A new metabotropic glutamate receptor agonist with in vivo anti-allodynic activity
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A new metabotropic glutamate receptor agonist with in vivo anti-allodynic activity. / Stanley, Nathan J; Hutchinson, Mark R; Kvist, Trine; Nielsen, Birgitte; Mathiesen, Jesper M; Bräuner-Osborne, Hans; Avery, Thomas D; Tiekink, Edward R T; Pedersen, Daniel Sejer; Irvine, Rodney J; Abell, Andrew D; Taylor, Dennis K.
In: Bioorganic & Medicinal Chemistry, Vol. 18, No. 16, 2010, p. 6089-6098.Research output: Contribution to journal › Journal article › Research › peer-review
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TY - JOUR
T1 - A new metabotropic glutamate receptor agonist with in vivo anti-allodynic activity
AU - Stanley, Nathan J
AU - Hutchinson, Mark R
AU - Kvist, Trine
AU - Nielsen, Birgitte
AU - Mathiesen, Jesper M
AU - Bräuner-Osborne, Hans
AU - Avery, Thomas D
AU - Tiekink, Edward R T
AU - Pedersen, Daniel Sejer
AU - Irvine, Rodney J
AU - Abell, Andrew D
AU - Taylor, Dennis K
N1 - Keywords: 1,2-Dioxines; Carboxycyclopropylglycines; Metabotropic glutamate receptors; In vivo; Neuropathic pain; Allodynia
PY - 2010
Y1 - 2010
N2 - As part of the vital search towards improved therapeutic agents for the treatment of neuropathic pain, the central nervous system glutamate receptors have become a major focus of research. Outlined herein are the syntheses of two new biologically active 3'-cycloalkyl-substituted carboxycyclopropylglycines, utilizing novel synthetic chemistry. The reaction between substituted 1,2-dioxines and an aminophosphonate furnished the cyclopropane core in a single step with all required stereochemistry of pendant groups. In vitro binding assays at metabotropic glutamate receptors revealed selective activity. In vivo testing in a rodent model of neuropathic pain indicated one amino acid significantly and dose-dependently decreased mechanical allodynia.
AB - As part of the vital search towards improved therapeutic agents for the treatment of neuropathic pain, the central nervous system glutamate receptors have become a major focus of research. Outlined herein are the syntheses of two new biologically active 3'-cycloalkyl-substituted carboxycyclopropylglycines, utilizing novel synthetic chemistry. The reaction between substituted 1,2-dioxines and an aminophosphonate furnished the cyclopropane core in a single step with all required stereochemistry of pendant groups. In vitro binding assays at metabotropic glutamate receptors revealed selective activity. In vivo testing in a rodent model of neuropathic pain indicated one amino acid significantly and dose-dependently decreased mechanical allodynia.
KW - Former Faculty of Pharmaceutical Sciences
U2 - 10.1016/j.bmc.2010.06.051
DO - 10.1016/j.bmc.2010.06.051
M3 - Journal article
C2 - 20638290
VL - 18
SP - 6089
EP - 6098
JO - Bioorganic & Medicinal Chemistry
JF - Bioorganic & Medicinal Chemistry
SN - 0968-0896
IS - 16
ER -
ID: 21361781