Search Of High Active And Low Toxic Newly Synthesized Derivatives Of Piperidine For Regional Anesthesia

comparative assessment of local anesthetic activity of newly synthesized derivatives of piperidine for regional anesthesia, depending on their chemical structure. local anesthesia was determined by the method of “tail-flick” on white rats. For research of activity of the compound at the particular type of anesthesia the great important index is duration of complete anesthesia. The duration of complete anaesthesia of LAS-174 was similar to trimecaine, slightly higher than that of novocaine and a little bit less than lidocaine (p>0.05). Total duration of action of LAS-174 is higher than the novocaine and trimekain, and a few exceeding that of lidocaine (p>0.05). LAS-175 index of full anesthesia was 2 times higher than trimekain, 2.5 times than novocaine and a few more than lidocaine (p>0.05). By the total duration this compound exceeds the matched values of trimethoprim, lidocaine and novocaine in 3.4, 1.9 and 4.6 times, respectively. Replacement of the propyl radical to Amillic in the side chain at the 4-th carbon atom of the piperidine ring enhances local activity by the similar toxicity. In 1% solution duration of anesthesia of LAS-190 is similar to the trimecaine and slightly lower than the lidocaine. LAS-189 shows a weaker effect than trimekain and lidocaine (p>0.05). LAS-189 and 190 by the duration of anesthesia was more effective than novocaine, but this difference is not statistically significant. Replacement of the propyl radical (LAS-189) to the phenyl (LAS-190) contributes to increase of local anesthetic activity, especially for the total duration. Acute toxicity of LAS-189 is 750±of 35.56, LAS-190 - 1284±43,87. the Introduction of a cyclopropane radical at the triple bind of the piperidine ring leads to increased local anesthetic effect, weighting of the radical at the 4th carbon atom contributes to the growth of activity and lower toxicity.