No abstract

Local Anaesthetic Activity of 1,2-Disubstituted Imidazo[1,2-a]benzimidazoles. -A series of new 1-dialkylaminoalkylimidazobenzimidazoles (VII) (11 examples) are synthesized, of which the majority displays marked local anaesthetic activity. Derivatives (VIIc) and (VIIe) appear to be the most active ones. -(ANISIMOVA, V. A.; OSIPOVA, M. M.; GALENKO-YAROSHEVSKII, A. P.; PONOMAREV, V. V.; POPKOV, V. L.; PRIKHOD'KO, A. K.; KADE, E. A.; SPASOV, A. A.; Khim.-Farm. Zh. 36 (2002) 8, 21-24; Nauchno-issled. inst. fiz. org. khim., Rostov. gos. univ., Rostov-na-Donu 344090, Russia; Russ.) -Koehler 03-103

We compared the effects of local anesthetics procaine, amethocaine (dicaine), bupivacaine, and a new agent RU-1148 on hydrolytic activity of human plasma butyrylcholinesterase. The butyrylcholinesterase-blocking activity of the test substances decreased in the following order: bupivacaine>amethocaine>procaine>RU-1148. The study of the capacity of these agents to form complexes with human plasma proteins and serum albumin showed that RU-1148 in therapeutic concentrations was transported by human serum albumin,beta-globulin, and acid glycoproteins. Study of the mechanisms of pharmacodynamic interactions between clonidine and RU-1148 demonstrated good prospects of their combined use.

Eine Gasphasencyclisierung des o‐Xenyloxydichlorphosphins (I) bei 550 ‐ 600°C zu 10‐Chlor‐lO‐phospha‐9‐oxa‐9,10‐dihydrophenanthren (II) gelingt nicht.

A microstructural model of thermorheological processes during the freezing of fine‐grained soils is described. Using electron microscopy and X‐ray diffractometry, the changes due to freezing in the microstructures of kaolin, bentonite and askangel were experimentally studied. Curves of aggregate distribution and pore size for different freezing periods are presented. It is shown that there is good agreement between experimental results and theoretical hypotheses.