High affinity subtype selective. Medical search. Frequent questions

It also acts as a high affinity sigma receptor ligand, selective for the σ2 subtype. (wikipedia.org)
Selective occlusion of the P/Q-type channel ligand ω-conotoxin MVIIC (but not ω-agatoxin IVA) from its binding site in Purkinje neurons suggests that DW13.3 binds to a site close to the pore of the channel. (aspetjournals.org)
we therefore tested for cannabinoid receptors in seven representative species, using tritiated ligand binding assays with [3H]CP55,940 displaced by the CB1-selective antagonist SR141716A. (researchgate.net)
Sig1R is an endoplasmic reticulum membrane protein that, in addition to its promiscuous high-affinity ligand binding, has been shown to have chaperone activity. (frontiersin.org)
High resolution crystal structure of Adenosine A2 receptor (AA2AR) in complex with agonist UK-432097 makes possible rational design of small molecules specifically targeting C5' substitutions of the agonist ribose ring, making possible more high affinity and subtype selective binding and potentially ligand specific modulation of adenosine receptor function. (nih.gov)
High resolution crystal structure makes possible rational design of small molecules specifically targeting C5' substitutions of the agonist ribose ring, making possible more high affinity and subtype selective binding and potentially ligand specific modulation of adenosine receptor function. (nih.gov)
In vitro studies showed it to be a full agonist ligand, which selectively binds to OR with high affinity, although it is not selective to a single OR subtype (inhibition constant, 0.4-1.6 nM across OR subtypes). (starrlifesciences.com)
DPhe 6 ,βAla 11 ,Phe 13 ,Nle 14 ]Bn(6−14) was found to have high affinity ( K i = 0.4 nM) for the fBB 4 receptor and 125 I-[DTyr 6 ,βala 11 ,Phe 13 ,Nle 14 ]Bn(6−14) to be an excellent ligand for this receptor. (acs.org)

The selective antagonists pirenzepine and AF-DX 116 bind to this receptor with a single affinity: low and high, respectively. (nih.gov)
We report here that an endogenous, intracellular factor alters the affinity of selective antagonists for muscarinic receptors in the heart. (nih.gov)
ZM241385 is one of the selective non-xanthine A2AR antagonists with high affinity in the nanomolar range. (simulations-plus.com)
I. Medicinal Chemistry: A panel of 50-75 novel benzamide derivatives of 2,3-dimethoxy-N-(p-flurobenzyl)piperdin-4-yl benzamide (MBP) and 2,3 - dimethoxy-N-(9-p-flurobenzyl)-azabicyclo[3.3.1]nonan-3beta-yl benzarnide (MABN), which are known to be high-affinity, nonselective antagonists for D2 and D3 receptors, will be synthesized. (unthsc.edu)
Ill. Behavioral Studies: Those benzamide derivatives exhibiting the greatest selectivity will be used 1) to determine their efficacy for antagonizing the reinforcing effects of cocaine self-administration in primates using behavioral paradigms, 2) to investigate the molecular properties of the D2-like neurotransmitter binding sites using affinity labeling techniques, and 3) to explore the potential for using receptor subtype selective irreversible antagonists as a therapeutic tools for drug abuse rehabilitation. (unthsc.edu)
One obstacle to defining which dopamine receptor subtype(s) are involved in reinforcing effects is the lack of high-affinity, selective antagonists for each of the receptor subtypes. (unthsc.edu)
This projection allowed to clearly distinguish between antagonists of mGluR1 and mGluR5 subtype. (uni-frankfurt.de)
Selective agonists and antagonists have been developed for each of the AR subtypes. (turkupetcentre.net)
Three of the five classes of Bn receptor antagonists that interacted with higher affinity with the fBB 4 -R functioned as fBB 4 -R antagonists and two as partial agonists. (acs.org)

Unlike 2,5-DMA derivatives, MDMA and MDA demonstrated little selectivity for 5-HT2 versus 5-HT1 subtypes of receptors. (erowid.org)
The status of these and other BZ site compounds with claimed, but often not explicitly stated, GABA(A) subtype selectivity (such as ELB-139 and ocinaplon) will be reviewed in relation to their development as non-sedating anxiolytics for the treatment of generalised anxiety disorder. (hhs.gov)
The selectivity of the muscarinic toxin MT3 from green mamba snake venom was corroborated by inhibition of the binding of [3H]NMS, a classical muscarinic radioligand, to native and cloned muscarinic receptors, showing 214-fold higher affinity for m4 than for m1 subtype, without significant binding to the others. (pasteur.fr)
Surprisingly, 77-LH-28-1 showed high affinity and selectivity for D4R over D2R and D3R. (unicam.it)
Pharmacology: Genetically engineered eukayotic cells, expressing high levels of D2-like dopamine (D2, D3 and D4) receptors, will be used to characterize the pharmacologic selectivity of each benzamide derivative for the three D2-like dopamine receptor subtypes. (unthsc.edu)
Promising molecules should be optimized with respect to activity/affinity and selectivity, their binding mode investigated and, finally, compared to existing lead compounds. (uni-frankfurt.de)

There are compounds that affect many subtypes of receptors in the same protein family, and modern pharmacology is looking for compounds that affect only one target, a single type of protein. (ub.edu)
Obtaining active compounds is now considered far better than developing new extraction methodologies in order to purify and test their activities, most notable among these technologies are mass spectrometry (MS), high performance liquid chromatography (HPLC) and two-dimensional electrophoresis. (scielo.br)
Other behavioral, cardiovascular, and toxic effects of MDMA and related derivatives may be mediated by actions at other central and/or peripheral recognition sites, including muscarinic cholinergic receptors and alpha 2-adrenergic receptors, for which these compounds exhibit relatively high affinity. (erowid.org)
Selective affinity relies on a compound binding with higher affinity to the alpha2/alpha3 compared with alpha1 subtypes, but to date no such compounds have been described. (hhs.gov)
To better understand the structural features required for the selective interaction with D4R, the aliphatic butyl chain of 77-LH-28-1 was modified and the novel compounds 1-6 were prepared. (unicam.it)
All the compounds were evaluated for their affinity at dopamine D2R, D3R and D4R subtypes, as well as at the five mAChR subtypes. (unicam.it)
Compounds showing the highest affinities at D4R were also evaluated for their functional activity considering both G-protein activation and β-arrestin recruitment. (unicam.it)
This technology includes adenosine receptor binding compounds which could potentially be used for development of more selective and safe treatment of cardiovascular, psychiatric and neurodegenerative disorders. (nih.gov)
This technology presents novel rationally designed small molecule compounds capable of selective binding to adenosine receptor (subtypes A2a, A1, A2b and A3) and inducing effector-biased downstream signaling. (nih.gov)
The detection of new scaffolds, in turn, was divided into two approaches: First the development of pharmacological assays to screen compounds at a certain target for bioactivity (here: affinity towards the allosteric recognition site of mGluR1 and mGluR5), and second the evaluation of computer assisted methods for the identification of virtual hits to be screened afterwards on the pharmacological assays established before. (uni-frankfurt.de)
The Asinex Gold-Collection was screened for each seed compound and some of the most similar compounds (according to the CATS descriptor) were ordered and tested forbinding affinity and functional activity at mGluR1. (uni-frankfurt.de)
28 compounds were ordered and tested on activity and affinity for mGluR1. (uni-frankfurt.de)
Endothelial cells have a very active transport system for adenosine, and also high rate of metabolism, converting adenosine to inosine, hypoxanthine, xanthine, uric acid, and other compounds. (turkupetcentre.net)

Grover GJ, Mellström K, Malm J. (2007) Therapeutic potential for thyroid hormone receptor-beta selective agonists for treating obesity, hyperlipidemia and diabetes. (guidetopharmacology.org)
Non-selective benzodiazepine (BZ) binding-site full agonists, exemplified by diazepam, act by enhancing the inhibitory effects of GABA at GABA(A) receptors containing either an alpha1, -2, -3 or -5 subunit. (hhs.gov)
In the late 1980s and early 1990s a number of non-selective partial agonists, exemplified by bretazenil, pazinaclone and abecarnil, were described. (hhs.gov)
However, the discovery of subtype-selective agonists is hampered by the high degree of homology among the M1-M5 mAChR subtypes at the orthosteric binding site. (unicam.it)
Agonists, including endogenous agonist adenosine, lead to the activation of all AR subtypes, and subsequent regulation by desensitization and trafficking ( Mundell and Kelly, 2011 ). (turkupetcentre.net)
The fBB 4 -R had a unique pharmacology for naturally occurring Bn-related agonists, with the presence of a penultimate phenylalanine being critical for high-affinity interaction. (acs.org)

Although cocaine's reinforcing effects are known to be mediated through dopamine neurotransmission, it is not clear which of the dopamine receptor subtypes play a predominant role in reinforcement. (unthsc.edu)
Based upon a forskolin-dependent activation of the adenylyl cyclase inhibition assay, LS-3-134 is a weak partial agonist at both D2 and D3 dopamine receptor subtypes (29% and 35% of full agonist activity, respectively). (elsevierpure.com)

Mutation of an aspartate at residue 89 in somatostatin receptor subtype 2 prevents Na+ regulation of agonist binding but does not alter receptor-G protein association. (uchicago.edu)
What is a selective beta 2 agonist? (wanderluce.com)
Naramig (Naratriptan) is a selective serotonin 5-HT1 receptor agonist. (unitedpharmacies-uk.md)
In the human prostate, Prazosin antagonizes phenylephrine (alpha1 agonist)-induced contractions, in vitro , and binds with high affinity to the alpha1c adrenoceptor, which is thought to be the predominant functional type in the prostate. (pharmacycode.com)
This tracer is attractive because it combines 18F labeling, is suited to the slow kinetics of high-affinity ligands, and has agonist binding, which has been shown to be more sensitive to changes in OR occupation than is antagonist binding. (starrlifesciences.com)
In contrast, a selective α-adrenergic agonist phenylephrine, elicited greater contractions both in the aged body and trigone than those in young rats. (scirp.org)

On the other hand, due to the scarcity of sigma2 selective ligands, less is understood about this subtype. (umsystem.edu)
Number of selective Sig1R and Sig2R ligands have been described confirming significant differences in the pharmacological regulation of these subtypes. (frontiersin.org)
It was based upon six selective, potent and structurally diverse ligands. (uni-frankfurt.de)

More specifically, the alpha2- and/or alpha3-containing GABA(A) receptors play a role in anxiety whereas the alpha1 subtype is involved in sedation, raising the possibility of a compound that selectively modulates alpha2- and/or alpha3-containing receptors but does not affect alpha1-containing receptors would be a non-sedating anxiolytic. (hhs.gov)
Accordingly, Prazosin is a selective inhibitor of the alpha1 subtype of alpha adrenergic receptors. (pharmacycode.com)

Thus, while cardiac muscarinic receptors are coded for by a single mRNA and are therefore genetically homogeneous, the resulting receptor protein might behave like a mixture of receptor subtypes in intact tissues due to the influence of intracellular factors on receptor conformation. (nih.gov)
A pharmacological profile of the methylenedioxy-substituted amphetamine derivatives indicates that MDMA and MDA exhibited highest affinity for serotonin uptake sites, 5-HT2 serotonin, alpha 2-adrenergic and M-1 muscarinic receptors. (erowid.org)
Tiotropium is structurally related to ipratropium bromide (Figure 2), but it has a significantly higher affinity for muscarinic receptors (Haddad et al. (wanderluce.com)

The results of the study demonstrated that silodosin binds with high affinity to the alpha-1A subtype. (globalrph.com)
This radioligand rapidly reaches equilibrium (10-15 min at 37C) and binds with high affinity to both human (K d = 0.06 ± 0.01 nM) and rat (K d = 0.2 ± 0.02 nM) D3 receptors expressed in HEK293 cells. (elsevierpure.com)
For mGluR5 the reference antagonist MPEP binds with high affinity to the receptor (binding IC50 13.8nM), which confirmed earlier findings from Anderson et al. (uni-frankfurt.de)

So the molecule is very potent and highly selective. (ub.edu)
Used together, these outcomes show that BIIE0246 is certainly an extremely potent, high affinity antagonist selective for the Y2 receptor subtype. (phytid.org)
For the mGluR1 assay the potent antagonist EMQMCM exhibited high affinity towards the binding site (Ki ~3nM), which is in accordance with published data from Mabire et al. (uni-frankfurt.de)

According to molecular biological and pharmacological criteria, rat heart membranes normally express only one muscarinic receptor subtype. (nih.gov)
However, the advent of molecular genetic and pharmacological approaches has begun to delineate which GABA(A) receptor subtypes are associated with the various pharmacological effects of the non-selective BZs. (hhs.gov)
This review will focus on the description of selective and non-selective allosteric modulators of Sig1R, including molecular structure properties and pharmacological activity both in vitro and in vivo , with the aim of providing the latest overview from compound discovery approaches to eventual clinical applications. (frontiersin.org)
To get more information about the pharmacological dopaminergic properties of 77-LH-28-1, this compound was evaluated for its affinity at dopamine D2-like receptor subtypes by radioligand binding assays. (unicam.it)
There is pharmacological evidence for subtypes of each receptor and other types of novel, less well-characterised opioid receptors, e , l , i , z , have also been postulated. (opioids.wiki)

12 Each radioligand appeared to bind to the same very high affinity site ( m 1 ) as well as to the appropriate high affinity site ( m , d or k ) depending on the radioligand used. (opioids.wiki)
In this study, [ 3 H]-labeled LS-3-134 was prepared and evaluated to further characterize its use as a D3 dopamine receptor selective radioligand. (elsevierpure.com)
Based upon these studies, we propose that [ 3 H]LS-3-134 represents a novel D3 dopamine receptor selective radioligand that can be used for studying the expression and regulation of the D3 dopamine receptor subtype. (elsevierpure.com)

Inhibition of cell proliferation by the somatostatin analogue RC-160 is mediated by somatostatin receptor subtypes SSTR2 and SSTR5 through different mechanisms. (uchicago.edu)
Gi alpha 1 selectively couples somatostatin receptor subtype 3 to adenylyl cyclase: identification of the functional domains of this alpha subunit necessary for mediating the inhibition by somatostatin of cAMP formation. (uchicago.edu)
The inhibition of different subtypes of calcium channels by DW13.3 reflects a common "macro" binding site present on all calcium channels except T-type. (aspetjournals.org)
3 The existence of the d -receptor was subsequently proposed to explain the profile of activity in vitro of the enkephalins (the first endogenous opioid peptides), and on the basis of the relative potency of the non-selective opioid antagonist naloxone to reverse endogenous opioid peptide inhibition of the nerve-evoked contractions of the mouse vas deferens. (opioids.wiki)

Both analogues exhibit selective high affinity for SRIF receptor subtype 2 (SSTR2). (endocrine-abstracts.org)
Immunological detection of isoforms of the somatostatin receptor subtype, SSTR2. (uchicago.edu)
Gi alpha 3 and G(o) alpha selectively associate with the cloned somatostatin receptor subtype SSTR2. (uchicago.edu)

First, it has high affinity: only a small amount of compound is needed to achieve a very large effect on metabotropic glutamate receptors (mGluR). (ub.edu)

In the several subtypes of adenosine receptors, especially, adenosine 2A receptors (A 2A Rs) are involved in neurodegenerative conditions. (simulations-plus.com)
All four adenosine receptor subtypes (A 1 , A 2A , A 2B , and A 3 ) are G protein-coupled receptors (GPCRs), either increasing or decreasing intracellular cAMP levels by affecting adenylate cyclase activity. (turkupetcentre.net)
Adenosine has the highest affinity to the A 1 R and A 2A R, intermediate affinity to A 3 R, and lowest affinity to A 2B R. Adenosine activates A 1 and A 2A receptors already in nanomolar concentrations. (turkupetcentre.net)

Ring-substituted psychoactive derivatives of amphetamine exhibited high affinities for a number of serotonin recognition sites. (erowid.org)
Derivatives of 2,5-DMA exhibited preferential high affinity at 5-HT2 serotonin receptors when compared to their relative affinities at 5-HT1 serotonin receptors. (erowid.org)
There were significant correlations between the in vitro affinities of 2,5-DMA derivatives at 5-HT2 serotonin receptors and their human hallucinogenic potencies as well as with their potencies in behavioral generalization studies, suggesting the importance of 5-HT2 serotonin receptors in mediating the hallucinogenic effects of the various 2,5-DMA derivatives. (erowid.org)
Naratriptan has a high affinity for 5-HT1b and 5-HT1d subtypes of human serotonin 5-HT1 receptors. (unitedpharmacies-uk.md)
It has little or no effect on other subtypes of serotonin 5-HT receptors (5-HT2, 5-HT3, 5-HT4, and 5-HT7). (unitedpharmacies-uk.md)

An in vitro study examining binding affinity of silodosin to the three subtypes of the alpha-1 adrenoreceptors (alpha-1A, alpha-1B, and alpha-1D) was conducted. (globalrph.com)

Although block occurred in a similar 1:1 manner for all subtypes, DW13.3 produced a partial block of both α1A currents and P-type currents in cerebellar Purkinje cells. (aspetjournals.org)

The highest concentrations of MT3 sites (putative m4 receptors) in the rat brain were found in striatum and olfactory tubercle, intermediate concentration in dentate gyrus and CA1, and lower but still conspicuous levels in CA3 and frontal cortex. (pasteur.fr)

Islet cells commonly are referred to as APUD cells, a name derived from their high amine content and capacity for amine precursor uptake with decarboxylation. (medscape.com)

Owing to the reactivity, the selective synthesis of aldehydic is a challenging task. (tuwien.ac.at)

However, animals treated with diazepam do have a transient ataxia at higher doses. (hhs.gov)
Various preclinical studies have investigated the effect of CBD on feeding behaviour in rodents [58, 93, 155,159,195], with results suggesting that higher doses may influence food intake several hours post-treatment. (researchgate.net)
Wistar rats) [155], failed to influence food intake during a 1 h ad libitum feeding period, moderate to high doses of CBD (4.4 mg·kg −1 , i.p. [58]. (researchgate.net)

BIIE0246, a newly synthesized non-peptide neuropeptide Y (NPY) Y2 receptor antagonist, could contend with high affinity (8 to 15?nM) for particular [125I]PYY3C36 binding sites in HEK293 cells transfected using the rat Con2 receptor cDNA, and in rat human brain and individual frontal cortex membrane homogenates. (phytid.org)
Nevertheless, few areas specifically in the hippocampal development, also exposed the presence of a little but significant percentage of [125I]PYY3C36/BIIE0246-insensitive sites probably from the Y5 subtype (Dumont bioassays. (phytid.org)
Telmisartan with a very high affinity displaces angiotensin II from its binding sites in the AT1 receptor subtype, which are responsible for the known action of angiotensin II. (bestpharmbuy.com)
The highest incidence rates were 1.49 per 100,000 in the lung, 3.56 per 100,000 in gastroenteropancreatic sites, and 0.84 per 100,000 in unknown primary sites. (medscape.com)

In concert with chronic visceral pain, there is a high comorbidity with stress-related psychiatric disorders including anxiety and depression. (frontiersin.org)

On the other hand, BIIE0246 acted like a powerful antagonist in the rat vas deferens and doggie saphenous vein, two prototypical Y2 bioassays (Pheng bioassays, we've also proven that BIIE0246 can stop the activation from the Y2 receptor 22338-71-2 supplier subtype without impacting the actions of NPY or its homologues in the Y1 and Y4 receptors. (phytid.org)
Passing the baton at high speed: time to hand over to a new editorial board. (jci.org)

Of the eight subtypes of mGluR receptors, it is specific to mGlu5. (ub.edu)
Telsartan® is an effective and specific (selective) antagonist of angiotensin II receptors (type AT1) for oral administration. (bestpharmbuy.com)

fBB 4 -R expression in cells widely used for other Bn receptor subtypes was unsuccessful as was expression in two frog cell lines. (acs.org)

Feature papers represent the most advanced research with significant potential for high impact in the field. (mdpi.com)

Flagship machine learning platform for ADMET modeling with extended capabilities for data analysis, metabolism prediction, high-throughput pharmacokinetic simulation (HTPK), and AI-driven drug design. (simulations-plus.com)

Silodosin is a selective antagonist of post-synaptic alpha-1 adrenoreceptors, which are located in the human prostate, bladder base, bladder neck, prostatic capsule, and prostatic urethra. (globalrph.com)
PET radiopharmaceuticals for each AR subtype have also been developed, although only radiopharmaceuticals for A 1 R and A 2A R are routinely used in human studies. (turkupetcentre.net)

Approximately 30% of the receptors bind pirenzepine with high affinity and AF-DX 116 with low affinity. (nih.gov)
The total excretion in the urine is less than 2% of the dose.The overall plasma clearance is high (approximately 900 ml / min) compared with the "hepatic" blood flow (approximately 1500 ml / min). (bestpharmbuy.com)

Cloned somatostatin receptors: identification of subtype-selective peptides and demonstration of high affinity binding of linear peptides. (uchicago.edu)

Cadieux bioassays Open up in another window Discussion We've exhibited that BIIE0246 offers high affinity for the Y2 receptor subtype while becoming inactive in the Y1, Y4 and Y5 subtypes in HEK 293 cells transfected using the particular receptor cDNA. (phytid.org)
No agonistic or antagonistic actions of BIIE0246 had been seen in isolated INHA cells where NPY-induced results are mediated from the activation from the Y1 and Y4 receptor subtypes. (phytid.org)

In some patients, the higher morning blood levels following use of the 12.5 mg dose increase the risk of next day impairment of driving and other activities that require full alertness [see Warnings and Precautions (5.1) ]. (drugs-library.com)

RAPAFLO is the brand name for silodosin, a selective antagonist of alpha-1 adrenoreceptors. (globalrph.com)

GH and TSH secretion are regulated by SSTR subtypes 2 & 5, with an additional effect on GH secretion via SSTR1. (endocrine-abstracts.org)

The A 1 R is expressed throughout in the body, with the highest densities in the brain . (turkupetcentre.net)
Receptor density is high in the striatum and thalamus, moderate in the cerebral cortex and pons, and low in the cerebellum, midbrain and brain stem. (turkupetcentre.net)

Anatomy19

Organisms22

Diseases1

Chemicals and Drugs116

Analytical, Diagnostic and Therapeutic Techniques and Equipment34

Phenomena and Processes64

Disciplines and Occupations2

Technology, Industry, Agriculture1

Information Science5

Health Care1

Ligand8

Antagonists9

Selectivity6

Compounds13

Agonists6

Dopamine receptor subtypes2

Agonist6

Ligands3

Alpha1 subtype2

Muscarinic receptors3

Binds3

Potent3

Pharmacological5

Radioligand3

Inhibition4

SSTR23

Metabotropic glutamate1

Adenosine3

Serotonin5

Vitro1

Partial1

Concentrations1

Uptake1

Synthesis1

Doses3

Sites4

Anxiety1

Hand2

Specific2

Expression1

Significant1

Metabolism1

Human2

Approximately2

Identification1

Cells2

Full1

Alpha1

Effect1

Brain2