SoRI-20041 (original) (raw)

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SoRI-20041 is an "antagonist-like" allosteric modulator of amphetamine-induced dopamine release (in contrast to the related research chemicals SoRI-9804 and , which are "agonist-like"). SoRI-20041 is believed to be the first example of a drug that separately modulates uptake versus release in the dopamine transporter (possibly showing how inward and outward transport represent distinct operational modes of DAT); it produces the same effects as SoRI-20040 and SoRI-9804 in uptake assays and binding assays, inhibiting the re-uptake of dopamine, but does not modulate d-amphetamine-induced DA release by inhibiting that as well, like 'agonists' of the series do.

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dbo:abstract SoRI-20041 is an "antagonist-like" allosteric modulator of amphetamine-induced dopamine release (in contrast to the related research chemicals SoRI-9804 and , which are "agonist-like"). SoRI-20041 is believed to be the first example of a drug that separately modulates uptake versus release in the dopamine transporter (possibly showing how inward and outward transport represent distinct operational modes of DAT); it produces the same effects as SoRI-20040 and SoRI-9804 in uptake assays and binding assays, inhibiting the re-uptake of dopamine, but does not modulate d-amphetamine-induced DA release by inhibiting that as well, like 'agonists' of the series do. This suggests the possibility of simultaneous action and increase of indirect-agonism through the dual action of DRA and DRI efficacy existing together. This increases the inhibition of re-uptake at synaptic dopamine concentrations without interfering in the flow of release of dopamine from amphetaminergic phosphorylation at the affected transporter. This overcomes the obstacle of a compromised binding site that would be rendered unusable through the action of amphetamine. Conventional dopamine re-uptake inhibitors (such as cocaine or methylphenidate) would otherwise ineffectively target such a site on each specific transporter so affected by amphetamine, making this an example of a DRI that does not have a mutually exclusive functionality against DRA action at individual instances of DAT. (en)
dbo:pubchem 44310972
dbo:thumbnail wiki-commons:Special:FilePath/SoRI-20041_Structure.svg?width=300
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dbp:iupacName N--2-phenyl-4-quinazolinamine (en)
dbp:n 3 (xsd:integer)
dbp:pubchem 44310972 (xsd:integer)
dbp:smiles c2ccccc2CCCNcc1ccccc1n4 (en)
dbp:stdinchi 1 (xsd:integer)
dbp:stdinchikey HQPGYRVHOIKOIE-UHFFFAOYSA-N (en)
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dcterms:subject dbc:Neurochemistry
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rdfs:comment SoRI-20041 is an "antagonist-like" allosteric modulator of amphetamine-induced dopamine release (in contrast to the related research chemicals SoRI-9804 and , which are "agonist-like"). SoRI-20041 is believed to be the first example of a drug that separately modulates uptake versus release in the dopamine transporter (possibly showing how inward and outward transport represent distinct operational modes of DAT); it produces the same effects as SoRI-20040 and SoRI-9804 in uptake assays and binding assays, inhibiting the re-uptake of dopamine, but does not modulate d-amphetamine-induced DA release by inhibiting that as well, like 'agonists' of the series do. (en)
rdfs:label SoRI-20041 (en)
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