Agents with selective κ-opioid receptor affinity
AssigneesThe University of Mississippi, Case Western Reserve University
InventorsJordan Zjawiony, Hesham Fahmy, David Jeremy Stewart, Bryan Roth
Life of this patent
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Abstract
Compounds and compositions that are salvinorin A and salvinorin B derivatives that demonstrate selectivity and/or potency for the k-opioid receptor (KOR), allowing for their use as medicines, as well as chemical probes (both radiolabeled and cold) for fields utilizing the techniques of radiolabeled binding assays.
Claims21
A compound of the following general formula, which includes salts thereof:
- wherein:
- R1 and/or R2 is hydrogen, halogen, alkyl, hydroxyl, alkoxyl, acyloxyl, hydroxyalkyl, amino, alkylamino, acylamino, acetylalkylamino, arylamino, arylalkylamino, Het-alkylamino, aminoalkyl, acylaminoalkyl, nitroalkyl, thiol, alkylthio, acylthio, arylthio, arylalkylthio, acetylalkylthio, carboxylic acid ester, amide, —CONH2, and nitrile derivatives thereof, provided that R1 is not
- when R2 is
A compound of formula 1 of the following formula:
- and salts thereof.
A compound of formula 1 of the following formula:
- and salts thereof.
A compound of formula 1 of the following formula:
- and salts thereof.
A compound of formula 1, of the following formula:
- and salts thereof.
A method of detecting or monitoring KOR activity, comprising:
- providing a compound of the following formula:
- wherein:
- R1 and/or R2 is hydrogen, halogen, alkyl, hydroxyl, alkoxyl, acyloxyl, hydroxyalkyl, amino, alkylamino, acylamino, acetylalkylamino, arylamino, arylalkylamino, Het-alkylamino, aminoalkyl, acylaminoalkyl, nitroalkyl, thiol, alkylthio, acylthio, arylthio, arylalkylthio, acetylalkylthio, carboxylic acid, —CONH2, derivatives thereof (such as esters, amides, and nitriles);
- or pharmaceutically acceptable salts thereof provided that the compound has an isotopic label;
- introducing said composition to a subject;
- and
- detecting the binding of the compound to KOR.
Dependencies are inferred from the claim text.