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Formula | C17H17NO2 |
Molar mass | 267.328 g·mol−1 |
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Dihydrexidine (DAR-0100) is a moderately selective full agonist at the dopamine D1 and D5 receptors.[1] It has approximately 10-fold selectivity for D1 and D5 over the D2 receptor.[2] Although dihydrexidine has some affinity for the D2 receptor, it has functionally selective (highly biased) D2 signaling,[3] thereby explaining why it lacks D2 agonist behavioral qualities.[4]
Dihydrexidine has shown impressive antiparkinson effects in the MPTP-primate model,[5] and has been investigated for the treatmentofParkinson's disease.[6] In an early clinical trial the drug was given intravenously and led to profound hypotensionsodevelopment was halted.[7] The drug was resurrected when it was shown that smaller subcutaneous doses were safe.[8] This led to a pilot study in schizophrenia[9] and current clinical trials to assess its efficacy in improving the cognitive and working memory deficitsinschizophrenia and schizotypal disorder.
There have been several reviews of relevance to the compound.[10][11][12]
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Sympatholytics (antagonize α-adrenergic vasoconstriction) |
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Other antagonists |
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D1-like |
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D2-like |
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