Description
Metergoline is a serotonin (5-HT) receptor antagonist. It is active at 5-HT1 (pKi=7.8 for 5-HT1B), 5-HT2 (pKi=8.64, 8.75 and 8.75 for 5-HT2A, 5-HT2B and 5-HT2C respectively) and 5-HT7 (pKi=16 nM) receptor subtypes. Metergoline potently inhibits 5-HT radiolabeling of the human 5-hydroxytryptamine(7) receptor, with an IC₅₀ value of 73 nM. It inhibits 5-HT7 receptor-stimulated cAMP production with an IC₅₀ of 321 nM in HEK293 cells.
Metergoline is a serotonin (5-HT) receptor antagonist. It is active at 5-HT1 (pKi=7.8 for 5-HT1B), 5-HT2 (pKi=8.64, 8.75 and 8.75 for 5-HT2A, 5-HT2B and 5-HT2C respectively) and 5-HT7 (pKi=16 nM) receptor subtypes. Metergoline potently inhibits 5-HT radiolabeling of the human 5-hydroxytryptamine(7) receptor, with an IC₅₀ value of 73 nM. It inhibits 5-HT7 receptor-stimulated cAMP production with an IC₅₀ of 321 nM in HEK293 cells.
Alternate Name/Synonyms: Liserdol; benzyl N-[[(6aR,9S,10aR)-4,7-dimethyl-6,6a,8,9,10,10a-hexahydroindolo[4,3-fg]quinolin-9-yl]methyl]carbamate; (((8-beta)-1,6-Dimethylergolin-8-yl)methyl)carbamic acid benzyl ester; (((8-beta)-1,6-Dimethylergolin-8-yl)methyl)carbamic acid phenylmethyl ester
Appearance: White to pale yellow powder
Formulation:
CAS Number: 17692-51-2
Structure Available?: TRUE
Peptide sequence:
Salt Form: FALSE
Molecular Formula: C₂₅H₂₉N₃O₂
Molecular Weight: 403.5
Cell-Permeable?: True
Purity: ≥ 98%
Solubilities: ~5 mg/ml in ethanol, ~30 mg/ml in DMF, ~25 mg/ml in DMSO
Handling: Do not take internally. Wear gloves and mask when handling the product! Avoid contact by all modes of exposure.
Country of Origin: USA
Tag Line: A serotonin (5-HT) receptor antagonist
MDL Number: MFCD00153829
PubChem CID: 28693
SMILES: CN1CC(CC2C1CC3=CN(C4=CC=CC2=C34)C)CNC(=O)OCC5=CC=CC=C5
InChi: InChI=1S/C25H29N3O2/c1-27-14-18(13-26-25(29)30-16-17-7-4-3-5-8-17)11-21-20-9-6-10-22-24(20)19(12-23(21)27)15-28(22)2/h3-10,15,18,21,23H,11-14,16H2,1-2H3,(H,26,29)/t18-,21+,23+/m0/s1
InChi Key: WZHJKEUHNJHDLS-QTGUNEKASA-N
Additional Information
Storage Condition: |
-20ºC |
Shipping Condition: |
RT |
Shelf Life: |
36 months |