Browse Items · NEOMED Bibliography Database

Testosterone causes direct relaxation of rat thoracic aorta.

Several recent studies have provided evidence that gonadal steroid hormones can exert acute (nongenomic) effects on both neural and vascular tissues. This study examines the acute effects of testosterone (T) on vascular reactivity of the rat thoracic…

Enhancing Studies of Pharmacodynamic Mechanisms via Measurements of Metabolic Flux: Fundamental Concepts and Guiding Principles for Using Stable Isotope Tracers.

Drug discovery and development efforts are largely based around a common expectation, namely, that direct or indirect action on a cellular process (e.g., statin-mediated enzyme inhibition or insulin-stimulated receptor activation) will have a…

A noninflammatory interleukin-1beta fragment stimulates fetal lung fluid absorption in guinea pigs.

We have previously demonstrated that full-length interleukin (IL)-1beta can induce and stimulate lung fluid absorption in near-term guinea pig fetuses via stimulation of fetal cortisol synthesis and release. To develop a potentially clinically useful…

Functional selectivity of NK1 receptor signaling: peptide agonists can preferentially produce receptor activation or desensitization.

A cascade of events follows binding of an agonist ligand to the tachykinin NK(1) receptor. These events include activation of multiple signal transduction pathways as well as cellular modulation of receptor function by the process of desensitization.…

Tags: 2006, Animals, CHO Cells, Cricetinae, Dose-Response Relationship, Drug, Humans, Neurokinin-1/agonists/drug effects/*physiology, Rana catesbeiana, Rats, Receptors, Signal Transduction/*physiology, Simmons Mark A, Substance P/metabolism/pharmacology, Tachykinins/metabolism/pharmacology, The Journal of pharmacology and experimental therapeutics

Neurokinin-1 receptor resensitization precedes receptor recycling.

Following agonist binding, neurokinin-1 receptors undergo rapid desensitization followed by internalization and recycling. Desensitization requires receptor phosphorylation but does not require internalization, whereas resensitization is thought to…

Tags: 2005, Adenosine Triphosphate/pharmacology, Animals, Bennett V J, Binding, Calcium/metabolism, CHO Cells, Competitive, Cricetinae, Guanylyl Imidodiphosphate/pharmacology, Neurokinin-1/*metabolism, Perrine S A, Phosphorylation, Rats, Receptors, Simmons M A, Substance P/metabolism, The Journal of pharmacology and experimental therapeutics

Activation of metabotropic glutamate receptor 1 dimers requires glutamate binding in both subunits.

Group I metabotropic glutamate receptors (mGluRs) form stable, disulfide-linked homodimers. Lack of a verifiably monomeric mGluR1 mutant has led to difficulty in assessing the role of dimerization in the molecular mechanism of mGluR1 activation. The…

A novel mechanism of neurokinin-1 receptor resensitization.

Prolonged or repeated activation of many G protein-coupled receptors induces rapid desensitization followed by a period during which receptors are resensitized. In this study, concanavalin A (Con A) and monensin were used to investigate the…

Tags: 2002, Animals, Bennett V J, Cell Membrane/drug effects/metabolism, CHO Cells, Concanavalin A/pharmacology, Cricetinae, Monensin/pharmacology, Neurokinin-1/*agonists/*metabolism, Perrine S A, Phosphorylation/drug effects, Rats, Receptors, Simmons M A, The Journal of pharmacology and experimental therapeutics

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