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| Targets |
Spiramide is a potent and selective antagonist of 5-HT2 and dopamine D2 receptors. It has Ki values of 2 nM for 5-HT2, 3 nM for D2, 50 nM for 5-HT1A, 2530 nM for D1, and 4300 nM for 5-HT1C receptors. Spiramide shows >2000-fold selectivity for 5-HT2 versus 5-HT1C receptors. Its mechanism involves competitive antagonism at serotonin and dopamine receptors, contributing to its antipsychotic activity.
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| 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].
In vitro, Spiramide is a potent and selective antagonist of 5-HT2 and dopamine D2 receptors. It has Ki values of 2 nM for 5-HT2, 3 nM for D2, 50 nM for 5-HT1A, 2530 nM for D1, and 4300 nM for 5-HT1C receptors. Its in vitro activity is characterized by high affinity for 5-HT2 and D2 receptors and low affinity for D1 and 5-HT1C receptors. Spiramide shows antipsychotic activity. |
| 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].
In vivo, Spiramide has been studied for its antipsychotic activity. In adult male squirrel monkeys, AMI-193 (0.003 and 0.01 mg/kg; i.m.) dose-dependently reduced response rates under a fixed-interval schedule of stimulus termination and reduced response rates under a second-order schedule of intravenous cocaine self-administration. AMI-193 attenuated the discriminative stimulus effects of cocaine. These findings demonstrate its in vivo activity at dopamine and serotonin receptors. |
| Enzyme Assay |
In vitro enzyme/receptor binding assays for Spiramide typically involve radioligand binding studies using membrane preparations expressing 5-HT2, D2, 5-HT1A, D1, or 5-HT1C receptors. The compound's affinity for these receptors is determined by measuring its ability to displace specific radioligands. Ki values are 2, 3, 50, 2530, and 4300 nM for 5-HT2, D2, 5-HT1A, D1, and 5-HT1C receptors, respectively. These assays confirm its mechanism of action as a receptor antagonist.
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| Cell Assay |
In vitro cellular assays for Spiramide typically involve treating cells expressing serotonin or dopamine receptors with the compound and measuring receptor-mediated signaling pathways. The compound antagonizes 5-HT2 and D2 receptor signaling. These cell-based studies demonstrate its functional antagonism at these receptors. Spiramide is used as a pharmacological tool in cellular assays to study serotonin and dopamine receptor function.
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| 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. In vivo animal models for Spiramide typically involve studying its effects on serotonin and dopamine receptor-mediated behaviors. In adult male squirrel monkeys, AMI-193 (0.003 and 0.01 mg/kg; i.m.) dose-dependently reduced response rates under a fixed-interval schedule and reduced response rates under a second-order schedule of intravenous cocaine self-administration. AMI-193 attenuated the discriminative stimulus effects of cocaine. These studies demonstrate its in vivo activity. |
| ADME/Pharmacokinetics |
Spiramide has a molecular weight of 383.46 and a molecular formula of C22H26FN3O2. It is soluble in DMSO (20.7 mg/mL). The compound is typically stored as a powder at -20°C for 3 years. Its CAS number is 510-74-7. Spiramide is also known as AMI-193 and Espiramida. It is an experimental antipsychotic that acts as a selective antagonist for serotonin and dopamine receptors.
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| Toxicity/Toxicokinetics |
Spiramide is a selective antagonist of 5-HT2 and dopamine D2 receptors with a well-characterized mechanism of action. As with any receptor antagonist, potential toxicity may include effects on serotonergic and dopaminergic signaling pathways. The compound's safety profile should be evaluated in preclinical toxicology studies. Spiramide is for research use only and is not approved for human therapeutic use.
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| References |
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| Additional Infomation |
Spinorphin is an azaspirocyclic compound composed of 1,3,8-triazaspiro[4.5]decane-4-one, with a phenyl group at the N-1 position and a 3-(4-fluorophenoxy)propyl group at the N-8 position. It is a selective 5-HT receptor antagonist, binding effectively to 5-HT2 receptors like spiroperon, but with lower affinity for 5-HT2C receptors. It is also a high-affinity D2 receptor antagonist (Ki = 3 nM). Unlike spiroperon, Spinorphin does not interfere with animal behavior. It functions as both a dopaminergic and serotonergic antagonist. It is an azaspirocyclic compound, an organofluorine compound, an aromatic ether, a tertiary amine compound, and a piperidine compound. Spinorphin has been reported to be found in Spiraea japonica, and relevant data exist.
Spiramide (CAS# 510-74-7), also known as AMI-193, is a potent and selective antagonist of 5-HT2 and dopamine D2 receptors. It has Ki values of 2, 3, 50, 2530, and 4300 nM for 5-HT2, D2, 5-HT1A, D1, and 5-HT1C receptors, respectively. Spiramide shows antipsychotic activity and has >2000-fold selectivity for 5-HT2 versus 5-HT1C receptors. The compound is for research use only and not for human therapeutic use. |
| Molecular Formula |
C22H26FN3O2
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| Molecular Weight |
383.46
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| Exact Mass |
383.201
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| CAS # |
510-74-7
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| Related CAS # |
3824-91-7 (mono-hydrochloride salt)
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| PubChem CID |
68186
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| Appearance |
White to off-white solid powder
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| Density |
1.26 g/cm3
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| Boiling Point |
609.1ºC at 760 mmHg
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| Flash Point |
322.2ºC
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| Index of Refraction |
1.621
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| LogP |
3.354
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
28
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| Complexity |
510
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
FJUKDAZEABGEIH-UHFFFAOYSA-N
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| 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)
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| Chemical Name |
8-[3-(4-fluorophenoxy)propyl]-1-phenyl-1,3,8-triazaspiro[4.5]decan-4-one
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| Synonyms |
R-5808; R 5808; Spiramide
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO : ~20 mg/mL (~52.16 mM)
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| 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.
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