| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| Other Sizes |
|
| ln Vitro |
Spinamide has a poor affinity for the dopamine D1 site (Ki=2530 nM), but it maintains affinity for the 5-HT1A site (Ki=50 nM) and binds to the dopamine D2 site (Ki=3 nM) [1].
|
|---|---|
| ln Vivo |
In monkeys following a fixed interval (FI) stimulus termination regimen, AMI-193 (0.003-0.01 mg/kg; im) dose-dependently lowers response rates [2]. In drug discrimination studies, the discriminative stimulus effect of cocaine is attenuated by AMI-193 (0.003-0.01 mg/kg; im) [2]. When administered intramuscularly, AMI-193 (0.003-0.01 mg/kg) lowers the rate of remission when combined with an intravenous cocaine regimen (0.1 mg/infusion) [2].
|
| Animal Protocol |
Animal/Disease Models: Adult male squirrel monkey (850-1300 g) [2]
Doses: 0.003, 0.01 mg/kg Route of Administration: intramuscularinjection on Tuesday, Wednesday and Thursday next week Experimental Results: diminished response rate. Cocaine reversed the heart-rate-lowering effects. |
| References |
|
| Additional Infomation |
Spiramide is an azaspiro compound that consists of 1,3,8-triazaspiro[4.5]decan-4-one having a phenyl group attached to N-1 and a 3-(4-fluorophenoxy)propyl attached to N-8. Selective 5-HT antagonist, which binds to 5-HT2 sites as potently as spiperone but has lower affinity for 5-HT2C receptors. Also a high affinity D2 receptor antagonist (Ki = 3 nM). Lacks the disruptive effect of spiperone on animal behaviour. It has a role as a dopaminergic antagonist and a serotonergic antagonist. It is an azaspiro compound, an organofluorine compound, an aromatic ether, a tertiary amino compound and a member of piperidines.
Spiramide has been reported in Spiraea japonica with data available. |
| Molecular Formula |
C22H26FN3O2
|
|---|---|
| Molecular Weight |
383.46
|
| Exact Mass |
383.201
|
| CAS # |
510-74-7
|
| Related CAS # |
3824-91-7 (mono-hydrochloride salt)
|
| PubChem CID |
68186
|
| Appearance |
White to off-white solid powder
|
| Density |
1.26 g/cm3
|
| Boiling Point |
609.1ºC at 760 mmHg
|
| Flash Point |
322.2ºC
|
| Index of Refraction |
1.621
|
| LogP |
3.354
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
6
|
| Heavy Atom Count |
28
|
| Complexity |
510
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
FJUKDAZEABGEIH-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C22H26FN3O2/c23-18-7-9-20(10-8-18)28-16-4-13-25-14-11-22(12-15-25)21(27)24-17-26(22)19-5-2-1-3-6-19/h1-3,5-10H,4,11-17H2,(H,24,27)
|
| Chemical Name |
8-[3-(4-fluorophenoxy)propyl]-1-phenyl-1,3,8-triazaspiro[4.5]decan-4-one
|
| Synonyms |
R-5808; R 5808; Spiramide
|
| 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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~20 mg/mL (~52.16 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2 mg/mL (5.22 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 20.0 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. Solubility in Formulation 2: 2 mg/mL (5.22 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline 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 | 2.6078 mL | 13.0392 mL | 26.0783 mL | |
| 5 mM | 0.5216 mL | 2.6078 mL | 5.2157 mL | |
| 10 mM | 0.2608 mL | 1.3039 mL | 2.6078 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.
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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
