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Metergoline
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Metergoline

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Metergoline
Metergoline.svg
Clinical data
Trade names Contralac, Liserdol
Other names Methergoline; FI-6337; [(8β)-1,6-Dimethylergolin-8-yl)methyl]carbamic acid phenylmethyl ester
Routes of
administration
Oral
ATC code
Legal status
Legal status
  • In general: ℞ (Prescription only)
Identifiers
  • benzyl N-[[(6aR,9S,10aR)-4,7-dimethyl-6,6a,8,9,10,10a-hexahydroindolo[4,3-fg]quinolin-9-yl]methyl]carbamate
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
UNII
ChEBI
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard 100.037.881
Chemical and physical data
Formula C25H29N3O2
Molar mass 403.526 g·mol−1
3D model (JSmol)
  • O=C(OCc1ccccc1)NC[C@@H]3C[C@@H]4c5cccc2c5c(cn2C)C[C@H]4N(C3)C
  • 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 checkY
  • Key:WZHJKEUHNJHDLS-QTGUNEKASA-N checkY
 ☒NcheckY (what is this?)  (verify)

Metergoline (INN, BAN), also known as methergoline and sold under the brand names Contralac (veterinary) and Liserdol (clinical), is a monoaminergic medication of the ergoline group which is used as a prolactin inhibitor in the treatment of hyperprolactinemia (high prolactin levels) and to suppress lactation.

Pharmacology

Pharmacodynamics

Metergoline is a ligand of various serotonin and dopamine receptors.

Activities of metergoline at various sites
Site Affinity (Ki [nM]) Efficacy (Emax [%]) Action
5-HT1A 4.3 ? Agonist
5-HT1B 5.2–36 ? Partial agonist
5-HT1D 0.60–11.7 ? Partial agonist
5-HT1E 776–1,122 ? ?
5-HT1F 339–341 ? ?
5-HT2A 0.12–2.3 ? Antagonist
5-HT2B 0.71–1.8 ? Antagonist
5-HT2C 0.18–1.8 ? Antagonist
5-HT3 >5,000–7,400 ? ?
5-HT4 354 ? ?
5-HT5A 630 ? ?
5-HT5B 1,000 ? ?
5-HT6 61–400 ? ?
5-HT7 6.4–6.5 ? Antagonist
D2 ? ? Agonist
Notes: All sites are human except 5-HT3 (rat/pig), 5-HT4 (pig), and 5-HT5B (rat—no human counterpart).

External links


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