LY165163
From the Halo Fan Fiction Wikia, writing 12,604 fan fiction articles
|
This article, LY165163, was written by RelentlessRecusant. Please do not edit this fiction without the writer's permission. |
.jpg)
LY165163, otherwise known as PPAP (p-Aminophenethyl-m-trifluoromethylphenyl piperazine) or LY 165,163, IUPAC name 4-[2-[4-[3-(Trifluoromethyl)phenyl]-1-piperazinyl]ethyl]benzeneamine, is a small-molecule chemical inhibitor of human and rat dopamine receptors 2 (D2) and 3 (D3) and is a chemical agonist of serotonin receptor 1A (5-HT1A).[1]
It was extensively characterized by Milan et. al in 1995 at the Institut de Recherches Servier at Croissy-sur-Seine, France.
PPAP has been previously shown in 2007 as a highly potent and specific inhibitor of neural stem cell (NSC) and neurosphere proliferation and survival, with a 702-fold selectivity of neurosphere cultures over astrocyte cultures, and having an EC50 = 31 nM in inhibition of neurosphere diameter, inducing caspase-3 and caspase-7 within 48 hours of compound addition to neurospheres, mediating caspase-mediated apoptosis. It has significant clinical utility in that it strongly inhibits proliferation of Ptch1+/- CD133+ neurospheres, that is, adult neural cancer stem cells shown to cause brain cancer in the adult human, with an EC50 = 169 nM, compared to cyclopamine, which in this model possesses an EC50 = 1 μM.[2]
[edit] References
- ↑ Millan et. al (1995). 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. The Journal of Pharmacology and Experimental Therapeutics (273): 1418-1427.
- ↑ Diamandis et. al (2007). Chemical genetics reveals a complex functional ground state of neural stem cells. Nature Chemical Biology (3): 268-273.
| Anticancer Drugs (Acumen Science Laboratories): Chemical Biology and Oncology | ||
|---|---|---|
| A-83-01 (Colon Cancer) · Bicuculline (Brain Cancer) · BMS-354825 (Chronic Myeloid Leukemia) · Dorsomorphin/LDN-193189 (Lung Cancer) · Cyclopamine/Robotnikinin/SANT1 (Skin, Brain, Prostate, and Colon Cancers) · LY165163 (Brain Cancer) · PK115-584 (Colon and Brain Cancer) | ||
| Source · Edit | ||
| Chemical Biology: Small-Molecule Control of Biological Systems (RelentlessRecusant) | ||
|---|---|---|
| | ||
| Receptor Tyrosine Kinases | A-83-01 (TGFβ/Activin) · BPIQ-II (EGFR) · Dorsomorphin/LDN-193189 (TGFβ/BMP) · SU5402 (FGFR) | |
| Signaling Kinases | A-769662 (AMPK) · BMS-354825 (BCR-ABL, Src)· BIO-Acetoxime (GSK3) · CHIR99021 (GSK3) · GO 6976 (PKC) · IMD-0354 (IκBa) · PD184352 (MAPK) · SB203580 (MAPK) · Y-27632 (ROCK) | |
| G Protein-Coupled Receptor | (+)-WIN-55212 (CB1/CB2) · ±-Sulpride (D2) · A 841720 (mGluR1) · BP-554 (5-HT1A) · Hh-Ag1.5 (Smo) · Cyclopamine/KAAD-Cyclopamine (Smo) · SANT1 (Smo) · SB-277011 (D3) | |
| Ion Channels | BAY K8644 (Cav1.2) · Bicuculline (GABAAR) · Cymarin (Na+/H+) · G-strophanthin (Na+/H+) · L-AP4 (Na+/H+) · Oxcarbazepine (Na+) · Resiniferatoxin (TRPV1) · Sarmentogenin (Na+/H+) · Theanine (AMPAR, NMDAR) | |
| Transporters | O-1783 (DAT) · WF-23 (DAT, SERT) | |
| Nuclear Receptor | All-trans retinoic acid (RAR/RXR) · GW501516 (PPARδ) · RU-486 (Nr3c1, Nr3c3) | |
| Protein Phosphatases | Endothall (PP2A) | |
| Polypharmacological | Phosphoserine (mGluR4) · PK115-584 (Tcf4/β-catenin, PKC) · Pluripotin · Reversine | |
| Other | 2C-E (DAT) · 4-methoxyphenyl-HTI-286 (α/β-tubulin) · Compound E/DAPT (presenilin-1) · D-cysteine · D-phenylalanine · Flurbiprofen (COX) · JZL184 (MAGL) · QS11 (RAFGAP1) · RO-28-1675 (glucokinase) · Robotnikinin (Shh) · Selegiline (MAOB) | |
| Uncharacterized | Neuropathiazol | |
| Libraries | Kinase Inhibitor Library | |
| Publications | ||
| Small molecule-mediated manipulation of the adult human induces selective and reversible control of physiological and psychological phenotype (Rubin et. al, 2590. Nature Medicine) | ||
| Source · Edit | ||
