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Stapling Amantadine to Melanostatin Neuropeptide: Discovery of Potent Positive Allosteric Modulators of the D2 Receptors

Title
Stapling Amantadine to Melanostatin Neuropeptide: Discovery of Potent Positive Allosteric Modulators of the D2 Receptors
Type
Article in International Scientific Journal
Year
2023
Authors
Silva-Reis, SC
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Correia, XC
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Costa-Almeida, HF
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Pires-Lima, BL
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Maronde, D
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Costa, VM
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García-Mera, X
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Luis Cruz
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Brea, J
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Loza, MI
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Rodriguez Borges, JE
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Sampaio-Dias, IE
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Journal
Vol. 14
Pages: 1656-1663
ISSN: 1948-5875
Other information
Authenticus ID: P-00Z-FJW
Abstract (EN): This work describes the synthesis and pharmacological and toxicological evaluation of melanostatin (MIF-1) bioconjugates with amantadine (Am) via a peptide linkage. The data from the functional assays at human dopamine D-2 receptors (hD(2)R) showed that bioconjugates 1 (EC50 = 26.39 +/- 3.37 nM) and 2 (EC50 = 17.82 +/- 4.24 nM) promote a 3.3- and 4.9-fold increase of dopamine potency, respectively, at 0.01 nM, with no effect on the efficacy (E-max = 100%). In this assay, MIF-1 was only active at the highest concentration tested (EC50 = 23.64 +/- 6.73 nM, at 1 nM). Cytotoxicity assays in differentiated SH-SY5Y cells showed that both MIF-1 (94.09 +/- 5.75%, p < 0.05) and carbamate derivative 2 (89.73 +/- 4.95%, p < 0.0001) exhibited mild but statistical significant toxicity (assessed through the MTT reduction assay) at 200 mu M, while conjugate 1 was found nontoxic at this concentration.
Language: English
Type (Professor's evaluation): Scientific
No. of pages: 8
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