Frosini, Maria; Sesti, Casilde; Saponara, Simona; Donati, Alessandro; Palmi, Mitri; Valoti, Massimo; Machetti, Fabrizio; Sgaragli, Gimpietro published an article in 2000, the title of the article was Effects of taurine and some structurally related analogues on the central mechanism of thermoregulation: A structure-activity relationship study.Category: pyridine-derivatives And the article contains the following content:
There is large body of evidences on the role of taurine in the central mechanisms of thermoregulation in mammals, but it is not clear, whether the hypothermic effect of taurine depends on its interaction with GABA receptors or with a specific receptor. In order to answer this question, the authors have performed a structure-activity relationship study by using both in vitro and in vivo preparations μM amounts of taurine or each of 20 analogs were injected intracerebroventricularly in conscious, restrained rabbits while rectal temperature was recorded. Receptor-binding studies, with synaptic membrane preparations from rabbit brain were used to determine the affinities of these compounds for GABAA and GABAB receptors. Furthermore, the interaction with presynaptic GABA and taurine uptake systems was studied using crude synaptosomal preparations from rabbit brain. Among the compounds tested, (±)-cis-2-aminocyclohexane sulfonic acid, induced hypothermia, but did not interact with GABAA and GABAB receptors neither did it affect GABA and taurine uptake, thus suggesting that its effect on body temperature is not mediated by the central GABA-ergic system. Interestingly, the trans-isomer was devoid of effects either in vivo or in vitro. In order to explain (±)-cis-2-aminocyclohexane sulfonic acid-induced hypothermia, a stereoscopic model was produced showing its possible interactions with a putative taurine brain receptor. The experimental process involved the reaction of Pyridine-3-sulfonic acid(cas: 636-73-7).Category: pyridine-derivatives
The Article related to taurine structure activity thermoregulation brain, gaba taurine receptor thermoregulation brain, Pharmacology: Structure-Activity and other aspects.Category: pyridine-derivatives