1. GPCR/G Protein
    Neuronal Signaling
  2. Melatonin Receptor
    5-HT Receptor
  3. Agomelatine (L(+)-Tartaric acid)

Agomelatine (L(+)-Tartaric acid) (Synonyms: S-20098 L(+)-Tartaric acid)

Cat. No.: HY-17038B
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Agomelatine L(+)-Tartaric acid (S-20098 L(+)-Tartaric acid) is a specific agonist of MT1 and MT2 receptors with Kis of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively. Agomelatine L(+)-Tartaric acid is a selective 5-HT2C receptor antagonist with pKis of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively.

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

Agomelatine (L(+)-Tartaric acid) Chemical Structure

Agomelatine (L(+)-Tartaric acid) Chemical Structure

CAS No. : 824393-18-2

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Description

Agomelatine L(+)-Tartaric acid (S-20098 L(+)-Tartaric acid) is a specific agonist of MT1 and MT2 receptors with Kis of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively[1]. Agomelatine L(+)-Tartaric acid is a selective 5-HT2C receptor antagonist with pKis of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively[2].

IC50 & Target

Ki: 0.1 nM (CHO-hMT1), 0.06 nM (HEK-hMT1), 0.12 nM (CHO-hMT2), and 0.27 nM (HEK-hMT2)[1]
pKi: 6.4 (native porcine 5-HT2C receptor), 6.2 (human 5-HT2C receptor)[2]

In Vitro

Agomelatine (S 20098) acts as a full agonist of MT1 and MT2 receptors with EC50s of 1.6±0.4, 0.10±0.04 nM for CHO hMT1 CHO-hMT2 (hΜΤ1 and hΜΤ2 receptors expressed in CHO or HEK cell membranes)[1].
Agomelatine (S20098) also interacts with h5-HT2B receptors (6.6), whereas it shows low affinity at native (rat)/cloned, human 5-HT2A (<5.0/5.3) and 5-HT1A (<5.0/5.2) receptors, and negligible (<5.0) affinity for other 5-HT receptors[2].

In Vivo

Agomelatine (25, 50, or 75 mg/kg; i.p.) has antioxidant activity in Strychnine (75 mg/kg, i.p.) or Pilocarpine (400 mg/kg, i.p.) induced seizure models in mice. Agomelatine dose not have any antioxidant effects on parameters of oxidative stress produced by Pentylenetetrazole (PTZ) or Picrotoxin (PTX) induced seizure models when compared to controls[3].

Animal Model: Female Swiss mice (20-30 g) were administered PTZ (85 mg/kg, i.p.), PTX (7 mg/kg, i.p.), strychnine (75 mg/kg, i.p.), Pilocarpine (400 mg/kg, i.p.), respectively[3]
Dosage: 25, 50, or 75 mg/kg
Administration: Administered intraperitoneally (i.p.)
Result: All dosages showed a significant decrease in thiobarbituric acid reactive substances (TBARS) levels and nitrite content in all brain areas when compared to controls in the Pilocarpine induced seizure model.
All dosages decreased TBARS levels in all brain areas, and at low doses (25 or 50 mg/kg) decreased nitrite contents, but only at 25 or 50 mg/kg showed a significant increase in catalase activity in three brain areas when compared to controls in the Strychnine-induced seizure model.
Did not have any antioxidant effects on parameters of oxidative stress produced by PTX- or PTZ-induced seizure models when compared to controls.
Clinical Trial
Molecular Weight

393.39

Formula

C₁₉H₂₃NO₈

CAS No.

824393-18-2

SMILES

CC(NCCC1=C2C=C(OC)C=CC2=CC=C1)=O.O=C(O)[[email protected]](O)[[email protected]@H](O)C(O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

Agomelatine (L(+)-Tartaric acid)S-20098 L(+)-Tartaric acidMelatonin Receptor5-HT ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorMT1MT2Agonist5-HT2CAntagonistdepressivedisorderantidepressantInhibitorinhibitorinhibit

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