Date published: 2026-4-24

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Metergoline (CAS 17692-51-2)

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Alternate Names:
N-Cbz-[(8β)-1,6-Dimethylergolin-8-yl]methylamine
Application:
Metergoline is an antagonist at 5-HT1, 5-HT2, and 5-HT7 serotonin receptors
CAS Number:
17692-51-2
Purity:
≥98%
Molecular Weight:
403.52
Molecular Formula:
C25H29N3O2
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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Metergoline is an antagonist at 5-HT1, 5-HT2, and SR-7 (5-HT7) serotonin receptors; also SR-1D (5-HT1D) ligand. Metergoline shows moderate affinity for 5-HT6 and high affinity for 5-HT7.


Metergoline (CAS 17692-51-2) References

  1. Agonist activity of sumatriptan and metergoline at the human 5-HT1D beta receptor: further evidence for a role of the 5-HT1D receptor in the action of sumatriptan.  |  Miller, KJ., et al. 1992. Eur J Pharmacol. 227: 99-102. PMID: 1330643
  2. Effects of various serotonin receptor subtype-selective antagonists alone and on m-chlorophenylpiperazine-induced neuroendocrine changes in rats.  |  Aulakh, CS., et al. 1992. J Pharmacol Exp Ther. 263: 588-95. PMID: 1432690
  3. Pharmacological characterization of serotonin receptor subtypes involved in vasopressin and plasma renin activity responses to serotonin agonists.  |  Bagdy, G., et al. 1992. Eur J Pharmacol. 210: 285-9. PMID: 1535317
  4. Metergoline blocks the behavioral and neuroendocrine effects of orally administered m-chlorophenylpiperazine in patients with obsessive-compulsive disorder.  |  Pigott, TA., et al. 1991. Biol Psychiatry. 29: 418-26. PMID: 2018816
  5. Metergoline-induced cell death in Candida krusei.  |  Kang, K., et al. 2011. Fungal Biol. 115: 302-9. PMID: 21354537
  6. Metergoline inhibits the neuronal Nav1.2 voltage-dependent Na(+) channels expressed in Xenopus oocytes.  |  Lee, JH., et al. 2014. Acta Pharmacol Sin. 35: 862-8. PMID: 24909513
  7. Molecular basis involved in the blocking effect of antidepressant metergoline on C-type inactivation of Kv1.4 channel.  |  Bai, HW., et al. 2019. Neuropharmacology. 146: 65-73. PMID: 30465811
  8. Metergoline Shares Properties with Atypical Antipsychotic Drugs Identified by Gene Expression Signature Screen.  |  Bortolasci, CC., et al. 2023. Neurotox Res. 41: 502-513. PMID: 37922109
  9. Effect of metergoline on human anxiety.  |  Graeff, FG., et al. 1985. Psychopharmacology (Berl). 86: 334-8. PMID: 3929304
  10. Metergoline in the management of hyperprolactinemic amenorrhea and anovulation.  |  Falsetti, L., et al. 1982. Gynecol Obstet Invest. 13: 108-16. PMID: 7035305

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

Metergoline, 10 mg

sc-204079
10 mg
$80.00

Metergoline, 50 mg

sc-204079A
50 mg
$292.00