2-Aryl tryptamines: selective high-affinity antagonists for the h5-HT2A receptor.

PubWeight™: 4.03‹?› | Rank: Top 1%

🔗 View Article (PMID 11133071)

Published in Bioorg Med Chem Lett on December 18, 2000

Authors

G I Stevenson1, A L Smith, S Lewis, S G Michie, J G Neduvelil, S Patel, R Marwood, S Patel, J L Castro

Author Affiliations

1: Merck Sharp & Dohme Research Laboratories, Thle Neuroscience Research Centre, Harlow, Essex, UK. graeme_stevenson@merck.com

Articles citing this

4-(2,4-Dichlorophenyl)-2-(1H-indol-3-yl)-6-(2-pyridyl)-1,4-dihydropyridine-4-carbonitrile. Acta Crystallogr Sect E Struct Rep Online (2008) 1.18

3'-Benz-yloxy-3-hydr-oxy-3,3'-bi-1H-indole-2,2'(3H,3'H)-dione monohydrate. Acta Crystallogr Sect E Struct Rep Online (2009) 1.08

4'-(4-Methoxy-phen-yl)-1,1',1''-trimethyl-dispiro-[indoline-3,2'-pyrrolidine-3',3''-pyrrolidine]-2,2'',5''-trione. Acta Crystallogr Sect E Struct Rep Online (2009) 0.94

3-(4-Fluoro-phenyl)-1-[1'-(4-fluoro-phenyl)-2-oxo-5',6',7',7a'-tetra-hydro-1H-indole-3(2H)-spiro-3'(2'H)-1H'-pyrrol-izin-2'-yl]prop-2-en-1-one. Acta Crystallogr Sect E Struct Rep Online (2008) 0.93

4-(2,4-Dichloro-phen-yl)-6-(1H-indol-3-yl)-2,2'-bipyridine-5-carbonitrile. Acta Crystallogr Sect E Struct Rep Online (2009) 0.88

Potential modes of interaction of 9-aminomethyl-9,10-dihydroanthracene (AMDA) derivatives with the 5-HT2A receptor: a ligand structure-affinity relationship, receptor mutagenesis and receptor modeling investigation. J Med Chem (2008) 0.88

1'-Methyl-2,2''-dioxoindoline-3-spiro-2'-pyrrolidine-3'-spiro-3''-indoline-4',4'-di-carbonitrile. Acta Crystallogr Sect E Struct Rep Online (2009) 0.82

Crystal structure of ethyl 1',1''-dimethyl-2'',3-dioxo-3H-di-spiro-[benzo[b]thio-phene-2,3'-pyrrolidine-2',3''-indoline]-4'-carboxyl-ate. Acta Crystallogr E Crystallogr Commun (2015) 0.75

Diethyl [(3-cyano-1-phenyl-sulfonyl-1H-indol-2-yl)meth-yl]phospho-nate. Acta Crystallogr Sect E Struct Rep Online (2011) 0.75

1-[2-Oxo-1'-phenyl-2',3',5',6',7',7a'-hexa-hydroindoline-3-spiro-3'-1'H-pyrrolizin-2'-yl]-3-phenyl-prop-2-en-1-one. Acta Crystallogr Sect E Struct Rep Online (2008) 0.75

1-Allyl-3,3-di-p-tolyl-indolin-2-one. Acta Crystallogr Sect E Struct Rep Online (2008) 0.75

2-(1H-indol-3-ylcarbon-yl)acetonitrile. Acta Crystallogr Sect E Struct Rep Online (2009) 0.75

1'-Butyl-2-methyl-1',2,2',3,4,9-hexa-hydro-spiro-[benzo[f]isoindole-1,3'-indole]-2',4,9-trione. Acta Crystallogr Sect E Struct Rep Online (2012) 0.75

Trimethyl 1-(2-methyl-1-phenylsulfonyl-1H-indol-3-yl)propane-1,2,3-tricarbox-ylate. Acta Crystallogr Sect E Struct Rep Online (2009) 0.75

Diethyl 2-oxo-3-(2-oxo-2,3-dihydro-1H-indol-3-yl-idene)butane-dioate. Acta Crystallogr Sect E Struct Rep Online (2009) 0.75

Crystal structures of three indole derivatives: 3-ethnyl-2-methyl-1-phenyl-sulfonyl-1H-indole, 4-phenyl-sulfonyl-3H,4H-cyclo-penta-[b]indol-1(2H)-one and 1-{2-[(E)-2-(5-chloro-2-nitro-phen-yl)ethen-yl]-1-phenyl-sulfonyl-1H-indol-3-yl}ethan-1-one chloro-form monosolvate. Acta Crystallogr E Crystallogr Commun (2015) 0.75

(1'S,12'R,13'S,17'S)-15',15'-Dimethyl-1,2-dihydro-11',14',16',18'-tetra-oxa-7'-aza-spiro-[indole-3,8'-penta-cyclo-[10.6.0.0(2,9).0(3,7).0(13,17)]octa-deca-ne]-2,10'-dione. Acta Crystallogr Sect E Struct Rep Online (2013) 0.75

Articles by these authors

Gene ontology: tool for the unification of biology. The Gene Ontology Consortium. Nat Genet (2000) 336.52

The Gene Ontology (GO) database and informatics resource. Nucleic Acids Res (2004) 54.37

Comparative genomics of the eukaryotes. Science (2000) 26.62

Functional annotation of a full-length mouse cDNA collection. Nature (2001) 23.61

Reactome: a knowledgebase of biological pathways. Nucleic Acids Res (2005) 20.05

Effect of aerosolized recombinant human DNase on exacerbations of respiratory symptoms and on pulmonary function in patients with cystic fibrosis. The Pulmozyme Study Group. N Engl J Med (1994) 7.98

Chromatin cleavage in apoptosis: association with condensed chromatin morphology and dependence on macromolecular synthesis. J Pathol (1984) 6.67

HOLE: a program for the analysis of the pore dimensions of ion channel structural models. J Mol Graph (1996) 6.48

Heterogeneity of coronary heart disease risk factors in Indian, Pakistani, Bangladeshi, and European origin populations: cross sectional study. BMJ (1999) 6.40

A rapid chemical assay for gentamicin. N Engl J Med (1972) 6.36

Organization and reorganization of immunoglobulin genes in A-MULV-transformed cells: rearrangement of heavy but not light chain genes. Cell (1981) 6.31

Intermittent administration of inhaled tobramycin in patients with cystic fibrosis. Cystic Fibrosis Inhaled Tobramycin Study Group. N Engl J Med (1999) 6.23

Sedative but not anxiolytic properties of benzodiazepines are mediated by the GABA(A) receptor alpha1 subtype. Nat Neurosci (2000) 5.53

Growth curves and survival characteristics of the animals used in the Biomarkers of Aging Program. J Gerontol A Biol Sci Med Sci (1999) 5.24

Inhibition of Bax channel-forming activity by Bcl-2. Science (1997) 5.10

Haemophilus influenzae meningitis in infant rats after intranasal inoculation. J Infect Dis (1974) 4.94

Longitudinal assessment of Pseudomonas aeruginosa in young children with cystic fibrosis. J Infect Dis (2000) 4.93

Production of Haemophilus influenzae b meningitis in infant rats by intraperitoneal inoculation. Infect Immun (1973) 4.80

The defect in murine severe combined immune deficiency: joining of signal sequences but not coding segments in V(D)J recombination. Cell (1988) 4.34

Characterization of non-beta-lactamase-mediated ampicillin resistance in Haemophilus influenzae. Antimicrob Agents Chemother (1984) 4.25

Photoactivated gamma-secretase inhibitors directed to the active site covalently label presenilin 1. Nature (2000) 4.12

The natural history of asthma in childhood. J Epidemiol Community Health (1986) 4.09

Changing patterns in surgical infections. Ann Surg (1973) 3.88

Human herpesvirus 8 variants in sarcoid tissues. Lancet (1997) 3.87

Continuing kappa-gene rearrangement in a cell line transformed by Abelson murine leukemia virus. Cell (1982) 3.86

Chronic Lyme borreliosis in the laboratory mouse. Am J Pathol (1993) 3.82

Comparison of percutaneous and surgical tracheostomies. Chest (1996) 3.56

The Genome Knowledgebase: a resource for biologists and bioinformaticists. Cold Spring Harb Symp Quant Biol (2003) 3.55

Orexin A activates locus coeruleus cell firing and increases arousal in the rat. Proc Natl Acad Sci U S A (1999) 3.42

Correction of hemophilia B in canine and murine models using recombinant adeno-associated viral vectors. Nat Med (1999) 3.39

Simvastatin has anti-inflammatory and antiatherosclerotic activities independent of plasma cholesterol lowering. Arterioscler Thromb Vasc Biol (2001) 3.38

Lung cancer and cryptogenic fibrosing alveolitis. A population-based cohort study. Am J Respir Crit Care Med (2000) 3.36

Improved enzymatic assay of chloramphenicol. Clin Chem (1978) 3.31

Seroprevalence, correlates, and characteristics of undetected coeliac disease in England. Gut (2003) 3.30

Occupational exposure to metal or wood dust and aetiology of cryptogenic fibrosing alveolitis. Lancet (1996) 3.28

Prevalence of wheeze and asthma and relation to atopy in urban and rural Ethiopia. Lancet (1997) 3.23

Fibroblast growth factor-2 (FGF-2) induces vascular endothelial growth factor (VEGF) expression in the endothelial cells of forming capillaries: an autocrine mechanism contributing to angiogenesis. J Cell Biol (1998) 3.12

Comparison of diameter and perimeter methods for tumor volume calculation. J Clin Oncol (2001) 3.09

Math5 is required for retinal ganglion cell and optic nerve formation. Development (2001) 3.07

Amplification of DNA of Mycobacterium tuberculosis from peripheral blood of patients with pulmonary tuberculosis. Lancet (1994) 3.04

BRCA2 mutations in primary breast and ovarian cancers. Nat Genet (1996) 2.91

Hemophilus influenzae type B susceptibility to 17 antibiotics. J Pediatr (1975) 2.74

Lyme borreliosis in genetically resistant and susceptible mice with severe combined immunodeficiency. Am J Trop Med Hyg (1992) 2.71

Which atypical antipsychotic. Br J Psychiatry (1998) 2.67

Identification of the major intestinal fatty acid transport protein. Mol Cell (1999) 2.65

Effect of two breathing exercises (Buteyko and pranayama) in asthma: a randomised controlled trial. Thorax (2003) 2.63

Screening and optimization strategies for macromolecular crystal growth. Acta Crystallogr D Biol Crystallogr (1994) 2.62

Safety and efficacy of linagliptin as add-on therapy to metformin in patients with type 2 diabetes: a randomized, double-blind, placebo-controlled study. Diabetes Obes Metab (2011) 2.59

A novel lysosome-associated membrane glycoprotein, DC-LAMP, induced upon DC maturation, is transiently expressed in MHC class II compartment. Immunity (1998) 2.56

Waiting for medical services in Canada: lots of heat, but little light. CMAJ (2000) 2.56

Hippocampal volumes in cognitively normal persons at genetic risk for Alzheimer's disease. Ann Neurol (1998) 2.48

Gentamicin:adenine mononucleotide transferase: partial purification, characterization, and use in the clinical quantitation of gentamicin. J Infect Dis (1974) 2.45

The Niemann-Pick C1 protein resides in a vesicular compartment linked to retrograde transport of multiple lysosomal cargo. J Biol Chem (1999) 2.45

Macrophage subpopulations in lamina propria of normal and inflamed colon and terminal ileum. Gut (1989) 2.44

Rapid detection of chloramphenicol resistance in Haemophilus influenzae. Antimicrob Agents Chemother (1981) 2.41

Failure to detect ampicillin-resistant, non-beta-lactamase-producing Haemophilus influenzae by standard disk susceptibility testing. Antimicrob Agents Chemother (1986) 2.38

A defect in cholesterol esterification in Niemann-Pick disease (type C) patients. Proc Natl Acad Sci U S A (1985) 2.38

L-685,458, an aspartyl protease transition state mimic, is a potent inhibitor of amyloid beta-protein precursor gamma-secretase activity. Biochemistry (2000) 2.36

Male pseudohermaphroditism caused by mutations of testicular 17 beta-hydroxysteroid dehydrogenase 3. Nat Genet (1994) 2.35

Treatment of acute myocardial infarction with anisoylated plasminogen streptokinase activator complex. Br Med J (Clin Res Ed) (1986) 2.33

Case-control study of acute renal failure in patients with cystic fibrosis in the UK. Thorax (2008) 2.32

Doctor-patient interactions in oncology. Soc Sci Med (1996) 2.30

Is the acetylcholine receptor a rabies virus receptor? Science (1982) 2.30

Relative penicillin G resistance in Neisseria meningitidis and reduced affinity of penicillin-binding protein 3. Antimicrob Agents Chemother (1988) 2.28

Stimulation of megakaryocyte and platelet production by a single dose of recombinant human thrombopoietin in patients with cancer. Ann Intern Med (1997) 2.22

Experience in third molar surgery: an update. Br Dent J (2010) 2.22

Transmission of human immunodeficiency virus by heterosexual contact with reference to antenatal screening. Br J Obstet Gynaecol (1989) 2.22

Arsenic trioxide induces a beclin-1-independent autophagic pathway via modulation of SnoN/SkiL expression in ovarian carcinoma cells. Cell Death Differ (2010) 2.17

Palindrome resolution and recombination in the mammalian germ line. Mol Cell Biol (1997) 2.17

Agreement and variability in the interpretation of early CT changes in stroke patients qualifying for intravenous rtPA therapy. Stroke (1999) 2.17

Clinical trial comparing nicotine replacement therapy (NRT) plus brief counselling, brief counselling alone, and minimal intervention on smoking cessation in hospital inpatients. Thorax (2003) 2.15

Severity prediction rules in community acquired pneumonia: a validation study. Thorax (2000) 2.14

Nonspecific proliferative responses of murine lymphocytes to Borrelia burgdorferi antigens. J Infect Dis (1992) 2.11

Investigation into the increase in hay fever and eczema at age 16 observed between the 1958 and 1970 British birth cohorts. BMJ (1997) 2.09

DNA elements are asymmetrically joined during the site-specific recombination of kappa immunoglobulin genes. Science (1985) 2.08

The 2011-2014 prevalence of eosinophilic oesophagitis in the elderly amongst 10 million patients in the United States. Aliment Pharmacol Ther (2015) 2.08

Characterization of chloramphenicol-resistant Haemophilus influenzae. Antimicrob Agents Chemother (1980) 2.07

Studies of the aetiology of neonatal hepatitis and biliary atresia. Arch Dis Child (1977) 2.04

Does examination of urinary sediment identify individuals with Gulf War syndrome? A pilot study. Am J Med Sci (1998) 2.03

Fundamental training. Br Dent J (2009) 2.03

Isolation and assay of rabies serogroup viruses in CER cells. Intervirology (1977) 2.03

The relationship between length of Barrett's oesophagus mucosa and body mass index. Aliment Pharmacol Ther (2014) 2.02

Nicardipine infusion for the prevention of radial artery spasm during myocardial revascularization. J Cardiothorac Vasc Anesth (1998) 2.01

The role of encapsulation and host age in the clearance of Haemophilus influenzae bacteremia. J Infect Dis (1977) 2.01

Characterization of Haemophilus influenzae type b fimbriae. Infect Immun (1984) 2.00

Antibiotics and invasive Haemophilus influenzae. N Engl J Med (1976) 2.00

Seroprotection against serogroup C meningococcal disease in adolescents in the United Kingdom: observational study. BMJ (2008) 1.99

Type C Niemann-Pick disease. Lysosomal accumulation and defective intracellular mobilization of low density lipoprotein cholesterol. J Biol Chem (1988) 1.98

Proximity of the home to roads and the risk of wheeze in an Ethiopian population. Occup Environ Med (2005) 1.98

The effect of bupivacaine skull block on the hemodynamic response to craniotomy. Anesth Analg (1996) 1.97

Selective media for the quantitation of bacteria in cystic fibrosis sputum. J Med Microbiol (1984) 1.95

Interleukin 2 receptor expression by macrophages in inflammatory bowel disease. Clin Exp Immunol (1988) 1.95

Current outcome of antenally diagnosed cystic lung disease. J Pediatr Surg (2004) 1.95

The paradox of Hemophilus infuenzae type B bacteremia in the presence of serum bactericidal activity. J Clin Invest (1976) 1.94

Sepsis and congenital asplenia. J Pediatr (1977) 1.93

T-cell alpha beta + and gamma delta + deficient mice display abnormal but distinct phenotypes toward a natural, widespread infection of the intestinal epithelium. Proc Natl Acad Sci U S A (1996) 1.92

Information preferences of patients with cancer. Lancet (1994) 1.89