Induction of analgesia in neuropathic pain
AssigneeThe University Court of the University of Edinburgh
InventorsSusan Fleetwood-Walker, Rory Mitchell, Clare W.J. Proudfoot
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Abstract
The present invention relates to agents which are capable of inducing analgesia in chronic neuropathic pain, associated methods and uses thereof. In particular, the present invention provides compounds capable of activating the TRPM8 receptor for the treatment of chronic neuropathic pain.
Claims30
1-44. (canceled)
A method of treating chronic neuropathic pain, said method comprising the step of administering an effective amount of a transient receptor potential (TRP) M8 cation cannel activating agent to a patient suffering from or experiencing chronic neuropathic pain, wherein the TRPM8 cation channel activating agent is selected from the group consisting of:
- (i) icilin (1-(2′-hydroxyphenyl)-4-(3″-nitrophenyl)-1,2,3,6-tetrahydropyrimidin-2-one);
- (ii) menthol (1R,2S,5R-(5-methyl-2-[1-methylethyl]cyclohexanol);
- (iii) WS-12 (2-isopropyl-5-methyl-cyclohexanecarboxylic acid (4-methoxyphenyl) amide);
- and
- (iv) derivatives of any of (i)-(iv).
A pharmaceutical composition comprising a TRPM8 cation channel activating agent selected from the group consisting of:
- (ii) icilin (1-(2′-hydroxyphenyl)-4-(3″-nitrophenyl)-1,2,3,6-tetrahydropyrimidin-2-one);
- (iii) menthol (1R,2S,5R-(5-methyl-2-[1-methylethyl]cyclohexanol);
- (iv) WS-12 (2-isopropyl-5-methyl-cyclohexanecarboxylic acid (4-methoxyphenyl) amide);
- and
- (v) derivatives of any of (i)-(iv).
- and a pharmaceutically acceptable carrier or excipient.
A method of detecting an agent potentially useful in a method of inducing analgesia in a patient suffering from or experiencing chronic neuropathic pain, said method comprising the step of;
- (a) contacting a test agent or agents with a TRPM8 receptor;
- and
- (b) detecting any activation of the TRPM8 receptor so as to identify an agent or agents which activates the TRPM8 receptor.
A method of detecting agents which are capable of binding to the TRPM8 receptor, said method comprising the steps of;
- (a) contacting a test agent or agents with a TRPM8 receptor;
- and
- (b) detecting any binding which occurs between the test agent and the TRPM8 receptor.
A method of treating a patient suffering from or experiencing chronic neuropathic pain, said method comprising the step of administering an effective amount of an agent or compound which directly activates a Group II/III mGluR and an agent or compound which indirectly activates a group II/III mGluR, wherein the agent capable of directly activating a Group II/III mGluR is selected from the group consisting of:
- (i) 2R,4R-APDC;
- (ii) ACPT-III;
- and
- (iii) AP-4;
- and the agent capable of indirectly activating a Group II/III mGluR is selected from the group consisting of:
- (iv) icilin (1-(2′-hydroxyphenyl)-4-(3″-nitrophenyl)-1,2,3,6-tetrahydropyrimidin-2-one);
- (v) menthol 1R,2S,5R-(5-methyl-2-[1-methylethyl]cyclohexanol);
- (vi) WS-12 (2-isopropyl-5-methyl-cyclohexanecarboxylic acid (4-methoxyphenyl) amide);
- and
- (vii) derivatives of any of (iv)-(vi).
Dependencies are inferred from the claim text.