| Stereochemistry | ACHIRAL |
| Molecular Formula | C30H35N3O3 |
| Molecular Weight | 485.6172 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
COC1=C(C=CC=C1)N2CCN(CCCCNC(=O)C3=CC=C(C=C3)C4=CC=C(C=C4)C(C)=O)CC2
InChI
InChIKey=JARNORYOPMINDY-UHFFFAOYSA-N
InChI=1S/C30H35N3O3/c1-23(34)24-9-11-25(12-10-24)26-13-15-27(16-14-26)30(35)31-17-5-6-18-32-19-21-33(22-20-32)28-7-3-4-8-29(28)36-2/h3-4,7-16H,5-6,17-22H2,1-2H3,(H,31,35)
| Molecular Formula | C30H35N3O3 |
| Molecular Weight | 485.6172 |
| Charge | 0 |
| Count |
MOL RATIO
1 MOL RATIO (average) |
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
GR 103691 is an effective and selective receptor antagonist of the D3DR (dopamine D3 receptor). GR 103691 was shown to have 100-fold higher selectivity for D3DR (dopamine D3 receptor) over the D2DR (dopamine D2 receptor) and D4DR (dopamine D4 receptor) sites. GR 103,691 is functionally active in vivo and will inhibit the hyperactivity response induced by intra-VTA (ventral tegmental area) injection of muscimol in rats.
Originator
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
| 0.32 nM [Kd] | |||
| 24.0 nM [Ki] | |||
| 81.0 nM [Ki] |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
PubMed
Patents
Sample Use Guides
Binding studies were carried out at recombinant hD2 receptors and hD3 receptors expressed in CHO cell lines. GR-103691 binding affinities at hD2 and hD3 receptors were determined using [125I]-iodosulpride (0.1 and 0.2 nM for D2 and D3, respectively), [3H]-(1)-S 14297 (7 nM for D3) and [3H]-(1)-PD 128,907 (2 nM for D3). Nonspecific binding was defined using 10 mM raclopride.