Characterization of RO4583298 as a novel potent, dual antagonist with in vivo activity at tachykinin NK₁ and NK₃ receptors.
Malherbe
P
P
Discovery Research CNS, F. Hoffmann-La Roche Ltd., Basel, Switzerland. parichehr.malherbe@roche.com
Knoflach
F
F
Hernandez
M C
MC
Hoffmann
T
T
Schnider
P
P
Porter
R H
RH
Wettstein
J G
JG
Ballard
T M
TM
Spooren
W
W
Steward
L
L
D000200:Action Potentials / Q000187:drug effects; D000577:Amides / Q000378:metabolism / Q000493:pharmacokinetics / Q000494:pharmacology*; D000631:Aminopyridines; D000818:Animals; D014150:Antipsychotic Agents / Q000378:metabolism / Q000493:pharmacokinetics / Q000494:pharmacology*; D044482:Benzeneacetamides; D004305:Dose-Response Relationship, Drug; D005260:Female; D005849:Gerbillinae; D006168:Guinea Pigs; D057809:HEK293 Cells; D006801:Humans; D066298:In Vitro Techniques; D007294:Inositol / Q000378:metabolism; D008024:Ligands; D008252:Macaca fascicularis; D008297:Male; D008636:Mesencephalon / Q000187:drug effects* / Q000502:physiology; D051379:Mice; D064729:Neurokinin-1 Receptor Antagonists; D009474:Neurons / Q000187:drug effects / Q000502:physiology; D010766:Phosphorylation / Q000187:drug effects; D011725:Pyridines / Q000378:metabolism / Q000493:pharmacokinetics / Q000494:pharmacology*; D051381:Rats; D018040:Receptors, Neurokinin-1 / Q000819:agonists / Q000235:genetics / Q000378:metabolism; D018042:Receptors, Neurokinin-3 / Q000819:agonists / Q000037:antagonists & inhibitors* / Q000235:genetics / Q000378:metabolism; D012559:Schizophrenia / Q000188:drug therapy; D013373:Substance P / Q000031:analogs & derivatives / Q000037:antagonists & inhibitors; D013378:Substantia Nigra / Q000187:drug effects / Q000502:physiology
C558113:2-(3,5-bis-trifluoromethylphenyl)-N-(4-(4-fluoro-2-methylphenyl)-6-(3-hydroxy-2-hydroxymethylpyrrolidin-1-yl)pyridin-3-yl)-N-methylisobutyramide; D000577:Amides; D000631:Aminopyridines; D014150:Antipsychotic Agents; D044482:Benzeneacetamides; D008024:Ligands; D064729:Neurokinin-1 Receptor Antagonists; D011725:Pyridines; D018040:Receptors, Neurokinin-1; D018042:Receptors, Neurokinin-3; D013373:Substance P; D007294:Inositol