Nicotine Adiction

submitted by: alex01
Linda Dwoskin (Univerisity of Kentucky, Lexington, KY) discussed drugs currently used for nicotine addiction, including various formulations of nicotine, bupropion (Zyban@) and varenicline (Chantix@) as well as her research on novel antagonists of nicotinic receptors. According to Dwoskin a6ß2 subtype of nicotinic receptors may represent a better target for novel antagonists for smoking cessation. This is, however, not the only receptor subtype involved in nicotine addiction. Other...

Drug Discovery for Alzheimer's Disease

submitted by: alex01

Gregory Rose from PharmExperts.com interviews J. Buccafusco (Medical College of Georgia, Augusta, GA) about his development of new anti-Altzheimer drugs, designed to act by multiple mechanisms to improve congnition. Desensitization of nicotinic receptors is one of the novel approaches proposed by Buccafusco. Three of his compounds are currently in advanced preclinical evaluation.

Calcium Channels

submitted by: alex01

Dr. Catterall describes autoinhibitory control of cardiac L-type cardiac calcium channels by protein
phosphorylation and macromolecular signaling as well as regulation of P/Q type calcium currents in
neurons. His research suggests novel targets for drugs affecting cardiovascular or central nervous
systems.

Sperm Selection for In Vitro Fertilization

submitted by: alex01

G. Huszar, MD - G. Huszar developed hyaluronic acid (HA) binding test for sperm selection for in vitro fertilization. The test allows better assessment of sperm maturity than previously used motility test. Dr. Huszar discusses also safety of cryopreservation of sperms and potential for male contraceptive drugs.

Obesity and Metabolic Syndrome

submitted by: alex01

F. X. Pi-Sunyer, MD defines metabolic syndrome and obesity and discusses the design and preliminary results of the Look AHEAD trial involving the importance of life style modification in the prevention of cardiovascular complications in patients with type II diabetes. Current and potential approaches to the therapy of obesity include modulators of the endocannabinoid system, drugs affecting free fatty acid synthesis and metabolism as drugs capable of increasing metabolic expenditure.

GABAB and Other Brain Receptors

submitted by: alex01

S. Enna, PhD. Discussing structure, function and clinical role of GABAB receptors in the central nervous system. Receptor dimerization is important for their function. The main use of baclofen is in the treatment of muscular spasticity. GABAB receptors may also play a role in depression.

Treatment of Depression

submitted by: alex01

P. Skolnick, PhD - Depression is a highly heterogenous disorder. Currently available therapy is not sufficiently effective. DOV Pharmaceuticals has triple (serotonin, norepinephrine, dopamine) uptake inhibitors in clinical evaluation. They are expected to be effective in a larger proportion of patients and have more rapid onset of action. They also reduce body weight and plasma triglycerides.

Drug Development: Perspective and Strategy

submitted by: alex01

R. Ruffolo, PhD - Wyeth’s pipeline has 11 potential anti-Alzheimer drugs, including two vaccines and two biotech products. Ruffolo defines breakthrough therapy and the “learn and confirm” concept in clinical trials.

Endothelial Function

submitted by: alex01

P. M. Vanhoutte, MD, PhD - Discussion of the importance of endothelium for vascular function, of endothelial factors as targets for new drugs and of vasoprotective effects of estrogens and polyphenols.

Endothelial Dysfunction

submitted by: alex01

D. Heistad, MD - Cardiovascular risk factors are associated with endothelial dysfunction. COX-1 inhibition may protect from arterial dysfunction. Potential use of gene therapy in stroke.