Setiptiline maleate

SKU: orb1708531

Description

Setiptiline maleate is the salt form of Setiptiline, a multi-target agent acting as a norepinephrine reuptake inhibitor, α2-adrenergic antagonist, H1 inverse agonist, and 5-HT antagonist. It is used in research for investigating antidepressant mechanisms and has been studied in both in vivo animal models and in vitro receptor binding assays.

Research Area

Immunology & Inflammation, Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 85650-57-3
• MW: 377.43
• Purity: 99.94%
• Formula: C₂₃H₂₃NO₄
• SMILES: C(=C\C(O)=O)\C(O)=O.CN1CC2=C(C=3C(CC=4C2=CC=CC4)=CC=CC3)CC1
• Target: 5-HT Receptor,Norepinephrine,Adrenergic Receptor,Histamine Receptor
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (8.74 mM);DMSO:80 mg/mL (211.96 mM)

Bioactivity

• In Vivo:
  Setiptiline maleate mildly increased spontaneous motor activity and ambulation in rats (open field test), and enhanced the locomotor stimulation induced by methamphetamine. Setiptiline maleate significantly reduced immobility time in the forced swim test in rats, indicating antidepressant-like properties. Setiptiline maleate inhibited haloperidol-induced catalepsy, physostigmine-induced yawning, 5-HTP + Ro4-4602-induced body shaking and head twitch, and morphine withdrawal-induced body shaking.
• In Vitro:
  Setiptiline maleate weakly inhibits norepinephrine reuptake in rat brain synaptosomes, thereby enhancing noradrenergic neurotransmission. In rat brain membrane preparations, Setiptiline maleate blocks presynaptic α2-adrenergic receptors, which facilitates the increased release of norepinephrine and serotonin. In HEK293 cells expressing human 5-HT2A receptors, setiptiline inhibited serotonin-induced calcium influx in a dose-dependent manner.

Storage & Handling

• Storage: keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

ORG8282, ORG-8282, MO 8282, MO8282, MO-8282, MOD20, MOD-20, Setiptiline Maleate

Compound Identifiers

PubChem CID

5282470