EFFECT OF 2-METHYLTAURINE AND ITS ENANTIOMERS ON ARTERIAL BLOOD-PRESSURE

Taurine has been shown to exert many biological effects. Among them, t he ability of this amino acid to induce a reduction of arterial blood pressure, when administered intracerebroventricularly (i.c.v.) to mamm als, has been established since a long time ago. To gain further infor mation on the structure-activity requirements for taurine's hypotensiv e effect, the synthesis of 2-methyltaurine (2-aminopropanesulphonic ac id) and the asymmetric synthesis of its enantiomers were performed; th e enantiomeric purity of (R)- and (S)-2-methyltaurine was assayed by d ifferential scanning calorimetry (DSC) and HPLC, The findings here rep orted show that the hypotensive effect elicited by the i.c.v, administ ration of racemate is mainly due to the (S)-enantiomer. The specificit y of this effect was proved by the ability of the taurine antagonist T AG (6-aminomethyl-4H-3-methyl-1,2,4-benzothiadiazine 1,1-dioxide) to p revent it. (C) 1996 The Italian Pharmacological Society