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Details

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
Structure of GR-103691

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)

HIDE SMILES / InChI

Molecular Formula C30H35N3O3
Molecular Weight 485.6172
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description
Curator's Comment: The description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/12763098 | https://www.ncbi.nlm.nih.gov/pubmed/9765337 | https://www.ncbi.nlm.nih.gov/pubmed/12711089

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.

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
0.32 nM [Kd]
24.0 nM [Ki]
81.0 nM [Ki]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
PubMed

PubMed

TitleDatePubMed
Patents

Sample Use Guides

20 mkg for 7 days
Route of Administration: Other
In Vitro Use Guide
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.
Substance Class Chemical
Created
by admin
on Sat Dec 16 08:40:06 GMT 2023
Edited
by admin
on Sat Dec 16 08:40:06 GMT 2023
Record UNII
0Y0CM1A77L
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
GR-103691
Common Name English
(1,1'-BIPHENYL)-4-CARBOXAMIDE, 4'-ACETYL-N-(4-(4-(2-METHOXYPHENYL)-1-PIPERAZINYL)BUTYL)-
Systematic Name English
GR 103691
Code English
Code System Code Type Description
PUBCHEM
4302960
Created by admin on Sat Dec 16 08:40:06 GMT 2023 , Edited by admin on Sat Dec 16 08:40:06 GMT 2023
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EPA CompTox
DTXSID6042602
Created by admin on Sat Dec 16 08:40:06 GMT 2023 , Edited by admin on Sat Dec 16 08:40:06 GMT 2023
PRIMARY
CAS
162408-66-4
Created by admin on Sat Dec 16 08:40:06 GMT 2023 , Edited by admin on Sat Dec 16 08:40:06 GMT 2023
PRIMARY
FDA UNII
0Y0CM1A77L
Created by admin on Sat Dec 16 08:40:06 GMT 2023 , Edited by admin on Sat Dec 16 08:40:06 GMT 2023
PRIMARY