Mapping the binding pocket of a novel, high-affinity, slow dissociating tachykinin NK3 receptor antagonist: Biochemical and electrophysiological characterization

Neuropharmacology

Volumn 86, Issue , 2014, Pages 259-272

  Malherbe, Pari ^a   Knoflach, Frédéric ^a   Marcuz, Anne ^a   Bohnert, Claudia ^a   Weber, Michael ^a   Knust, Henner ^a   Ratni, Hasane ^a   Spooren, Will ^a   Ballard, Theresa M ^a   Bissantz, Caterina ^a  

^a F HOFFMANN LA ROCHE LTD   (Switzerland)

Author keywords

Dual NK2 NK3 antagonist; Firing frequency; Inositol phosphate accumulation; Locomotor activity; RO5328673

Indexed keywords

NEUROKININ 2 RECEPTOR; NEUROKININ 3 RECEPTOR; NEUROKININ 3 RECEPTOR ANTAGONIST; OSANETANT; RHODOPSIN; RO 5328673; SENKTIDE; TACHYKININ RECEPTOR; UNCLASSIFIED DRUG; [4 (3,4 DICHLORO PHENYL) 1 [1 (1 METHYLCYCLPROPANECARBONYL)PIPERIDINE 4 5 CARBONYL]PYRROLIDIN 3 YL]METHYL CARBAMIC ACID 4 FLUORO PHENYL ESTER; 4-(3,4-DICHLOROPHENYL)-1-(1-(1-METHYLCYCLOPROPANECARBONYL)PIPERIDINE-4-5 CARBONYL)PYRROLIDIN-3-YL)METHYLCARBAMIC ACID 4-FLUORO-PHENYL ESTER; AGENTS INTERACTING WITH TRANSMITTER, HORMONE OR DRUG RECEPTORS; CARBAMIC ACID DERIVATIVE; CENTRAL NERVOUS SYSTEM AGENTS; NEUROLEPTIC AGENT; PEPTIDE FRAGMENT; PIPERIDINE DERIVATIVE; SUBSTANCE P; ADENOSINE RECEPTOR; APREPITANT; BETA 2 ADRENERGIC RECEPTOR; DOPAMINE 3 RECEPTOR; G PROTEIN COUPLED RECEPTOR; NEUROKININ 2 RECEPTOR ANTAGONIST; NEUROKININ 3 RECEPTOR AGONIST; RADIOLIGAND; SAREDUTANT; TACHYKININ RECEPTOR ANTAGONIST; TALNETANT;

AMINO ACID SEQUENCE; ANIMAL CELL; ANIMAL EXPERIMENT; ARTICLE; BINDING AFFINITY; BRAIN ELECTROPHYSIOLOGY; CONCENTRATION RESPONSE; CONTROLLED STUDY; DOPAMINERGIC NERVE CELL; DRUG MECHANISM; DRUG RECEPTOR BINDING; DRUG STRUCTURE; FEMALE; GERBIL; GUINEA PIG; HUMAN; HUMAN CELL; IN VITRO STUDY; IN VIVO STUDY; INOSITOL PHOSPHATE ACCUMULATION ASSAY; LOCOMOTION; MALE; NONHUMAN; PRIORITY JOURNAL; SITE DIRECTED MUTAGENESIS; AGONISTS; ANALOGS AND DERIVATIVES; ANIMAL; ANTAGONISTS AND INHIBITORS; BINDING SITE; CHEMICAL STRUCTURE; DRUG EFFECTS; GENETICS; HEK293 CELL LINE; METABOLISM; MOLECULAR GENETICS; MUTATION; PHYSIOLOGY; SUBSTANTIA NIGRA PARS COMPACTA; TISSUE CULTURE TECHNIQUE; ACTION POTENTIAL; ANIMAL MODEL; ANIMAL TISSUE; BINDING KINETICS; BIOCHEMISTRY; DISSOCIATION; DRUG ACTIVITY; DRUG BINDING; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG DETERMINATION; DRUG DISTRIBUTION; DRUG EFFECT; DRUG HALF LIFE; DRUG STABILITY; EMBRYO; GERBIL MODEL; LIGAND BINDING; MOLECULAR DOCKING; NUCLEOTIDE SEQUENCE; RAT; SINGLE DRUG DOSE; WILD TYPE;

AMINO ACID SEQUENCE; ANIMALS; ANTIPSYCHOTIC AGENTS; BINDING SITES; CARBAMATES; CENTRAL NERVOUS SYSTEM AGENTS; DOPAMINERGIC NEURONS; FEMALE; GERBILLINAE; GUINEA PIGS; HEK293 CELLS; HUMANS; LOCOMOTION; MALE; MODELS, MOLECULAR; MOLECULAR SEQUENCE DATA; MUTATION; NEUROTRANSMITTER AGENTS; PARS COMPACTA; PEPTIDE FRAGMENTS; PIPERIDINES; RECEPTORS, NEUROKININ-2; RECEPTORS, NEUROKININ-3; SUBSTANCE P; TISSUE CULTURE TECHNIQUES;

EID: 84907325112     PISSN: 00283908     EISSN: 18737064     Source Type: Journal    
DOI: 10.1016/j.neuropharm.2014.07.017     Document Type: Article

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