Molecular modelling, synthesis, crystallographic studies, in vitro biological assays and behavioral studies in vivo were performed. (bvsalud.org)
The target compounds were evaluated using in vivo behavioral assays for hallucinogen-like and 5-HT(1A) agonist activity and in vitro radioligand competition assays for their affinity at 5-HT(2A), 5-HT(2C), and 5-HT(1A) receptor sites. (erowid.org)
Agonist1
In functional antagonist assays a dose-response curve measures the effect of the ability of a range of concentrations of antagonists to reverse the activity of an agonist. (chemeurope.com)
Receptor3
Examination of cyproheptadine in radioligand receptor-binding assays shoed that it was some five orders of magnitude more active in displacing appropriate radioligands from central histamine, 5-HT-2 and muscarinic cholinergic receptor sites than in inhibiting depolarization dependent calcium fluxes (Donatsch et al 1980). (erowid.org)
The results indicate that fluorination of hallucinogenic tryptamines generally has little effect on 5-HT(2A/2C) receptor affinity or intrinsic activity. (erowid.org)
We used the highly selective 5-HT(6) receptor radioligand [(125)I]SB-258585 (4-iodo-N-[4-methoxy-3-(4-methylpiperazin-1-yl)phenyl]benzene-sulfonamide) to perform autoradiographic binding studies on the rat brain. (ox.ac.uk)
Cholinergic1
Thus, the striatal binding sites seen in this study may be on intrinsic GABAergic or cholinergic neurones, or on terminals of projection neurones from the thalamus or cerebral cortex. (ox.ac.uk)
Active1
Blood and urine samples were collected over 24 h and assayed by a validated liquid chromatography-tandem mass spectrometry (LC-MS/MS) assay for psilocybin and psilocin, the active metabolite. (researchgate.net)
Inhibition2
In a functional assay, the molar concentration of an agonist or antagonist which produces 50% of its maximum possible inhibition. (stratech.co.uk)
The capacity for production of migration inhibitory factor was assessed by the agarose droplet cell migration inhibition assay, using peritoneal exudate cells and a CVB3(m) cell lysate or KCl extracted antigens from heart tissues of CVB3(m)-inoculated mice. (nih.gov)
Receptors4
The maximum amount of drug or radioligand, usually expressed as picomoles (pM) per mg protein, which can bind specifically to the receptors in a membrane preparation. (stratech.co.uk)
It is the molar concentration of radioligand which, at equilibrium, occupies 50% of the receptors. (stratech.co.uk)
Measured using a radioligand competition binding assay, it is the molar concentration of the competing ligand that would occupy 50% of the receptors if no radioligand was present. (stratech.co.uk)
In the 1970s, the development of radioligand-binding assays furthered our understanding of subtypes of receptors for serotonin. (nih.gov)
Ligand1
We examined [ 3 H]BPA in the saturation binding assay using the ligand binding domain of ERR-γ and analyzed the result using Scatchard plot analysis. (nih.gov)
Functional2
The compounds are evaluated via the use of an operational model of allosterism to determine values of functional affinity (Kʙ), cooperativity (αβ) and intrinsic agonism (τʙ) for all compounds. (monash.edu)
The focused library of compounds was profiled in both radioligand binding assays in addition to functional assays at the M₁ mAChR, D₂R and 5-HT2AR. (monash.edu)
Label1
Replacing an atom with its own radioisotope is an intrinsic label that does not alter the structure of the molecule. (wikipedia.org)
Brain2
FUS efficiently enhanced the delivery of both C4 radioligands in the brain with high reproducibility. (thno.org)
Pediatric diffuse intrinsic pontine glioma (DIPG) represents one of the most devastating and lethal brain tumors in children with a median survival of 12 months. (biomedcentral.com)
Competitive1
A number of BPA derivatives were tested in the competitive binding assay using [ 3 H]BPA as a tracer and in the luciferase reporter gene assay. (nih.gov)
Cells2
In recent years, microglia as the brain's intrinsic immune cells have emerged as having new roles in the pathophysiology of psychiatric disorders such as schizophrenia. (nature.com)
Moreover, IK-175 led to a decrease in suppressive IL17A - , IL-22 + expressing T cells in a Th17 differentiation assay. (aacrjournals.org)
Specific1
Detection of viral genomic sequences in autopsy tissue, serum, or cerebral spinal fluid (CSF) samples via reverse-transcriptase polymerase chain reaction (RT-PCR) assay: RT-PCR provides earlier and more specific diagnosis. (medscape.com)