| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
| Other Sizes |
| ln Vitro |
Like other 5-HT1A agonists, BMY-14802 hydrochloride modifies 5-HT-mediated behavior in a 5-HT1A-sensitive way by influencing the firing of serotonergic and catecholaminergic neurons. D2 receptors are not significantly favored by BMY-14802 hydrochloride [3].
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| ln Vivo |
BMY-14802 (5 mg/kg, 10 mg/kg, or 20 mg/kg intraperitoneally; once) hydrochloride is effective in decreasing D1 and D2 receptor-induced dyskinesias and demonstrates antidyskinetic activity over a 4-fold dose range in L-DOPA-induced dyskinesia (LID). Crucially, BMY-14802 hydrochloride did not diminish L-DOPA's ability to prevent lesion-induced akinesia when administered at anti-LID dosages [2].
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| Animal Protocol |
6-OHDA Lesion Model:** Male Sprague-Dawley rats received unilateral infusions of 6-OHDA (22.8 μg/2μl per site) into two sites of the right medial forebrain bundle to model Parkinson's disease. Rats with significant hemi-parkinsonism, defined as an average of ≥5 turns/min over 10 minutes in response to amphetamine (5 mg/kg, i.p.), were selected for the study. [1]
* **L-DOPA Treatment and AIM Induction:** Selected rats were treated once daily for 21 days with L-DOPA methyl ester HCl (7.5 mg/kg, i.p.) combined with benserazide (15 mg/kg, i.p.) and ascorbic acid (2.6 mg/kg, i.p.) to induce stable AIM expression. Following this, they were maintained on a regimen of 2 L-DOPA injections per week. [1] * **Drug Testing Protocol:** To test the efficacy of BMY-14802 and other compounds on AIM expression, test drugs were administered during the maintenance phase. BMY-14802 (15 mg/kg), buspirone (1, 4, 10 mg/kg), and other sigma agents were dissolved in either milliQ water, 0.9% saline, or β-cyclodextrin solutions. They were administered intraperitoneally (i.p.) at a volume of 1 ml/100 gm body weight, 30 minutes prior to L-DOPA injection. Finasteride was administered 22 hours prior to L-DOPA at a volume of 5 ml/100 gm body weight to avoid acute motor effects. In the pharmacological reversal studies, the 5-HT1A antagonist WAY-100635 (0.1, 0.5 mg/kg, i.p.) or the α-1 antagonist prazosin (0.1 mg/kg, i.p.) was co-administered with BMY-14802 30 minutes before L-DOPA. [1] * **AIM Assessment:** An investigator blinded to the treatment groups rated the severity of limb, axial, and oral AIMs, as well as contraversive rotation. Ratings were performed every 20 minutes for 3 hours, starting 20 minutes after L-DOPA injection, using a scale of 0-4. A total AIM score (limb + axial + oral) was calculated for analysis. [1] |
| References |
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| Additional Infomation |
See also: Bmy-14802 (Notes moved to).
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| Molecular Formula |
C18H23CLF2N4O
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|---|---|
| Molecular Weight |
384.8558
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| Exact Mass |
384.153
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| CAS # |
105565-55-7
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| PubChem CID |
3086514
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| Appearance |
White to off-white solid powder
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| Boiling Point |
520.8ºC at 760mmHg
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| Flash Point |
268.8ºC
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| Vapour Pressure |
1.13E-11mmHg at 25°C
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| LogP |
3.195
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
26
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| Complexity |
379
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
NIBVEFRJDFVQLM-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H22F2N4O.ClH/c19-15-5-3-14(4-6-15)17(25)2-1-7-23-8-10-24(11-9-23)18-21-12-16(20)13-22-18;/h3-6,12-13,17,25H,1-2,7-11H2;1H
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| Chemical Name |
1-(4-fluorophenyl)-4-[4-(5-fluoropyrimidin-2-yl)piperazin-1-yl]butan-1-ol;hydrochloride
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| Synonyms |
BMS-181100 BMS181100 BMS181100
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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, 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 : ~125 mg/mL (~324.80 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.40 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 20.8 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: ≥ 2.08 mg/mL (5.40 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 20.8 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. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (5.40 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5983 mL | 12.9917 mL | 25.9835 mL | |
| 5 mM | 0.5197 mL | 2.5983 mL | 5.1967 mL | |
| 10 mM | 0.2598 mL | 1.2992 mL | 2.5983 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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