# BMB-201

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> Markdown URL: https://mediated.wiki/source/BMB-201.md
> Source: https://en.wikipedia.org/wiki/BMB-201
> Source revision: 1356285813
> License: Creative Commons Attribution-ShareAlike 4.0 International (https://creativecommons.org/licenses/by-sa/4.0/)

{{Short description|Serotonergic drug}}
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| class = Non-[hallucinogen](/source/hallucinogen)ic [serotonin](/source/serotonin) [5-HT<sub>2A</sub>](/source/5-HT2A_receptor) and [5-HT<sub>2C</sub> receptor](/source/5-HT2C_receptor) [partial agonist](/source/partial_agonist)<ref name="AdisInsight" /><ref name="Synapse" /><ref name="Pryzm" /><ref name="VasilkevichDuanLovera2024" /><ref name="BrightMindsBio2024" /><ref name="VasilkevichLoveraDuan2025" />
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| synonyms = BMB201; BMB-A39a prodrug

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'''BMB-201''' is a [serotonin](/source/serotonin) [5-HT<sub>2A</sub>](/source/5-HT2A_receptor) and [5-HT<sub>2C</sub> receptor](/source/5-HT2C_receptor) [agonist](/source/agonist) of the [tryptamine](/source/substituted_tryptamine) family described as a non-[hallucinogen](/source/hallucinogen)ic [psychoplastogen](/source/psychoplastogen) which is under development for the treatment of [depression](/source/depression_(mood)), [anxiety](/source/anxiety), [pain](/source/pain), and other indications.<ref name="AdisInsight">{{cite web | title=BMB 201 | website=AdisInsight | date=10 September 2025 | url=https://adisinsight.springer.com/drugs/800080130 | access-date=1 April 2026}}</ref><ref name="Synapse">{{cite web | title=Delving into the Latest Updates on BMB-201 with Synapse | website=Synapse | date=29 October 2024 | url=https://synapse.patsnap.com/drug/6842dbd395934d75aeaf38cf4dbeb43d | access-date=30 October 2024}}</ref><ref name="Pryzm">{{cite web | title=BMB-201 Drug Profile | website=Ozmosi | url=https://pryzm.ozmosi.com/product/bmb-201 | access-date=30 October 2024}}</ref><ref name="VasilkevichDuanLovera2024">{{cite conference | vauthors = Vasilkevich A, Duan J, Lovera A, McCorvy J, Pedersen JT | title = Novel 5-HT2A/2C mixed and partial agonist and its efficacy in preclinical pain models | conference = Society for Neuroscience 2024 Annual Meeting, Chicago, October 5-9 | date = October 2024 | url = https://brightmindsbio.com/wp-content/uploads/2024/10/BMB-201-poster-PSPP-final.pdf}}</ref><ref name="BrightMindsBio2024">{{cite web | url = https://brightmindsbio.com/wp-content/uploads/2024/09/BMB_investor_deck_September.pdf | title = Bright Minds Investor Deck | work =  Bright Minds Biosciences Inc. | date = September 2024  }}</ref> Its [route of administration](/source/route_of_administration) is unspecified.<ref name="AdisInsight" />

==Pharmacology==
{| class="wikitable floatleft" style="font-size:small;"
|+ {{Nowrap|BMB-A39a activities}}
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! [Target](/source/Biological_target) !! Affinity (K<sub>i</sub>, nM)
|-
| [5-HT<sub>1F</sub>](/source/5-HT1F_receptor) || {{Abbr|ND|No data}} (K<sub>i</sub>)<br />23 ({{Abbrlink|EC<sub>50</sub>|half-maximal effective concentration}})<br />92% ({{Abbrlink|E<sub>max</sub>|maximal efficacy}})
|-
| [5-HT<sub>2A</sub>](/source/5-HT2A_receptor) || {{Abbr|ND|No data}} (K<sub>i</sub>)<br />70–71 ({{Abbr|EC<sub>50</sub>|half-maximal effective concentration}})<br />68–69% ({{Abbr|E<sub>max</sub>|maximal efficacy}})
|-
| [5-HT<sub>2B</sub>](/source/5-HT2B_receptor) || {{Abbr|ND|No data}} (K<sub>i</sub>)<br />{{Abbr|ND|No data}} ({{Abbr|EC<sub>50</sub>|half-maximal effective concentration}})<br /><20% ({{Abbr|E<sub>max</sub>|maximal efficacy}})
|-
| [5-HT<sub>2C</sub>](/source/5-HT2C_receptor) || {{Abbr|ND|No data}} (K<sub>i</sub>)<br />6.7 ({{Abbr|EC<sub>50</sub>|half-maximal effective concentration}})<br />79% ({{Abbr|E<sub>max</sub>|maximal efficacy}})
|-
| [5-HT<sub>6</sub>](/source/5-HT6_receptor) || {{Abbr|ND|No data}} (K<sub>i</sub>)<br />9 ({{Abbr|EC<sub>50</sub>|half-maximal effective concentration}})<br />48% ({{Abbr|E<sub>max</sub>|maximal efficacy}})
|-
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| colspan="2" style="width: 1px; background-color:var(--background-color-notice-subtle,#eaecf0); color:inherit; text-align: center;" | '''Notes:''' The smaller the value, the more avidly the drug binds to the site. All proteins are human unless otherwise specified. '''Refs:''' <ref name="VasilkevichDuanLovera2024" /><ref name="BrightMindsBio2024" />
|}

BMB-201 is a [prodrug](/source/prodrug) of another compound known as BMB-A39a.<ref name="VasilkevichDuanLovera2024" /><ref name="BrightMindsBio2024" /> This [active metabolite](/source/active_metabolite) acts as a [biased](/source/biased_agonist) [partial agonist](/source/partial_agonist) of the [serotonin](/source/serotonin) [5-HT<sub>2A</sub>](/source/5-HT2A_receptor) and [5-HT<sub>2C</sub> receptor](/source/5-HT2C_receptor)s.<ref name="Synapse" /><ref name="Pryzm" /><ref name="VasilkevichDuanLovera2024" /><ref name="BrightMindsBio2024" /><ref name="VasilkevichLoveraDuan2025" /> BMB-A39a is slightly less [efficacious](/source/intrinsic_activity) in activating [G<sub>q</sub>](/source/Gq_protein) [signaling](/source/cell_signaling) at the serotonin 5-HT<sub>2A</sub> and 5-HT<sub>2C</sub> receptors compared to [psilocin](/source/psilocin) ({{Abbrlink|E<sub>max</sub>|Maximal efficacy}} = 68% vs. 82% at 5-HT<sub>2A</sub> and 79% vs. 95% at 5-HT<sub>2C</sub>, respectively).<ref name="BrightMindsBio2024" /> It is about 9-fold less [potent](/source/potency_(pharmacology)) in activating the serotonin 5-HT<sub>2A</sub> receptor than psilocin, whereas its potency in activating the serotonin 5-HT<sub>2C</sub> receptor is similar to that of psilocin.<ref name="BrightMindsBio2024" /> Relatedly, whereas psilocin shows balanced activation of both the serotonin 5-HT<sub>2A</sub> and 5-HT<sub>2C</sub> receptors, BMB-A39a is about 11-fold more potent in activating the serotonin 5-HT<sub>2C</sub> receptor over the serotonin 5-HT<sub>2A</sub> receptor.<ref name="BrightMindsBio2024" />

In addition to the serotonin 5-HT<sub>2A</sub> and 5-HT<sub>2C</sub> receptors, BMB-A39a is a potent partial agonist of the serotonin [5-HT<sub>1F</sub>](/source/5-HT1F_receptor) and [5-HT<sub>6</sub> receptor](/source/5-HT6_receptor)s.<ref name="VasilkevichDuanLovera2024" /><ref name="VasilkevichLoveraDuan2025" /> On the other hand, it shows minimal or negligible activity in activating the serotonin [5-HT<sub>2B</sub> receptor](/source/5-HT2B_receptor) ({{Abbr|E<sub>max</sub>|maximal efficacy}} < 20%), and does not activate other [serotonin receptor](/source/serotonin_receptor)s, for instance the serotonin [5-HT<sub>1B</sub>](/source/5-HT1B_receptor) and [5-HT<sub>1D</sub> receptor](/source/5-HT1D_receptor)s.<ref name="VasilkevichDuanLovera2024" /><ref name="BrightMindsBio2024" /><ref name="VasilkevichLoveraDuan2025" />

BMB-A39a shows less than 70% efficacy in activating [G<sub>q</sub>](/source/Gq_protein) [signaling](/source/cell_signaling) at the serotonin 5-HT<sub>2A</sub> receptor, which has been associated with absence of [hallucinogen](/source/hallucinogen)ic-like activity.<ref name="VasilkevichDuanLovera2024" /><ref name="WallachCaoCalkins2023">{{cite journal | vauthors = Wallach J, Cao AB, Calkins MM, Heim AJ, Lanham JK, Bonniwell EM, Hennessey JJ, Bock HA, Anderson EI, Sherwood AM, Morris H, de Klein R, Klein AK, Cuccurazzu B, Gamrat J, Fannana T, Zauhar R, Halberstadt AL, McCorvy JD | title = Identification of 5-HT2A receptor signaling pathways associated with psychedelic potential | journal = Nat Commun | volume = 14 | issue = 1 | pages = 8221 | date = December 2023 | pmid = 38102107 | pmc = 10724237 | doi = 10.1038/s41467-023-44016-1 | url = https://isomerdesign.com/bitnest/external/10.1038/s41467-023-44016-1}}</ref> Accordingly, BMB-201 is said to have minimal or absent [psychedelic](/source/serotonergic_psychedelic) effects due to its reduced serotonin 5-HT<sub>2A</sub> receptor intrinsic activity but to potently induce [neuroplasticity](/source/neuroplasticity).<ref name="VasilkevichDuanLovera2024" /><ref name="BrightMindsBio2024" /> It has been reported to show effectiveness in [animal model](/source/animal_model)s of [depression](/source/depression_(mood)), [anxiety](/source/anxiety), [pain](/source/pain), and [substance use disorder](/source/substance_use_disorder).<ref name="VasilkevichDuanLovera2024" /><ref name="BioSpace2024">{{cite web | title=Bright Minds Biosciences proprietary compound, BMB-201, 5-HT2C/2A mixed agonist, demonstrated similar efficacy to morphine in preclinical pain models | website=BioSpace | date=17 October 2024 | url=https://www.biospace.com/press-releases/bright-minds-biosciences-proprietary-compound-bmb-201-5-ht2c-2a-mixed-agonist-demonstrated-similar-efficacy-to-morphine-in-preclinical-pain-models | access-date=30 October 2024}}</ref><ref name="BrightMindsBio2024" />

==Chemistry==
[[File:7-Methylpsilocin.svg|thumb|right|185px|class=skin-invert-image|7-Methylpsilocin, a lead compound with the same ''[in-vitro](/source/in-vitro)'' [pharmacology](/source/pharmacology) as BMB-A39a [patent](/source/patent)ed by [Bright Minds Biosciences](/source/Bright_Minds_Biosciences).<ref name="PubChem-7-Methylpsilocin">{{cite web | title=3-[2-(Dimethylamino)ethyl]-7-methyl-1H-indol-4-ol | website=PubChem | url=https://pubchem.ncbi.nlm.nih.gov/compound/166138173 | access-date=2 April 2026}}</ref><ref name="WO2022246554" /><!-- Note: 5-HT1F and 5-HT6 EC50/Emax values identical to BMB-A39a's values, while 5-HT2A/2C EC50/Emax values are slightly different but near-identical --> 7-Methyl{{shy}}psilocybin was also patented.<ref name="WO2022246554" />]]

The exact [chemical structure](/source/chemical_structure) of BMB-201 does not yet appear to have been disclosed.<ref name="AdisInsight" /><ref name="Synapse" /><ref name="Pryzm" /><ref name="VasilkevichLoveraDuan2025">{{cite conference | vauthors = Vasilkevich A, Lovera A, Duan J, McDonald I, Collins SD, Pedersen JT | title = Overview of Bright Minds Biosciences: Pioneering Serotonin Pharmacology | conference = 2025 AES Annual Meeting, December 5–9, Atlanta, Georgia | date = 7 December 2025 | url = https://brightmindsbio.com/wp-content/uploads/2025/12/1.-Overview-of-Bright-Minds-Biosciences.-Pioneering-Serotonin-Pharmacology-_compressed.pdf}}</ref> However, it is known to be a [tryptamine](/source/substituted_tryptamine) [derivative](/source/chemical_derivative).<ref name="VasilkevichLoveraDuan2025" /> In addition, Bright Mind Biosciences has [patent](/source/patent)ed tryptamines and [prodrug](/source/prodrug)s as [serotonin](/source/serotonin) [5-HT<sub>2</sub> receptor](/source/5-HT2_receptor) [modulator](/source/receptor_modulator)s, including for example 7-methylpsilocin and 7-methylpsilocybin.<ref name="WO2022246554">{{cite web | title=Heterocyclic compounds and methods of preparation thereof | website=Google Patents | date=25 May 2022 | url=https://patents.google.com/patent/WO2022246554A1/en | access-date=2 April 2026}}</ref><ref name="DuanCaoWang2024">{{cite journal | vauthors = Duan W, Cao D, Wang S, Cheng J | title = Serotonin 2A Receptor (5-HT2AR) Agonists: Psychedelics and Non-Hallucinogenic Analogues as Emerging Antidepressants | journal = Chem Rev | volume = 124 | issue = 1 | pages = 124–163 | date = January 2024 | pmid = 38033123 | doi = 10.1021/acs.chemrev.3c00375 | url = | quote = A recent patent from Bright Minds Bioscience disclosed a series of psilocin analogues with alkyl substitutions on the indole nitrogen, exemplified by compounds 13−16. 137 Among them, compounds 13−15 showed significantly decreased functional activities (13, EC50 = 196 nM, Emax = 65%; 14, EC50 = 188 nM, Emax = 48%; 15, EC50 = 1803 nM, Emax = 18%) compared to that of psilocin (EC50 = 8.34 nM at 5-HT2AR) in the Gq dissociation BRET assay, although all of them displayed excellent potency at 5-HT2CR and high selectivity against the 5-HT2BR. Compound 16, which contains a cyclopropylmethyl substitution on the indole nitrogen, exhibited potent partial agonist activity (EC50 = 28 nM, Emax = 29%) at the rat 5- HT2AR.137 No animal behavioral data have been reported on these compounds yet.}}</ref><ref name="WO2021179091">{{cite web | title=3-(2-(aminoethyl)-indol-4-ol derivatives, methods of preparation thereof, and the use as 5-ht2 receptor modulators | website=Google Patents | date=12 March 2021 | url=https://patents.google.com/patent/WO2021179091A1/en | access-date=1 April 2026}}</ref>

==Research==
BMB-201 is under development by [Bright Minds Biosciences](/source/Bright_Minds_Biosciences).<ref name="AdisInsight" /><ref name="Synapse" /><ref name="Pryzm" /> As of September 2025, it is in the [preclinical research](/source/preclinical_research) stage of development for the treatment of [depressive disorder](/source/depressive_disorder)s and [pain](/source/pain).<ref name="AdisInsight" /><ref name="Synapse" /><ref name="Pryzm" />

==See also==
* [List of investigational hallucinogens and entactogens](/source/List_of_investigational_hallucinogens_and_entactogens)
* [Substituted tryptamine](/source/Substituted_tryptamine)
* [Non-hallucinogenic 5-HT<sub>2A</sub> receptor agonist](/source/Serotonin_5-HT2A_receptor_agonist)
* [BMB-101](/source/BMB-101) 
* [BMB-105](/source/BMB-105)
* [BMB-202](/source/BMB-202)
* [Pharm-136](/source/Pharm-136)

==References==
{{Reflist}}

==External links==
* [https://brightmindsbio.com/pipeline/ Pipeline - Bright Minds Biosciences]
* [https://isomerdesign.com/pihkal/explore/13850 7-Methylpsilocin - Isomer Design]

{{Serotonin receptor modulators}}
{{Tryptamines}}

Category:5-HT1F agonists
Category:5-HT2C agonists
Category:5-HT6 agonists
Category:Biased ligands
Category:Bright Minds Biosciences
Category:Drugs with undisclosed chemical structures
Category:Experimental drugs
Category:Experimental non-hallucinogens
Category:Non-hallucinogenic 5-HT2A receptor agonists
Category:Prodrugs
Category:Psychoplastogens
Category:Tryptamines

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Adapted from the Wikipedia article [BMB-201](https://en.wikipedia.org/wiki/BMB-201) by Wikipedia contributors ([contributor history](https://en.wikipedia.org/wiki/BMB-201?action=history)). Available under [Creative Commons Attribution-ShareAlike 4.0 International](https://creativecommons.org/licenses/by-sa/4.0/). Changes may have been made.