholine receptor genes
8. Cloning and expression of the human and rat m5 muscarinic acetylcholine receptor genes
9. Pharmacology of muscarinic acetylcholine receptor subtypes (m1-m5): High throughput assays in mammalian cells
10. Interactions of muscarinic receptors with the heterotrimeric G proteins Gq and G12: Transduction of proliferative signals
11. Pharmacology of muscarinic receptor subtypes constitutively activated by G proteins
12. Radioreceptor binding profile of the atypical antipsychotic olanzapine
13. Dopamine receptor binding predicts clinical and pharmacological potencies of antischizophrenic drugs
14. The neuroleptics: A historical survey
15. 2A receptor by site-directed mutagenesis: Revelation of inverse agonist activity of antagonists
16. 2A receptor by site-directed mutagenesis: Inverse agonist activity of antipsychotic drugs
17. Differences in agonist-independent activity of 5-HT2A and 5-HT2C receptors revealed by heterologous expression
18. Muscarinic cholinergic and histamine H1 receptor binding of phenothiazine drug metabolites
19. 2C receptors
20. Initial sequencing and analysis of the human genome
21. Preclinical characterization of the potential of the putative atypical antipsychotic MDL 100,907 as a potent 5-HT2A antagonist with a favorable CNS safety profile
22. Constitutive activity of receptors coupled to guanine nucleotide regulator proteins
23. Serotonergic component of neuroleptic receptors
24. Characterization of the human dopamine D3 receptor expressed in transfected cell lines
25. Dopaminergic stimulation disrupts sensorimotor gating in the rat
26. Rodent data and general hypothesis: Antipsychotic action exerted through 5-HT2A receptor antagonism is dependent on increased serotonergic tone
27. MK-801-induced hyperlocomotion: Differential effects of M100907, SDZ PSD 958 and raclopride
28. The effects of clozapine, risperidone, and olanzapine on cognitive function in schizophrenia
29. Inverse agonism: Pharmacological curiosity or potential therapeutic strategy?
30. High constitutive activity of native H3 receptors regulates histamine neurons in brain
31. Treatment with inverse agonists enhances baseline atrial contractility in transgenic mice with chronic beta2-adrenoceptor activation
32. RNA editing of the human serotonin 5-hydroxytryptamine 2C receptor silences constitutive activity
33. Binding of typical and atypical antipsychotic agents to transiently expressed 5-HT1C receptors
34. Antipsychotic drug doses and neuroleptic/dopamine receptors
35. Pharmacology of a constitutively active muscarinic receptor generated by random mutagenesis
36. Characterization of typical and atypical antipsychotic drugs based on in vivo occupancy of serotonin2 and dopamine2 receptors
37. Molecular cloning and expression of a dopamine D2 receptor from human retina
38. Cloning of the gene for a human dopamine D5 receptor with higher affinity for dopamine than D1
39. Human dopamine D1 receptor encoded by an intronless gene on chromosome 5
40. A randomized, controlled, dose-ranging trial of sertindole in patients with schizophrenia
41. M100907, a serotonin 5-HT2A receptor antagonist and putative antipsychotic, blocks dizocilpine-induced prepulse inhibition deficits in Sprague-Dawley and Wistar rats