UR-AK49
UR-AK49 is a drug used in scientific research which acts as a potent antagonist for the Neuropeptide Y / Pancreatic polypeptide receptor Y4, and also as a partial agonist at the histamine receptors H1 and H2. UR-AK49 is a pure antagonist at Y4 with no partial agonist effects, and although it is only slightly selective for Y4 over the related Y1 and Y5 receptors, as the first non-peptide Y4 antagonist developed UR-AK49 is expected to be useful in the study of this receptor and its role in the body.
References
- ^ Xie SX, Kraus A, Ghorai P, Ye QZ, Elz S, Buschauer A, Seifert R (June 2006). "N1-(3-cyclohexylbutanoyl)-N2-guanidine (UR-AK57), a potent partial agonist for the human histamine H1- and H2-receptors" (PDF). The Journal of Pharmacology and Experimental Therapeutics. 317 (3): 1262–1268. doi:10.1124/jpet.106.102897. PMID 16554355. S2CID 26028129.
- ^ Ziemek R, Schneider E, Kraus A, Cabrele C, Beck-Sickinger AG, Bernhardt G, Buschauer A (2007). "Determination of affinity and activity of ligands at the human neuropeptide Y Y4 receptor by flow cytometry and aequorin luminescence". Journal of Receptor and Signal Transduction Research. 27 (4): 217–233. doi:10.1080/10799890701505206. PMID 17885919. S2CID 26579625.
Histamine receptor modulators |
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H1 | Agonists |
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Antagonists |
- Others: Atypical antipsychotics (e.g., aripiprazole, asenapine, brexpiprazole, brilaroxazine, clozapine, iloperidone, olanzapine, paliperidone, quetiapine, risperidone, ziprasidone, zotepine)
- Phenylpiperazine antidepressants (e.g., hydroxynefazodone, nefazodone, trazodone, triazoledione)
- Tetracyclic antidepressants (e.g., amoxapine, loxapine, maprotiline, mianserin, mirtazapine, oxaprotiline)
- Tricyclic antidepressants (e.g., amitriptyline, butriptyline, clomipramine, desipramine, dosulepin (dothiepin), doxepin, imipramine, iprindole, lofepramine, nortriptyline, protriptyline, trimipramine)
- Typical antipsychotics (e.g., chlorpromazine, flupenthixol, fluphenazine, loxapine, perphenazine, prochlorperazine, thioridazine, thiothixene)
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H2 | |
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H3 | |
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H4 | |
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See also
Receptor/signaling modulators
Monoamine metabolism modulators
Monoamine reuptake inhibitors
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