The pharmacokinetics of pentacaine, a new local anaesthetic agent from the group of carbanilates, was investigated in the rat at a dose of 2 mg kg-1 i.v. and per os. A three-compartment open model gave the best fit to the data. The model parameters are: t1/2 99.0 +/- 14.1 min, Vss 7411.1 ml kg-1, Cl 77.9 ml min-1 kg-1; after oral administration t1/2ab 4.9 +/- 1.9 min, bioavailability 59.1 per cent, and extent of absorption 79.3 per cent. Pentacaine is eliminated almost entirely by metabolism. The metabolites are excreted equally in the urine and faeces at a relatively slow rate. The pharmacokinetics of pentacaine was linear in the dose range 0.008-4 mg kg-1. The whole-body autoradiography in mice showed rapid transfer of 3H radioactivity from the vessels to tissues and a markedly heterogeneous disposition pattern in organs.

Administration, Oral↗

PubMedDate not supplied

Experimental studies of some microrheological factors in serious brain ischemia after stobadine pretreatment.

Serious brain ischemia was induced by occlusion of cerebral arteries in dogs. The occlusion time was 7 min. The blood was collected at various intervals of reperfusion (5, 60, 180, 240 min and 24 h). Thirty minutes before ischemization, stobadine was given (1, 2, or 5 mg/kg). The changes of erythrocyte membrane fluidity were evaluated using colloid-osmotic hemolysis induced by brilliant cresyl blue. In the control group (without stobadine) the colloid-osmotic hemolysis was significantly increased immediately after ischemization and after 5 and 60 min. However, after 240 min of reperfusion, a significant decrease of hemolysis was observed. The increase of colloid-osmotic hemolysis after ischemization in the control group was prevented after stobadine pretreatment. The thrombotization of microcirculation that was observed in the control group was not present after stobadine pretreatment.

Animals↗

PubMedDate not supplied

Two novel cell specific receptor proteins, CRLR and CD 117 in human glial tumors.

OBJECTIVE: CRLR (calcitonin receptor-like receptor) and CD 117, the gene product of c-kit have been shown to be expressed in cells of glial tumors, especially in those with higher malignancy. Here we report the distribution of these peptides in various cellular compartments within those tumors. MATERIAL: Both receptor proteins have been investigated in 95 glial tumor biopsies of different grades. METHODS: Both proteins were visualized by immunohistochemistry with antibodies either commercially available or raised for this purpose. RESULTS: Both receptor peptides can be identified in or around tumor blood vessels. CRLR occurs in some endothelial cells, especially in the microvascular proliferations of glioblastoma multiforme, whereas CD 117 preferentially occurs in cells of the thickened vascular wall within cells of pericyte or fibroblast morphology. Both antigens are found in addition in few neoplastic cells of overt astrocyte morphology. CONCLUSIONS: The occurrence of identical antigens in glial tumor blood vessels and in neighboring tumor cells underlines the common origin of "mesenchymal" and "neuroepithelial" components of such (malignant) glial neoplasms.

Actins↗