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
| Molecular Formula | C19H22F3N3 |
| Molecular Weight | 349.3933 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
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
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
| 8.9 null [pKi] | |||
Target ID: CHEMBL217 |
7.2 null [pKi] | ||
Target ID: CHEMBL234 |
7.8 null [pKi] | ||
Target ID: CHEMBL265 |
5.7 null [pKi] | ||
Target ID: P11614 Gene ID: 403963.0 Gene Symbol: HTR1D Target Organism: Canis lupus familiaris (Dog) (Canis familiaris) |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | Unknown Approved UseUnknown |
PubMed
| Title | Date | PubMed |
|---|---|---|
| Design and synthesis of novel insecticides based on the serotonergic ligand 1-[(4-aminophenyl)ethyl]-4-[3-(trifluoromethyl)phenyl]piperazine (PAPP). | 2010-03-10 |
|
| Agonist and antagonist actions of antipsychotic agents at 5-HT1A receptors: a [35S]GTPgammaS binding study. | 1998-08-21 |
|
| Antagonist properties of LY 165,163 at pre- and postsynaptic dopamine D2, D3 and D1 receptors: modulation of agonist actions at 5-HT1A receptors in vivo. | 1995-06 |
|
| Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. | 1993-03 |
|
| The serotonin (5-HT)1A agonist, LY 165,163, induces contralateral rotation in unilateral substantia nigra-lesioned rats via dopamine receptors. | 1991-09-16 |
|
| Central serotonin agonist actions of LY 165163, 1-(m-trifluoromethylphenyl)-4-(p-aminophenylethyl) piperazine, in rats. | 1986-11 |
|
| 5-HT-1a and 5-HT-1b selectivity of two phenylpiperazine derivatives: evidence for 5-HT-1b heterogeneity. | 1985-04-01 |
Patents
Sample Use Guides
| Substance Class |
Chemical
Created
by
admin
on
Edited
Mon Mar 31 19:03:34 GMT 2025
by
admin
on
Mon Mar 31 19:03:34 GMT 2025
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| Record UNII |
8HAJ699EWG
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| Record Status |
Validated (UNII)
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| Record Version |
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DTXSID30171136
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ACTIVE MOIETY |
