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Adoprazine

Cat No.:V10365 Purity: ≥98%
Adoprazine (SLV313) is a full agonist of the 5-HT 1A receptor with pEC50 of 9 at the h5-HT1A receptor.
Adoprazine
Adoprazine Chemical Structure CAS No.: 222551-17-9
Product category: New1
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
5mg
10mg
50mg
Other Sizes
Official Supplier of:
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Product Description
Adoprazine (SLV313) is a full agonist of the 5-HT 1A receptor with pEC50 of 9 at the h5-HT1A receptor. Adoprazine (SLV313) is a complete antagonist of D2 and D3 receptors, with pA2 values of 9.3 at hD2 receptors and 8.9 at hD3 receptors. Adoprazine (SLV313) has atypical antipsychotic properties.
Biological Activity I Assay Protocols (From Reference)
ln Vitro
Adoprazine (SLV313) SLV313) exhibits a strong affinity for human recombinant D2, D3, D4, 5-HT2B, and 5-HT1A receptors, with pKs of 8.4, 8.4, 8.0, 7.9 and 9.1 respectively [1]. Adoprazine (SLV313) has a pKB value of 8.5 and an Emax value (% impact of 10 μM 5-HT) of 73, making it a highly potent serotonin 5-HT1A receptor agonist as well as a highly potent antagonist of the dopamine D2 receptor [2].
ln Vivo
Adorazine (SLV313) (0.1-10 mg/kg; oral; single dosage) is adequate to lower extracellular 5-HT and enhance dopamine levels in the nucleus accumbens in a dose- and time-dependent manner [1].
Animal Protocol
Animal/Disease Models: Male Wistar rat (275-350 g) [1]
Doses: 0.1 mg/kg, 0.3 mg/kg, 1 mg/kg, 3 mg/kg, 10 mg/kg
Route of Administration: Oral; single outcome
Experimental Results: Causes a dose- and time-dependent increase in extracellular DA, DOPAC and HVA levels. On the contrary, it resulted in a decrease in 5-HT levels without a change in 5-HIAA levels.
References
[1]. Andrew C McCreary, et al. SLV313 (1-(2,3-dihydro-benzo[1,4]dioxin-5-yl)-4- [5-(4-fluoro-phenyl)-pyridin-3-ylmethyl]-piperazine monohydrochloride): a novel dopamine D2 receptor antagonist and 5-HT1A receptor agonist potential antipsychotic drug. Neuropsych
[2]. Liesbeth A Bruins Slot, et al. Differential profile of antipsychotics at serotonin 5-HT1A and dopamine D2S receptors coupled to extracellular signal-regulated kinase. Eur J Pharmacol. 2006 Mar 18;534(1-3):63-70.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C24H24N3O2F
Molecular Weight
405.46466
Exact Mass
405.185
CAS #
222551-17-9
PubChem CID
9887537
Appearance
Light yellow to yellow solid powder
LogP
3.984
Hydrogen Bond Donor Count
0
Hydrogen Bond Acceptor Count
6
Rotatable Bond Count
4
Heavy Atom Count
30
Complexity
537
Defined Atom Stereocenter Count
0
SMILES
FC1=CC=C(C2=CN=CC(CN3CCN(C4=C5OCCOC5=CC=C4)CC3)=C2)C=C1
InChi Key
IUVSEUFHPNITEQ-UHFFFAOYSA-N
InChi Code
InChI=1S/C24H24FN3O2/c25-21-6-4-19(5-7-21)20-14-18(15-26-16-20)17-27-8-10-28(11-9-27)22-2-1-3-23-24(22)30-13-12-29-23/h1-7,14-16H,8-13,17H2
Chemical Name
1-(2,3-dihydro-1,4-benzodioxin-5-yl)-4-[[5-(4-fluorophenyl)pyridin-3-yl]methyl]piperazine
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 : ~50 mg/mL (~123.32 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 30 mg/mL (73.99 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 300.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

Solubility in Formulation 2: ≥ 3 mg/mL (7.40 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (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 30.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.4663 mL 12.3317 mL 24.6633 mL
5 mM 0.4933 mL 2.4663 mL 4.9327 mL
10 mM 0.2466 mL 1.2332 mL 2.4663 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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g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

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.

Biological Data
  • The effect of SLV313 on dopamine D2, D3 and 5-HT1A receptors. Upper panel: quinpirole alone (open circles) completely attenuated forskolin-induced accumulation of cAMP in CHO cells transfected with the D2 receptor with a pEC50 of 6.8. SLV313 (closed circles) concentration dependently antagonized quinpirole (1 μM) effects (pA2 of 9.3±0.3). Middle panel: in D3 receptor-transfected cells SLV313 possessed antagonist properties in the presence of dopamine (0.3 μM), using a GTPγS assay (filled circles; pA2 of 8.9±0.2; dopamine alone was also tested for control purposes open triangles). Lower panel: in CHO cells transfected with the 5-HT1A receptor SLV313 concentration dependently reduced forskolin-stimulated cAMP production in a concentration-dependent manner (filled circles; pEC50 of 9.0±0.2), similar to the 5-HT1A receptor agonist 8-OHDPAT (filled squares). All graphs demonstrate percentage difference from control and means±SEM from at least triplicate experiments, where SEM are not visible the symbols obscure the SEM.
  • SLV313 and haloperidol dose dependently attenuated climbing behavior induced by the dopamine agonist apomorphine (1 mg/kg s.c.). The ED50 for SLV313 was 0.41 (0.30–056) mg/kg p.o. and for haloperidol 0.10 (0.08–0.15) mg/kg p.o. *p<0.05 cf. control data are expressed as percent control (100%). Data shown are means±SEM.
  • The effect of SLV313 in a flesinoxan drug discrimination procedure. Upper panel: SLV313 (open circles) fully generalized to the flesinoxan-appropriate key in pigeons trained to discriminate flesinoxan from vehicle. In antagonist tests, WAY100635 antagonized the effects of SLV313 (filled circles). Lower panel: in either study the response rates were not affected.
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