5-Alkoxy-1-aryl-3-polyfluoroalkylpyrazoles with Antinociceptive Activity: Partial Agonists of TRPV1 Ion Channels.
Sign Up to like & getrecommendations! Published in 2023 at "ChemMedChem"
DOI: 10.1002/cmdc.202300063
Abstract: Chemoselective O-alkylation of 1-aryl-3-polyfluoroalkylpyrazol-5-oles under basic conditions resulted in a series of 5-alkoxypyrazoles (26 derivatives). They were showed to have an acceptable ADME profile (in silico). In experiments in vivo (CD-1 mice), it was found… read more here.
Keywords: partial agonists; trpv1 ion; agonists trpv1; aryl polyfluoroalkylpyrazoles ... See more keywords
Discovery research and development history of the dopamine D2 receptor partial agonists, aripiprazole and brexpiprazole
Sign Up to like & getrecommendations! Published in 2021 at "Neuropsychopharmacology Reports"
DOI: 10.1002/npr2.12180
Abstract: Otsuka Pharmaceutical Co., Ltd. successfully developed the first dopamine D2 receptor partial agonist approved for schizophrenia, the antipsychotic aripiprazole (Abilify®). The drug was approved for this indication in the United States in 2002 and has… read more here.
Keywords: receptor partial; disorder; dopamine receptor; partial agonists ... See more keywords
Exploring the binding energy profiles of full agonists, partial agonists, and antagonists of the α7 nicotinic acetylcholine receptor
Sign Up to like & getrecommendations! Published in 2017 at "Journal of Molecular Modeling"
DOI: 10.1007/s00894-017-3419-4
Abstract: Nicotinic acetylcholine receptors (nAChRs) belong to the Cys-loop receptor family and are important drug targets for the treatment of neurological diseases. However, the precise determinants of the binding efficacies of ligands for these receptors are… read more here.
Keywords: energy profiles; binding energy; agonists partial; agonists antagonists ... See more keywords
Dopamine Receptor Partial Agonists for the Treatment of Bipolar Disorder
Sign Up to like & getrecommendations! Published in 2019 at "Drugs"
DOI: 10.1007/s40265-019-01189-8
Abstract: Bipolar disorder is a chronic, disabling, and costly illness with frequent relapses and recurrences, high rates of co-morbid conditions, and poor adherence to treatment. Mood stabilizers and antipsychotics are the cornerstones of treatment. Dopamine receptor… read more here.
Keywords: receptor partial; treatment; partial agonists; bipolar disorder ... See more keywords
Partial agonists go molecular.
Sign Up to like & getrecommendations! Published in 2021 at "Trends in pharmacological sciences"
DOI: 10.1016/j.tips.2021.04.008
Abstract: Single-channel analysis previously revealed a key role for a short-lived 'flipped' state during glycine receptor activation by partial agonists. Structures solved by Yu and colleagues now reveal a surprising mechanism involving a partially activated agonist-bound… read more here.
Keywords: state; partial agonists; agonists molecular;
Truncated (N)-Methanocarba Nucleosides as Partial Agonists at Mouse and Human A3 Adenosine Receptors: Affinity Enhancement by N6-(2-Phenylethyl) Substitution.
Sign Up to like & getrecommendations! Published in 2020 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.0c00235
Abstract: Dopamine-derived N6-substituents, compared to N6-(2-phenylethyl), in truncated (N)-methanocarba (bicyclo[3.1.0]hexyl) adenosines favored high A3 adenosine receptor (AR) affinity/selectivity, e.g., C2-phenylethynyl analogue 15 (MRS7591, Ki = 10.9/17.8 nM, at human/mouse A3AR). 15 was a partial agonist in… read more here.
Keywords: methanocarba nucleosides; nucleosides partial; truncated methanocarba; partial agonists ... See more keywords
Dopamine D3/D2 Receptor Ligands Based on Cariprazine for the Treatment of Psychostimulant Use Disorders That May Be Dual Diagnosed with Affective Disorders.
Sign Up to like & getrecommendations! Published in 2023 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.2c01624
Abstract: Highly selective dopamine D3 receptor (D3R) partial agonists/antagonists have been developed for the treatment of psychostimulant use disorders (PSUD). However, none have reached the clinic due to insufficient potency/efficacy or potential cardiotoxicity. Cariprazine, an FDA-approved… read more here.
Keywords: partial agonists; dopamine receptor; agonists antagonists; treatment psychostimulant ... See more keywords
Transformation of a Dopamine D2 Receptor Agonist to Partial Agonists as Novel Antipsychotic Agents.
Sign Up to like & getrecommendations! Published in 2023 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.3c00098
Abstract: Designed ligands of G protein-coupled receptors can exert a spectrum of modulating effects, varying from full agonists and partial agonists to antagonists and inverse agonists. For the dopamine D2 receptor (D2R), partial agonist activity is… read more here.
Keywords: partial agonists; dopamine receptor; agonist partial; transformation dopamine ... See more keywords
Toward Understanding the Structural Basis of Partial Agonism at the Dopamine D3 Receptor.
Sign Up to like & getrecommendations! Published in 2017 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.6b01148
Abstract: Both dopamine D3 receptor (D3R) partial agonists and antagonists have been implicated as potential medications for substance use disorders. In contrast to antagonists, partial agonists may cause fewer side effects since they maintain some dopaminergic… read more here.
Keywords: structural basis; basis partial; dopamine receptor; partial agonism ... See more keywords
Neuroprotective potential of adenosine A1 receptor partial agonists in experimental models of cerebral ischemia
Sign Up to like & getrecommendations! Published in 2019 at "Journal of Neurochemistry"
DOI: 10.1111/jnc.14660
Abstract: Cerebral ischemia is the second most common cause of death and a major cause of disability worldwide. Available therapies are based only on anticoagulants or recombinant tissue plasminogen activator. Extracellular adenosine increases during ischemia and… read more here.
Keywords: experimental models; cerebral ischemia; partial agonists; neuroprotective potential ... See more keywords
The position statement of the Working Group of the Polish Psychiatric Association on the use of D2/D3 dopamine receptor partial agonists in special populations.
Sign Up to like & getrecommendations! Published in 2021 at "Psychiatria polska"
DOI: 10.12740/pp/140287
Abstract: D2/D3 dopamine receptor partial agonists (aripiprazole, brexpiprazole, cariprazine) are increasingly often used in the treatment of mental disorders due to a more favourable tolerability profile as compared to other antipsychotics. The article presents the position… read more here.
Keywords: position statement; partial agonists; receptor partial; dopamine receptor ... See more keywords