The effects of two selective serotonin reuptake inhibitors (SSRIs) on 5-hydroxytryptamine (5-HT) in the hippocampus were studied in wildtype and in 5-HT1B receptor knockout (KO) mice using in vivo microdialysis. Basal 5-HT levels were not different between the two genotypes. The functional absence of 5-HT1B receptors was examined in the knockout mice by local infusion of the 5-HT1B receptor ago...

The behaviour of two cyclen-based bismacrocycles linked by aromatic spacers as receptors of adenosine monophosphate (AMP), adenosine diphosphate (ADP) and adenosine triphosphate (ATP) anions is explored. The two bismacrocycles differ from one another by the nature of their spacers, which are respectively 1,3-dimethylbenzene (BMC), or 2,6-dimethylpyridine (BPyC). Potentiometric investigations su...

We have established that bipyridinium radicals can be reversibly π-dimerized under the combined effects of chemical (proton transfer) and electrochemical (electron transfer) stimuli. Our investigations also led to the discovery that a bis-pyridinyl appended calixarene intermediate is involved in a fully reversible redox-triggered σ-dimerization process. The structure of the most stable intramol...

Vernonia oil obtained by Soxhlet extraction from the seeds of Vernonia galamensis ssp. nairobensis was reacted with 2-aminopyridine, 2-(aminomethyl)pyridine and 2(aminoethyl)pyridine using a 1:3 mole ratio of vernonia oil to amine at varied temperatures to give the corresponding vernolamides. The expected vernolamide from the reaction of 2-aminopyridine and the oil was not formed. N-(2-pyridiny...

The synthesis of three pyridinyl imines (L1-L3) with electron-donating and electron-withdrawing functional groups, as well their silver(I) complexes (1a-3a, 1b-3b 1c-3c), resulted from our ongoing search for novel metallodrugs potential pharmacological activity. Various analytical spectroscopic analyses were used to characterize the Ag(I) complexes. single crystal X-ray diffraction analysis 3a ...

Nicotine [(S)-3-(1-methyl-2-pyrrolidinyl)pyridine] is a major component of tobacco and a highly efficient acetylcholine receptor (nAChR) agonist that triggers the cholinergic anti-inflammatory pathway. We demonstrate that pre-treatment of monocytes with the stable nicotine catabolite, cotinine [(S)-1-methyl-5-(3-pyridinyl)-2-pyrrolidinone], dramatically alters the nature of the inflammatory res...

Aldosterone synthase (CYP11B2) is a promising therapeutic target for the treatment of cardiovascular diseases related to abnormally high aldosterone levels. On the basis of our previously identified lead compounds I-III, a series of 3-pyridinyl substituted aliphatic cycles were designed, synthesized and tested as CYP11B2 inhibitors. Aromaticity abolishment of the core was successfully applied t...