| Identification | Back Directory | [Name]
3,6A,11,14-TETRAHYDRO-9-METHOXY-2-METHYL-(12H)-ISOQUINO[1,2-B]PYRROLO[3,2-F][1,3]BENZOXAZINE-1-CARBOXYLIC ACID, ETHYL ESTER | [CAS]
23062-91-1 | [Synonyms]
PD 102807
3,6a,11,14-Tetrahydro-9-methoxy-2-methyl-(12H)-isoquino[1.2-b]pyrrolo[3.2-f][1.3]benzoxazine-1-carboxylicacidethyles]
3,6a,11,14-Tetrahydro-9-methoxy-2-methyl-(12H)-isoquino[1,2-b]pyrrolo[3,2-f][1,3]benzoxazine-1-carboxylic acid ethyl ester
3,6A,11,14-TETRAHYDRO-9-METHOXY-2-METHYL-(12H)-ISOQUINO[1,2-B]PYRROLO[3,2-F][1,3]BENZOXAZINE-1-CARBOXYLIC ACID, ETHYL ESTER | [Molecular Formula]
C23H24N2O4 | [MDL Number]
MFCD04118313 | [MOL File]
23062-91-1.mol | [Molecular Weight]
392.45 |
| Chemical Properties | Back Directory | [Boiling point ]
586.0±50.0 °C(Predicted) | [density ]
1.34±0.1 g/cm3(Predicted) | [storage temp. ]
Store at RT | [solubility ]
Soluble to 100 mM in DMSO | [form ]
Powder | [pka]
15.77±0.20(Predicted) | [color ]
Off-white to light yellow |
| Hazard Information | Back Directory | [Uses]
PD 102807 is a selective mAChR M4 antagonist. | [Definition]
ChEBI: LSM-1888 is an indolyl carboxylic acid. | [Biological Activity]
Selective M 4 muscarinic receptor antagonist. IC 50 values are 91, 6559, 3441, 950 and 7412 nM for human M 4 , M 1 , M 2 , M 3 , and M 5 receptors respectively. | [in vivo]
Striatal perfusion of PD-102807 (3 μM) alleviates levodopa-induced dyskinesia (LID) and inhibits nigral GABA and Glu along with striatal Glu release[3]. | Animal Model: | Male Sprague-Dawley rats[3] | | Dosage: | 3 μM | | Administration: | Administration:Perfusion started 40 min prior to L-DOPA (6 mg/Kg plus 12 mg/Kg benserazide, s.c.) administration and continued until the end of experiment. | | Result: | Basal dialysate levels in PD-102807 experiment were 19.19±2.62 nM and 47.77±3.42 nM for GABA and Glu in SNr, respectively, and 41.38±4.25 nM for Glu in striatum.
Reduced global Axial Limb Orolingual (ALO) Abnormal Involuntary Movements (AIM) expression from 70.75±5.64 to 25.38±6.64, significantly attenuating limb, axial and orolingual AIMs at 3 μM.
Inhibited the L-DOPA-induced rise of substantia nigra pars reticulata (SNr) GABA, SNr Glu, and striatal Glu at 3 μM.
|
| [IC 50]
mAChR4 | [storage]
Room temperature |
|
| Company Name: |
Energy Chemical
|
| Tel: |
021-58432009 400-005-6266 |
| Website: |
http://www.energy-chemical.com |
| Company Name: |
cjbscvictory
|
| Tel: |
13348960310 |
| Website: |
https://www.weikeqi-biotech.com/ |
|