2-Bromo-LSD
Based on 1 Customer Validation
2-Bromo-LSD (BOL-148) is a blood-brain barrier-permeable 5-HT2A partial agonist and competitive partial antagonist. 2-Bromo-LSD 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 exhibits partial agonist activity at multiple aminergic GPCRs, including 5-HT2A. 2-Bromo-LSD lacks 5-HT2B agonist activity. 2-Bromo-LSD induces dendritogenesis and spinogenesis. 2-Bromo-LSD 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: 97.26%
- CAS No.: 478-84-2
- Formula: C20H24BrN3O
- Molecular Weight:402.33
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Storage:
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, 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
- 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 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 exerts weak blocking effects on hERG channels (IC50 = 31.6 μM)[2].
2-Bromo-LSD (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 (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 alone at matching doses[1].
2-Bromo-LSD (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. 478-84-2
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Appearance Solid
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Molecular Weight 402.33
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Formula C20H24BrN3O
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Color Off-white to light yellow
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SMILES
[H][C@]1(C2)N(C[C@@H](C=C1C3=CC=CC4=C3C2=C(N4)Br)C(N(CC)CC)=O)C
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Synonyms
BOL-148; Bromolysergide
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
Purity & Documentation
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Data Sheet (275 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Handling Instructions (2659 KB)
References
[1]. Persson SA. The effect of LSD and 2-bromo LSD on the striatal DOPA accumulation after decarboxylase inhibition in rats. Eur J Pharmacol. 1977 May 1;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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
2-Bromo-LSD Related Classifications
HY-121675 Related Classifications
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