4869-96-9Relevant academic research and scientific papers
GUANIDINE BASED COMPOUNDS
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Page/Page column 24; 26, (2011/01/05)
The adrenergic receptors or adrenoceptors are a family of G-protein coupled receptors split into α and β subclasses. The adrenoceptors have important roles in regulating a myriad of physiological conditions and their malfunction has been implicated in the pathophysiology of a number of diseases. Disclosed herein are a series of novel guanidine and 2-aminoimidazoline compounds which are ligands of the alpha2-adrenoceptor (α2-ARs) subclass of adrenergic receptors. The invention also provides for pharmaceutical compositions comprising the novel compounds. The compounds are suitable for use in the manufacture of medicaments for the treatment of α2-ARs associated disorders, such as depression, schizophrenia, glaucoma and analgesia.
Guanidine and 2-aminoimidazoline aromatic derivatives as α2-adrenoceptor antagonists. 2. Exploring alkyl linkers for new antidepressants
Rodriguez, Fernando,Rozas, Isabel,Ortega, Jorge E.,Erdozain, Amaia M.,Meana, J. Javier,Callado, Luis F.
supporting information; experimental part, p. 3304 - 3312 (2009/04/07)
The preparation of a number of (bis)guanidine and (bis)2-aminoimidazoline derivatives as potential α2-adrenoceptor antagonists for the treatment of depression is presented. Human brain tissue was used to measure their affinity toward the α2-adrenoceptors in vitro. Compounds 6b, 8b, 9b, 10b, 15b, 17b, 18b, 20b, and 21b displayed a good affinity (pK i > 7) and were evaluated in in vitro functional [ 35S]GTPγS binding assays in human prefrontal cortex to determine their agonistic or antagonistic activity. Among these compounds, 17b and 20b showed the expected behavior for an antagonist and were subject to in vivo microdialysis experiments in rats. Significantly, these experiments confirmed the antagonistic properties of 17b and 20b, and therefore both compounds can be considered as potential antidepressants.
