Buprenorphine is a potent, semi-synthetic opioid analgesic derived from thebaine. The drug displays the characteristics of an agonist at the mu receptors and antagonist at the kappa receptors. Although buprenorphine has shown some pharmacological effects on delta and kappa opioid receptors, the action on the mu receptors appears to be responsible for most of the analgesic effects associated wit...

Antagonistic properties of buprenorphine for and -opioid receptors were characterized in -endorphinand [D-Ala,NMe-Phe,Gly-ol]-enkephalin (DAMGO)-induced antinociception, respectively, with the tail-flick test in male ICR mice. -Opioid receptor agonist -endorphin (0.1–1 g), -opioid receptor agonist DAMGO (0.5–20 ng), or buprenorphine (0.1–20 g) administered i.c.v. dose dependently produced antin...

I am old enough to have taken part in the international project to sequence the first eukaryotic genome—that of Saccharomyces cerevisiae—which was released in 1996. Twenty years later, scientists from academic and commercial institutions are now involved in the first wholesale construction of a eukaryotic genome: the Yeast 2.0 Project [1]. The construction of whole genomes from scratch is defin...

A reverse phase high performance liquid chromatographic (RPHPLC) method has been developed and validated for simultaneous estimation of Naloxone Hydrochloride and Buprenorphine Hydrochloride in pure and marketed formulations. Separation was carried out using column Hypersil ODS C18 (250 mm x 4.6mm x 5μm particle size) in isocratic mode using mobile phase composition pH 6.0 ammonium acetate Buff...

Thomas Anderson (1819-1874), a physician turned chemist, did most of his research in organic chemistry. He discovered butylamine, collidine, lutidine, picoline, and pyridine during the pyrolysis of coal and destruction of bone oil, studied the constitution of anthracene, piperidine, and codeine; the analysis and properties of alkaloids derived from opium, and prepared a large number of new deri...

Previous research has shown that compounds with mixed and activity may have utility for the treatment of cocaine abuse and dependence. The present study characterizes the pharmacological profile of a bivalent morphinan that was shown to be a opioid receptor agonist and a opioid receptor agonist/antagonist. MCL-145 [bis(N-cyclobutylmethylmorphinan) fumarate] is related to the morphinan cyclorpha...

Opium poppy (Papaver somniferum L.) produces a large variety of isoquinoline alkaloids. The aim of this investigation is to understand the regulation of biosynthesis and the ecological function of the alkaloids in the plant. Agrobacterium-mediated transformations of opium poppy were used to introduce the berberine bridge enzyme cDNA bbe 1 in the antisense orientation into seedling explants. Aft...