Details
Stereochemistry | ACHIRAL |
Molecular Formula | C19H22F3N3 |
Molecular Weight | 349.3933 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
NC1=CC=C(CCN2CCN(CC2)C3=CC=CC(=C3)C(F)(F)F)C=C1
InChI
InChIKey=GAAKALASJNGQKD-UHFFFAOYSA-N
InChI=1S/C19H22F3N3/c20-19(21,22)16-2-1-3-18(14-16)25-12-10-24(11-13-25)9-8-15-4-6-17(23)7-5-15/h1-7,14H,8-13,23H2
LY-165163 is a partial agonist of serotonin receptors 5-HT1A and 5-HT1D. It exhibits marked activity at both pre- and postsynaptic dopaminergic D2 (D3 and D1) receptors. LY-165163 caused a significant and dose-dependent hypothermia in rats. As a 5-HT1D receptor agonist, LY-165163 was proposed for the ocular pain treatment.
CNS Activity
Originator
Sources: https://www.ncbi.nlm.nih.gov/pubmed/3982214
Curator's Comment: # Eli Lilly and Co.
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
8.9 null [pKi] | |||
Target ID: CHEMBL217 Sources: https://www.ncbi.nlm.nih.gov/pubmed/7791116 |
7.2 null [pKi] | ||
Target ID: CHEMBL234 Sources: https://www.ncbi.nlm.nih.gov/pubmed/7791116 |
7.8 null [pKi] | ||
Target ID: CHEMBL265 Sources: https://www.ncbi.nlm.nih.gov/pubmed/7791116 |
5.7 null [pKi] | ||
Target ID: P11614 Gene ID: 403963.0 Gene Symbol: HTR1D Target Organism: Canis lupus familiaris (Dog) (Canis familiaris) Sources: https://www.ncbi.nlm.nih.gov/pubmed/8584040 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | Unknown Approved UseUnknown |
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/2430093
Rat: 1.25 to 20 mg/kg
Route of Administration:
Intraperitoneal
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/2933490
With either 10 microM 5-HT or 1 microM 8-hydroxy-2-(di-n-propylamino)tetralin to define nonspecific binding, [3H]PAPP bound to a single class of sites in rat cortical membranes with a KD of 1.6 nM and a maximal binding density (Bmax) of 162 fmol/mg of protein.
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DTXSID30171136
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ACTIVE MOIETY