[CAS NO. 17692-51-2] Metergoline

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PRODUCTS SPECIFICATIONS [17692-51-2]

Catalog

AS164051

Brand

Arctom Scientific

CAS

17692-51-2

DESCRIPTION [17692-51-2]

Overview

MDL	MFCD00153829
Molecular Weight	403.52
Molecular Formula	C25H29N3O2
SMILES	O=C(OCC1=CC=CC=C1)NC[C@H](C[C@@]23[H])CN(C)[C@]2([H])CC4=CN(C)C5=CC=CC3=C54

For research use only. We do not sell to patients.

Summary

Metergoline is a serotonin (5-HT) receptor and dopamine receptors antagonist, with pK _i s of 8.64, 8.75 and 8.75 for 5-HT _2A , 5-HT _2B and 5-HT _2C , respectively. Metergoline is a high-affinity ligand for the h5-HT ₇ receptor, with a K _i 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] .

IC50 & Target

5-HT _2A Receptor

8.64 (pKi)

5-HT _2B Receptor

8.75 (pKi)

5-HT _2C Receptor

8.75 (pKi)

Human 5-HT ₇ Receptor

16 nM (Ki)

In Vitro

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] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Metergoline (5 mg/kg; i.p.) completely blocks the response to intrathecal 5-HT (2 μg) ^[4] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male albino mice (25-40 g) ^[4]
Dosage:	5 mg/kg
Administration:	Intraperitoneal injection
Result:	Inhibited bites or scratches induced by 5-HT (2 μg).

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 125 mg/mL ( 309.77 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.4782 mL	12.3910 mL	24.7819 mL
5 mM	0.4956 mL	2.4782 mL	4.9564 mL
10 mM	0.2478 mL	1.2391 mL	2.4782 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.08 mg/mL (5.15 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.08 mg/mL (5.15 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.08 mg/mL (5.15 mM); Clear solution

* All of the co-solvents are available by MCE.

References

Synonyms

Carbamic acid, N-[[(8β)-1,6-dimethylergolin-8-yl]methyl]-, phenylmethyl ester

Carbamic acid, [(1,6-dimethylergolin-8β-yl)methyl]-, benzyl ester

Carbamic acid, [[(8β)-1,6-dimethylergolin-8-yl]methyl]-, phenylmethyl ester

Lysergamine, N-carboxy-9,10-dihydro-1-methyl-, benzyl ester

Indolo[4,3-fg]quinoline, carbamic acid deriv.

Ergoline, carbamic acid deriv.

(+)-N-Carboxy-1-methyl-9,10-dihydrolysergamide benzyl ester

Metergoline

8β-Carbobenzyloxyaminomethyl-1,6-dimethyl-10α-ergoline

Methergoline

AHR 3009

D-8β-[(Carbobenzoxyamino)methyl]-1,6-dimethyl-10α-ergoline

D-N-Carbobenzoxydihydro-1-methyllysergamine I

D-8β-[(Carboxyamino)methyl]-1,6-dimethylergoline I benzyl ester

D-N-Carboxydihydro-1-methyllysergamine I benzyl ester

D-[(4,6,6a,7,8,9,10,10a-Octahydro-4,7-dimethyl-10aα-indolo[4,3-fg]quinolin-9β-yl)methyl]carbamic acid benzyl ester

Liserdol

Metergolin

MCE

Contralac

FI 6337