| Bioactivity | Metergoline is a serotonin (5-HT) receptor and dopamine receptors antagonist, with pKis of 8.64, 8.75 and 8.75 for 5-HT2A, 5-HT2B and 5-HT2C, respectively. Metergoline is a high-affinity ligand for the h5-HT7 receptor, with a Ki of 16 nM. Metergoline is also a reversible neural Na+ channels inhibitor. Metergoline is commonly used for the research of seasonal affective disorder, prolactin hormone regulation[1][2][3]. | |||||||||
| Invitro | Metergoline (3 μM) causes a 6.8±1.2 mV depolarizing shift of the steady-state activation curve of the Na+currents, and does not alter the inactivation curve[3]. | |||||||||
| In Vivo | Metergoline (5 mg/kg; i.p.) completely blocks the response to intrathecal 5-HT (2 μg)[4]. Animal Model: | |||||||||
| Name | Metergoline | |||||||||
| CAS | 17692-51-2 | |||||||||
| Formula | C25H29N3O2 | |||||||||
| Molar Mass | 403.52 | |||||||||
| Appearance | Solid | |||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | |||||||||
| Storage |
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| Reference | [1]. Antony R Knight, et al. Pharmacological characterisation of the agonist radioligand binding site of 5-HT(2A), 5-HT(2B) and 5-HT(2C) receptors. Naunyn Schmiedebergs Arch Pharmacol. 2004 Aug;370(2):114-23. [2]. Jessica A. Knight, et al. Pharmacological Analysis of the Novel, Rapid, and Potent Inactivation of the Human 5-Hydroxytryptamine7 Receptor by Risperidone, 9-OH-Risperidone, and Other Inactivating Antagonists. Mol Pharmacol. 2009 Feb; 75(2): 374-380. [3]. Jun-ho Lee, et al. Metergoline inhibits the neuronal Nav1.2 voltage-dependent Na+ channels expressed in Xenopus oocytes. Acta Pharmacol Sin. 2014 Jul; 35(7): 862-868. [4]. P K Eide, et al. The behavioural response to intrathecal serotonin is changed by acute but not by repeated treatment with zimelidine or metergoline. Pharmacol Toxicol. 1991 Nov;69(5):361-4. |
Metergoline
CAS: 17692-51-2 F: C25H29N3O2 W: 403.52
Metergoline is a serotonin (5-HT) receptor and dopamine receptors antagonist, with pKis of 8.64, 8.75 and 8.75 for 5-HT2
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