Lazewska, Dorota and Kiec-Kononowicz, Katarzyna and Pertz, H. H. and Stark, Holger and Schunack, W. and Elz, Sigurd (2001) Piperidine-containing histamine H-3-receptor antagonists of the carbamate series: variation of the spacer length. PHARMAZIE, 56 (12). pp. 927-932. ISSN 0031-7144
Full text not available from this repository. (Request a copy)Abstract
Ten carbamate derivatives have been prepared from appropriate isocyanates and omega -piperidino-1-alkanols. All compounds belong to the new generation of non-imidazole histamine H-3-receptor ligands which may have beneficial pharmacokinetic properties compared with the classical imidazole-containing H-3-receptor antagonists. The carbamates were evaluated in vitro for antagonist activity at guinea-pig (gp) H-3, H-2, H-1, and M-3 receptors, respectively. They displayed moderate affinity for H-3 receptors (pA(2) 5.8-7.0 in the gp ileum assay) as well as low to moderate selectivities vis-a-vis H-2 (gp atrium), H-1 (gp ileum), and M-3 (gp ileum) receptors. A typical member of this series is 7-piperidino-1-heptyl N-(4-phenyl-1-butyl)carbarnate (17) with pA(2) values of 7.02 (H-3), 5.92 (H-1), and 6.38 (M-3), respectively, and a pD'(2) value of 5.46 (H-2).
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | H-3 RECEPTOR ANTAGONISTS; GUINEA-PIG ILEUM; IN-VIVO ACTIVITY; RELEASE; LIGANDS; POTENT; HETEROGENEITY; THIOPERAMIDE; IODOPROXYFAN; CLONING; |
| Subjects: | 600 Technology > 615 Pharmacy |
| Divisions: | Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical/Medicinal Chemistry I (Prof. Elz) |
| Depositing User: | Dr. Gernot Deinzer |
| Date Deposited: | 24 Nov 2021 08:21 |
| Last Modified: | 24 Nov 2021 08:21 |
| URI: | https://pred.uni-regensburg.de/id/eprint/40915 |
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