In vivo quantification of calcitonin gene-related peptide receptor occupancy by telcagepant in rhesus monkey and human brain using the positron emission tomography tracer [11C]MK-4232

Journal of Pharmacology and Experimental Therapeutics

Volumn 347, Issue 2, 2013, Pages 478-486

  Hostetler, Eric D ^a   Joshi, Aniket D ^a   Sanabria Bohórquez, Sandra ^a   Fan, Hong ^a   Zeng, Zhizhen ^a   Purcell, Mona ^a   Gantert, Liza ^a   Riffel, Kerry ^a   Williams, Mangay ^a   O'Malley, Stacey ^a   Miller, Patricia ^a   Selnick, Harold G ^a   Gallicchio, Steven N ^a   Bell, Ian M ^a   Salvatore, Christopher A ^a   Kane, Stefanie A ^a   Li, Chi Chung ^a   Hargreaves, Richard J ^a   De Groot, Tjibbe ^b   Bormans, Guy ^a   Van Hecken, Anne ^b   Derdelinckx, Inge ^b   De Hoon, Jan ^b   Reynders, Tom ^c   Declercq, Ruben ^c   De Lepeleire, Inge ^c   Kennedy, W P ^d   Blanchard, Rebecca ^d,e   Marcantonio, Eugene E ^f   Sur, Cyrille ^a   Cook, Jacquelynn J ^a   Van Laere, Koen ^b   Evelhoch, Jeffrey L ^a   more..

^a MERCK RESEARCH LABORATORIES   (United States)

^b UNIVERSITY HOSPITALS LEUVEN   (Belgium)

^c UNIVERSITY OF LEUVEN   (Belgium)

^d Merck Sharp and Dohme   (Belgium)

^e Merck Clinical Pharmacology   (United States)

^f Merck Clinical Pharmacology   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

2 [8 (3,5 DIFLUOROPHENYL) 10 OXO 6,9 DIAZASPIRO[4.5]DEC 9 YL] N [[2' OXO 1,1',2',3 TETRAHYDROSPIROINDENE 2,3' PYRROLO[2,3 B]PYRIDIN] 5 YL]ACETAMIDE; 2 [8 (3,5 DIFLUOROPHENYL) 6,8 DIMETHYL 10 OXO 6,9 DIAZASPIRO[4.5]DEC 9 YL] N [2' OXO 1,1',2',3 TETRAHYDROSPIRO(INDENE 2,3' PYRROLO[2,3 B]PYRIDIN) 5 YL]ACETAMIDE; 2 [8 (3,5 DIFLUOROPHENYL) 6,8 DIMETHYL 10 OXO 6,9 DIAZASPIRO[4.5]DEC 9 YL] N [2' OXO 1,1',2',3 TETRAHYDROSPIRO(INDENE 2,3' PYRROLO[2,3 B]PYRIDIN) 5 YL]ACETAMIDE C 11; AGENTS INTERACTING WITH TRANSMITTER, HORMONE OR DRUG RECEPTORS; CALCITONIN GENE RELATED PEPTIDE RECEPTOR; MK 3207; MK 4232; N [[1 (3,5 DIFLUOROPHENYL)ETHYL]] 1,4 DIMETHYL N [2 OXO 2 [[2' OXO 1,1',2',3 TETRAHYDROSPIRO(INDENE 2,3' PYRROLO[2,3 B]PYRIDIN) 5 YL]AMINO]ETHYL]PIPERIDINE 4 CARBOXAMIDE C 11; TELCAGEPANT; TRACER; TRITIUM; UNCLASSIFIED DRUG;

ADULT; ANIMAL EXPERIMENT; ARTICLE; BINDING AFFINITY; BOLUS INJECTION; BRAIN REGION; CONTROLLED STUDY; DRUG ANTAGONISM; DRUG BLOOD LEVEL; DRUG DOSE COMPARISON; DRUG EFFICACY; DRUG MEGADOSE; DRUG POTENCY; DRUG RECEPTOR BINDING; DRUG SPECIFICITY; FEMALE; HUMAN; HUMAN EXPERIMENT; HUMAN TISSUE; IN VITRO STUDY; IN VIVO STUDY; MALE; MIGRAINE; NONHUMAN; NORMAL HUMAN; POSITRON EMISSION TOMOGRAPHY; PRIORITY JOURNAL; QUANTITATIVE ANALYSIS; RECEPTOR OCCUPANCY; RHESUS MONKEY;

ACETANILIDES; ADULT; ANALGESICS; ANIMALS; AZEPINES; BRAIN; CARBON RADIOISOTOPES; FEMALE; HUMANS; IMIDAZOLES; MACACA MULATTA; MALE; MIDDLE AGED; MIGRAINE DISORDERS; MOLECULAR STRUCTURE; POSITRON-EMISSION TOMOGRAPHY; PROTEIN BINDING; RADIOPHARMACEUTICALS; RECEPTORS, CALCITONIN GENE-RELATED PEPTIDE; SPECIES SPECIFICITY; SPIRO COMPOUNDS; TISSUE DISTRIBUTION; YOUNG ADULT;

EID: 84886024087     PISSN: 00223565     EISSN: 15210103     Source Type: Journal    
DOI: 10.1124/jpet.113.206458     Document Type: Article

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