List of investigational anxiolytics

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This is a list of investigational anxiolytics, or anxiolytics that are currently under development for clinical use but are not yet approved. Chemical/generic names are listed first, with developmental code names, synonyms, and brand names in parentheses.

## Contents

* 1 Generalized anxiety disorder
* 2 Panic disorder
* 3 Post-traumatic stress disorder
* 4 Social anxiety disorder
* 5 Others/unspecified
* 6 See also
* 7 References
* 8 External links

## Generalized anxiety disorder

* Riluzole sublingual (BHV-0223) – undefined mechanism of action[1]
* TGFK08AA – 5-HT1A receptor modulator[2]
* TGW00AA (FKW00GA) – 5-HT1A receptor agonist, 5-HT2A receptor antagonist [3]

## Panic disorder

* Darigabat (PF-06372865) – GABAA receptor positive allosteric modulator [4]
* JNJ-61393215 – orexin OX1 receptor antagonist [5]

## Post-traumatic stress disorder

* 7-Oxoprasterone (7-keto-DHEA; HBL-9001) – "immunomodulator" / undefined mechanism of action [6]
* BNC-210 (IW-2143) – "GABA modulator"[1] / undefined mechanism of action[2][7]
* Brexpiprazole (Lu AF41156, OPC-34712; Rexulti) – atypical antipsychotic / 5-HT1A, D2 and D3 receptor partial agonist and 5-HT2A, 5-HT2B, 5-HT7, α1-adrenergic, α2-adrenergic, and H1 receptor antagonist [8]
* Iloperidone (HP-873, ILO-522; Fanapt, Fiapta, Zomaril) – atypical antipsychotic / 5-HT2A, 5-HT6, 5-HT7, D2, D3, D4, and α1-adrenergic receptor antagonist [9]
* MDMA (Midomafetamine, 3,4-methylenedioxymethamphetamine, "ecstasy") – serotonin–norepinephrine–dopamine releasing agent and 5-HT1 and 5-HT2 receptor agonist – specifically under development as an aid to psychotherapy for post-traumatic stress disorder [10][3][4]
* NBTX-001 (Xenon) – NMDA receptor antagonist [11]
* Pomaglumetad methionil (DB-103, LY-2140023) – mGluR2 and mGluR3 agonist [12]
* Tianeptine oxalate/naloxone (TNX-601) – atypical μ-opioid receptor agonist [13]

## Social anxiety disorder

* Fasedienol (Aloradine; PH94B; 4-androstadienol) – vomeropherine / neurosteroid[14]
* JNJ-42165279 – FAAH inhibitor[5][6]
* TGW00AA (FKW00GA) – 5-HT1A receptor agonist, 5-HT2A receptor antagonist [15]

## Others/unspecified

* AVN-101 – 5-HT6 receptor antagonist [16]
* BNC-210 (IW-2143) – "GABA modulator"[1] / undefined mechanism of action / α7 subunit-containing nicotinic acetylcholine receptor antagonist[2][17]
* Deuterated etifoxine (GRX-917) – translocator protein (TSPO) agonist and GABAA receptor positive allosteric modulator[18][7]
* JNJ-42165279 – FAAH inhibitor[19]
* JNJ-61393215 – orexin OX1 receptor antagonist [20]
* MP-20X – CB1 and 5-HT1A receptor modulator [21]
* SRX-246 – vasopressin V1A receptor antagonist [22]

## See also

* List of investigational drugs

## References

1. ↑ 1.0 1.1 Garakani, Amir; Murrough, James W.; Iosifescu, Dan V. (2014). "Advances in Psychopharmacology for Anxiety Disorders". FOCUS 12 (2): 152–162. doi:10.1176/appi.focus.12.2.152. ISSN 1541-4094.
2. ↑ 2.0 2.1 Doggrell, S. A. (2007). Novel drugs and products in neuroscience. Drugs of the Future, 32(11), 1007-1017. https://journals.prous.com/journals/servlet/xmlxsl/pk_journals.xml_summary_pr?p_JournalId=2&p_RefId=3853&p_IsPs=Y
3. ↑ "MDMA and PTSD treatment: "PTSD: From novel pathophysiology to innovative therapeutics"". Neurosci. Lett. 649: 176–180. 2017. doi:10.1016/j.neulet.2016.07.004. PMID 27394687.
4. ↑ Philipps, Dave (29 November 2016). "F.D.A. Agrees to New Trials for Ecstasy as Relief for PTSD Patients". The New York Times. https://www.nytimes.com/2016/11/29/us/ptsd-mdma-ecstasy.html.
5. ↑ "JNJ 42165279 - AdisInsight". https://adisinsight.springer.com/drugs/800036911.
6. ↑ "A Safety and Efficacy Study of JNJ-42165279 in Participants With Social Anxiety Disorder | Clinical Research Trial Listing ( Claustrophobia ) ( NCT02432703 )". https://www.centerwatch.com/clinical-trials/listings/72570/phobic-disorders-safety-efficacy-study-jnj-42165279/.
7. ↑ "Neurosteroids and translocator protein 18 kDa (TSPO) in depression: implications for synaptic plasticity, cognition, and treatment options". Eur Arch Psychiatry Clin Neurosci 273 (7): 1477–1487. December 2022. doi:10.1007/s00406-022-01532-3. PMID 36574032.

## External links

* AdisInsight – Springer
* 2016 Medicines in Development for Mental Health - PhRMA

* v
* t
* e

Anxiolytics (N05B)

5-HT1AR agonists|

* Buspirone
* Gepirone†
* Tandospirone

GABAAR PAMs|

* 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)
* Chlormezanone‡
* Ethanol (alcohol)
* Etifoxine
* Imepitoin; Herbs:
* Kava
* Skullcap
* Valerian

Gabapentinoids
(α2δ VDCC blockers)|

* Gabapentin
* Gabapentin enacarbil
* Phenibut
* Pregabalin

Antidepressants|

* SSRIs (e.g., escitalopram)
* SNRIs (e.g., duloxetine)
* SARIs (e.g., trazodone)
* TCAs (e.g., clomipramine#)
* TeCAs (e.g., mirtazapine)
* MAOIs (e.g., phenelzine); Others: Agomelatine
* Bupropion
* Tianeptine
* Vilazodone
* Vortioxetine

Sympatholytics
(Antiadrenergics)|

* Alpha-1 blockers (e.g., prazosin)
* Alpha-2 agonists (e.g., clonidine, dexmedetomidine, guanfacine)
* Beta blockers (e.g., propranolol)

Others|

* Benzoctamine
* Cannabidiol
* Cycloserine
* Fabomotizole
* Hydroxyzine
* Kanna
* Lavender
* 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

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*[GABA]: γ-aminobutyric acid
*[v]: View this template
*[t]: Discuss this template
*[e]: Edit this template
*[5-HT1AR]: 5-HT1A receptor
*[GABAAR]: GABAA receptor
*[PAMs]: positive allosteric modulators
*[α2δ]: alpha2delta subunit
*[VDCC]: voltage-dependent calcium channel
*[SSRIs]: Selective serotonin reuptake inhibitors
*[SNRIs]: Serotonin-norepinephrine reuptake inhibitors
*[SARIs]: Serotonin antagonist and reuptake inhibitors
*[TCAs]: Tricyclic antidepressants
*[TeCAs]: Tetracyclic antidepressants
*[MAOIs]: Monoamine oxidase inhibitors