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Setiptiline

Cat No.:V30083 Purity: ≥98%
Setiptiline (Org-8282) is a serotonin receptor blocker (antagonist).
Setiptiline
Setiptiline Chemical Structure CAS No.: 57262-94-9
Product category: New1
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
50mg
100mg
Other Sizes

Other Forms of Setiptiline:

  • Setiptiline maleate
  • Setiptiline-d3 (Setiptiline-d3)
Official Supplier of:
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Top Publications Citing lnvivochem Products
Product Description
Setiptiline (Org-8282) is a serotonin receptor blocker (antagonist). Setiptiline is a tetracyclic antidepressant compound (TeCA) and a noradrenergic and specific serotonergic antidepressant compound (NaSSA). Setiptiline works as a norepinephrine reuptake inhibitor, 2-adrenergic receptor blocker (antagonist) and 5-HT2A, 5-HT2C and/or 5-HT3 subtype serotonin receptor blocker (antagonist), and H1 receptor inverse agonist /Antihistamines.
Biological Activity I Assay Protocols (From Reference)
References

[1]. Yamada K, Furukawa T. [Behavioral effects of a new antidepressant, setiptiline]. Nihon Yakurigaku Zasshi. 1991 Jan;97(1):31-9.

[2]. The effect of age on plasma level of setiptiline maleate in depressed patients. Prog Neuropsychopharmacol Biol Psychiatry. 1994 Oct;18(6):1015-26.

[3]. Kuniyoshi M, Nakamura J, Miura C, Inanaga K. Effectiveness of concomitant setiptiline maleate (Tecipul) on negative symptoms of schizophrenia. Prog Neuropsychopharmacol Biol Psychiatry. 1994 Mar;18(2):339-46.

[4]. Niho T, Ito C, Shibutani Y, Hashizume H, Yamaguchi K. [Pharmacological properties of MO-8282, a novel antidepressant]. Nihon Yakurigaku Zasshi. 1986 Oct;88(4):309-20.

Additional Infomation
Setiptiline is a tetracyclic antidepressant that is 2,3,4,9-tetrahydro-1H-dibenzo[3,4:6,7]cyclohepta[1,2-c]pyridine carrying a methyl group at position 2. Its maleate salt is used for the treatment of depression in Japan. It has a role as an alpha-adrenergic antagonist and a serotonergic antagonist. It is a tetracyclic antidepressant and a tertiary amino compound. It is a conjugate base of a setiptiline(1+).
Setiptiline is a tetracyclic antidepressant (TeCA) which acts as a noradrenergic and specific serotonergic antidepressant (NaSSA). In Japan, the company Mochida started its commercialization for the treatment of depression started in 1989.
Drug Indication
For the treatment of depression.
Mechanism of Action
Setiptiline is an antagonist at the α2 adrenergic receptor and at serotonin receptors. The antagonism of the α2 receptors likely relieves presynaptic inhibition of adrenergic neurotransmission, allowing for greater and longer sustained release of noradrenaline into the synapse. The antagonism of serotonin receptors may produce an upregulation of the receptors leading to an eventual increase in serotonergic signalling. The actual physiological mechanisms behind the antidepressant effect of setiptiline is unknown but the listed possibilities exist as likely explanations.
Pharmacodynamics
Setiptiline is a tertacyclic antidepressant. It acts to reduce the symptoms of major depressive disorder.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C19H19N
Molecular Weight
261.36086
Exact Mass
261.152
CAS #
57262-94-9
Related CAS #
Setiptiline maleate;85650-57-3;Setiptiline-d3;1795024-97-3
PubChem CID
5205
Appearance
White to off-white solid powder
Density
1.15
Boiling Point
421.7ºC at 760mmHg
Flash Point
185.5ºC
Index of Refraction
1.656
LogP
3.775
Hydrogen Bond Donor Count
0
Hydrogen Bond Acceptor Count
1
Rotatable Bond Count
0
Heavy Atom Count
20
Complexity
397
Defined Atom Stereocenter Count
0
InChi Key
GVPIXRLYKVFFMK-UHFFFAOYSA-N
InChi Code
InChI=1S/C19H19N/c1-20-11-10-18-16-8-4-2-6-14(16)12-15-7-3-5-9-17(15)19(18)13-20/h2-9H,10-13H2,1H3
Chemical Name
4-methyl-4-azatetracyclo[13.4.0.02,7.08,13]nonadeca-1(19),2(7),8,10,12,15,17-heptaene
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO : ~25 mg/mL (~95.65 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.5 mg/mL (9.57 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 3.8261 mL 19.1307 mL 38.2614 mL
5 mM 0.7652 mL 3.8261 mL 7.6523 mL
10 mM 0.3826 mL 1.9131 mL 3.8261 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

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What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

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