Design and synthesis of the potent, orally available, brain-penetrable arylpyrazole class of neuropeptide Y5 receptor antagonists

Journal of Medicinal Chemistry

Volumn 46, Issue 5, 2003, Pages 666-669

  Sato, Nagaaki ^a   Takahashi, Toshiyuki ^a   Shibata, Takunobu ^a   Haga, Yuji ^a   Sakuraba, Aya ^a   Hirose, Masaaki ^a   Sato, Miki ^a   Nonoshita, Katsumasa ^a   Koike, Yuko ^a   Kitazawa, Hidefumi ^a   Fujino, Naoko ^a   Ishii, Yasuyuki ^a   Ishihara, Akane ^a   Kanatani, Akio ^a   Fukami, Takehiro ^a  

^a BANYU PHARMACEUTICAL CO LTD   (Japan)

Author keywords

[No Author keywords available]

Indexed keywords

AMIDE; CGP 71683; COMPOUND 7; N [5 (4 CHLOROPHENYL) 1H PYRAZOL 3 YL]2 INDANECARBOXAMIDE; NEUROPEPTIDE RECEPTOR ANTAGONIST; NEUROPEPTIDE Y RECEPTOR ANTAGONIST; NEUROPEPTIDE Y5 RECEPTOR; NEUROPEPTIDE Y5 RECEPTOR ANTAGONIST; PYRAZOLE DERIVATIVE; UNCLASSIFIED DRUG;

ARTICLE; BINDING AFFINITY; CHIRALITY; DRUG ANTAGONISM; DRUG BIOAVAILABILITY; DRUG BRAIN LEVEL; DRUG DESIGN; DRUG POTENCY; DRUG PROTEIN BINDING; DRUG SYNTHESIS; EVALUATION; FEEDING BEHAVIOR; FOOD INTAKE; NONHUMAN; PEPTIDE ANALYSIS; RAT; STATISTICAL SIGNIFICANCE;

ADMINISTRATION, ORAL; ANIMALS; BRAIN; CATTLE; EATING; HUMANS; INJECTIONS, INTRAVENTRICULAR; NAPHTHALENES; PANCREATIC POLYPEPTIDE; PERMEABILITY; PYRAZOLES; RATS; RATS, SPRAGUE-DAWLEY; RECEPTORS, NEUROPEPTIDE Y; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 0037468535     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm025513q     Document Type: Article

References (27)

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25. See Supporting Information for the library construction method.
26. The quantities of ICV-dosed bPP and NPY were 5 μg/head. See ref 27 for the protocol used for the in vivo feeding experiments described herein.
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