2. GPCR/G Protein Neuronal Signaling
  3. 5-HT Receptor G protein-coupled Bile Acid Receptor 1
  4. 2-Bromo-LSD D-Tartrate

2-Bromo-LSD D-Tartrate  (Synonyms: BOL-148 D-Tartrate; Bromolysergide D-Tartrate)

Cat. No.: HY-121675A Purity: 99.91%
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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.

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2-Bromo-LSD D-Tartrate

2-Bromo-LSD D-Tartrate Chemical Structure

CAS No. : 2855123-30-5

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Other Forms of 2-Bromo-LSD D-Tartrate:

2-Bromo-LSD D-Tartrate Related Antibodies

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Description

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[1][2].

IC50 & Target[1]

5-HT2A Receptor

0.81 nM (EC50)

5-HT2A Receptor

0.18 nM (Kb)

In Vitro

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 Related Antibodies
In Vivo

2-Bromo-LSD D-Tartrate (0.125-4 mg/kg; i.p.) dose-dependently increases striatal DOPA accumulation in rats, with maximum effects at 2-4 mg/kg that exceed those of equimolar LSD, acts as an antagonist of Apomorphine (HY-12723)-induced DOPA accumulation reduction, and blocks LSD's inhibitory effect on GBL-stimulated DOPA accumulation[1].
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.

Animal Model: Sprague-Dawley (male, 188-298 g)[1]
Dosage: 0.125 mg/kg; 0.250 mg/kg; 0.5 mg/kg; 2 mg/kg; 4 mg/kg
Administration: i.p.; single dose; 30 minutes before sacrifice
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.
Animal Model: C57BL/6J (male and female, 7-8 weeks old)[2]
Dosage: 0.3 mg/kg; 1.0 mg/kg; 3.0 mg/kg
Administration: three dose
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).
Molecular Weight

477.39

Formula

C20H24BrN3O·1/2C4H6O6
CAS No.
Appearance

Solid

Color

Light yellow to brown

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]
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0947 mL 10.4736 mL 20.9472 mL
5 mM 0.4189 mL 2.0947 mL 4.1894 mL
View the 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.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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C2

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In Vivo:

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.

  • Protocol 1

    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.
  • Protocol 2

    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.
In Vivo Dissolution Calculator
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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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: 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)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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
References

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
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2-Bromo-LSD D-Tartrate Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

2-Bromo-LSD2855123-30-5BOL-148BromolysergideBOL148BOL 1485-HT ReceptorG protein-coupled Bile Acid Receptor 1Serotonin Receptor5-hydroxytryptamine ReceptorG-protein coupled receptor 19GPCR19TGR5GPBAR1primary rat cortical neuronshuman 5-HT7a receptorshuman Nav1.5 sodium channelsmale C57BL/6J micehuman hERG channelshuman 5-HT2A receptorshuman α2C adrenergic receptorshuman 5-HT6 receptorshuman D4 receptorshuman D2 receptorsInhibitorinhibitorinhibit

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