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Chemical compound
Pharmaceutical compound
TM-38837 |
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1-(2,4-Dichlorophenyl)-4-ethyl-5-(5-(2-(4-(trifluoromethyl)phenyl)ethynyl)thiophen-2-yl)-N-(piperidin-1-yl)-1H-pyrazole-3-carboxamide
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| Formula | C30H25Cl2F3N4OS |
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| Molar mass | 617.51 g·mol−1 |
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| 3D model (JSmol) | |
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O=C(C1=NN(C2=CC=C(Cl)C=C2Cl)C(C3=CC=C(C#CC4=CC=C(C(F)(F)F)C=C4)S3)=C1CC)NN5CCCCC5
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InChI=1S/C30H25Cl2F3N4OS/c1-2-23-27(29(40)37-38-16-4-3-5-17-38)36-39(25-14-11-21(31)18-24(25)32)28(23)26-15-13-22(41-26)12-8-19-6-9-20(10-7-19)30(33,34)35/h6-7,9-11,13-15,18H,2-5,16-17H2,1H3,(H,37,40) Key:VQOCBFYUDSBDCZ-UHFFFAOYSA-N
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TM-38837 is a small molecule inverse agonist/antagonist of the CB1 cannabinoid receptor, with peripheral selectivity. It is being developed for the treatment of obesity and metabolic disorders by 7TM Pharma.[1] The company has announced phase I clinical trials.
TM-38837 is among the first of a new generation of cannabinoid receptor antagonist designed to avoid the central nervous system liabilities of the first generation CB1 receptor antagonists such as rimonabant.[2]
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Synthetic cannabinoid receptor agonists / neocannabinoids | Classical cannabinoids (dibenzopyrans) | |
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Indazole-3- carboxamides | |
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Tetramethylcyclo- propanoylindoles | |
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| Allosteric CBRTooltip Cannabinoid receptor ligands | |
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Endocannabinoid enhancers (inactivation inhibitors) | |
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Anticannabinoids (antagonists/inverse agonists/antibodies) | |
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Receptor (ligands) | | CB1Tooltip Cannabinoid receptor type 1 | Agonists (abridged, full list) | |
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| Inverse agonists | |
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| Antagonists | |
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| 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
- Tedalinab
- THC (dronabinol)
- THCV
- Tetrahydromagnolol
- Virodhamine
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| Antagonists | |
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NAGly (GPR18) | |
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| GPR55 | |
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| GPR119 | |
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Transporter (modulators) | | eCBTsTooltip Endocannabinoid transporter | |
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Enzyme (modulators) | |
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| Others |
- Others: 2-PG (directly potentiates activity of 2-AG at CB1 receptor)
- ARN-272 (FAAH-like anandamide transporter inhibitor)
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