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Page 1
Did you mean dopamine agonists (48,355 results)?
Transformation of a Dopamine D(2) Receptor Agonist to Partial Agonists as Novel Antipsychotic Agents.
Liu R, Qi J, Wang H, Fan L, Zhang P, Yu J, Tan L, Wang S, Cheng J. Liu R, et al. J Med Chem. 2023 May 11;66(9):6274-6287. doi: 10.1021/acs.jmedchem.3c00098. Epub 2023 May 2. J Med Chem. 2023. PMID: 37130037
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 D(2) receptor (D(2)R), partial agonist activity is …
Designed ligands of G protein-coupled receptors can exert a spectrum of modulating effects, varying from full agonists and partial …
Dopamine agonist-responsive depression.
Hori H, Kunugi H. Hori H, et al. Psychogeriatrics. 2013 Sep;13(3):189-95. doi: 10.1111/psyg.12014. Psychogeriatrics. 2013. PMID: 25913769 Free article. Review.
Both preclinical and clinical data suggest that adjunctive dopamine agonists could be a promising option for the treatment of such a condition, indicating that there is a dopamine agonist-responsive subgroup of depression. Future clinical studies are w …
Both preclinical and clinical data suggest that adjunctive dopamine agonists could be a promising option for the treatment of …
Dopamine-receptor agonists: mechanisms underlying autoreceptor selectivity. I. Review of the evidence.
Clark D, Hjorth S, Carlsson A. Clark D, et al. J Neural Transm. 1985;62(1-2):1-52. doi: 10.1007/BF01260414. J Neural Transm. 1985. PMID: 3894582 Review.
The behavioural, biochemical, neuroendocrinological and electrophysiological actions of the enantiomers of the dopamine (DA) analogue 3-(3-hydroxyphenyl)-N-n-propylpiperidine, 3-PPP, are extensively reviewed. (+)-3-PPP acts in a fashion similar to classical direct-acting D …
The behavioural, biochemical, neuroendocrinological and electrophysiological actions of the enantiomers of the dopamine (DA) analogue …
In Vitro Comparison of Ulotaront (SEP-363856) and Ralmitaront (RO6889450): Two TAAR1 Agonist Candidate Antipsychotics.
Ågren R, Betari N, Saarinen M, Zeberg H, Svenningsson P, Sahlholm K. Ågren R, et al. Int J Neuropsychopharmacol. 2023 Sep 25;26(9):599-606. doi: 10.1093/ijnp/pyad049. Int J Neuropsychopharmacol. 2023. PMID: 37549917 Free PMC article.
BACKGROUND: Trace amine-associated receptor-1 (TAAR1) agonists have been proposed as potential antipsychotics, with ulotaront and ralmitaront having reached clinical trials. ...Moreover, ralmitaront lacked detectable activity at 5-HT1AR and dopamine D2. CONCLUSIONS: …
BACKGROUND: Trace amine-associated receptor-1 (TAAR1) agonists have been proposed as potential antipsychotics, with ulotaront and ral …
A(3) adenosine receptor agonists containing dopamine moieties for enhanced interspecies affinity.
Tosh DK, Salmaso V, Campbell RG, Rao H, Bitant A, Pottie E, Stove CP, Liu N, Gavrilova O, Gao ZG, Auchampach JA, Jacobson KA. Tosh DK, et al. Eur J Med Chem. 2022 Jan 15;228:113983. doi: 10.1016/j.ejmech.2021.113983. Epub 2021 Nov 19. Eur J Med Chem. 2022. PMID: 34844790 Free PMC article.
Following our study of 4'-truncated (N)-methanocarba-adenosine derivatives that displayed unusually high mouse (m) A(3)AR affinity, we incorporated dopamine-related N(6) substituents in the full agonist 5'-methylamide series. ...Parallel functional assays of G prote …
Following our study of 4'-truncated (N)-methanocarba-adenosine derivatives that displayed unusually high mouse (m) A(3)AR affinity, we incor …
Structure-Guided Design of Nurr1 Agonists Derived from the Natural Ligand Dihydroxyindole.
Sai M, Vietor J, Kornmayer M, Egner M, López-García Ú, Höfner G, Pabel J, Marschner JA, Wein T, Merk D. Sai M, et al. J Med Chem. 2023 Oct 12;66(19):13556-13567. doi: 10.1021/acs.jmedchem.3c00852. Epub 2023 Sep 26. J Med Chem. 2023. PMID: 37751901 Free PMC article.
The neuroprotective transcription factor Nurr1 was recently found to bind the dopamine metabolite 5,6-dihydroxyindole (DHI) providing access to Nurr1 ligand design from a natural template. ...Three out of six primary hits were validated as novel Nurr1 agonists with …
The neuroprotective transcription factor Nurr1 was recently found to bind the dopamine metabolite 5,6-dihydroxyindole (DHI) providing …
The role of dopamine in epilepsy.
Starr MS. Starr MS. Synapse. 1996 Feb;22(2):159-94. doi: 10.1002/(SICI)1098-2396(199602)22:2<159::AID-SYN8>3.0.CO;2-C. Synapse. 1996. PMID: 8787131 Review.
The clinical benefits of dopamine agonists in the management of epilepsy can be traced back over a century, whilst the introduction of neuroleptics into psychiatry practice 40 years ago witnessed the emergence of fits as a side effect of dopamine receptor blo …
The clinical benefits of dopamine agonists in the management of epilepsy can be traced back over a century, whilst the introdu …
Discovery of endogenous inverse agonists for G protein-coupled receptor 6.
Shrader SH, Song ZH. Shrader SH, et al. Biochem Biophys Res Commun. 2020 Feb 19;522(4):1041-1045. doi: 10.1016/j.bbrc.2019.12.004. Epub 2019 Dec 7. Biochem Biophys Res Commun. 2020. PMID: 31818461 Free PMC article.
Here, we demonstrate for the first time that N-arachidonoyl dopamine, N-docosahexaenoyl dopamine, N-oleoyl dopamine and N-palmitoyl dopamine exert inverse agonism at GPR6. ...Our discovery of these N-acyl dopamines as endogenous inverse agoni …
Here, we demonstrate for the first time that N-arachidonoyl dopamine, N-docosahexaenoyl dopamine, N-oleoyl dopamine and …
The role of the D3 dopamine receptor and its partial agonist cariprazine in patients with schizophrenia and substance use disorder.
Grunze H. Grunze H. Expert Opin Pharmacother. 2023 Sep-Dec;24(18):1985-1992. doi: 10.1080/14656566.2023.2266359. Epub 2024 Jan 5. Expert Opin Pharmacother. 2023. PMID: 37817489 Review.
AREAS COVERED: This article reports the current evidence on the role of dopamine dysregulations in DD, the pharmacological profile of cariprazine, a partial agonist of D3 and D2 dopamine receptors, and first clinical observations that may support its usefulne …
AREAS COVERED: This article reports the current evidence on the role of dopamine dysregulations in DD, the pharmacological profile of …
Unveiling the Differences in Signaling and Regulatory Mechanisms between Dopamine D(2) and D(3) Receptors and Their Impact on Behavioral Sensitization.
Kim KM. Kim KM. Int J Mol Sci. 2023 Apr 4;24(7):6742. doi: 10.3390/ijms24076742. Int J Mol Sci. 2023. PMID: 37047716 Free PMC article. Review.
Dopamine receptors are classified into five subtypes, with D(2)R and D(3)R playing a crucial role in regulating mood, motivation, reward, and movement. ...Whereas D(2)R maintains continuous signal transduction through agonist-induced receptor phosphorylation, arrest …
Dopamine receptors are classified into five subtypes, with D(2)R and D(3)R playing a crucial role in regulating mood, motivation, rew …
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