Brofaromine References

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

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^Y
PubChem CID	44571
ChemSpider	40549^Y
UNII	6WV4B8Q07H
KEGG	D02560^Y
ChEMBL	ChEMBL160347^Y
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^Y Key:WZXHSWVDAYOFPE-UHFFFAOYSA-N^Y
(verify)

Pharmacology

See also

References