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. 2023 May 3;8:177. doi: 10.1038/s41392-023-01427-2

Table 3.

Candidate drugs under development

Drug Structure Indication Phase status NCT Targets (protein short names) Mechanism Ki (nM) Reference
Resveratrol graphic file with name 41392_2023_1427_Tabcp_HTML.gif

Alzheimer’s disease;

schizophrenia;

Parkinson’s disease;

depression

1;

2;

2;

4

NCT01504854;

NCT02062190;

NCT03384329;

NCT03095105;

NCT03093389;

NCT03094156;

NCT03097211

 Mel-1A-R / / 808
Mel-1B-R / /
SGS-742 graphic file with name 41392_2023_1427_Tabcq_HTML.gif

Alzheimer’s disease;

schizophrenia;

attention deficit hyperactivity disorder

 2 NCT00093951 GABBR1 / / /
GABBR2 / /
SUVN-502 graphic file with name 41392_2023_1427_Tabcr_HTML.gif Alzheimer’s disease 2 NCT02580305 5-HT-6 / / /
Nabilone graphic file with name 41392_2023_1427_Tabcs_HTML.gif Alzheimer’s disease 3 NCT02351882 CB-R Agonist / 349
CB-2 Agonist /
Caffeine graphic file with name 41392_2023_1427_Tabct_HTML.gif Alzheimer’s disease 3 NCT04570085 adenosine receptors / / 350
5-HT-1 Regulator
Velusetrag graphic file with name 41392_2023_1427_Tabcu_HTML.gif Alzheimer’s disease 1 NCT01467726 5-HT-4 / / /
Brexpiprazole graphic file with name 41392_2023_1427_Tabcv_HTML.gif Alzheimer’s disease 3 NCT03620981 DRD2 Partial Agonist / 354
Prazosin graphic file with name 41392_2023_1427_Tabcw_HTML.gif Alzheimer’s disease 3 NCT03710642 ADRA1A Antagonist / 809
CB-2 / /
GPR12 Inverse agonist /
GPR18 / /
GPR55 / /
5-HT-1A / /
5-HT-2A / /
DOR-1 / /
MOR-1 / /
Sarizotan graphic file with name 41392_2023_1427_Tabcx_HTML.gif Parkinson’s disease

2;

3

NCT00009048;

NCT00314288;

NCT00105508;

NCT00105521

 DRD2 Partial agonist / /
DRD3 Ligand /
5-HT-1A / /
Melperone graphic file with name 41392_2023_1427_Tabcy_HTML.gif

Parkinson’s disease;

schizophrenia;

anxiety disorders;

depression

2;

3

NCT02374567;

NCT00125138;

 DRD2 Antagonist / /
Pardoprunox graphic file with name 41392_2023_1427_Tabcz_HTML.gif Parkinson’s disease 3

NCT00407095;

NCT00406588;

NCT00335166;

NCT00335374;

NCT00332917;

NCT00269516

 DRD2 / / /
DRD3 / /
DRD4 / /
5-HT-1A / /
Piribedil graphic file with name 41392_2023_1427_Tabda_HTML.gif Parkinson’s disease 3 NCT01007864 DRD2 / / 810
DRD3 / /
Centanafadine graphic file with name 41392_2023_1427_Tabdb_HTML.gif Attention deficit hyperactivity disorder 3

NCT03605849;

NCT03605680;

NCT03605836;

NCT05257265;

NCT05279313;

NCT05428033

 / / /
Raclopride graphic file with name 41392_2023_1427_Tabdc_HTML.gif

Parkinson’s disease;

depression

1;

4

 NCT00832221; NCT05282277 DRD2 Antagonist / 811
Dipraglurant graphic file with name 41392_2023_1427_Tabdd_HTML.gif Parkinson’s disease

2;

2/3

NCT01336088;

NCT05116813;

NCT04857359

 MGLUR5 / / /
Arbaclofen Placarbil graphic file with name 41392_2023_1427_Tabde_HTML.gif Multiple sclerosis 3 NCT01359566 GABBR1 Agonist / 812
GABBR2 Agonist /
Plozalizumab Biotech Multiple sclerosis 2 NCT01199640 CMKBR2 / / /
Nabiximols graphic file with name 41392_2023_1427_Tabdf_HTML.gif Multiple sclerosis

3;

4

NCT01964547;

NCT00678795;

NCT00681538;

NCT00702468;

NCT00711646

 GPR12 Inverse agonist / 658
CB-R / /
CB-2 / /
GPR55 / /
5-HT-1A / /
5-HT-2A / /
DOR-1 / /
MOR-1 / /
Ceralifimod graphic file with name 41392_2023_1427_Tabdg_HTML.gif Multiple sclerosis 2 NCT01226745 S1PR1 Modulator / 813
Tiapride graphic file with name 41392_2023_1427_Tabdh_HTML.gif

Huntington’s disease;

schizophrenia;

depression;

anxiety disorders

1;

3

NCT00632645;

NCT02374567

 DRD2 Blocker / 814
DRD3 Blocker /
5-HT Antagonist /
ADRA1 Antagonist /
ADRA2 Antagonist /
LY2140023 Not Available Schizophrenia

1;

2;

2/3;

3

NCT01307800;

NCT01328093;

NCT01487083;

NCT01452919;

NCT01129674;

NCT01125358;

NCT01052103;

NCT00149292;

NCT00520923;

NCT00845026; NCT01086748;

NCT01606436;

NCT01354353

 MGLUR2 / / /
MGLUR3 / /
BL-1020 Not available Schizophrenia

2;

2/3

NCT00480571;

NCT00722176

 DRD2 / / /
5-HT-2A / /
Norclozapine graphic file with name 41392_2023_1427_Tabdi_HTML.gif Schizophrenia

1;

2

NCT00628420;

NCT00490516

 CHRM1 / / /
DRD2 / /
DRD3 / /
Talnetant graphic file with name 41392_2023_1427_Tabdj_HTML.gif Schizophrenia 2

NCT00049946;

NCT00103727;

NCT00300963;

NCT00101985

 NK3R Antagonist 1 815
Blonanserin graphic file with name 41392_2023_1427_Tabdk_HTML.gif Schizophrenia

4;

3

NCT01516424;

NCT03784222

 DRD2 Antagonist / 816
DRD3 Antagonist /
5-HT-2A Antagonist /
Pipamperone graphic file with name 41392_2023_1427_Tabdl_HTML.gif

Schizophrenia;

depression;

anxiety disorders

2;

3

NCT00672659; NCT01450514; NCT02374567;

NCT01312922

 DRD2 Antagonist / /
5-HT-2A Agonist /
ADRA1 Antagonist /
DRD4 Antagonist /
DRD1 Antagonist /
DRD3 / /
5-HT-2B / /
ADRA2A Antagonist /
Pavinetant graphic file with name 41392_2023_1427_Tabdm_HTML.gif Schizophrenia 2 NCT00686998 NK3R Antagonist / 817
Tetrahydrocannabivarin graphic file with name 41392_2023_1427_Tabdn_HTML.gif Schizophrenia 2 NCT01491490 CB-R Antagonist / 818
GPR55 Partial agonist /
5-HT-1A Agonist /
CB-2 Partial agonist /
JNJ-37822681 graphic file with name 41392_2023_1427_Tabdo_HTML.gif Schizophrenia 2

NCT00728195;

NCT01812642

 DRD2 Antagonist / 819
SEP-363856 graphic file with name 41392_2023_1427_Tabdp_HTML.gif

Schizophrenia;

Parkinson’s disease

1;

2;

2/3;

3

NCT04865835;

NCT03370640;

NCT04325737;

NCT04369391;

NCT01940159;

NCT01972711;

NCT01994473;

NCT04038957;

NCT02970929;

NCT02969382;

NCT04825860;

NCT05359081;

NCT04092686;

NCT04072354;

NCT04109950;

NCT02969369

 TAAR1 Agonist / 820
5-HT-1A Agonist /
Dimethyltryptamine graphic file with name 41392_2023_1427_Tabdq_HTML.gif Depression

1;

1/2

 NCT04711915; NCT04698603 5-HT-6 / 68 821,822
5-HT-2A / 65
Serotonin graphic file with name 41392_2023_1427_Tabdr_HTML.gif

Depression;

bipolar disorder;

anxiety disorders

2;

3;

2/3;

4

NCT02137369; NCT01324700; NCT01811147;

NCT00183274;

NCT00157547;

NCT02356107’

NCT01155661;

NCT00361218

 5-HT-2A / / 823
5-HT-3A / /
5-HT-3B / /
5-methoxy-N,N-dimethyltryptamine graphic file with name 41392_2023_1427_Tabds_HTML.gif Depression 1/2 NCT04698603 5-HT-1A Agonist / 824
5-HT-2A Agonist /
Tianeptine graphic file with name 41392_2023_1427_Tabdt_HTML.gif

Bipolar disorder;

depression

3;

4

NCT00879372;

NCT01309776;

NCT04249596

 MOR-1 Agonist / 440,441
5-HT-1A Inhibitor /
DRD3 Agonist /
Vofopitant graphic file with name 41392_2023_1427_Tabdu_HTML.gif Bipolar disorder 1 NCT00907985 SPR / / 825
Naluzotan graphic file with name 41392_2023_1427_Tabdv_HTML.gif

Anxiety disorders;

depression

3;

2

NCT00248183;

NCT00448292

 5-HT-1A Agonist / 435
Ansofaxine graphic file with name 41392_2023_1427_Tabdw_HTML.gif Depression 3 NCT04853407 5-HT / / /
Roluperidone graphic file with name 41392_2023_1427_Tabdx_HTML.gif Schizophrenia 3 NCT03397134 5-HT-2A / / 402
Eltoprazine graphic file with name 41392_2023_1427_Tabdy_HTML.gif

Schizophrenia;

Parkinson’s disease (PD)

 2

NCT01266174;

NCT02439125

 5-HT-1A / / 401
5-HT-2B / /
Zicronapine graphic file with name 41392_2023_1427_Tabdz_HTML.gif Schizophrenia 3 NCT01295372 5-HT-2A / / 400
5-HT-2C / /
DRD1 / /
DRD2 / /
Brilaroxazine graphic file with name 41392_2023_1427_Tabea_HTML.gif Schizophrenia

2;

3

NCT01490086;

NCT05184335

 5-HT-7 / / 399
5-HT-2A / /
5-HT-1A / /
DRD2 / /
DRD3 / /
DRD4 / /
5-HT-6 / /

5-HT 5-hydroxytryptamine receptor, 5-HT-1 5-hydroxytryptamine receptor 1, 5-HT-6 5-hydroxytryptamine receptor 6, 5-HT-1A 5-hydroxytryptamine receptor 1A, 5-HT-1B 5-hydroxytryptamine receptor 1B, 5-HT-1C 5-hydroxytryptamine receptor 1C, 5-HT-1D 5-hydroxytryptamine receptor 1D, 5-HT-1E 5-hydroxytryptamine receptor 1E, 5-HT-1F 5-hydroxytryptamine receptor 1F, 5-HT-2A 5-hydroxytryptamine receptor 2A, 5-HT-2B 5-hydroxytryptamine receptor 2B, 5-HT-2C 5-hydroxytryptamine receptor 2C, 5-HT-3 5-hydroxytryptamine receptor 3A, 5-HT-3A 6-hydroxytryptamine receptor 3A, 5-HT-3B 5-hydroxytryptamine receptor 3B, 5-HT-4 5-hydroxytryptamine receptor 4, 5-HT-7 5-hydroxytryptamine receptor 7, ADRA1 alpha-1 adrenergic receptor, ADRA1A alpha-1A adrenergic receptor, ADRA1B alpha-1B adrenergic receptor, ADRA1D alpha-1D adrenergic receptor, ADRA2 alpha-2 adrenergic receptor, ADRA2A alpha-2A adrenergic receptor, ADRA2B alpha-2B adrenergic receptor, ADRA2C alpha-2C adrenergic receptor, ADRB2 beta-2 adrenergic receptor, ADRB3 beta-3 adrenergic receptor, ADRB1 beta-1 adrenergic receptor, CB-2 cannabinoid receptor 2, CB-R or CB1 cannabinoid receptor 1, CHRM cholinergic receptor muscarinic, CHRM1 muscarinic acetylcholine receptor M1, CHRM2 muscarinic acetylcholine receptor M2, CHRM3 muscarinic acetylcholine receptor M3, CHRM4 muscarinic acetylcholine receptor M4, CHRM5 muscarinic acetylcholine receptor M5, DOR-1 delta-type opioid receptor, DRD1 D(1A) dopamine receptor, DRD2 D(2) dopamine receptor, DRD3 D(3) dopamine receptor, DRD4 D(4) dopamine receptor, DRD5 D(5) dopamine receptor, GABBR1 gamma-aminobutyric acid type B receptor subunit 1, GABBR2 gamma-aminobutyric acid type B receptor subunit 2, GPR18 N-arachidonyl glycine receptor, GPR12 G-protein coupled receptor 12, GPR55 G-protein coupled receptor 55, HH1R histamine H1 receptor, HH2R histamine H2 receptor, HH3R histamine H3 receptor, HH4R histamine H4 receptor, KOR-1 kappa-type opioid receptor, MCHR1 melanin-concentrating hormone receptor 1, MOR-1 mu-type opioid receptor, SPR neurokinin 1 receptor, S1PR1 sphingosine 1-phosphate receptor 1, TAAR1 trace amine-associated receptor 1, Mel-1A-R melatonin receptor type 1A, Mel-1B-R melatonin receptor type 1B, MGLUR5 metabotropic glutamate receptor 5, MGLUR2 metabotropic glutamate receptor 2, MGLUR3 metabotropic glutamate receptor 3, CMKBR2 C-C chemokine receptor type 2, NK3R neuromedin-K receptor

Overview of the clinical stage drugs targeting GPCR for the treatment of neuropsychiatric disorders. The clinical stage compounds and their affiliated items including structure, indication, phase status, NCT number, GPCR targets, mechanism, binding affinity (Ki) and related references were collected from the DrugBank database (Accessed May 2022).