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.

Generalized anxiety disorder

• Riluzole sublingual (BHV-0223) – undefined mechanism of action[1]
• TGFK08AA – 5-HT_1A receptor modulator[2]
• TGW00AA (FKW00GA) – 5-HT_1A receptor agonist, 5-HT_2A receptor antagonist [3]

Panic disorder

• Darigabat (PF-06372865) – GABA_A 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) – "GABATooltip γ-aminobutyric acid modulator"^[1] / undefined mechanism of action^[2][7]
• Brexpiprazole (Lu AF41156, OPC-34712; Rexulti) – atypical antipsychotic / 5-HT_1A, D₂ and D₃ receptor partial agonist and 5-HT_2A, 5-HT_2B, 5-HT₇, α₁-adrenergic, α₂-adrenergic, and H₁ receptor antagonist [8]
• Iloperidone (HP-873, ILO-522; Fanapt, Fiapta, Zomaril) – atypical antipsychotic / 5-HT_2A, 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-HT_1A receptor agonist, 5-HT_2A 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 GABA_A receptor positive allosteric modulator[18]^[7]
• JNJ-42165279 – FAAH inhibitor[19]
• JNJ-61393215 – orexin OX₁ receptor antagonist [20]
• MP-20X – CB₁ and 5-HT_1A receptor modulator [21]
• SRX-246 – vasopressin V_1A receptor antagonist [22]