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Advances and challenges in the search for D2 and D3 dopamine receptor-selective compounds.
Moritz AE, Free RB, Sibley DR. Moritz AE, et al. Among authors: sibley dr. Cell Signal. 2018 Jan;41:75-81. doi: 10.1016/j.cellsig.2017.07.003. Epub 2017 Jul 14. Cell Signal. 2018. PMID: 28716664 Free PMC article. Review.
This review summarizes the progress that has been made in developing D(2)R- or D(3)R-selective antagonists and agonists, and also describes the experimental conditions that need to be considered when determining the selectivity of a given compound, as apparent selec …
This review summarizes the progress that has been made in developing D(2)R- or D(3)R-selective antagonists and agonists, and a …
The hyperthyroid economy.
Sibley DE. Sibley DE. J R Soc Med. 1995 Jun;88(6):305-6. J R Soc Med. 1995. PMID: 7629759 Free PMC article. No abstract available.
Pharmacology and Therapeutic Potential of Benzothiazole Analogues for Cocaine Use Disorder.
Boateng CA, Nilson AN, Placide R, Pham ML, Jakobs FM, Boldizsar N, McIntosh S, Stallings LS, Korankyi IV, Kelshikar S, Shah N, Panasis D, Muccilli A, Ladik M, Maslonka B, McBride C, Sanchez MX, Akca E, Alkhatib M, Saez J, Nguyen C, Kurtyan E, DePierro J, Crowthers R, Brunt D, Bonifazi A, Newman AH, Rais R, Slusher BS, Free RB, Sibley DR, Stewart KD, Wu C, Hemby SE, Keck TM. Boateng CA, et al. Among authors: sibley dr. J Med Chem. 2023 Sep 14;66(17):12141-12162. doi: 10.1021/acs.jmedchem.3c00734. Epub 2023 Aug 30. J Med Chem. 2023. PMID: 37646374 Free PMC article.
This study focused on the synthesis and evaluation of a novel series of benzothiazole analogues designed to target D(4)R. We identified several compounds with high D(4)R binding affinity (K(i) 6.9 nM) and >91-fold selectivity over other D(2)-like receptors (D(2) …
This study focused on the synthesis and evaluation of a novel series of benzothiazole analogues designed to target D(4)R. We identifi …
Synthesis and Pharmacological Characterization of Novel trans-Cyclopropylmethyl-Linked Bivalent Ligands That Exhibit Selectivity and Allosteric Pharmacology at the Dopamine D(3) Receptor (D(3)R).
Kumar V, Moritz AE, Keck TM, Bonifazi A, Ellenberger MP, Sibley CD, Free RB, Shi L, Lane JR, Sibley DR, Newman AH. Kumar V, et al. Among authors: sibley dr. J Med Chem. 2017 Feb 23;60(4):1478-1494. doi: 10.1021/acs.jmedchem.6b01688. Epub 2017 Feb 10. J Med Chem. 2017. PMID: 28186762 Free PMC article.
The structural similarities between dopamine D(3) receptor (D(3)R)-selective molecules that display bitopic or allosteric pharmacology and those that are simply competitive antagonists are subtle and intriguing. ...Incorporating a trans-cyclopropylmethyl linker between pha …
The structural similarities between dopamine D(3) receptor (D(3)R)-selective molecules that display bitopic or allosteric pharmacolog …
Dopamine D4 Receptor-Selective Compounds Reveal Structure-Activity Relationships that Engender Agonist Efficacy.
Keck TM, Free RB, Day MM, Brown SL, Maddaluna MS, Fountain G, Cooper C, Fallon B, Holmes M, Stang CT, Burkhardt R, Bonifazi A, Ellenberger MP, Newman AH, Sibley DR, Wu C, Boateng CA. Keck TM, et al. Among authors: sibley dr. J Med Chem. 2019 Apr 11;62(7):3722-3740. doi: 10.1021/acs.jmedchem.9b00231. Epub 2019 Apr 1. J Med Chem. 2019. PMID: 30883109 Free PMC article.
The dopamine D(4) receptor (D(4)R) plays important roles in cognition, attention, and decision making. ...To identify new D(4)R-selective ligands, and to understand the molecular determinants of agonist efficacy at D(4)R, we report a series of eighteen novel …
The dopamine D(4) receptor (D(4)R) plays important roles in cognition, attention, and decision making. ...To identify new D(4)R
Dopamine D5 receptor-mediated decreases in mitochondrial reactive oxygen species production are cAMP and autophagy dependent.
Lee H, Jiang X, Perwaiz I, Yu P, Wang J, Wang Y, Hüttemann M, Felder RA, Sibley DR, Polster BM, Rozyyev S, Armando I, Yang Z, Qu P, Jose PA. Lee H, et al. Among authors: sibley dr. Hypertens Res. 2021 Jun;44(6):628-641. doi: 10.1038/s41440-021-00646-w. Epub 2021 Apr 5. Hypertens Res. 2021. PMID: 33820956 Free PMC article.
In HEK293 cells overexpressing D(5)R, fenoldopam, an agonist of the two D(1)-like receptors, D(1)R and D(5)R, decreased the production of mitochondria-derived ROS (mito-ROS). ...In human renal proximal tubule cells with DRD1 gene silencing to eliminate the co …
In HEK293 cells overexpressing D(5)R, fenoldopam, an agonist of the two D(1)-like receptors, D(1)R and D(5)R, decreased …
Upregulation of renal sodium transporters in D5 dopamine receptor-deficient mice.
Wang X, Luo Y, Escano CS, Yang Z, Asico L, Li H, Jones JE, Armando I, Lu Q, Sibley DR, Eisner GM, Jose PA. Wang X, et al. Among authors: sibley dr. Hypertension. 2010 Jun;55(6):1431-7. doi: 10.1161/HYPERTENSIONAHA.109.148643. Epub 2010 Apr 19. Hypertension. 2010. PMID: 20404220 Free PMC article.
D(5) dopamine receptor (D(5)R)-deficient (D(5)(-/-)) mice have hypertension that is aggravated by an increase in sodium intake. ...Our findings suggest that the increased protein expression of sodium transporters/channels in distal nephron segments may be the direct conseq …
D(5) dopamine receptor (D(5)R)-deficient (D(5)(-/-)) mice have hypertension that is aggravated by an increase in sodium intake. ...Ou …
D1-D2 dopamine receptor synergy promotes calcium signaling via multiple mechanisms.
Chun LS, Free RB, Doyle TB, Huang XP, Rankin ML, Sibley DR. Chun LS, et al. Among authors: sibley dr. Mol Pharmacol. 2013 Aug;84(2):190-200. doi: 10.1124/mol.113.085175. Epub 2013 May 16. Mol Pharmacol. 2013. PMID: 23680635 Free PMC article.
The D(1) dopamine receptor (D(1)R) has been proposed to form a hetero-oligomer with the D(2) dopamine receptor (D(2)R), which in turn results in a complex that couples to phospholipase C-mediated intracellular calcium release. ...Our data suggest that the mechanism …
The D(1) dopamine receptor (D(1)R) has been proposed to form a hetero-oligomer with the D(2) dopamine receptor (D(2)R), which …
Target deconvolution studies of (2R,6R)-hydroxynorketamine: an elusive search.
Bonaventura J, Gomez JL, Carlton ML, Lam S, Sanchez-Soto M, Morris PJ, Moaddel R, Kang HJ, Zanos P, Gould TD, Thomas CJ, Sibley DR, Zarate CA Jr, Michaelides M. Bonaventura J, et al. Among authors: sibley dr. Mol Psychiatry. 2022 Oct;27(10):4144-4156. doi: 10.1038/s41380-022-01673-w. Epub 2022 Jun 29. Mol Psychiatry. 2022. PMID: 35768639 Free PMC article.
The main goals of this study were to perform an in-depth pharmacological characterization of (2R,6R)-HNK at known ketamine targets, to use target deconvolution approaches to discover novel proteins that bind to (2R,6R)-HNK, and to characterize the biodistribution and behavioral e …
The main goals of this study were to perform an in-depth pharmacological characterization of (2R,6R)-HNK at known ketamine targets, to use t …
Pharmacological characterization of 2-methoxy-N-propylnorapomorphine's interactions with D2 and D3 dopamine receptors.
Skinbjerg M, Namkung Y, Halldin C, Innis RB, Sibley DR. Skinbjerg M, et al. Among authors: sibley dr. Synapse. 2009 Jun;63(6):462-75. doi: 10.1002/syn.20626. Synapse. 2009. PMID: 19217026 Free PMC article.
Recently, agonist radioligands of D(2)/D(3) DARs have begun to be developed and employed. One such agonist is (R)-2-(11)CH(3)O-N-n-propylnorapomorphine (MNPA). Here, we perform a pharmacological characterization of MNPA using recombinant D(2) and D(3) DARs expressed in HEK …
Recently, agonist radioligands of D(2)/D(3) DARs have begun to be developed and employed. One such agonist is (R)-2-(11)CH(3)O-N-n-pr …
29 results