Rats experimentally infected with the neurotropic RNA virus, Borna disease virus, have a hyperactive movement disorder. Because locomotor activity is modulated by the nucleus accumbens (N. Acc.) dopamine (DA) system, high-affinity DA uptake, DA D1, D2, and D3 receptor binding sites were examined in N. Acc. subregions of normal and infected rats by quantitative receptor autoradiography. The N. A...

BACKGROUND AND PURPOSE Sigma-1 receptors are atypical receptors with potentially two transmembrane domains. Antagonists require doses significantly higher than their published affinities to have biological effects. We have reassessed the binding characteristics of these ligands and found antagonists bind to high- and low-affinity states not distinguished by agonists. EXPERIMENTAL APPROACH The...

introduction: bombesin is a 14-aminoacid peptide isolated from frog skin. the mammalian counterparts of the frog peptide are neuromedin b (nmb) and gastrin-releasing peptide (grp). bombesin (bbn) is a peptide showing high affinity for the gastrin releasing peptide receptor (grpr). prostate, small cell lung cancer, breast, gastric, and colon cancers are known to over express receptors to bombesi...

Background and Purpose The ?4?2 nicotinic ACh receptor (nAChR), a subtype of the ligand-gated ion channel, is abundantly expressed in brain implicated several neurological disorders. endocytosis nAChRs plays important roles pathogenesis diseases, but underlying molecular mechanisms remain poorly understood. Experimental Approach Loss-of-function approaches mutants that display different endocyt...

Neurosteroids are endogenous steroids acting in the central nervous system. They participate in synaptic plasticity, memory and learning, Alzheimer's disease, and certain drug reward. Some mechanisms behind these effects are thought to be nongenomic, e.g., they modulate the function of the N-methyl-d-aspartate (NMDA) receptor complex. In this study, we used a Chinese hamster ovary cell line sta...

  Introduction: Bombesin is a 14-aminoacid peptide isolated from frog skin. The mammalian counterparts of the frog peptide are neuromedin B (NMB) and gastrin-releasing peptide (GRP). Bombesin (BBN) is a peptide showing high affinity for the gastrin releasing peptide receptor (GRPr). Prostate, small cell lung cancer, breast, gastric, and colon cancers are known to over...

OBJECTIVE To determine whether intestinal epithelial cells have a receptor for intestinal trefoil factor and characterize receptor-ligand binding kinetics. METHODS Radioligand binding assays were performed to characterize the binding kinetics between [(125)I]-labeled ITF and IEC-6, HT-29, Caco2 and HaCaT cells. The K d, Bmax and other kinetic variables describing the interaction between ITF a...

An endogenous substance in brain, clonidine-displacing substance, binds to the same receptor populations as clonidine and is biologically active. Since receptor binding sites can be modeled by using specific antiligand antibodies, we tested the hypothesis that polyclonal antibodies raised in rat and rabbit against the clonidine analog p-aminoclonidine coupled to hemocyanin would recognize compo...

Imidafenacin is a potent and selective antagonist of M1 and M3 muscarinic receptors that is safe, efficacious, and well tolerated for controlling the symptoms of overactive bladder (OAB). However, the precise mechanisms responsible for the bladder-selective pharmacological effects of this agent remain unclear. The in vivo pharmacologic effects of imidafenacin result from receptor occupancy. The...

introduction: 5-ht1a receptor is related with a variety of neuropsychiatric disorders. . in this study a phenolic analogue derived from dway [desmethyl way-100635 (n-(2-(1-(4-(2-methoxyphenyl)piperazinyl)-ethyl))-n-(2-pyridinyl) cyclohexanecarboxamide)] is used to design the desired structure of 5-ht1a receptor imaging agents after labeling with [99mtc (co) 3(h2o) 3] + core via dithiocarbamate ...