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BenzothiepinsBenzazepines2,3,4,5-Tetrahydro-7,8-dihydroxy-1-phenyl-1H-3-benzazepineReceptors, Dopamine D1Dopamine AntagonistsBenzocycloheptenesDopamine AgonistsReceptors, Dopamine D2QuinpiroleDihydroxycholecalciferolsReceptors, DopamineHydroxycholecalciferolsDopamineRicinoleic AcidsCalcitriolTaurodeoxycholic AcidBehavior, AnimalLeukotriene A4Dose-Response Relationship, DrugRats, Sprague-DawleyGlycodeoxycholic AcidDeoxycholic AcidChenodeoxycholic AcidArachidonate LipoxygenasesHydroxylationTaurocholic AcidReceptors, CalcitriolStereoisomerismChromatography, Thin LayerChromatography, High Pressure LiquidHydro-LyasesHydroxy AcidsChromatography, GasCatecholsMass SpectrometryMolecular StructureUrsodeoxycholic AcidStructure-Activity RelationshipCholic AcidsGas Chromatography-Mass SpectrometryIsoleucineBileLipoxygenaseBiotransformationIntestinal AbsorptionKineticsPhenyl EthersMagnetic Resonance SpectroscopyArachidonic AcidsMixed Function OxygenasesVitamin D DeficiencyTaurineIntestine, SmallOxidation-ReductionBiological Transport, ActiveVitamin DCytochrome P-450 Enzyme SystemMicrosomes, LiverLiverCalciumFatty AcidsSpecies SpecificityCholesterol4,5-Dihydro-1-(3-(trifluoromethyl)phenyl)-1H-pyrazol-3-amineMolecular Sequence DataCells, Cultured3-Pyridinecarboxylic acid, 1,4-dihydro-2,6-dimethyl-5-nitro-4-(2-(trifluoromethyl)phenyl)-, Methyl esterTime FactorsPhenylacetates
PotentSelectiveDerivative
Potent2
  • SKF-89145 SKF-89626 7,8-Dihydroxy-5-phenyl-octahydrobenzo[h]isoquinoline: extremely potent, high-affinity full agonist Cabergoline - weak D1 agonism, highly selective for D2, and various serotonin receptors Pergolide - (similar to cabergoline) weak D1 agonism, highly selective for D2, and various serotonin receptors A photoswitchable agonist of D1-like receptors (azodopa) has been described that allows reversible control of dopaminergic transmission in wildtype animals. (wikipedia.org)
  • Benzazepine derivatives SCH-23,390 - 100-fold selectivity for D1 over D5 Ecopipam (SCH-39,166) - a selective D1/D5 antagonist that was being developed as an anti-obesity medication but was discontinued However, it has showed promise in reducing stuttering and is currently in Phase 2 Trials for this purpose DETQ − PAM LY-3154207 - potent and subtype selective PAM, in phase 2 studies for Lewy body dementia. (wikipedia.org)
Selective3
  • As a result, none of the known orthosteric ligands is selective for the D1 vs. the D5 receptor, but the benzazepines generally are more selective for the D1 and D5 receptors versus the D2-like family. (wikipedia.org)
  • SKF-89145 SKF-89626 7,8-Dihydroxy-5-phenyl-octahydrobenzo[h]isoquinoline: extremely potent, high-affinity full agonist Cabergoline - weak D1 agonism, highly selective for D2, and various serotonin receptors Pergolide - (similar to cabergoline) weak D1 agonism, highly selective for D2, and various serotonin receptors A photoswitchable agonist of D1-like receptors (azodopa) has been described that allows reversible control of dopaminergic transmission in wildtype animals. (wikipedia.org)
  • Benzazepine derivatives SCH-23,390 - 100-fold selectivity for D1 over D5 Ecopipam (SCH-39,166) - a selective D1/D5 antagonist that was being developed as an anti-obesity medication but was discontinued However, it has showed promise in reducing stuttering and is currently in Phase 2 Trials for this purpose DETQ − PAM LY-3154207 - potent and subtype selective PAM, in phase 2 studies for Lewy body dementia. (wikipedia.org)
Derivative1
  • To date, most of the known ligands are based on dihydrexidine or the prototypical benzazepine partial agonist SKF-38393 (one derivative being the prototypical antagonist SCH-23390). (wikipedia.org)