A hydrophobic residue in position 15 of the rP2X3 receptor slows desensitization and reveals properties beneficial for pharmacological analysis and high-throughput screening

Neuropharmacology

Volumn 79, Issue , 2014, Pages 603-615

  Hausmann, Ralf ^a   Bahrenberg, Gregor ^b   Kuhlmann, Daniel ^a   Schumacher, Michaela ^a   Braam, Ursula ^a   Bieler, Dagmar ^b   Schlusche, Ilka ^b   Schmalzing, Günther ^a  

^a RWTH AACHEN UNIVERSITY   (Germany)

^b GRÜNENTHAL GMBH   (Germany)

Author keywords

Calcium imaging; Desensitization; Drug screening; Mechanism of antagonism; P2X3 receptor

Indexed keywords

2',3' O (2,4,6 TRINITROPHENYL) ADENOSINE TRIPHOSPHATE; 5 [[(3 PHENOXYBENZYL)(1,2,3,4 TETRAHYDRO 1 NAPHTHYL)AMINO]CARBONYL]TRIMELLITIC ACID; ISOLEUCINE; METHIONINE; PROLINE; PURINERGIC P2X RECEPTOR ANTAGONIST; PURINERGIC P2X2 RECEPTOR; PURINERGIC P2X3 RECEPTOR; SERINE; SHAKER POTASSIUM CHANNEL; TRYPTOPHAN; UNCLASSIFIED DRUG; VALINE; VOLTAGE GATED SODIUM CHANNEL; ADENOSINE TRIPHOSPHATE; CALCIUM;

AMINO ACID SEQUENCE; AMINO TERMINAL SEQUENCE; ANIMAL CELL; ARTICLE; ASTROCYTOMA CELL; CALCIUM CELL LEVEL; CALCIUM IMAGING BASED ASSAY; CELL LINE; CELL SIGNALING ASSAY; CELL STRAIN 1321N1; CHIMERA; CONCENTRATION RESPONSE; CONTROLLED STUDY; DESENSITIZATION; DRUG ANTAGONISM; DRUG MECHANISM; DRUG SCREENING; FLUORESCENCE IMAGING; HUMAN; HYDROPHOBICITY; MOLECULAR LIBRARY; NONHUMAN; PRIORITY JOURNAL; PROTEIN EXPRESSION; RAT; RECEPTOR DOWN REGULATION; XENOPUS LAEVIS; ANIMAL; CHEMICAL PHENOMENA; DRUG EFFECTS; GENETICS; HIGH THROUGHPUT SCREENING; MEMBRANE POTENTIAL; METABOLISM; MOLECULAR GENETICS; MUTATION; PATCH CLAMP TECHNIQUE; PHYSIOLOGY; TUMOR CELL LINE;

ADENOSINE TRIPHOSPHATE; AMINO ACID SEQUENCE; ANIMALS; CALCIUM; CELL LINE, TUMOR; HIGH-THROUGHPUT SCREENING ASSAYS; HUMANS; HYDROPHOBIC AND HYDROPHILIC INTERACTIONS; MEMBRANE POTENTIALS; MOLECULAR SEQUENCE DATA; MUTATION; OPTICAL IMAGING; PATCH-CLAMP TECHNIQUES; PURINERGIC P2X RECEPTOR ANTAGONISTS; RATS; RECEPTORS, PURINERGIC P2X2; RECEPTORS, PURINERGIC P2X3; XENOPUS LAEVIS;

EID: 84896711394     PISSN: 00283908     EISSN: 18737064     Source Type: Journal    
DOI: 10.1016/j.neuropharm.2014.01.010     Document Type: Article

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