• The present study aimed to clarify the role of NKB-neurokinin 3 receptor (NK3R) signaling in the pulsatile pattern of GnRH/gonadotropin secretion in postpartum lactating cattle.We examined the effects of the administration of an NK3R-selective agonist, senktide, on gonadotropin secretion in lactating cattle. (bioone.org)
  • Orexin 2 Receptor Agonist is a potent selective OX2R agonist with an EC 50 of 23 nM. (medchemexpress.com)
  • Design and Synthesis of Non-Peptide, Selective Orexin Receptor 2 Agonists. (medchemexpress.com)
  • A selective novel KOP receptor agonist emerged as a notable result and is proposed as a new chemotype for the study of the KOP receptor in the etiology of drug addiction, depression, and/or pain. (acs.org)
  • Salvinorin (Sal) A is a naturally occurring, selective kappa opioid receptor (KOPR) agonist with a short duration of action in vivo. (erowid.org)
  • We set out to examine the pattern of cortico-basal ganglia oscillations induced by selective agonists of D1 and D2 receptors in a rat model of LID. (lu.se)
  • Selective agonists targeting these receptors, such as triptans and ditans, are effective in aborting acute migraine attacks and inhibit the in vivo release of calcitonin gene-related peptide (CGRP) in human and animal models. (lu.se)
  • The 5-HT 1B and 5-HT 1D receptor antagonist, GR127935, could reverse the inhibitory effect of Lasmiditan (a selective 5-HT 1F receptor agonist) on CGRP release in the soma-rich TG but not in soma-poor TG or dura mater. (lu.se)
  • To combine these properties with the application of boron neutron capture therapy (BNCT), we design and synthesize a potent VDR agonist based on the skeleton of the hormone 1α,25-dihydroxyvitamin D 3 (1,25D) and an o -carborane (dicarba- o-closo -1,2-dodecaborane) at the end of its side chain. (nih.gov)
  • In Chinese hamster ovary cells stably expressing KOPR, all three kappa agonists internalized or down-regulated KOPR to similar extents, with MOM-Sal B being the most potent. (erowid.org)
  • In summary, MOM-Sal B is a potent and efficacious KOPR agonist with longer lasting in vivo effects than Sal A. (erowid.org)
  • The naturally occurring B1 agonist Lys-des-Arg9-BK was more potent than des-Arg9-BK in the in vivo model, but the effect of either natural sequence was brief. (aspetjournals.org)
  • Alchemedicine Inc. has prepared and tested new angiotensin AT1 receptor (AGTR1) antagonists reported to be useful for the treatment of cancer, hypertension, glaucoma and renal disorders. (bioworld.com)
  • Values for the control samples were obtained without addition of receptor antagonists. (avma.org)
  • There are new developments, which are small molecules that are antagonists at the calcitonin gene-related peptide (CGRP) receptor. (medscape.com)
  • In order to confirm the participation of the adenosine A2A receptor in the effects mediated by PDRN, 8 mg/kg 7-dimethyl-1-propargylxanthine (DMPX), adenosine A2A receptor antagonist, was treated with PDRN. (iasp-pain.org)
  • DR=EC 50 with the addition of various concentrations of receptor antagonist)/EC 50 without the addition of a receptor antagonist. (avma.org)
  • These findings may be explained by the existence of discrete agonist and antagonist states of the alpha receptor, which preferentially bind [ 3 H]clonidine and [ 3 H]WB-4101, respectively. (aspetjournals.org)
  • BACKGROUND: Nicotine receptor partial agonists may help people to stop smoking by a combination of maintaining moderate levels of dopamine to counteract withdrawal symptoms (acting as an agonist) and reducing smoking satisfaction (acting as an antagonist). (who.int)
  • The incretin system: glucagon-like peptide-1 receptor agonists and dipeptidyl peptidase-4 inhibitors in type 2 diabetes. (medscape.org)
  • We performed this meta-analysis to evaluate the efficacy and safety of glucagon-like peptide-1 receptor-agonists (GLP-1RA) treatment on cardio-metabolic parameters among antipsychotic-treated patients with schizophrenia. (frontiersin.org)
  • SEARCH STRATEGY: We searched the Cochrane Tobacco Addiction Group's specialised register for trials, using the terms ('varenicline' or 'cytisine' or 'Tabex' or 'nicotine receptor partial agonist') and 'smoking' in the title or abstract, or as keywords. (who.int)
  • Allosteric conversion of partial to full agonism may be a general mechanism for reversibly scaling the efficacy of GABA A receptors to endogenous partial agonists. (jneurosci.org)
  • Although the physiological relevance of endogenous partial agonists remains poorly understood, the possibility of reversible augmentation of partial agonist efficacy by endogenous modulators raises the interesting possibility of plasticity at the level of agonist-dependent gating. (jneurosci.org)
  • Heat-stable enterotoxin peptides (ST's) are expressed by enterotoxigenic strains of bacteria in order to co-opt an endogenous ligand-receptor system that regulates fluid homeostasis within the gut. (umsystem.edu)
  • Allianthera (Suzhou) Biopharmaceutical Co. Ltd. has patented new aryl hydrocarbon receptor (AhR) agonists reported to be useful for the treatment of cancer, lung diseases, bone, dermatological, eye, gastrointestinal, neurological and pancreatic disorders, among others. (bioworld.com)
  • Aryl Hydrocarbon Receptor Agonists " has 5 results in Products. (rndsystems.com)
  • The central hypothesis underlying this proposal is that drugs targeting CNS nicotinic acetylcholine receptors (nAChRs) may be of therapeutic value for the treatment of levodopa-induced dyskinesias in Parkinson's disease. (michaeljfox.org)
  • Though the mechanisms mediating these metabolic effects are uncertain, the data suggest that β3 agonists could have therapeutic utility in disorders of glucose homeostasis. (jci.org)
  • The studies proposed in this project will test the hypotheses that in the non-human primate 1 the functions and behavioral effects of the NOP receptor are independent of classical opioid receptors, 2 activation of the NOP receptor produces strong antinociception without abuse liability, and 3 NOP receptor agonists possess a promising therapeutic profile as analgesics compared to mu opioids following repeated administration in primates. (dtic.mil)
  • Second, intrathecal administration of NOFQ produced antinociception without eliciting itchscratching responses, indicating that NOP receptor agonists represent a therapeutic target as spinal analgesics. (dtic.mil)
  • Indeed, the therapeutic possibilities of orexin agonists extend well beyond NT1 into other rare primary hypersomnia disorders, such as narcolepsy type 2 and idiopathic hypersomnia, and into a broad range of additional indications characterized by excessive daytime sleepiness. (sleepreviewmag.com)
  • Adenosine A2A receptor agonist polydeoxyribonucleotide ameliorates short-term memory impairment by suppressing cerebral ischemia-induced inflammation via MAPK pathway. (iasp-pain.org)
  • Adenosine A2A receptor agonist, polydeoxyribonucleotide (PDRN), suppresses the secretion of pro-inflammatory cytokines and exhibits anti-inflammatory effect. (iasp-pain.org)
  • In this free pharmacology continuing education course, Eryn Bryant, RN, MS, ANP discusses the use of GLP-1 Receptor Agonists (GLP-1 RAs) in clinical practice. (pcna.net)
  • Pieri L, Pieri M, Haefely W. "LSD as an agonist dopamine receptors in the striatum" Nature . (erowid.org)
  • It will also help determine whether nicotine and/or nicotinic agonists are of benefit in the treatment of dyskinesias that occur with levodopa treatment for Parkinson's disease. (michaeljfox.org)
  • Benzodiazepine receptor agonists are the mainstay in treatment of insomnia. (medscape.com)
  • Zolpidem binds at a benzodiazepine receptor subtype (omega I). This receptor is found more in the central nervous system (CNS) than in the peripheral nervous system, which helps to account for the drug's hypnotic effect without significant muscle-relaxant properties. (medscape.com)
  • It interacts with the GABA-benzodiazepine receptor complex, causing sedation. (medscape.com)
  • The umbrella term for benzodiazepines and benzodiazepine-like drugs is 'benzodiazepine receptor agonists', which have similar benefits, side effects and risks. (findings.org.uk)
  • Predictive Models to Identify Small Molecule Activators and Inhibitors of Opioid Receptors. (acs.org)
  • The European Medicines Agency (EMA) announced on July 11, 2023 that its Pharmacovigilance Risk Assessment Committee (PRAC) is reviewing data on glucagon-like peptide-1 (GLP-1) receptor agonists, which are used to treat type 2 diabetes and weight loss, after reports were received of suicidal thoughts in patients taking the drug. (pharmtech.com)
  • Objective To determine whether treatment with agonists of glucagon-like peptide-1 receptor (GLP-1R) result in weight loss in overweight or obese patients with or without type 2 diabetes mellitus. (bmj.com)
  • Conclusions The present review provides evidence that treatment with GLP-1R agonists leads to weight loss in overweight or obese patients with or without type 2 diabetes mellitus. (bmj.com)
  • BOSTON - A novel oral formulation of a glucagonlike peptide-1 (GLP-1) receptor agonist has shown "robust" dose-dependent glucose lowering and weight reductions in patients with early type 2 diabetes in a phase 2 study. (medscape.com)
  • We therefore propose to test the effect of nAChR agonists that preferentially stimulate brain nAChRs and not those in the peripheral nervous system. (michaeljfox.org)
  • We suggest that neurosteroids preferentially enhance low-efficacy GABA A receptor activity independent of subunit composition. (jneurosci.org)
  • Although GABA activates synaptic (αβγ) GABA A receptors with high efficacy, partial agonist activation of αβγ isoforms and GABA activation of the primary extrasynaptic (αβδ) GABA A receptors are limited to low-efficacy activity, characterized by minimal desensitization and brief openings. (jneurosci.org)
  • Partial agonist ergot alkaloids display similar affinities for the binding sites of both [ 3 H]ligands. (aspetjournals.org)
  • Varenicline was developed as a nicotine receptor partial agonist from cytisine, a drug widely used in central and eastern Europe for smoking cessation. (who.int)
  • OBJECTIVES: The primary objective of this review is to assess the efficacy and tolerability of nicotine receptor partial agonists, including varenicline and cytisine, for smoking cessation. (who.int)
  • Furthermore, Lasmiditan works as a partial agonist on 5-HT 1B/1D receptors in clinically relevant dose regiments. (lu.se)
  • Vasopressin V2 Receptor (V2R) Agonist - Pipeline Insight, 2022" report by the publisher offers comprehensive insights of the pipeline (under development) therapeutics scenario and growth prospects across Vasopressin V2 Receptor (V2R) Agonist development. (researchandmarkets.com)
  • Orexin 2 Receptor Agonist replaces Orexin-A to bind to hOX1R and hOX2R in a concentration-dependent manner in CHO cells overexpressing hOX1R and HEK-293 cells overexpressing hOX2R with K i values of 0.14 μM and 0.77 μM, respectively [1] . (medchemexpress.com)
  • The collaboration represents the first time Schrödinger's technology will be applied in an orexin agonist setting at scale. (sleepreviewmag.com)
  • While prevailing treatment approaches only address the symptoms associated with narcolepsy type 1 (NT1), we believe orexin agonists offer a disruptive approach, with the capacity to address the underlying pathology of the disorder. (sleepreviewmag.com)
  • We are committed to exploring the full potential of orexin agonists to help patients across a wide range of indications," says Mario Alberto Accardi, PhD, Orexia CEO, in a release. (sleepreviewmag.com)
  • Repeated exposure to drugs of abuse and stress increase dynorphin, a kappa opioid receptor (KOR) ligand, in the nucleus accumbens (NAc). (erowid.org)
  • Kappa-opioid (KOP) receptor agonists exhibit analgesic effects without activating reward pathways. (acs.org)
  • Third, NOP receptor agonists produced antinociceptive effects comparable to clinically used mu opioids such as morphine and alfentanil in three different primate pain models, indicating that the analgesic effectiveness of NOP receptor agonists may be similar to that of mu opioid analgesics in humans. (dtic.mil)
  • Many commonly used sedative and anxiolytic drugs that affect the GABA receptor complex are not agonists. (wikipedia.org)
  • These drugs act instead as positive allosteric modulators (PAMs) and while they do bind to the GABA receptors, they bind to an allosteric site on the receptor and cannot induce a response from the neuron without an actual agonist being present. (wikipedia.org)
  • Drugs that fall into this class exert their pharmacodynamic action by increasing the effects that an agonist has when potentiation is achieved. (wikipedia.org)
  • These drugs bind to a special benzodiazepine site on the gamma-aminobutyric acid (GABA) receptor complex, enhancing the activity of this neurotransmitter. (medscape.com)
  • Why don't we move on now to the thrombopoietin receptor agonists [TPO-RA], which is a large class of drugs with now a broad experience. (onclive.com)
  • The present ligand is the first secosteroidal analog with the carborane unit that efficiently binds to VDR and functions as an agonist with 1,25D-like potency in transcriptional assay on vitamin D target genes. (nih.gov)
  • We have generated the peptide GENDWDWCCELCCNPACFGC both with and without an N-terminal DOTA chelating moiety and characterized its receptor binding affinity and ability to stimulate cGMP production in comparison to other peptides in this class. (umsystem.edu)
  • Our findings indicate that the Yersinia peptide possesses receptor binding affinity and cyclase stimulating activity intermediate between known E. coli ST analogs and human uroguanylin. (umsystem.edu)
  • BACKGROUND Mirabegron is a β3-adrenergic receptor (β3-AR) agonist approved only for the treatment of overactive bladder. (jci.org)
  • Encouraging preclinical results suggest that β3-AR agonists could also improve obesity-related metabolic disease by increasing brown adipose tissue (BAT) thermogenesis, white adipose tissue (WAT) lipolysis, and insulin sensitivity.METHODS We treated 14 healthy women of diverse ethnicities (27.5 ± 1.1 years of age, BMI of 25.4 ± 1.2 kg/m2) with 100 mg mirabegron (Myrbetriq extended-release tablet, Astellas Pharma) for 4 weeks in an open-label study. (jci.org)
  • report that chronic administration of the approved β3 agonist mirabegron to human subjects was without effect on body weight or fat mass, but improved several measures of glucose homeostasis. (jci.org)
  • Synergistic activation of estrogen receptor with combinations of environmental chemicals. (cdc.gov)
  • A GABA receptor agonist is a drug that is an agonist for one or more of the GABA receptors, producing typically sedative effects, and may also cause other effects such as anxiolytic, anticonvulsant, and muscle relaxant effects. (wikipedia.org)
  • The two receptors GABA-α and GABA-ρ are ion channels that are permeable to chloride ions which reduces neuronal excitability. (wikipedia.org)
  • The GABA-β receptor belongs to the class of G-Protein coupled receptors that inhibit adenylyl cyclase, therefore leading to decreased cyclic adenosine monophosphate (cAMP). (wikipedia.org)
  • GABA-α and GABA-ρ receptors produce sedative and hypnotic effects and have anti-convulsion properties. (wikipedia.org)
  • GABA-β receptors also produce sedative effects. (wikipedia.org)
  • General anaesthetics act primarily as PAMs of GABA-A receptor. (wikipedia.org)
  • Positive allosteric modulators work by increasing the frequency with which the chloride channel opens when an agonist binds to its own site on the GABA receptor. (wikipedia.org)
  • However, some general anaesthetics like propofol and high doses of barbiturates may not only be positive allosteric modulators of GABA-A receptors but also direct agonists of these receptors. (wikipedia.org)
  • Alcohol is an indirect GABA agonist. (wikipedia.org)
  • Alcohol is believed to mimic GABA's effect in the brain, binding to GABA receptors and inhibiting neuronal signaling. (wikipedia.org)
  • Many GABA A receptor modulators exhibit clear subunit selectivity ( Olsen and Macdonald, 2002 ). (jneurosci.org)
  • It is even more intriguing to consider the potential plasticity of allosteric modulation given the observation of agonist-dependent functional properties of GABA A receptors. (jneurosci.org)
  • We have now 5 years' experience with the monoclonal antibodies against CGRP or the CGRP receptor like eptinezumab, erenumab , fremanezumab , and galcanezumab . (medscape.com)
  • The functional role of these receptors was examined ex vivo with a capsaicin/potassium induced 5-HT and CGRP release. (lu.se)
  • None of the 5-HT 1 receptors co-localized with CGRP-ir in C-fibres. (lu.se)
  • Characterization of dendritic cells generated in vivo by an E. coli derived chimeric dual receptor agonist. (medscimonit.com)
  • The present study was performed using an established in vivo model of B1 receptor-mediated cardiovascular action. (aspetjournals.org)
  • The functional profiles of spinal NOP receptors are different between primates and rodents. (dtic.mil)
  • Additionally, the D1 agonist induced strong functional connectivity between the recorded structures and the phase analysis revealed that the primary motor cortex (forelimb area) was leading a supplementary motor area and striatum. (lu.se)
  • The study aimed to examine the localization, genetic expression and functional aspects of 5- HT 1B/1D/1F receptors in the trigeminal system in order to further understand the molecular sites of action of triptans (5-HT 1B/1D ) and ditans (5-HT 1F ). (lu.se)
  • The proposed studies represent a new research direction for the treatment of levodopa-induced dyskinesias using nicotine or nicotinic receptor agonists. (michaeljfox.org)
  • Following treatment with the D2 agonist, narrowband gamma oscillations were detected only in forelimb motor cortex and dorsolateral striatum, while prominent oscillations in the theta band occurred in the globus pallidus and nigra reticulata. (lu.se)
  • We used intracranial self-stimulation (ICSS), a method that provides a behavioral index of reward sensitivity, to measure the effects of repeated administration of the KOR agonist salvinorin A (salvA) (2 mg/kg) on the reward-potentiating effects of cocaine (5.0 mg/kg). (erowid.org)
  • Dr. Quik found that the targeted nAChR agonist varenicline resulted in significant declines in levodopa-induced AIMs at a relatively low dose of the agonist, with no worsening of parkinsonism. (michaeljfox.org)
  • Learn about GLP-1 Receptor Agonists (GLP-1 RAs) in clinical practice and the cardiovascular and heart failure outcomes associated with this important hormone. (pcna.net)
  • Assessing indoor dust interference with human nuclear hormone receptors in cell-based luciferase reporter assays. (cdc.gov)
  • Dr. Quik is currently doing further work to identify the optimal agonists for reducing dyskinesias. (michaeljfox.org)
  • Might β3-adrenergic receptor agonists be useful in disorders of glucose homeostasis? (jci.org)
  • Usage information: Might β3-adrenergic receptor agonists be useful in disorders of glucose homeostasis? (jci.org)
  • Glucagon-like peptide 1 receptor (or GLP-1R) agonists are a frontline treatment for diabetes - improving glycaemic control by reducing glucose concentrations in the blood. (cureparkinsons.org.uk)
  • In the overall analysis, GLP-1R agonists had beneficial effects on systolic and diastolic blood pressure, plasma concentrations of cholesterol, and glycaemic control, but did not have a significant effect on plasma concentrations of liver enzymes. (bmj.com)
  • Although dexamethasone and terbutaline also caused significant changes in development of beta-receptor binding capabilities, in neither tissue could these effects account for the direction or magnitude of the changes in adenylate cyclase reactivity. (rti.org)
  • Hypotensive effects of Lys-des-Arg9-bradykinin and metabolically protected agonists of B1 receptors for kinins. (aspetjournals.org)
  • Concentration of cAMP in equine neutrophils induced by 5 adenosine A 2A receptor agonists (A) and effects of ZM241385 and MRS1706 on ATL313-induced accumulation of cAMP (B). Each point represents the mean ± SEM of 3 replicates. (avma.org)
  • Our results reveal that the dyskinetic effects of D1 and D2 receptor agonists are associated with distinct patterns of cortico-basal ganglia oscillations, suggesting a recruitment of partially distinct networks. (lu.se)
  • 1994. Ah receptor in embryonic mouse palate and effects of TCDD on receptor expression. (cdc.gov)
  • αβγ) of neurosteroid modulation could be reversed by conditions that reversed isoform-specific activity modes, including the use of β-alanine to achieve increased efficacy with αβδ receptors and taurine to render αβγ receptors low efficacy. (jneurosci.org)
  • In the current study, rats were exposed to dexamethasone or terbutaline during late gestation and the development of beta-receptor binding capabilities and adenylate cyclase activity evaluated in membrane preparations from kidney and lung. (rti.org)
  • Abnormal involuntary movements were elicited by the D1 agonist SKF82958 or the D2 agonist sumanirole, while overall motor activity was quantified using video analysis (DeepLabCut). (lu.se)
  • The 5-HT 1D receptor co-localized with receptor activity-modifying protein 1 (RAMP1) in Aδ-fibres in the TG, while 5-HT 1B -ir was weakly expressed and 5-HT 1F -ir was not detected in these fibres. (lu.se)
  • In today's post, we will discuss what GLP-1R agonists are, what has previously been done with them in Parkinson's, and what the new report found. (cureparkinsons.org.uk)
  • In conclusion, the present study lends support to the idea that stimulation of CB2 receptors ameliorates several altered parameters in Alzheimer's disease such as impaired memory and learning, neuroinflammation, oxidative stress damage and oxidative stress responses, selected tau kinases, and tau hyperphosphorylation around plaques. (nih.gov)
  • Glucorticoids and adrenergic stimulation are both thought to control the development of beta-adrenergic receptors/responses. (rti.org)
  • E. coli derived chimeric receptor agonists such as ProGP-4 may enable further investigations of immunotherapeutic approaches to the treatment of diseases such as cancer and autoimmunity. (medscimonit.com)
  • The collaboration will be enabled by Orexia's structural biology capabilities, including the stabilized OX2R StaR protein exclusively licensed from Sosei Heptares, and high-resolution crystal structures in agonist conformation. (sleepreviewmag.com)
  • Orexia's utilization of OX2R stabilized receptors (StaR technology) provides the foundation for R&D which could significantly benefit patients with NT1. (sleepreviewmag.com)
  • The unusual sensitivity of αβδ receptor channels to neurosteroid modulation prompted investigation of whether this high sensitivity was dependent on the δ subunit or the low-efficacy channel function that it confers. (jneurosci.org)
  • RESULTS: Administration of this dual receptor agonist to mice resulted in dose-dependent increases in the numbers of total white blood cells and Class II+/CD11c+ cells in spleen and peripheral blood. (medscimonit.com)
  • The specific CB2 cannabinoid receptor agonist JWH-133 induced cognitive improvement in double AβPP/PS1 transgenic mice, a genetic model of Alzheimer's disease. (nih.gov)
  • Background: 5-Hydroxytryptamine (5-HT) receptors 1B, 1D and 1F have key roles in migraine pharmacotherapy. (lu.se)
  • Rabbits pretreated with bacterial lipopolysaccharide (LPS) (25 micrograms/kg) and anesthetized 5 h later exhibit acute and transient hypotension in response to intra-arterial boluses of B1 receptor agonists. (aspetjournals.org)
  • Shared insight on thrombopoietin receptor agonist (TPO-RA) use in the pediatric setting of immune thrombocytopenia management. (onclive.com)
  • BACKGROUND: Progenipoietin-4 (ProGP-4) is an E. coli derived chimeric growth factor that activates the human Flt3 and G-CSF receptors. (medscimonit.com)
  • Computational Interspecies Translation Between Alzheimer's Disease Mouse Models and Human Subjects Identifies Innate Immune Complement, TYROBP, and TAM Receptor Agonist Signatures, Distinct From Influences of Aging. (bvsalud.org)
  • Ghrelin Receptor Agonists " has 4 results in Products. (rndsystems.com)
  • Results are reported as the percentage of radioligand binding without addition of an agonist. (avma.org)
  • Cardioprotective and vasodilatory actions of glucagon-like peptide 1 receptor are mediated through both glucagon-like peptide 1 receptor-dependent and -independent pathways. (medscape.org)
  • The vitamin D nuclear receptor (VDR) is a potential target for cancer therapy. (nih.gov)