Abstract
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, we have performed a structure-activity relationship study by using both in vitro and in vivo preparations. μM amounts of taurine or each of 20 analogues 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-aminocyclohexanesulfonic 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-aminocyclohexanesulfonic acid-induced hypothermia, a stereoscopic model was produced showing its possible interactions with a putative taurine brain receptor.
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References
Barbeau, A., Inove, N., Tsukada, Y., and Butterworth, R.F., 1975, The neuropharmacology of taurine. Life Sci. 17(5): 669–677.
Bowery, N.G., Hill, D.R., and Hudson, A.L., 1985, [3Hl(-)Baclofen: an improved ligand for GABAB sites. Neuropharmacology 24(3): 207–10.
Bureau, M.H., and Olsen, R.W., 1991, Taurine acts on a subclass of GABAA receptors in mammalian brain in vitro, Eur. J. Pharmacol. 207(1): 9–16.
Frosini, M., Sesti, C., Palmi, M., Valoti, M., Fusi, F., Bianchi, L., Della Corte, L., and Sgaragli, G.P., Changes in CSF composition in heat-stressed rabbits: the possible role of taurine and GABA as cryogens. This book.
Hill, D.R., and Bowery, N.G., 1981, 3H-baclofen and 3H-GABA bind to bicuculline-insensitive GABAB sites in rat brain. Nature 12;290(5802):149–52.
Hruska, RE., Padjen, A., Bressler, R., and Yamamura, H.I., 1978, Taurine: sodium-dependent, high-affinity transport into rat brain synaptosomes. Mol. Pharmacol. 14(1): 77–85.
Insel, P.A., 1996, Analgesic-antipyretic and antiinflammatory agents and drugs employed in the treatment of gout. In Goodman and Gilman’ s-The pharmacological basis of therapeutics, (Hardman, J.G., Limbird, L.E., Molinoff, P.B., Ruddon, R.W., Goodman Gilman, A., eds) McGraw-Hill, New York, NY, USA, 9th edition, pp. 617–657.
Kontro, P., and Oja, S.S., 1987, Co-operativity in sodium-independent taurine binding to brain membranes in the mouse. Neuroscience 23(2): 567–70.
Kontro, P., and Oja S.S., 1990, Interactions of taurine with GABAB binding sites in mouse brain. Neuropharmacol. 29(3): 243–7.
Krogsgaard-Larsen, P., Falch, E., Schousboe, A., Curtis, D.R., and Lodge, D., 1980, Piperidine-4-sulphonic acid, a new specific GABA agonist. J. Neurochem. 34(3): 756–9.
Lipton, J.M., and Ticknor, C.B., 1978, Central effect of taurine and its analogues on fever caused by intravenous leukocytic pyrogen in the rabbit. J. Physiol. (London) 287: 535–543.
Palmi, M., Frosini, M., and Sgaragli, G.P., 1992, Calcium changes in rabbit CSF during endotoxin, IL-1β and PGE2fever. Pharmacol. Biochem. Behav. 43: 1253–1262.
Sancibrian, M., Serrano, J.S., and Minano, F.J., 1991, Opioid and prostaglandin mechanisms involved in the effects of GABAergic drugs on body temperature. Gen. Pharmacol. 22(2): 259–62.
Sesti, C., Frosini, M., and Sgaragli, G.P., 1999, Rabbit rectal temperature and ECoG spectrum changes induced by intracerebroventricular injection of GABA, taurine and analogues. Pharmacol. Res. 39: 61.
Sgaragli, G.P., Carlà, V., Magnani, M., and Galli, A., 1981, Hypothennia induced in rabbits by intracerebroveniicular taurine: specificity and relationship with central serotonin(5-HT) systems. J. Pharmacol. Exp. Ther. 219: 778–785.
Sgaragli, G.P., Frosini, M., Palmi, M., Bianchi, L., and Della Corte, L., 1994, Calcium and taurine interaction in mammalian brain metabolism. Adv. Exp. Med. Biol. 359: 299–308.
Sgaragli, G.P., Frosini, M., Palmi, M., Dixon, H.B., Desmond-Smith, N., Bianchi, L., and Della Corte, L., 1996, Role of taurine in thermoregulation and motor control. Behavioural and cellular studies Adv. Exp. Med. Biol. 403: 527–35.
Watabe, S., Yamaguchi, H., and Ashida, S., 1993, DM-9384, a new cognition-enhancing agent, increases the turnover of components of the GABAergic system in the rat cerebral cortex. Eur. J. Pharmacol. 238: 303–9.
Wu, J.Y., Liao, C.C., Lin, C.J., Lee, Y.H., Ho, J.Y. and Tsai, W.H., 1987, Taurine receptor in the mammalian brain. Prog. Clin. Biol. Res., 351:147–56.
Yang, J.S. and Olsen, R.W., 1987, gamma-Aminobutyric acid receptor binding in fresh mouse brain membranes at 22∘ C: ligand-induced changes in affinity. Mol Pharmacol., 32(1):266–77.
Yarbrough, G.G., Singh, D.K. and Taylor, D.A., 1981, Neuropharmacological characterization of a taurine antagonist. J. Pharmacol. Exp. Ther., 219:604–613.
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Frosini, M. et al. (2002). Effects of Taurine and some Structurally Related Analogues on the Central Mechanism of Thermoregulation. In: Della Corte, L., Huxtable, R.J., Sgaragli, G., Tipton, K.F. (eds) Taurine 4. Advances in Experimental Medicine and Biology, vol 483. Springer, Boston, MA. https://doi.org/10.1007/0-306-46838-7_30
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DOI: https://doi.org/10.1007/0-306-46838-7_30
Publisher Name: Springer, Boston, MA
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