Fused bicyclic pyrrolizinones as new scaffolds for human NK1antagonists

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Bibliographic Details
Published inBioorganic & medicinal chemistry Vol. 16; no. 5; pp. 2156 - 2170
Main Authors MORRIELLO, Gregori J, DEVITA, Robert J, CARLSON, Emma, TOWNSON, Karen, WHEELDON, Alan, BOYCE, Susan, COLLINSON, Neil, RUPNIAK, Nadia, MOORE, Stephen, MILLS, Sander G, YOUNG, Jonathan R, LIN, Peter, DOSS, George, CHICCHI, Gary G, DEMARTINO, Julie, KURTZ, Marc M, TSAO, Kwei-Lan C
Format Journal Article
LanguageEnglish
Published Oxford Elsevier Science 2008
Subjects
Biological and medical sciences
Medical sciences
Neuropharmacology
Neurotransmitters. Neurotransmission. Receptors
Peptidergic system (neuropeptide, opioid peptide, opiates...). Adenosinergic and purinergic systems
Pharmacology. Drug treatments
Human
NK1 Tachykinin receptor
Intravenous administration
Angular nitrogen heterocycle
Rodentia
Benzene derivatives
Lactam
Blood brain barrier
Organic carbamate
In vitro
In vivo
Vertebrata
Mammalia
Structure activity relation
Animal
Bicyclic compound
Affinity
Fluorine Organic compounds
Antagonist
Chemical synthesis
Gerbil
Oxygen nitrogen heterocycle
Online AccessGet full text

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Author WHEELDON, Alan
KURTZ, Marc M
BOYCE, Susan
YOUNG, Jonathan R
MORRIELLO, Gregori J
COLLINSON, Neil
CARLSON, Emma
RUPNIAK, Nadia
MILLS, Sander G
MOORE, Stephen
LIN, Peter
DOSS, George
TOWNSON, Karen
DEMARTINO, Julie
DEVITA, Robert J
TSAO, Kwei-Lan C
CHICCHI, Gary G
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  organization: Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, 126 E. Lincoln Avenue, Rahway, NJ 07065, United States
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  givenname: Robert J
  surname: DEVITA
  fullname: DEVITA, Robert J
  organization: Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, 126 E. Lincoln Avenue, Rahway, NJ 07065, United States
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  givenname: Emma
  surname: CARLSON
  fullname: CARLSON, Emma
  organization: Department of Behavioral Neuroscience, Merck Research Laboratories, Terlings Park, United Kingdom
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  givenname: Karen
  surname: TOWNSON
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  organization: Department of Behavioral Neuroscience, Merck Research Laboratories, Terlings Park, United Kingdom
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  fullname: BOYCE, Susan
  organization: Department of Behavioral Neuroscience, Merck Research Laboratories, Terlings Park, United Kingdom
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  givenname: Neil
  surname: COLLINSON
  fullname: COLLINSON, Neil
  organization: Department of Behavioral Neuroscience, Merck Research Laboratories, Terlings Park, United Kingdom
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  givenname: Nadia
  surname: RUPNIAK
  fullname: RUPNIAK, Nadia
  organization: Department of Behavioral Neuroscience, Merck Research Laboratories, Terlings Park, United Kingdom
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  givenname: Stephen
  surname: MOORE
  fullname: MOORE, Stephen
  organization: Department of Behavioral Neuroscience, Merck Research Laboratories, Terlings Park, United Kingdom
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  givenname: Sander G
  surname: MILLS
  fullname: MILLS, Sander G
  organization: Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, 126 E. Lincoln Avenue, Rahway, NJ 07065, United States
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  givenname: Jonathan R
  surname: YOUNG
  fullname: YOUNG, Jonathan R
  organization: Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, 126 E. Lincoln Avenue, Rahway, NJ 07065, United States
– sequence: 12
  givenname: Peter
  surname: LIN
  fullname: LIN, Peter
  organization: Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, 126 E. Lincoln Avenue, Rahway, NJ 07065, United States
– sequence: 13
  givenname: George
  surname: DOSS
  fullname: DOSS, George
  organization: Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, 126 E. Lincoln Avenue, Rahway, NJ 07065, United States
– sequence: 14
  givenname: Gary G
  surname: CHICCHI
  fullname: CHICCHI, Gary G
  organization: Department of Immunology, Merck Research Laboratories, Terlings Park, United Kingdom
– sequence: 15
  givenname: Julie
  surname: DEMARTINO
  fullname: DEMARTINO, Julie
  organization: Department of Immunology, Merck Research Laboratories, Terlings Park, United Kingdom
– sequence: 16
  givenname: Marc M
  surname: KURTZ
  fullname: KURTZ, Marc M
  organization: Department of Immunology, Merck Research Laboratories, Terlings Park, United Kingdom
– sequence: 17
  givenname: Kwei-Lan C
  surname: TSAO
  fullname: TSAO, Kwei-Lan C
  organization: Department of Immunology, Merck Research Laboratories, Terlings Park, United Kingdom
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Issue 5
Keywords Human
NK1 Tachykinin receptor
Intravenous administration
Angular nitrogen heterocycle
Rodentia
Benzene derivatives
Lactam
Blood brain barrier
Organic carbamate
In vitro
In vivo
Vertebrata
Mammalia
Structure activity relation
Animal
Bicyclic compound
Affinity
Fluorine Organic compounds
Antagonist
Chemical synthesis
Gerbil
Oxygen nitrogen heterocycle
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PublicationYear 2008
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StartPage 2156
SubjectTerms Biological and medical sciences
Medical sciences
Neuropharmacology
Neurotransmitters. Neurotransmission. Receptors
Peptidergic system (neuropeptide, opioid peptide, opiates...). Adenosinergic and purinergic systems
Pharmacology. Drug treatments
Title Fused bicyclic pyrrolizinones as new scaffolds for human NK1antagonists
Volume 16
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