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BW-723C86: Wikis

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BW-723C86
Systematic (IUPAC) name
5-((thiophen-2-yl)methoxy)-α-methyltryptamine
Identifiers
CAS number 160521-72-2
ATC code  ?
PubChem 5311036
Chemical data
Formula C 16H18N2OS 
Mol. mass 286.391 g/mol
SMILES eMolecules & PubChem
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life  ?
Excretion  ?
Therapeutic considerations
Pregnancy cat.  ?
Legal status
Routes  ?

BW-723C86 is a tryptamine derivative drug which acts as a 5-HT2B receptor agonist. It has anxiolytic effects in animal studies,[1][2] and is also used for investigating the function of the 5-HT2B receptor in a range of other tissues.[3][4][5]

BW-723C86 is actually a mixed 5-HT2B / 5-HT2C agonist, and while it has good selectivity over 5-HT2A and other serotonin receptor subtypes, it has only around 3x selectivity for 2B over 2C and so is much less selective than most research ligands, but as of 2009 no superior 5-HT2B agonist is yet available. Highly selective 5-HT2C antagonists are available however, and so a combination of BW-723C86 with a selective 5-HT2C antagonist allows 5-HT2B mediated responses to be studied in isolation.

References

  1. ^ Kennett GA, Bright F, Trail B, Baxter GS, Blackburn TP. Effects of the 5-HT2B receptor agonist, BW 723C86, on three rat models of anxiety. British Journal of Pharmacology. 1996 Apr;117(7):1443-8. PMID 8730737
  2. ^ Kennett GA, Trail B, Bright F. Anxiolytic-like actions of BW 723C86 in the rat Vogel conflict test are 5-HT2B receptor mediated. Neuropharmacology. 1998 Dec;37(12):1603-10. PMID 9886683
  3. ^ Knowles ID, Ramage AG. Evidence that activation of central 5-HT(2B) receptors causes renal sympathoexcitation in anaesthetized rats. British Journal of Pharmacology. 2000 Jan;129(1):177-83. PMID 10694218
  4. ^ Günther S, Maroteaux L, Schwarzacher SW. Endogenous 5-HT2B receptor activation regulates neonatal respiratory activity in vitro. Journal of Neurobiology. 2006 Aug;66(9):949-61. PMID 16758492
  5. ^ Ryan BK, Anwyl R, Rowan MJ. 5-HT2 receptor-mediated reversal of the inhibition of hippocampal long-term potentiation by acute inescapable stress. Neuropharmacology. 2008 Aug;55(2):175-82. PMID 18538800
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