Assessment of pain and associated factors in people living with HIV/AIDS.

Objective: to evaluate pain in people living with human immunodeficiency virus/acquired immunodeficiency syndrome and to relate it to sociodemographic and clinical factors, depressive symptoms and health-related quality of life.

Method: descriptive, analytical, observational, cross-sectional and quantitative study. Three hundred and two (302) people assisted at a specialized care service participated in the study.

Orvinols with mixed kappa/mu opioid receptor agonist activity.

Dual-acting kappa opioid receptor (KOR) agonist and mu opioid receptor (MOR) partial agonist ligands have been put forward as potential treatment agents for cocaine and other psychostimulant abuse. Members of the orvinol series of ligands are known for their high binding affinity to both KOR and MOR, but efficacy at the individual receptors has not been thoroughly evaluated. In this study, it is shown that a predictive model for efficacy at KOR can be derived, with efficacy being controlled by the length of the group attached to C20 and by the introduction of branching into the side chain.

Efficient clocked electron transfer on superfluid helium.

Unprecedented transport efficiency is demonstrated for electrons on the surface of micron-scale superfluid helium-filled channels by co-opting silicon processing technology to construct the equivalent of a charge-coupled device. Strong fringing fields lead to undetectably rare transfer failures after over a billion cycles in two dimensions. This extremely efficient transport is measured in 120 channels simultaneously with packets of up to 20 electrons, and down to singly occupied pixels.

G protein independent phosphorylation and internalization of the delta-opioid receptor.

Agonist activation of the delta-opioid receptor leads to internalization via G betagamma recruitment of G protein coupled receptor kinase-2, which phosphorylates the receptor at several sites, including Ser363, allowing beta-arrestin binding and localization to clathrin coated pits. Using human embryonic kidney cells expressing a delta-opioid receptor we tested the hypothesis that prevention of receptor coupling to G protein by treatment with pertussis toxin (PTX) will block these processes. PTX treatment did not reduce phosphorylation of delta-opioid receptor Ser363 in response to the agonist [D-Pen2, D-Pen5]enkephalin, or recruitment of beta-arrestin 2-green fluorescent protein to the membrane and only slowed, but did not prevent, [D-Pen2, D-Pen5]enkephalin-induced internalization.

Mixed kappa/mu opioid receptor agonists: the 6 beta-naltrexamines.

Ligands from the naltrexamine series have consistently demonstrated agonist activity at kappa opioid receptors (KOR), with varying activity at the mu opioid receptor (MOR). Various 6 beta-cinnamoylamino derivatives were made with the aim of generating ligands with a KOR agonist/MOR partial agonist profile, as ligands with this activity may be of interest as treatment agents for cocaine abuse. The ligands all displayed the desired high affinity, nonselective binding in vitro and in the functional assays were high efficacy KOR agonists with some partial agonist activity at MOR.