Brofaromine

Brofaromine
Clinical data
Routes of; administration	Oral
ATC code	none;
Legal status
Legal status	In general: ℞ (Prescription only);
Pharmacokinetic data
Protein binding	98%
Elimination half-life	9-14 hours
Identifiers
	IUPAC name 4-(7-bromo-5-methoxybenzofuran-2-yl)piperidine;
CAS Number	63638-91-5 ;
PubChem CID	44571;
ChemSpider	40549 ;
UNII	6WV4B8Q07H;
KEGG	D02560 ;
ChEMBL	ChEMBL160347 ;
CompTox Dashboard (EPA)	DTXSID10213008 ;
Chemical and physical data
Formula	C14H16BrNO2
Molar mass	310.191 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES Brc3cc(OC)cc1c3oc(c1)C2CCNCC2;
	InChI InChI=1S/C14H16BrNO2/c1-17-11-6-10-7-13(9-2-4-16-5-3-9)18-14(10)12(15)8-11/h6-9,16H,2-5H2,1H3 ; Key:WZXHSWVDAYOFPE-UHFFFAOYSA-N ;
	(verify)

Brofaromine (proposed brand name Consonar) is a reversible inhibitor of monoamine oxidase A (RIMA) discovered by Ciba-Geigy.^[1] The compound was primarily researched in the treatment of depression and anxiety but its development was dropped before it was brought to market.^[2]

Brofaromine also acts as a serotonin reuptake inhibitor, and its dual pharmacologic effects offered promise in the treatment of a wide spectrum of depressed patients while producing less severe anticholinergic side effects in comparison with older standard drugs like certain of the tricyclic antidepressants.

Pharmacology

Brofaromine is a reversible inhibitor of monoamine oxidase A (RIMA, a type of monoamine oxidase inhibitor (MAOI)) and acts on epinephrine (adrenaline), norepinephrine (noradrenaline), serotonin, and dopamine. Unlike standard MAOIs, possible side effects do not include cardiovascular complications (hypertension) with encephalopathy, liver toxicity or hyperthermia.

References

^ US Patent 4210655
^ Lotufo-Neto F, Trivedi M, Thase ME (1999). "Meta-analysis of the reversible inhibitors of monoamine oxidase type A moclobemide and brofaromine for the treatment of depression". Neuropsychopharmacology. 20 (3): 226–47. doi:10.1016/S0893-133X(98)00075-X. PMID 10063483. Free full text

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[1] US Patent 4210655

[Lotufo-2] Lotufo-Neto F, Trivedi M, Thase ME (1999). "Meta-analysis of the reversible inhibitors of monoamine oxidase type A moclobemide and brofaromine for the treatment of depression". Neuropsychopharmacology. 20 (3): 226–47. doi:10.1016/S0893-133X(98)00075-X. PMID 10063483. Free full text

[1]

[2]

v t e Anxiolytics (N05B)
5-HT_1ARTooltip 5-HT1A receptor agonists	Buspirone Gepirone Tandospirone
GABA_ARTooltip GABAA receptor PAMsTooltip positive allosteric modulators	Benzodiazepines: Adinazolam Alprazolam Bromazepam Camazepam Chlordiazepoxide Clobazam Clonazepam Clorazepate Clotiazepam Cloxazolam Diazepam^# Ethyl loflazepate Etizolam Fludiazepam Halazepam Ketazolam Lorazepam^# Medazepam Nordazepam Oxazepam Pinazepam Prazepam; Others: Alpidem^‡ Barbiturates (e.g., phenobarbital) Carbamates (e.g., meprobamate) Carisoprodol Chlormezanone^‡ Ethanol (alcohol) Etifoxine
Hypnotics	Zopiclone
Gabapentinoids (α₂δ VDCC blockers)	Gabapentin Gabapentin enacarbil Phenibut Pregabalin
Antidepressants	SSRIsTooltip Selective serotonin reuptake inhibitors (e.g., escitalopram) SNRIsTooltip Serotonin-norepinephrine reuptake inhibitors (e.g., duloxetine) SARIsTooltip Serotonin antagonist and reuptake inhibitors (e.g., trazodone) TCAsTooltip Tricyclic antidepressants (e.g., clomipramine^#) TeCAsTooltip Tetracyclic antidepressants (e.g., mirtazapine) MAOIsTooltip Monoamine oxidase inhibitors (e.g., phenelzine); Others: Agomelatine Bupropion Tianeptine Vilazodone Vortioxetine
Antipsychotics	Quetiapine Flupentixol
Sympatholytics (Antiadrenergics)	Alpha-1 blockers (e.g., prazosin) Alpha-2 agonists (e.g., clonidine, dexmedetomidine, guanfacine) Beta blockers (e.g., propranolol)
Others	Benzoctamine Cycloserine Fabomotizole Hydroxyzine Lorpiprazole Mebicar Mepiprazole Nicotine Opipramol Oxaflozane^‡ Phenaglycodol Phenibut Picamilon Selank Tiagabine Tofisopam Validolum
^#WHO-EM ^‡Withdrawn from market Clinical trials: ^†Phase III ^§Never to phase III

Pharmacology

See also

References