Introduction. The solubility of an active pharmaceutical ingredient plays a major role in drug absorption. Hot melt extrusion is batch or continuous process that allows creating solid dispersion systems based on various carriers order to increase and bioavailability substances. Development effective safe analgesics one the most vital tasks organic medicinal chemistry. An innovative non-opioid a...

Prostaglandin (PG) E2 is a major cyclooxygenase (COX) product at inflammatory sites where it contributes to local increases in blood flow, edema formation, and pain sensitization. Using rats in vivo and rat and human blood in vitro, we have examined the roles of COX-1 and COX-2 in the production of PGE2. In anesthetized rats treated with bacterial lipopolysaccharide (LPS) to induce the expressi...

Conserved serines of transmembrane segment (TM) five (TM5) are critical for the interactions of endogenous catecholamines with alpha(1)- and alpha(2)-adrenergic, beta(2)-adrenergic, and D1, D2, and D3 dopamine receptors. The unique high-affinity interaction of the D4 dopamine receptor subtype with both norepinephrine and dopamine, and the fact that TM5 serine interactions have never been studie...

Tahseldar-Roumieh, Rima, Rana Ghali-Ghoul, Claire Lugnier, and Ramzi Sabra. Effect of phosphodiesterase 5 inhibitor on alteration in vascular smooth muscle sensitivity and renal function in rats with liver cirrhosis. Am J Physiol Heart Circ Physiol 290: H481–H488, 2006; doi:10.1152/ajpheart.00507.2005.—Previous studies suggested that increased activity of phosphodiesterase (PDE)5 in the kidneys...

The mechanisms coupled to adenosine A(1)- and histamine H(3)-receptors have been examined in the presynaptic inhibition of acetylcholine (ACh) release from the guinea pig ileum. Electrically evoked twitch contractions were used as a measure of neuronal ACh release. A(1)- and H(3)-receptors were activated by adenosine and R-(alpha)-methylhistamine (RAMH), respectively. The neuroinhibitory effect...

Cysteinyl leukotrienes (CysLTs) are potent inflammatory mediators that predominantly exert their effects by binding to cysteinyl leukotriene receptors of the G protein-coupled receptor family. CysLT receptor 2 (CysLT(2)R), expressed in endothelial cells of some vascular beds, has been implicated in a variety of cardiovascular functions. Endothelium-specific overexpression of human CysLT(2)R in ...