Novel methods and compositions for alleviating pain
AssigneeAllergan, Inc.
InventorsDaniel W. Gil, John E. Donello
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Abstract
The present invention provides a method for the long-term relief of chronic pain in a subject by activating in the subject an analgesic α-adrenergic receptor in the absence of α-2A receptor activation over a period of at least three days, such that relief of chronic pain is maintained in the absence of continued activation of said receptor. The analgesic α-adrenergic receptor can be, for example, the α-2B receptor.
Claims114
A method of alleviating pain in a subject, comprising
- administering to said subject a pharmaceutical composition comprising an effective amount of an α-adrenergic agonist and a pharmaceutical composition comprising an effective amount of a selective α-2A antagonist.
An analgesic composition, comprising an α-adrenergic agonist with minimal α-2A agonist activity, said agonist having the ability to produce peripheral analgesia without concomitant sedation.
A method of alleviating pain in a subject, comprising peripherally administering to said subject a pharmaceutical composition comprising an effective amount of an α-adrenergic agonist with minimal α-2A agonist activity, thereby producing peripheral analgesia without concomitant sedation.
A method of screening for effective agents that produce peripheral analgesia without concomitant sedation, comprising the steps of:
- (a) contacting an α-2A receptor with an α-adrenergic agonist having analgesic activity;
- and
- (b) determining whether said agonist has α-2A agonist activity, wherein the absence of α-2A agonist activity indicates that said α-adrenergic agonist having analgesic activity is an effective agent that produces peripheral analgesia without concomitant sedation.
A method of screening for effective agents that produce peripheral analgesia without concomitant sedation, comprising the steps of:
- (a) contacting an α-2A receptor with an agent;
- (b) determining whether said agent has α-2A agonist activity;
- (c) contacting an α-2B receptor with said agent;
- and
- (d) determining whether said agent has α-2B agonist activity,
- wherein the absence of α-2A agonist activity and the presence of α-2B agonist activity indicate that said agent is an effective agent that produces peripheral analgesia without concomitant sedation.
A method of screening for effective agents that produce peripheral analgesia without concomitant sedation, comprising the steps of:
- (a) peripherally administering an α-adrenergic agonist to a control animal having at least wild type levels of α-2A receptor activity;
- (b) assaying for analgesia in said control animal;
- (c) peripherally administering to a corresponding animal having reduced levels of α-2A receptor expression or activity an amount of said α-adrenergic agonist similar or greater than the amount administered to said control animal;
- and
- (d) assaying for analgesia in said corresponding animal having reduced levels of α-2A receptor expression or activity,
- wherein the absence of analgesia in said control animal and the presence of analgesia in said corresponding animal having reduced levels of α-2A receptor expression or activity indicate that said α-adrenergic agonist has excessive α-2A agonist activity;
- and
- wherein the presence of analgesia in said control animal and the presence of analgesia in said corresponding animal having reduced levels of α-2A receptor expression or activity indicate that said α-adrenergic agonist is an effective agent that produces peripheral analgesia without concomitant sedation.
A method of screening for effective agents that produce peripheral analgesia without concomitant sedation, comprising the steps of:
- (a) peripherally administering an α-adrenergic agonist to a control animal having at least wild type levels of α-2B receptor activity;
- (b)assaying for analgesia in said control animal;
- (c) peripherally administering said α-adrenergic agonist to a corresponding animal having reduced levels of α-2B receptor expression or activity;
- and
- (d) assaying for analgesia in said corresponding animal having reduced levels of α-2B receptor expression or activity,
- wherein the presence of analgesia in said control animal and the absence of analgesia in said corresponding animal having reduced levels of α-2B receptor expression or activity indicate that said α-adrenergic agonist is an effective agent that produces peripheral analgesia without concomitant sedation.
A method for the long-term relief of chronic pain in a subject, comprising activating in said subject an analgesic α-adrenergic receptor in the absence of α-2A receptor activation over a period of at least three days,
- such that relief of chronic pain is maintained in the absence of continued activation of said receptor.
Dependencies are inferred from the claim text.