Tedalinab |
|
(4S,7R)-1-(2,4-difluorophenyl)-N-(1,1-dimethylethyl)-4,5,6,7-tetrahydro-4,7-methano-1H-indazole-3-carboxamide
|
| CAS Number | |
|---|
| PubChem CID | |
|---|
| ChemSpider | |
|---|
| UNII | |
|---|
| CompTox Dashboard (EPA) | |
|---|
|
| Formula | C19H21F2N3O |
|---|
| Molar mass | 345.394 g·mol−1 |
|---|
| 3D model (JSmol) | |
|---|
CC(C)(C)NC(=O)C1=NN(C2=C1[C@@H]3CC[C@H]2C3)C4=C(C=C(C=C4)F)F
|
InChI=1S/C19H21F2N3O/c1-19(2,3)22-18(25)16-15-10-4-5-11(8-10)17(15)24(23-16)14-7-6-12(20)9-13(14)21/h6-7,9-11H,4-5,8H2,1-3H3,(H,22,25)/t10-,11+/m0/s1 Key:NTPZXHMTJGOMCJ-WDEREUQCSA-N
|
Tedalinab (GRC-10693) is a drug developed by Glenmark Pharmaceuticals for the treatment of osteoarthritis and neuropathic pain, which acts as a potent and selective cannabinoid CB2 receptor agonist. It has a very high selectivity of 4700x for CB2 over the related CB1 receptor, has good oral bioavailability and has shown promising safety results and effective analgesic and antiinflammatory actions in early clinical trials.[1] Many related compounds are known, most of which also show high CB2 selectivity.[2]
See also
References
|
|---|
Phytocannabinoids (comparison) | | Cannabibutols | |
|---|
| Cannabichromenes | |
|---|
| Cannabicyclols | |
|---|
| Cannabidiols | |
|---|
| Cannabielsoins | |
|---|
| Cannabigerols | |
|---|
| Cannabiphorols | |
|---|
| Cannabinols |
- CBN
- CBNA
- CBN-C1
- CBN-C2
- CBN-C4
- CBNM
- CBND
- CBNP
- CBVD
|
|---|
| Cannabitriols | |
|---|
| Cannabivarins | |
|---|
| Delta-3-tetrahydrocannabinols | |
|---|
| Delta-4-tetrahydrocannabinols | |
|---|
| Delta-7-tetrahydrocannabinols | |
|---|
| Delta-8-tetrahydrocannabinols | |
|---|
| Delta-9-tetrahydrocannabinols | |
|---|
| Delta-10-Tetrahydrocannabinols | |
|---|
| Delta-11-Tetrahydrocannabinols | |
|---|
| Miscellaneous cannabinoids | |
|---|
| Active metabolites | |
|---|
|
|---|
| Endocannabinoids | |
|---|
Synthetic cannabinoid receptor agonists / neocannabinoids | Classical cannabinoids (dibenzopyrans) | |
|---|
Non-classical cannabinoids | |
|---|
| Adamantoylindoles | |
|---|
| Benzimidazoles | |
|---|
| Benzoylindoles |
- 1-Butyl-3-(2-methoxybenzoyl)indole
- 1-Butyl-3-(4-methoxybenzoyl)indole
- 1-Pentyl-3-(2-methoxybenzoyl)indole
- AM-630
- AM-679
- AM-694
- AM-1241
- AM-2233
- GW-405,833 (L-768,242)
- Pravadoline
- RCS-4
- WIN 54,461
|
|---|
| Cyclohexylphenols | |
|---|
| Eicosanoids |
- AM-883
- AM-1346
- ACEA
- ACPA
- Methanandamide (AM-356)
- O-585
- O-689
- O-1812
- O-1860
- O-1861
|
|---|
Indazole-3- carboxamides | |
|---|
| Indole-3-carboxamides | |
|---|
| Indole-3-carboxylates | |
|---|
| Naphthoylindazoles | |
|---|
| Naphthoylindoles | |
|---|
| Naphthoylpyrroles |
- JWH-030
- JWH-031
- JWH-032
- JWH-033
- JWH-036
- JWH-044
- JWH-045
- JWH-145
- JWH-146
- JWH-147
- JWH-150
- JWH-156
- JWH-243
- JWH-244
- JWH-245
- JWH-246
- JWH-292
- JWH-293
- JWH-307
- JWH-308
- JWH-309
- JWH-346
- JWH-347
- JWH-348
- JWH-363
- JWH-364
- JWH-365
- JWH-366
- JWH-367
- JWH-368
- JWH-369
- JWH-370
- JWH-371
- JWH-372
- JWH-373
|
|---|
| Naphthylmethylindenes | |
|---|
| Naphthylmethylindoles |
- JWH-175
- JWH-184
- JWH-185
- JWH-192
- JWH-194
- JWH-195
- JWH-196
- JWH-197
- JWH-199
|
|---|
| Phenylacetylindoles | |
|---|
| Pyrazolecarboxamides | |
|---|
Tetramethylcyclo- propanoylindazoles | |
|---|
Tetramethylcyclo- propanoylindoles | |
|---|
| Others | |
|---|
|
|---|
| Allosteric CBRTooltip Cannabinoid receptor ligands | |
|---|
Endocannabinoid enhancers (inactivation inhibitors) | |
|---|
Anticannabinoids (antagonists/inverse agonists/antibodies) | |
|---|
|
|
|---|
Receptor (ligands) | | CB1Tooltip Cannabinoid receptor type 1 | Agonists (abridged, full list) | |
|---|
| Inverse agonists | |
|---|
| Antagonists | |
|---|
|
|---|
| CB2Tooltip Cannabinoid receptor type 2 | | Agonists |
- 2-AG
- 2-AGE (noladin ether)
- 3,3'-Diindolylmethane
- 4-O-Methylhonokiol
- α-Amyrin · β-Amyrin
- A-796,260
- A-834,735
- A-836,339
- AM-1172
- AM-1221
- AM-1235
- AM-1241
- AM-2232
- Anandamide
- AZ-11713908
- Cannabinol
- Caryophyllene
- CB-13
- CBS-0550
- CP 55,940
- GW-405,833 (L-768,242)
- GW-842,166X
- HU-308
- JTE 7-31
- JWH-007
- JWH-015
- JWH-018
- JWH-73
- JWH-133
- L-759,633
- L-759,656
- Lenabasum (anabasum)
- Magnolol
- MDA-19
- Nabitan
- NADA
- Olorinab (APD-371)
- PF-03550096
- S-444,823
- SER-601
- Serinolamide A
- UR-144
- THC (dronabinol)
- THCV
- Tetrahydromagnolol
- Virodhamine
|
|---|
| Antagonists | |
|---|
|
|---|
NAGly (GPR18) | |
|---|
| GPR55 | |
|---|
| GPR119 | |
|---|
|
|---|
Transporter (modulators) | | eCBTsTooltip Endocannabinoid transporter | |
|---|
|
|---|
Enzyme (modulators) | | FAAHTooltip Fatty acid amide hydrolase | |
|---|
| MAGL | |
|---|
| ABHD6 |
- Inhibitors: JZP-169
- JZP-430
- KT182
- KT185
- KT195
- KT203
- LEI-106
- ML294
- ML295
- ML296
- UCM710
- WWL-70
|
|---|
| ABHD12 | |
|---|
|
|---|
| Others |
- Precursors: Phosphatidylethanolamine
- NAPE
- Diacylglycerol
- Others: 2-PG (directly potentiates activity of 2-AG at CB1 receptor)
- ARN-272 (FAAH-like anandamide transporter inhibitor)
|
|---|
- See also
- Receptor/signaling modulators
- Cannabinoids (cannabinoids by structure)
|