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Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)
 

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Importance of the lipophilic group in carbamates having histamine H3-receptor antagonist activity.

In order to evaluate changes in the lipophilic part of designed carbamates concerning their potential histamine H3-receptor antagonist properties a new series of O-[3-(1H-imidazol-4-yl)propanol]carbamates was derived containing N-mono- or di-alkenyl, alkynyl, cycloalkyl, or double-branched alkyl substituents. The compounds were tested in vitro for their H3-receptor antagonist activity on synaptosomes of rat cerebral cortex and shared moderate to high antagonist activity in vitro. In this series 3-(1H-imidazol-4-yl)propyl N-(4-pentenyl)carbamate (4) was the most potent compound in vitro (Ki = 6.3 nM). H3-receptor antagonist activity in the central nervous system (CNS) was detected for most compounds in the in vivo H3-receptor assay based upon measurement of brain N tau-methylhistamine levels after p.o. administration to mice. The most effective carbamate in vivo, 3-(1H-imidazol-4-yl)propyl N-(allyl)carbamate (3), showed higher CNS potency (ED50 = 0.48 mg/kg p.o.) than the reference antagonist thioperamide. For some novel carbamates their histamine H1- and H2-receptor activities were determined on isolated organs of guinea-pig thereby demonstrating their high H3-receptor selectivity.[1]

References

  1. Importance of the lipophilic group in carbamates having histamine H3-receptor antagonist activity. Kieć-Kononowicz, K., Wiecek, M., Sasse, A., Ligneau, X., Elz, S., Ganellin, C.R., Schwartz, J.C., Stark, H., Schunack, W. Die Pharmazie. (2000) [Pubmed]
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