• His Stereochemistry study combines topics in areas such as Antagonist, Partial agonist, Ring and Alkyl. (research.com)
  • It acts as a histamine H3 receptor antagonist/inverse agonist, which modulates the release of various neurotransmitters in the brain. (musechem.com)
  • The 'neutral' competitive antagonist burimamide alone was without effect but prevented ranitidine actions indicating that inverse agonist effects result from constitutive H(2)R activity independent of HA tone. (ox.ac.uk)
  • Position 5 seems to be responsible for the agonist or inverse agonist behaviour independently of the substituent in position 4', with the exception of the methoxyl group which transforms both full agonists and inverse agonists into neutral antagonists. (nih.gov)
  • LPA GPCR agonists Since the discovery of the three-Edg family of LPA receptors, the development of selective receptor-subtype agonists and antagonists has accelerated. (cckn-ia.org)
  • Among these mGlu receptors, numerous ligands (agonists, antagonists, positive modulators or negative modulators) have been developed for the mGlu2/3 and mGlu5 receptors. (openmedicinalchemistryjournal.com)
  • Selective H(2)R antagonists (inverse agonists) ranitidine and tiotidine enhanced 5-HT release while the agonist amthamine suppressed release. (ox.ac.uk)
  • LXR-like Receptor Inverse Agonists " has 2 results in Products. (rndsystems.com)
  • INDIGO's RAR-related Orphan Receptor Gamma (RORγ) assay kit is an all-inclusive firefly luciferase reporter assay system that includes, in addition to RORγ Reporter Cells, two optimized media for use during cell culture and (optionally) in diluting the test samples, a reference inverse-agonist, Luciferase Detection Reagent, a cell culture-ready assay plate, and a detailed protocol. (stratech.co.uk)
  • Erratum: Discovery of Nanomolar Melanocortin-3 Receptor (MC3R)-Selective Small Molecule Pyrrolidine Bis-Cyclic Guanidine Agonist Compounds Via a High Throughput 'Unbiased' Screening Campaign (J. Med. (umn.edu)
  • Synthesis of LPA derivatives with phosphonate or thiophosphate groups instead of the phosphate group showed receptor-subtype selective Sntb1 activity similar to 1-oleoyl-2-configuration of S1P was demonstrated using the cloned receptors77. (cckn-ia.org)
  • The Pharmacology study combines topics in areas such as Selective receptor modulator, Endocrinology and Internal medicine. (research.com)
  • His primary areas of study are Receptor, Stereochemistry, GABAA receptor, Inverse agonist and Pharmacology. (research.com)
  • His scientific interests lie mostly in Inverse agonist, Receptor, GABAA receptor, Pharmacology and Chemical synthesis. (research.com)
  • To date, several ligands selective for each mGlu receptor have been synthesized, and pharmacological significances of these ligands have been demonstrated in animal models. (openmedicinalchemistryjournal.com)
  • Among them, mGlu2/3 receptor agonists have been proven to be effective for treating schizophrenia and anxiety disorders in clinical studies, which may prove utilities of mGlu receptor ligands for the treatment of psychiatric disorders. (openmedicinalchemistryjournal.com)
  • Pitolisant(CAT: I003332) is a novel and selective nonimidazole inverse agonist at the recombinant human H3 receptor. (musechem.com)
  • 15 However, most compounds that modulate CBI receptor activity have the pharmacological property of inverse agonism which reduces basal CBI receptor signal transduction as well as the activity of blocking CBI agonist dependent receptor stimulation. (allindianpatents.com)
  • A number of selective, centrally acting CBt receptor compounds are currently in development for the treatment of obesity. (allindianpatents.com)
  • Ironically, these chemicals turned out to be selective or non-selective agonists of cloned LPA receptors (see details below). (cckn-ia.org)
  • Compound and pharmaceutical compositions of Forumla by blockade of the CB1 receptors via an inverse agonism mechanism, and are useful for reducing body weight in mammals, cognitive impairment associated with schizophrenia, mitigating treatment emergent weight gain observed during treatment with antipsychotics and have increased bioavailabilty. (allindianpatents.com)
  • High-throughput screening (HTS) of an available chemical library showed that SEW2871 acted as an active heterocyclic S1P1 selective agonist81, 82 and compound 26 was synthesized as a potent 3,5-diphenyl-12,4-oxadiazole S1P1 agonist83. (cckn-ia.org)
  • Using computational modeling, CYM-5442 was developed as an S1P1 selective agonist that was Beta-Lapachone more potent than CYM518185. (cckn-ia.org)
  • Finally, phytosphingosine-1-phosphate was shown to act as a potent and selective agonist on the S1P4 receptor76. (cckn-ia.org)
  • In this work we synthesized 18 biphenylic carboxamides as new CB2-selective ligands and evaluated their pharmacological profiles. (nih.gov)
  • Inhibition of RORγ activity by inverse agonists has been shown to reduce the production of pro-inflammatory cytokines and alleviate disease symptoms in animal models of autoimmune diseases. (stratech.co.uk)
  • In addition to appentency disorders, CBi inverse agonists have been shown to further potentiate the activity of antipsychotic agents in assays. (allindianpatents.com)
  • type":"entrez-protein","attrs":"text":"VPC01091″,"term_id":"1657354296″VPC01091, a cyclized analogue of FTY720, was shown to act as an orally active S1P1 agonist and an S1P3 antagonist87. (cckn-ia.org)
  • the phosphorylated form of KRP-203 was shown to be a selective S1P1 agonist88, 89. (cckn-ia.org)
  • Modification of the FTY720-phosphate structure led to the development of "type":"entrez-protein","attrs":"text":"VPC23019″,"term_id":"1643589982″VPC23019 and "type":"entrez-protein","attrs":"text":"VPC25239″,"term_id":"1668388349″VPC25239 as selective S1P1/S1P3 antagonists95. (cckn-ia.org)
  • In another study, Hauser looked at 321 patients with early stage Parkinson's whose symptoms weren't handled well by a medicine called a dopamine agonist, typically the first drug prescribed for Parkinson's patients. (med-chemist.com)
  • The third category of symptoms includes a number of cognitive abnormalities such as disturbances in selective attention, working memory, executive control, episodic memory, language comprehension, and social-emotional processing. (hindawi.com)
  • Dopamine agonists such as pramipexole and ropinirole can be used as monotherapy to improve symptoms in early disease or as adjuncts to levodopa in patients whose response to levodopa is deteriorating and in those who are experiencing fluctuations in their response to levodopa. (medscape.com)
  • Dopamine agonists are effective as monotherapy in early PD and as adjuncts to levodopa/PDI (peripheral decarboxylase inhibitor) in moderate to advanced disease. (medscape.com)
  • Dopamine agonists directly stimulate postsynaptic dopamine receptors to provide antiparkinsonian benefit. (medscape.com)
  • All available dopamine agonists stimulate D2 receptors, an action that is thought to be clinically beneficial. (medscape.com)
  • Dopamine agonists are effective to treat motor features of early PD, and they cause less development of motor fluctuations and dyskinesia than levodopa. (medscape.com)
  • The clinical definition of multiple system atrophy (MSA) is a progressive, idiopathic, degenerative process beginning in adulthood, manifesting in various degrees of autonomic failure, parkinsonism, cerebellar dysfunction, and pyramidal signs that are poorly responsive to levodopa or dopamine agonists. (medscape.com)
  • Dopamine agonists (ropinirole, pramipexole) provide moderate symptomatic benefit and delay the development of dyskinesia compared with levodopa. (medscape.com)
  • Proactively screen patients receiving oral dopamine agonists for adverse events. (medscape.com)
  • Current projects include optimization of neuropeptide Y Y2 receptor antagonists, orexin-1 receptor antagonists, (GABA) B receptor positive allosteric modulators, neurotensin 1 receptor agonists, a5* nicotinic acetylcholine receptors, positive allosteric modulators, kappa opioid receptor antagonists, and functionally biased mu opioid receptor agonists. (ufl.edu)
  • Global Supplier of Chemical Probes, Inhibitors & Agonists. (probechem.com)
  • Nuclear receptors, PPAR, ROR, and LXRs are involved in this inflammation process and as such we are developing inverse agonists or agonists of those nuclear receptors. (scripps.edu)
  • For patients with motor fluctuations on levodopa/PDI, the addition of a dopamine agonist reduces off time, improves motor function, and allows lower levodopa doses. (medscape.com)
  • Development of a putative Zn2+-chelating but highly selective MMP-13 inhibitor. (ufl.edu)
  • BnOCPA is a potent and powerful analgesic and a highly selective and potent, full agonist at human adenosine A1 receptors (A1Rs) with pEC50 of 7.23 in a NanoBRET agonist binding assay. (probechem.com)
  • DG 172 dihydrochloride is a potent PPAR β / δ inverse agonist (IC 50 = 26.9 nM). (tocris.com)
  • Recently we published the efficacy of a novel PPARγ antagonist (SR1664) and a potent and selective inverse agonist of RORγ (SR2211). (scripps.edu)
  • Both of these agonist are able stimulate cannabinoid signaling, with no preference between the two receptors. (lktlabs.com)
  • AM630, a selective CB2 inverse agonist, activates TRPA1 in sensory neurons. (lktlabs.com)
  • We conclude that phenethylamine and indoleamine hallucinogens may exert their hallucinogenic effect by interacting with 5-HT2A receptors via a Ca2+/CaM-KII-dependent signal transduction pathway as partial agonists and modulating the NMDA receptors-mediated sensory, perceptual, affective and cognitive processes. (neurotransmitter.net)
  • Beltramo M., Stella N., Calignano A., Lin S.Y., Makriyannis A., Piomelli D. (1997) Functional role of high-affinity anandamide transport, as revealed by selective inhibition. (adicciones.es)
  • Synthetic CB2 agonists have been used to study the role of endocannabinoids in neurodegenerative disorders, diabetes, obesity and cancer. (lktlabs.com)
  • Mixed agonists (which interact with both CB1 and CB2) include WIN 55,212-2 and CP 55,940. (lktlabs.com)