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Bicuculline

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Bicuculline
Bicuculline
Chemical information
IUPAC Nomenclature

(R)-6-((S)-6-methyl-5,6,7,8-tetrahydro-[1,3]dioxolo[4,5-g]isoquinolin-5-yl)isobenzofuro[4,5-d][1,3]dioxol-8(6H)-one

Chemical Formula

C20H17NO6

Molecular Weight

367.35 g/mol

Clinical information
Clinical Usage

Promotion of neural stem cell (NCS) self-renewal

Mechanism of Action

GABAAR inhibitor

Known Side Effects
  • Significantly increased occurrence of non-familial epilepsy[1]
  • Significantly increased occurrence of central nervous cancer [2]
Route of Administration

Oral

  [Source]

Bicuculline, IUPAC name (R)-6-((S)-6-methyl-5,6,7,8-tetrahydro-[1,3]dioxolo[4,5-g]isoquinolin-5-yl)isobenzofuro[4,5-d][1,3]dioxol-8(6H)-one, is an alkaloid natural product that is a small-molecule chemical inhibitor of gamma-aminobutyric acid type A receptors (GABAAR)[3], IC50 = 3 μM for inhibitory activity.

Its blockade of GABAAR activity leads to significant promotion of embryonic stem (ES) and neural stem (NSC) cell proliferation and cell-cycle progression.[3]

Its in vivo clinical administration to humans is contraindicated because it significantly increases the occurrence on non-familial cases of juvenile myoclonic epilepsy and childhood absence epilepsy because of its blockade of endogenous GABAergic inhibitory central nervous signaling[1] and it is believed to significantly increase the occurrence of central nervous cancer by its promotion of neural stem cell and neural progenitor cell (NPC) self-renewal.[2]

References

  1. 1.0 1.1 Rogawski and Löscher (2004). The Neurobiology of Antiepileptic Drugs. Nature Reviews Neuroscience (5): 553-564.
  2. 2.0 2.1 Singh et. al (2004). Identification of human brain tumour initiating cells. Nature (432): 396-401.
  3. 3.0 3.1 Andang et. al (2008). Histone H2AX-dependent GABAA receptor regulation of stem cell proliferation. Nature (451): 460-465.



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)
Compound Names (Biological Targets)
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 (R)-(+)-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

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