Structure-activity relation studies have established that the alkyl side chain in tetrahydrocannabinol (THC) plays a crucial role in the activation of the cannabinoid receptor. Unfortunately, the flexible nature of this side chain has hampered efforts to elucidate the precise nature of the interaction of THC with its receptors. Therefore, a series of analogs with structurally restrained side ch...

Background: Follicle stimulating hormone (FSH) receptor plays an important role in FSH signaling during reproductive development. Any changes in FSHR gene is resulted in alteration of amino acid in protein chain, consequence to affect the binding affinity, intracellular signaling and expression levels of FSHR. FSHR polymorphisms can be involved in etiology of many reproductive disorders such as...

The effects of potassium thiocyanate on the binding of DL-aamino-3-hydroxy-5-methylisoxazolepropionic acid (AMPA), 6-cyano-7-nitroquinoxaline-2,3-dione (CNQX), and L-glutamate to the AMPA receptor complex were studied in rat brain membranes. Thiocyanate increased the affinity of AMPA receptors for both AMPA and i.-glutamate and decreased the affinity for CNQX. Displacement of [3H]CNQX binding b...

Introduction: Neurotensin (NT) is a tridecapeptide that binds specifically to neurotensin receptors. Several forms of cancer, including small cell lung cancer, colon, pancreatic and prostate carcinomas especially exocrine pancreatic carcinomas express receptors for neurotensin peptide. Radiolabeled neurotensin derivatives with a high affinity for these receptors might be used for scintigraphy. ...

To obtain drugs which are more selective at benzodiazepine (BZD) receptors, design and synthesis of functionally selective ligands for BZD receptors is the current strategy of our pharmaceutical chemistry department. The affinity of newly synthesized ligands is assessed by radioligand receptor binding assays. Based on our previous studies, 2-phenyl-5-oxo-7-methyl-1,3,4-oxadiazolo[a,2,3]-pyrimid...

ER proteins of widely differing abundance are retrieved from the Golgi by KDEL-receptor. Abundant tend to have KDEL rather than HDEL signals, whereas ADEL and DDEL not used in most organisms. Here, we explore mechanism selective retrieval signal capture KDEL-receptor how binds with 10-fold higher affinity KDEL. Our results show carboxyl-terminus moves along a ladder arginine residues as it ente...

Receptor activity can be described in terms of ligand-induced transitions between functional states. The nicotinic acetylcholine receptor (nAChR), a prototypic ligand-gated ion channel, is an "unconventional allosteric protein" which exists in at least three interconvertible conformations, referred to as resting (low agonist affinity, closed channel), activated (open channel), and desensitized ...

Binding kinetics of Shiga toxin to HeLa CCL-2 cells and to cell lines cloned by limiting dilutions were determined. Lines with a wide range of sensitivity to Shiga toxin were obtained. Binding data, analyzed by a computer-based Scatchard model program, revealed two classes of binding sites, one of low affinity and high capacity and one of high affinity and low capacity. The number of high affin...

Adenosine analogs such as P-(L-phenylisopropyl) adenosine and 5'-N-ethylcarboxamide adenosine inhibit the basal adenylate cyclase activity in membrane preparations of rat hippocampus. In the same preparations three affinity states of the adenosine receptor for agonist ligands can be detected. In the absence of added guanine nucleotide the agonist [3HJW-cyclohexyladenosine binds to a single high...