2-Bromo-LSD D-Tartrate
Based on 1 Customer Validation
2-Bromo-LSD D-Tartrate (BOL-148 D-Tartrate) is a blood-brain barrier-permeable 5-HT2A partial agonist and competitive partial antagonist. 2-Bromo-LSD D-Tartrate acts as both a potent partial agonist (with an EC50 of 0.81 nM for Gq dissociation) and a potent partial antagonist (with a KB of 0.18 nM for Gq dissociation) at the 5-HT2A receptor. 2-Bromo-LSD D-Tartrate exhibits partial agonist activity at multiple aminergic GPCRs, including 5-HT2A. 2-Bromo-LSD D-Tartrate lacks 5-HT2B agonist activity. 2-Bromo-LSD D-Tartrate induces dendritogenesis and spinogenesis. 2-Bromo-LSD D-Tartrate reverses the behavioral effects of chronic stress and increases active coping behaviors in mice.
For research use only. We do not sell to patients.
- Purity: 99.91%
- CAS No.: 2855123-30-5
- Formula: C20H24BrN3O·1/2C4H6O6
- Molecular Weight:477.39
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Storage:
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
All 5-HT Receptor Isoforms
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Biological Activity
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5-HT2A Receptor 0.81 nM (EC50) |
5-HT2A Receptor 0.18 nM (Kb) |
2-Bromo-LSD D-Tartrate acts as both a potent partial agonist (EC50 = 0.81 nM, Eₘₐₓ = 59.8% for Gq dissociation) and a potent partial antagonist (KB = 0.18 nM for Gq dissociation) at the 5-HT2A receptor[2].
2-Bromo-LSD D-Tartrate exerts weak blocking effects on hERG channels (IC50 = 31.6 μM)[2].
2-Bromo-LSD D-Tartrate (1-10 μM; 3 h) promotes dendrogenesis and dendritic spine density in primary rat cortical neurons[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
2-Bromo-LSD D-Tartrate (0.125-2.0 mg/kg; i.p.) co-administered with LSD does not produce a statistically significant change in striatal DOPA accumulation compared to 2-Bromo-LSD D-Tartrate alone at matching doses[1].
2-Bromo-LSD D-Tartrate (0.1-10 mg/kg; i.p.; single dose) does not induce the hallucinogen-associated head-twitch response in male C57BL/6J mice, but dose-dependently blocks DOI-induced head-twitch responses, achieving 76% inhibition at the 3 mg/kg dose[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley (male, 188-298 g)[1]
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Dosage:0.125 mg/kg; 0.250 mg/kg; 0.5 mg/kg; 2 mg/kg; 4 mg/kg
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Administration:i.p.; single dose; 30 minutes before sacrifice
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Result:Increased striatal DOPA accumulation to 1386 ± 106 ng/g (n=6), significantly higher than saline control (1042 ± 77 ng/g, p<0.001) at 0.125 mg/kg.
Increased striatal DOPA accumulation to 1951 ± 380 ng/g (n=6), significantly higher than saline control (p<0.001) at 0.250 mg/kg.
Increased striatal DOPA accumulation to 1924 ± 131 ng/g (n=9), significantly higher than saline control (p<0.001) at 0.5 mg/kg; restored apomorphine (0.5 mg/kg)-reduced DOPA accumulation to 781 ± 28 ng/g from 472 ± 51 ng/g, and apomorphine (5 mg/kg)-reduced levels to 594 ± 42 ng/g from 249 ± 31 ng/g; showed no effect on reserpine-induced increased DOPA accumulation (2465 ± 243 ng/g vs.
2618 ± 136 ng/g, p=N.S.) and did not inhibit GBL-induced increased DOPA accumulation.
Increased striatal DOPA accumulation to 2630 ± 169 ng/g (n=6), significantly higher than saline control (p<0.001) at 2 mg/kg; produced larger maximum increase than equimolar LSD; restored apomorphine (0.5 mg/kg)-reduced DOPA accumulation to 2888 ± 111 ng/g from 472 ± 51 ng/g (levels not significantly different from BOL 2 mg/kg alone), and apomorphine (5 mg/kg)-reduced levels to 828 ± 190 ng/g from 249 ± 31 ng/g; showed no effect on haloperidol-induced or reserpine-induced increased DOPA accumulation, did not inhibit cerebral hemisection-induced increased DOPA accumulation on the sectioned side (1915 ± 215 ng/g vs.
2647 ± 400 ng/g, p=N.S.) but increased levels on the unsectioned side to 2058 ± 158 ng/g from 901 ± 232 ng/g (p<0.02); blocked LSD-induced inhibition of GBL-stimulated DOPA accumulation.
Significantly increased striatal DOPA accumulation compared to saline control and produced larger maximum increase than equimolar LSD at 4 mg/kg.
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Animal Model:C57BL/6J (male and female, 7-8 weeks old)[2]
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Dosage:0.3 mg/kg; 1.0 mg/kg; 3.0 mg/kg
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Administration:three dose
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Result:Increased time spent in the center of the OFT by 88.18 ± 18.89 seconds (female, 1.0 mg/kg) and showed a non-significant trend (female, 3.0 mg/kg).
Reduced FST immobility time by 35.18 ± 10.03 seconds (female, 1.0 mg/kg), 20.89 ± 8.249 seconds (male, 0.3 mg/kg), 27.27 ± 8.226 seconds (male, 1.0 mg/kg), and 31.36 ± 8.226 seconds (male, 3.0 mg/kg).
Showed a non-significant trend toward increased center time in the OFT (male, all doses).
Increased average PFC spine density compared to vehicle controls (both sexes, 1.0 mg/kg).
Chemical Information
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CAS No. 2855123-30-5
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Appearance Solid
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Molecular Weight 477.39
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Formula C20H24BrN3O·1/2C4H6O6
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Color Light yellow to brown
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SMILES
OC([C@@H](O)[C@H](O)C(O)=O)=O.BrC1=C2C3=C(N1)C=CC=C3C4=C[C@@H](C(N(CC)CC)=O)CN(C)[C@]4([H])C2.[1/2]
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Synonyms
BOL-148 D-Tartrate; Bromolysergide D-Tartrate
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Solvent & Solubility
DMSO : 100 mg/mL (209.47 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.24 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.24 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (284 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Persson SA, et al. The effect of LSD and 2-bromo LSD on the striatal DOPA accumulation after decarboxylase inhibition in rats. Eur J Pharmacol. 1977;43(1):73-83. [Content Brief]
[2]. Lewis V, et al. A non-hallucinogenic LSD analog with therapeutic potential for mood disorders. Cell Rep. 2023;42(3):112203. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.0947 mL | 10.4736 mL | 20.9472 mL | 52.3681 mL |
| 5 mM | 0.4189 mL | 2.0947 mL | 4.1894 mL | 10.4736 mL | |
| 10 mM | 0.2095 mL | 1.0474 mL | 2.0947 mL | 5.2368 mL | |
| 15 mM | 0.1396 mL | 0.6982 mL | 1.3965 mL | 3.4912 mL | |
| 20 mM | 0.1047 mL | 0.5237 mL | 1.0474 mL | 2.6184 mL | |
| 25 mM | 0.0838 mL | 0.4189 mL | 0.8379 mL | 2.0947 mL | |
| 30 mM | 0.0698 mL | 0.3491 mL | 0.6982 mL | 1.7456 mL | |
| 40 mM | 0.0524 mL | 0.2618 mL | 0.5237 mL | 1.3092 mL | |
| 50 mM | 0.0419 mL | 0.2095 mL | 0.4189 mL | 1.0474 mL | |
| 60 mM | 0.0349 mL | 0.1746 mL | 0.3491 mL | 0.8728 mL | |
| 80 mM | 0.0262 mL | 0.1309 mL | 0.2618 mL | 0.6546 mL | |
| 100 mM | 0.0209 mL | 0.1047 mL | 0.2095 mL | 0.5237 mL |
2-Bromo-LSD D-Tartrate Related Classifications
HY-121675A Related Classifications
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- 2-Bromo-LSD
- 2855123-30-5
- BOL-148
- Bromolysergide
- BOL148
- BOL 148
- 5-HT Receptor
- G protein-coupled Bile Acid Receptor 1
- primary rat cortical neurons
- human 5-HT7a receptors
- human Nav1.5 sodium channels
- male C57BL/6J mice
- human hERG channels
- human 5-HT2A receptors
- human α2C adrenergic receptors
- human 5-HT6 receptors
- human D4 receptors
- human D2 receptors
- Inhibitor
- inhibitor
- inhibit