Igel, Patrick and Schneider, Erich and Schnell, David and Elz, Sigurd and Seifert, Roland and Buschauer, Armin (2009) N-G-Acylated Imidazolylpropylguanidines as Potent Histamine H-4 Receptor Agonists: Selectivity by Variation of the N-G-Substituent. JOURNAL OF MEDICINAL CHEMISTRY, 52 (8). pp. 2623-2627. ISSN 0022-2623, 1520-4804
Full text not available from this repository. (Request a copy)Abstract
3-(1H-Imidazol-4-yl)propylguanidine (SK&F 91486, 4) was identified as a potent partial agonist at the human histamine H-3 receptor (hH(3)R) and human histamine H-4 receptor (hH(4)R). With the aim to increase selectivity for the hH4R, the guanidine group in 4 was acylated. N-1-Acetyl-N-2-[3-(1H-imidazol-4-yl)propyl]guanidine (UR-PI288, 13) was a potent full agonist at the hH(4)R (pEC(50) = 8.31; alpha = 1.00), possessing more than 1000- and 100-fold selectivity relative to the hH(1)R and hH(2)R, respectively, and possessing only low intrinsic activity (alpha = 0.27) at the hH(3)R.
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | H-4-RECEPTOR AGONIST; 1ST POTENT; H-2-RECEPTOR; H-1-RECEPTOR; BINDING; H4; |
| Subjects: | 600 Technology > 615 Pharmacy |
| Divisions: | Chemistry and Pharmacy > Institute of Pharmacy > Alumni or Retired Professors > Pharmaceutical/Medicinal Chemistry II (Prof. Buschauer) |
| Depositing User: | Dr. Gernot Deinzer |
| Date Deposited: | 17 Sep 2020 09:40 |
| Last Modified: | 17 Sep 2020 09:40 |
| URI: | https://pred.uni-regensburg.de/id/eprint/29113 |
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