Sigma receptors are protein chaperones with the unexpected characteristic of being activated by ligand binding. As such, they represent intriguing new targets for potential drug development. a chaperone, these “receptors” escort proteins from endoplasmic reticulum to their destinations and act correct misfolded proteins. The two subtypes sigma receptors, named σ1 σ2, markedly distinct each othe...

The influence of naloxone (NAL), a competitive antagonist of mu, kappa, delta and sigma receptors; D-Phe-Cys-Tyr-D-Trp-Orn-Thr-Pen-Thr-NH(2) (CTOP), selective antagonist of mu-opioid receptors; nor-binaltorphimine (NOR-BNI), a potent and higly selective kappa opioid receptor antagonist; naltrindole (NTI), a delta-opioid receptor antagonist and naltriben (NTB), a highly selective delta(2)-opioid...

Dopamine systems are intimately involved with opioid actions. Pharmacological studies suggest an important modulatory effect of dopamine and its receptors on opioid analgesia. We have now examined these interactions in a knock-out model in which the dopamine(2) (D(2)) receptor has been disrupted. Loss of D(2) receptors enhances, in a dose-dependent manner, the analgesic actions of the mu analge...

Sigma sites, originally proposed as opioid receptor subtypes, are currently thought to represent unique receptors with a specific pattern of drug selectivity, a well-established anatomical distribution and broad range of functional roles including potential involvement in nociceptive mechanisms. We have recently demonstrated that intrathecal (i.t.) treatment with a sigma-1 receptor antagonist r...

the aim of this study was to use site directed mutagenesis technique to construct a vector in which serine363 and serine375 residues of the cooh-terminal portion of the μ-opioid receptor (mor) were substituted by alanine. these constructs are essential in studying g-protein coupled receptor kinase-mediated mor desensiti-zation. the nested pcr carried out for conversion of serine363 and serine37...

Sigma-1 antagonism potentiates the antinociceptive effects of opioid drugs, so sigma-1 receptors constitute a biological brake to opioid drug-induced analgesia. The pathophysiological role of this process is unknown. We aimed to investigate whether sigma-1 antagonism reduces inflammatory pain through the disinhibition of the endogenous opioidergic system in mice. The selective sigma-1 antagonis...

objective(s): we aimed to examine association of gene expression of mor1 and glun1 at mrna level in the lumbosacral cord and midbrain with morphine tolerance in male wistar rats. materials and methods: analgesic effects of morphine administrated intraperitoneally at doses of 0.1, 1, 5 and 10 mg/kg were examined using a hot plate test in rats with and without a history of 15 days morphine (10 mg...

Correspondence: Kenji Hashimoto Division of Clinical Neuroscience, Chiba University for Forensic Mental Health, Chiba 260-8670, Japan Tel +81 43 226 2149 Fax +81 43 226 2150 email [email protected] Abstract: The endoplasmic reticulum protein sigma-1 receptors, first regarded as opioid receptors and later confused as the phencyclidine (PCP) binding sites of the N-methyl-D-aspartate (N...

Bombesin, a tetradecapeptide originally isolated from the skin of the frog Bombina bombina,’ elicits dose-related excessive grooming when injected centrally in rats2-‘ as well as other specie^.^ The grooming induced by intracerebroventricular (i.cv.) bombesin in rats consists of hindlimb scratching directed primarily at the head and neck, although facial grooming, body washing, nail licking and...