BIIE-0246

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BIIE-0246
300px
Systematic (IUPAC) name
N-[(1S)-4-[(Aminoiminomethyl)amino]-1-[([2-(3,5-dioxo-1,2-diphenyl-1,2,4-triazolidin-4-yl)ethyl]amino)carbonyl]butyl]-1-(2-[4-(6,11-dihydro-6-oxo-5H-dibenz[b,e]azepin-11-yl)-1-piperazinyl]-2-oxoethyl)cyclopentaneacetamide
Identifiers
CAS Number 246146-55-4 YesY
PubChem CID: 9811493
IUPHAR/BPS 1547
ChemSpider 7987248 N
Synonyms BIIE-0246
Chemical data
Formula C49H57N11O6
Molecular mass 896.045 g/mol
  • O=C3N(c1ccccc1)N(c2ccccc2)C(=O)N3CCNC(=O)[C@@H](NC(=O)CC4(CCCC4)CC(=O)N8CCN(C7c5c(cccc5)NC(=O)c6ccccc67)CC8)CCC/N=C(\N)N
  • InChI=1S/C49H57N11O6/c50-46(51)53-25-13-22-40(45(64)52-26-27-58-47(65)59(34-14-3-1-4-15-34)60(48(58)66)35-16-5-2-6-17-35)54-41(61)32-49(23-11-12-24-49)33-42(62)56-28-30-57(31-29-56)43-36-18-7-8-19-37(36)44(63)55-39-21-10-9-20-38(39)43/h1-10,14-21,40,43H,11-13,22-33H2,(H,52,64)(H,54,61)(H,55,63)(H4,50,51,53)/t40-,43?/m0/s1 N
  • Key:RSJAXPUYVJKAAA-JPGJPTAESA-N N
 NYesY (what is this?)  (verify)

BIIE-0246 is a drug used in scientific research which acts as a potent and selective antagonist for the Neuropeptide Y receptor Y2.[1] It was one of the first non-peptide Y2-selective antagonists developed, and remains among the most widely used tools for studying this receptor. It has been used to demonstrate a role for the Y2 subtype as a presynaptic autoreceptor limiting further neuropeptide Y release,[2][3] as well as modulating dopamine[4] and acetylcholine release.[5] It has also been shown to produce several behavioural effects in animals, including reducing alcohol consumption in addicted rats[6][7] and anxiolytic effects,[8] although while selective Y2 agonists are expected to be useful as anorectics,[9][10] BIIE-0246 did not appear to increase appetite when administered alone.[11]

References

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