Dihydrexidine

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

Clinical data
ATC code	none
Identifiers
IUPAC name 5,6,6a,7,8,12b-hexahydro-benzo(a)phenanthridine-10,11-diol
CAS Number	123039-93-0 Y
PubChem CID	5311070
ChemSpider	5036130 N
UNII	32D64VH037
ChEMBL	ChEMBL25856 N
CompTox Dashboard (EPA)	DTXSID00894188
Chemical and physical data
Formula	C17H17NO2
Molar mass	267.328 g·mol−1
3D model (JSmol)	Interactive image
SMILES c1ccc2c(c1)CN[C@H]3[C@H]2c4cc(c(cc4CC3)O)O
InChI InChI=1S/C17H17NO2/c19-15-7-10-5-6-14-17(13(10)8-16(15)20)12-4-2-1-3-11(12)9-18-14/h1-4,7-8,14,17-20H,5-6,9H2/t14-,17-/m1/s1 N Key:BGOQGUHWXBGXJW-RHSMWYFYSA-N N
NY (what is this?)  (verify)

Dihydrexidine has shown impressive antiparkinson effects in the MPTP-primate model,^[5] and has been investigated for the treatment of Parkinson's disease.^[6] In an early clinical trial the drug was given intravenously and led to profound hypotension so development 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 deficits in schizophrenia and schizotypal disorder.

There have been several reviews of relevance to the compound.^[10][11][12]