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Setiptiline maleate is the salt form of Setiptiline.Setiptiline (Org-8282) is a norepinephrine reuptake inhibitor, 2-adrenergic receptor antagonist, H1 receptor inverse agonist, and 5-HT serotonin receptor antagonist with antidepressant activity.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
2 mg | $46 | In Stock | |
1 mL x 10 mM (in DMSO) | $85 | In Stock |
Description | Setiptiline maleate is the salt form of Setiptiline.Setiptiline (Org-8282) is a norepinephrine reuptake inhibitor, 2-adrenergic receptor antagonist, H1 receptor inverse agonist, and 5-HT serotonin receptor antagonist with antidepressant activity. |
In vitro | Setiptiline maleate weakly inhibits norepinephrine reuptake in rat brain synaptosomes, thereby enhancing noradrenergic neurotransmission.[1] In rat brain membrane preparations, Setiptiline maleate blocks presynaptic α2-adrenergic receptors, which facilitates the increased release of norepinephrine and serotonin.[2] In HEK293 cells expressing human 5-HT2A receptors, setiptiline inhibited serotonin-induced calcium influx in a dose-dependent manner.[3] |
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. [4] |
Alias | ORG-8282, ORG8282, MOD-20, MOD20, MO-8282, MO8282 |
Molecular Weight | 377.43 |
Formula | C23H23NO4 |
Cas No. | 85650-57-3 |
Smiles | C(=C\C(O)=O)\C(O)=O.CN1CC2=C(C=3C(CC=4C2=CC=CC4)=CC=CC3)CC1 |
Relative Density. | 1.31g/cm3 |
Storage | keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 80 mg/mL (211.96 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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