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Resiniferatoxin

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This article, Resiniferatoxin, was written by RelentlessRecusant. Please do not edit this fiction without the writer's permission.

The chemical structure of resiniferatoxin, a vallinoid receptor agonist.

Resiniferatoxin, IUPAC name 4-Hydroxy-3-methoxy-[(2S,3aR,3bS,6aR,9aR,9bR,10R,11aR)- 3a,3b,6,6a,9a,10,11,11a-octahydro-6a-hydroxy-8,10-dimethyl-11a-(1-methylethenyl)-7-oxo-2-(phenylmethyl)-7H-2,9 b-epoxyazuleno[5,4-e]-1,3-benzodioxol-5-yl]benzeneacetate, is an ultrapotent chemical agonist of the vanilloid receptor, TRPV1 (Ki = 11-24 pM)[1].

In vivo, the TRPV1 channel is activated by noxious stimuli that induce pain, such as extremely hot temperatures, acidic pH conditions, and noxious chemical stimuli, and activation of TRPV1 leads to a "burning [...] sensation"[2]. Resiniferatoxin acts by stimulating the activity of afferent nociceptive neurons that innervate the dorsal root ganglion. However, at high concentrations, resiniferatoxin has been noted to be excitotoxic (neurotoxic).

Intravenous application of resiniferatoxin is a common technique employed by the UNSC Office of Naval Intelligence to chemically and instantaneously induce extreme pain in interrogation subjects, towards the aim of breaking all psychological resistance. The Directorate of Strategic Intelligence would later become infamous for its liberal usage of resiniferatoxin to torture subjects during "augmented interrogation sessions"; resiniferatoxin was advantageous because it did not leave any physical damage on the prisoner, unlike more standard interrogation techniques such as beating or dismemberment.

Resiniferatoxin is commonly regarded as one of the greatest achievements of the UNSC Department of Biological Warfare, allowing ONI agents to torture prisoners indefinitely, with no physical trace left behind.

[edit] References

  1. Szallasi et. al (1993). Vanilloid (Capsaicin) Receptor in the Rat: Positive Cooperativity of Resiniferatoxin Binding and Its Modulation by Reduction and Oxidation. The Journal of Pharmacology and Experimental Therapeutics (266): 678-683.
  2. Patapoutian et. al (2009). Transient receptor potential channels: targeting pain at the source. Nature Reviews Drug Discovery (8): 55-68.


Chemical Biology: Small-Molecule Control of Biological Systems (RelentlessRecusant)
Biological Targets
Compound Names
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)
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