BW-723C86

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BW-723C86
Identifiers
  • 1-[5-(2-Thienylmethoxy)-1H-indol-3-yl]-2-propanamine
JSmol)
  • c2c1c([nH]cc1CC(C)N)ccc2OCc3cccs3
  • InChI=1S/C16H18N2OS/c1-11(17)7-12-9-18-16-5-4-13(8-15(12)16)19-10-14-3-2-6-20-14/h2-6,8-9,11,18H,7,10,17H2,1H3 ☒N
  • Key:ALFGDCNSEBJYSP-UHFFFAOYSA-N ☒N
 ☒NcheckY (what is this?)  (verify)

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 is around only 3 times as selective for 2B compared to 2C and so is much less selective than most research ligands, but no superior 5-HT2B agonist was available until the potent and selective 5-HT2B activity of 6-APB was discovered in 2012.[6] 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.

An

inhibit the activity of tyrosinase.[notes 2]

See also

Notes

  1. ^ "In summary, results of our study indicated that BW723C86 inhibits melanin synthesis by suppressing the expression of melanogenesis-related proteins (tyrosinase, TRP-1, and TRP-2) at the transcriptional level. The decreased expression of these proteins is a result of reduced MITF expression. Furthermore, the reduced level of MITF was associated with inhibition of the PKA/CREB/MITF pathway and direct inhibition of MITF transcription."[7]: 9 
  2. ^ "BW723C86 treatment reduced melanin content in melan-A cells and in normal human melanocytes (NHM) without affecting cellular viability. BW723C86 reduced intracellular tyrosinase activity but did not affect tyrosinase activity in cell extracts, indicating that BW723C86 does not have a direct effect on tyrosinase activity."[7]: 8 

References

  1. PMID 8730737
    .
  2. S2CID 7310462
    .
  3. PMID 10694218
    .
  4. S2CID 26716284
    .
  5. S2CID 17626074
    .
  6. PMID 23261499
    .
  7. ^
    PMID 27077852
    .
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