A fundamental feature of any drug designed to treat a disease of the central nervous system is the ability to cross the blood-brain barrier. Passage across the blood-brain barrier of AIT-082, a cognitive enhancer, was investigated in mice. [(14)C]AIT-082 crossed the blood-brain barrier in young male Swiss-Webster mice with a mean influx constant (K(i)) of 0.6 +/- 0.2 microl g(-1) min(-1). Furth...

Metabotropic glutamate receptors (mGluRs) represent a potential therapeutic target. Possible anticonvulsant action of AMN 082, an agonist of mGluR7 subtype, was studied in immature rats using pentylenetetrazol (PTZ)-induced seizures as a model. Five age groups of rats (7-, 12-, 18-, 25-day-old and adult animals) were pretreated with AMN 082 in doses of 0.5, 1, 2, and 5 mg/kg i.p. and 30 min lat...

James Colgrove, State of immunity: the politics of vaccination in twentieth-century America, Berkeley, University of California Press, and New York, Milbank Memorial Fund, 2006, pp. xiii, 332, illus., £29.00, $39.95 (hardback 0-520-24749-3; 978-0-52024749-3). Gordon C Cook, The Incurables Movement: an illustrated history of The British Home, Oxford, Radcliffe Publishing, 2006, pp. vii, 219, ill...

Lindsay A. Turnbull, Cloé Paul-Victor, Bernhard Schmid, and Drew W. Purves. 2008. Growth rates, seed size, and physiology: Do small-seeded species really grow faster? Ecology 89:1352–1363. Appendix B. PARAMETER ESTIMATION FOR THE DAILY GROWTH MODEL. The likelihood analysis used measurements of aboveand belowground biomass of individual plants, growing in different temperature and nutrient regim...

Aquaporins (AQP) are involved in rapid and active gating of water across biological membranes. The molecular regulation of AQP is unknown. Here we report the isolation, identification and reconstitution of the regulatory complex of AQP-1. AQP-1 and Galphai3 have been implicated in GTP-induced gating of water in zymogen granules (ZG), the secretory vesicles in exocrine pancreas. In the present s...

Previous studies have indicated a role of serotonin (5-HT)2 receptors in modulation of the behavioral effects of cocaine. In the present study, the efficacy of SR 46349B (a 5-HT(2A) receptor antagonist) or SDZ SER-082 (a 5-HT(2C) receptor antagonist) in altering cocaine seeking behavior was examined in rats. Rats were trained to press a lever for cocaine (0.5 mg/kg/infusion, iv) paired with the...

The Na(+)/dicarboxylate cotransporter NaDC1 absorbs citric acid cycle intermediates from the lumen of the small intestine and kidney proximal tubule. No effective inhibitor has been identified yet, although previous studies showed that the nonsteroidal anti-inflammatory drug, flufenamate, inhibits the human (h) NaDC1 with an IC(50) value of 2 mM. In the present study, we have tested compounds r...