BMB-201

{{Short description|Serotonergic drug}} {{cs1 config|name-list-style=vanc|display-authors=6}} {{Infobox drug | drug_name = | image = | width = | caption = <!-- Clinical data --> | pronounce = | tradename = | Drugs.com = | MedlinePlus = | licence_CA = | licence_EU = | DailyMedID = | licence_US = | pregnancy_AU = | pregnancy_category = | dependency_liability = | addiction_liability = | class = Non-hallucinogenic serotonin 5-HT_2A and 5-HT_2C receptor partial agonist<ref name="AdisInsight" /><ref name="Synapse" /><ref name="Pryzm" /><ref name="VasilkevichDuanLovera2024" /><ref name="BrightMindsBio2024" /><ref name="VasilkevichLoveraDuan2025" /> | ATC_prefix = None | ATC_suffix = <!-- Legal status --> | legal_status = <!-- Pharmacokinetic data --> | bioavailability = | protein_bound = | metabolism = | metabolites = | onset = | elimination_half-life = | duration_of_action = | excretion = <!-- Identifiers --> | CAS_number = | CAS_supplemental = | PubChem = | PubChemSubstance = | IUPHAR_ligand = | DrugBank = | ChemSpiderID = | UNII = | KEGG = | ChEBI = | ChEMBL = | NIAID_ChemDB = | PDB_ligand = | synonyms = BMB201; BMB-A39a prodrug

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'''BMB-201''' is a serotonin 5-HT_2A and 5-HT_2C receptor agonist of the tryptamine family described as a non-hallucinogenic psychoplastogen which is under development for the treatment of depression, anxiety, 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 is unspecified.<ref name="AdisInsight" />

==Pharmacology== {| class="wikitable floatleft" style="font-size:small;" |+ {{Nowrap|BMB-A39a activities}} |- ! Target !! Affinity (K_i, nM) |- | 5-HT_1F || {{Abbr|ND|No data}} (K_i)<br />23 ({{Abbrlink|EC₅₀|half-maximal effective concentration}})<br />92% ({{Abbrlink|E_max|maximal efficacy}}) |- | 5-HT_2A || {{Abbr|ND|No data}} (K_i)<br />70–71 ({{Abbr|EC₅₀|half-maximal effective concentration}})<br />68–69% ({{Abbr|E_max|maximal efficacy}}) |- | 5-HT_2B || {{Abbr|ND|No data}} (K_i)<br />{{Abbr|ND|No data}} ({{Abbr|EC₅₀|half-maximal effective concentration}})<br /><20% ({{Abbr|E_max|maximal efficacy}}) |- | 5-HT_2C || {{Abbr|ND|No data}} (K_i)<br />6.7 ({{Abbr|EC₅₀|half-maximal effective concentration}})<br />79% ({{Abbr|E_max|maximal efficacy}}) |- | 5-HT₆ || {{Abbr|ND|No data}} (K_i)<br />9 ({{Abbr|EC₅₀|half-maximal effective concentration}})<br />48% ({{Abbr|E_max|maximal efficacy}}) |- |- class="sortbottom" | 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 of another compound known as BMB-A39a.<ref name="VasilkevichDuanLovera2024" /><ref name="BrightMindsBio2024" /> This active metabolite acts as a biased partial agonist of the serotonin 5-HT_2A and 5-HT_2C receptors.<ref name="Synapse" /><ref name="Pryzm" /><ref name="VasilkevichDuanLovera2024" /><ref name="BrightMindsBio2024" /><ref name="VasilkevichLoveraDuan2025" /> BMB-A39a is slightly less efficacious in activating G_q signaling at the serotonin 5-HT_2A and 5-HT_2C receptors compared to psilocin ({{Abbrlink|E_max|Maximal efficacy}} = 68% vs. 82% at 5-HT_2A and 79% vs. 95% at 5-HT_2C, respectively).<ref name="BrightMindsBio2024" /> It is about 9-fold less potent in activating the serotonin 5-HT_2A receptor than psilocin, whereas its potency in activating the serotonin 5-HT_2C receptor is similar to that of psilocin.<ref name="BrightMindsBio2024" /> Relatedly, whereas psilocin shows balanced activation of both the serotonin 5-HT_2A and 5-HT_2C receptors, BMB-A39a is about 11-fold more potent in activating the serotonin 5-HT_2C receptor over the serotonin 5-HT_2A receptor.<ref name="BrightMindsBio2024" />

In addition to the serotonin 5-HT_2A and 5-HT_2C receptors, BMB-A39a is a potent partial agonist of the serotonin 5-HT_1F and 5-HT₆ receptors.<ref name="VasilkevichDuanLovera2024" /><ref name="VasilkevichLoveraDuan2025" /> On the other hand, it shows minimal or negligible activity in activating the serotonin 5-HT_2B receptor ({{Abbr|E_max|maximal efficacy}} < 20%), and does not activate other serotonin receptors, for instance the serotonin 5-HT_1B and 5-HT_1D receptors.<ref name="VasilkevichDuanLovera2024" /><ref name="BrightMindsBio2024" /><ref name="VasilkevichLoveraDuan2025" />

BMB-A39a shows less than 70% efficacy in activating G_q signaling at the serotonin 5-HT_2A receptor, which has been associated with absence of hallucinogenic-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 effects due to its reduced serotonin 5-HT_2A receptor intrinsic activity but to potently induce neuroplasticity.<ref name="VasilkevichDuanLovera2024" /><ref name="BrightMindsBio2024" /> It has been reported to show effectiveness in animal models of depression, anxiety, pain, and 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'' pharmacology as BMB-A39a patented by 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 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 derivative.<ref name="VasilkevichLoveraDuan2025" /> In addition, Bright Mind Biosciences has patented tryptamines and prodrugs as serotonin 5-HT₂ receptor modulators, 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.<ref name="AdisInsight" /><ref name="Synapse" /><ref name="Pryzm" /> As of September 2025, it is in the preclinical research stage of development for the treatment of depressive disorders and pain.<ref name="AdisInsight" /><ref name="Synapse" /><ref name="Pryzm" />

==See also== * List of investigational hallucinogens and entactogens * Substituted tryptamine * Non-hallucinogenic 5-HT_2A receptor agonist * BMB-101 * BMB-105 * BMB-202 * 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