Design of novel neurokinin 1 receptor antagonists based on conformationally constrained aromatic amino acids and discovery of a potent chimeric opioid agonist-neurokinin 1 receptor antagonist

Journal of Medicinal Chemistry

Volumn 54, Issue 7, 2011, Pages 2467-2476

  Ballet, Steven ^a   Feytens, Debby ^a   Buysse, Koen ^a   Chung, Nga N ^b   Lemieux, Carole ^b   Tumati, Suneeta ^c   Keresztes, Attila ^c   Van Duppen, Joost ^d   Lai, Josephine ^c   Varga, Eva ^c   Porreca, Frank ^c   Schiller, Peter W ^b   Vanden Broeck, Jozef ^d   Tourwé, Dirk ^a  

^a VRIJE UNIVERSITEIT BRUSSEL   (Belgium)

^b CLIN RESEARCH INSTITUTE OF MONTREAL   (Canada)

^c UNIVERSITY OF ARIZONA COLLEGE OF MEDICINE   (United States)

^d UNIVERSITY OF LEUVEN   (Belgium)

Author keywords

[No Author keywords available]

Indexed keywords

AROMATIC AMINO ACID; DELTA OPIATE RECEPTOR AGONIST; ENKEPHALIN[2 DEXTRO ALANINE 4 METHYLPHENYLALANINE 5 GLYCINE]; LEUCINE ENKEPHALIN[2 DEXTRO SERINE 6 THREONINE]; MU OPIATE RECEPTOR AGONIST; N METHYL N [7 (1 PYRROLIDINYL) 1 OXASPIRO[4.5]DEC 8 YL]BENZENEACETAMIDE; NEUROKININ 1 RECEPTOR; NEUROKININ 1 RECEPTOR ANTAGONIST; SUBSTANCE P; TYROSYL DEXTRO ARGINYLPHENYLALANYLLYSINAMIDE;

ANIMAL CELL; ANIMAL TISSUE; ARTICLE; BIOLOGICAL ACTIVITY; CHO CELL; CONTROLLED STUDY; DRUG CONFORMATION; DRUG DESIGN; DRUG POTENCY; DRUG SCREENING; DRUG SYNTHESIS; IC 50; MOUSE; NONHUMAN; PHARMACOPHORE; RECEPTOR AFFINITY;

AMINO ACIDS, AROMATIC; ANIMALS; CHO CELLS; CRICETINAE; CRICETULUS; DRUG DESIGN; HUMANS; LIGANDS; MODELS, MOLECULAR; MOLECULAR CONFORMATION; RECEPTORS, NEUROKININ-1; RECEPTORS, OPIOID; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 79953777227     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm1016285     Document Type: Article

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