buserelin indications/contra

Stem definitionDrug idCAS RN
pituitary hormone-release stimulating peptides 436 57982-77-1

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • buserelin
  • etilamide
  • receptal
A potent synthetic analog of GONADOTROPIN-RELEASING HORMONE with D-serine substitution at residue 6, glycine10 deletion, and other modifications.
  • Molecular weight: 1239.45
  • Formula: C60H86N16O13
  • CLOGP: -1.45
  • LIPINSKI: 3
  • HAC: 29
  • HDO: 16
  • TPSA: 438.27
  • ALOGS: -4.51
  • ROTB: 33

Drug dosage:

DoseUnitRoute
0.11 mg implant
1.20 mg N
1.50 mg P

Approvals:

DateAgencyCompanyOrphan
Jan. 1, 1984 YEAR INTRODUCED

FDA Adverse Event Reporting System

None

Pharmacologic Action:

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SourceCodeDescription
ATC L02AE01 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ENDOCRINE THERAPY
HORMONES AND RELATED AGENTS
Gonadotropin releasing hormone analogues
MeSH PA D005299 Fertility Agents
MeSH PA D005300 Fertility Agents, Female
MeSH PA D012102 Reproductive Control Agents

Drug Use (View source of the data)

None

Acid dissociation constants calculated using MoKa v3.0.0

None

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Gonadotropin-releasing hormone receptor GPCR AGONIST EC50 10.52 IUPHAR IUPHAR
Lutropin-choriogonadotropic hormone receptor GPCR Kd 8.57 WOMBAT-PK
Gonadotropin-releasing hormone receptor GPCR AGONIST EC50 10.05 IUPHAR

External reference:

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IDSource
3860 IUPHAR_LIGAND_ID
N0000170309 NUI
C0006456 UMLSCUI
D07259 KEGG_DRUG
N0000170309 NDFRT
1825 RXNORM
395744006 SNOMEDCT_US
003708 NDDF
008310 NDDF
327301004 SNOMEDCT_US
D002064 MESH_DESCRIPTOR_UI
DB06719 DRUGBANK_ID
CHEMBL2110824 ChEMBL_ID
50225 PUBCHEM_CID
PXW8U3YXDV UNII
4045 INN_ID
CHEBI:135907 CHEBI

Pharmaceutical products:

None