A 841720
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This article, A 841720, was written by RelentlessRecusant. Please do not edit this fiction without the writer's permission. |
A 841720, alternatively known as A-841720, IUPAC name 7-Azepan-1-yl-4-dimethylamino-7H-9-thia-1,5,7-triaza-fluoren-8-one, is a chemical non-competitive antagonist to metabotropic glutamate receptor 1 (mGluR1).
It displays an IC50 = 10 nM to mGluR1 and an IC50 = 342 nM to mGluR5, demonstrating significant selectivity for mGluR1 versus mGluR5. It was originally synthesized by Zheng et. al in 2005 and has been subsequently characterized to be psychoactive, acting as an analgesic and also impairing motor and cognitive function. It acts as a pan-central nervous system (CNS) depressant, diminishing electrophysiological activity broadly across spinal neurons.[1]
A 841720 has been employed by the UNSC Office of Naval Intelligence as a useful interrogation drug during the Galactic Era; its impairment of cognitive function by blockade of metabotropic glutamate receptor signaling has been highly desirable during interrogation sessions.
[edit] References
- ↑ El-Kouhen et. al (2006). Blockade of mGluR1 receptor results in analgesia and disruption of motor and cognitive performances: effects of A-841720, a novel non-competitive mGluR1 receptor antagonist. British Journal of Pharmacology (149), 761–774.
| UNSC Drugs for Interrogation and Torture: Small Molecule Modulators of Psychology and Perception | ||
|---|---|---|
| A 841720 (mGluR1) · L-741,626 (D2) · Salvinorin A (κ-opioid) · WF-23 (DAT, SERT) | ||
| Source · Edit | ||
| Chemical Biology: Small-Molecule Control of Biological Systems (RelentlessRecusant) | ||
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| 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 | ||
