Potent NK1 Receptor Antagonists: synthesis and antagonistic Activity of Various Heterocycles with an N-[3, 5-Bis (trifluoromethyl) benzyl]-N-methylcarbamoyl …

Y Ikeura, T Tanaka, Y Kiyota, S MORIMOTO… - Chemical and …, 1997 - jstage.jst.go.jp
抄録 Various N-[3, 5-bis (trifluoromethyl) benzyl]-N-methylcarbamoyl heterocycles (1, 2 and
3) modified at rings A and B in the isoquinolone (1a) and pyrido [3, 4-b] pyridine (2a) nuclei …

SCH 206272: a potent, orally active tachykinin NK1, NK2, and NK3 receptor antagonist

JC Anthes, RW Chapman, C Richard, S Eckel… - European journal of …, 2002 - Elsevier
Experiments were performed to characterize the pharmacology of SCH 206272 [(R, R)-1′[5-
[(3, 5-dichlorobenzoyl) methylamino]-3-(3, 4-dichlorophenyl)-4 (Z)-(methoxyimino) pentyl]-N …

Cytochrome P450-catalyzed metabolism of ezlopitant alkene (CJ-12,458), a pharmacologically active metabolite of ezlopitant: enzyme kinetics and mechanism of an …

RS Obach - Drug metabolism and disposition, 2001 - ASPET
Experiments were conducted to characterize the metabolism of ezlopitant alkene (CJ-
12,458), an active metabolite of ezlopitant, in human liver microsomes. In incubations with …

Synthesis of a Tetrahydropyran NK1 Receptor Antagonist via Asymmetric Conjugate Addition

MA Huffman, JH Smitrovich, JD Rosen… - The Journal of …, 2005 - ACS Publications
Two asymmetric syntheses of the NK1 receptor antagonist 1-[2-(R)-{1-(R)-[3, 5-bis
(trifluoromethyl) phenyl] ethoxy}-3-(R)-(3, 4-difluorophenyl)-4-(R)-tetrahydro-2 H-pyran-4 …

Anxiolytic effect of NKP608, a NK1-receptor antagonist, in the social investigation test in gerbils

C Gentsch, M Cutler, A Vassout, S Veenstra… - Behavioural brain …, 2002 - Elsevier
NKP608 is a potent, selective and orally active non-peptidic neurokinin-1 (NK1)-receptor
antagonist for which anxiolytic-and antidepressant-like effects have been described in …

Neurokinin receptor antagonists

CJ Swain - Progress in medicinal chemistry, 1998 - books.google.com
A number of extensive reviews have been published which cover much of the current
literature on receptor distribution, in vitro and in vivo pharmacology, potential clinical utilities …

Enantioselective synthesis of an axially chiral 1, 7-naphthyridine-6-carboxamide derivative having potent antagonist activity at the NK 1 receptor

Y Ikeura, T Doi, A Fujishima, H Natsugari - Chemical Communications, 1998 - pubs.rsc.org
A new and highly potent NK1 antagonist,(aR, 9R)-3 [(aR, 9R)-7-[3, 5-bis (trifluoromethyl)
benzyl]-8, 9, 10, 11-tetrahydro-9-methyl-5-(4-methylphenyl)-7H-[1, 4] diazocino [2, 1-g][1, 7] …

Synthesis of a Potent hNK-1 Receptor Antagonist via an SN2 Reaction of an Enantiomerically Pure α-Alkoxy Sulfonate

TD Nelson, JD Rosen, JH Smitrovich, J Payack… - Organic …, 2005 - ACS Publications
The concise synthesis of a stereochemically rich hNK-1 receptor antagonist is described.
The synthesis is highlighted by an SN2 reaction of an enantiomerically pure α-alkoxy …

Neurokinin receptor antagonists

J Elliott, EM Seward - Expert Opinion on Therapeutic Patents, 1997 - Taylor & Francis
The competitive area of neurokinin (NK) receptor antagonists has recently seen the
publication of early clinical results which provide strong support for their use in the treatment …

Neurokinin receptor antagonists: therapeutic potential in the treatment of pain syndromes

T Sakurada, C Sakurada, K Tan-No, K Kisara - CNS drugs, 1997 - Springer
The involvement of tachykinin neuropeptides, such as substance P and the neurokinins, in
pain transmission is supported by a wealth of evidence. At present. the therapeutic potential …