| 摘要 |
A therapeutic composition is provided that comprises a 1-R1-phenyl, 4-R2- phenyl substituted 1,2,3,6-tetrahydropyrimidine-2-one cold receptor agonist in a therapeutically effective amount. The composition preferably further comprises one or more pharmaceutically active drugs such as an anti- inflammatory glucocorticosteroid, a sympathomimetic amine decongestant, an antihistamine, a local anesthetic, menthol or a menthol analog, an immunosuppressant, and mixtures thereof. The cold receptor agonist may be represented by the general formula (1)-[R1-phenyl]-4-[R2-phenyl]-1,2,3,6- tetrahydropyrimidine-2-one wherein: R1 is -hydroxy, -chloro, - fluoro, -alky l, -acetoxy, -trifluoromethyl ; and R2 is -nitro, -chloro, -fluoro, -alkyl, - trifluoromethyl. Therapeutic compositions of the invention elicit long-lasti ng cooling or soothing, particularly when formulated for delivery to suppress t he sensations of itch and pain, such as for delivery to inflamed skin, to the mucous membranes of the eyelids, of the anogenital areas and of the airways, and to the enteric mucosa.
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