Chemistry:GET-73
 | |
| Identifiers | |
|---|---|
| |
| CAS Number | |
| PubChem CID | |
| PubChem SID | |
| DrugBank | |
| ChemSpider | |
| UNII | |
| KEGG | |
| ChEMBL | |
| Chemical and physical data | |
| Formula | C13H16F3NO2 |
| Molar mass | 275.271 g·mol−1 |
| 3D model (JSmol) | |
| |
| |
GET 73 is an investigational new drug, developed by Laboratorio Farmaceutico CT SRL, that is being evaluated for treating alcohol use disorder (AUD). It acts as a negative allosteric modulator (NAM) of the metabotropic glutamate receptor 5 (mGluR5), a receptor system implicated in the neurobiology of addiction and alcohol-related behaviors.[1][2][3][4]
Preclinical studies indicate that GET 73 reduces voluntary alcohol intake, diminishes the alcohol deprivation effect, and demonstrates neuroprotective properties against alcohol-induced neurotoxicity in animal models.[3][2] It has also been evaluated in early-phase human trials for safety and potential efficacy in reducing alcohol craving and consumption.[5][2]
GET 73 is a more structurally complex analog of GHB.[6]
References
- ↑ "The new compound GET73, N-[(4-trifluoromethyl)benzyl]4-methoxybutyramide, Regulates hippocampal Aminoacidergic transmission possibly via an allosteric modulation of mGlu5 receptor. Behavioural evidence of its "anti-alcohol" and anxiolytic properties". Current Medicinal Chemistry 20 (27): 3339–57. 2013. doi:10.2174/09298673113209990167. PMID 23862615.
- ↑ 2.0 2.1 2.2 "Novel Agents for the Pharmacological Treatment of Alcohol Use Disorder". Drugs 82 (3): 251–274. February 2022. doi:10.1007/s40265-021-01670-3. PMID 35133639.
- ↑ 3.0 3.1 "Administration of the metabotropic glutamate receptor subtype 5 allosteric modulator GET 73 with alcohol: A translational study in rats and humans". Journal of Psychopharmacology 32 (2): 163–173. February 2018. doi:10.1177/0269881117746904. PMID 29361897.
- ↑ "Negative Allosteric Modulators of Metabotropic Glutamate Receptors Subtype 5 in Addiction: a Therapeutic Window". The International Journal of Neuropsychopharmacology 19 (7). July 2016. doi:10.1093/ijnp/pyw002. PMID 26802568.
- ↑ "An inpatient human laboratory study assessing the safety and tolerability, pharmacokinetics, and biobehavioral effect of GET 73 when co-administered with alcohol in individuals with alcohol use disorder". Psychopharmacology 239 (1): 35–46. January 2022. doi:10.1007/s00213-021-06008-1. PMID 34731268.
- ↑ "GET-73". Synapse. PatSnap. https://synapse.patsnap.com/drug/f54382fe65114d168e44a8e756baa917.
Further reading
- "In Vitro Functional Characterization of GET73 as Possible Negative Allosteric Modulator of Metabotropic Glutamate Receptor 5". Frontiers in Pharmacology 9. 5 April 2018. doi:10.3389/fphar.2018.00327. PMID 29674969.
- "An inpatient human laboratory study assessing the safety and tolerability, pharmacokinetics, and biobehavioral effect of GET 73 when co-administered with alcohol in individuals with alcohol use disorder". Psychopharmacology 239 (1): 35–46. January 2022. doi:10.1007/s00213-021-06008-1. PMID 34731268.
- "Clinical investigations of compounds targeting metabotropic glutamate receptors". Pharmacology, Biochemistry, and Behavior 219. September 2022. doi:10.1016/j.pbb.2022.173446. PMID 35987339.
 |  |
