GET-73
(Redirected from Draft:GET-73)
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| Formula | C13H16F3NO2 |
| Molar mass | 275.271 g·mol−1 |
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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
[edit]- ^ Ferraro L, Loche A, Beggiato S, Tomasini MC, Antonelli T, Colombo G, et al. (2013). "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". review. Current Medicinal Chemistry. 20 (27): 3339–57. doi:10.2174/09298673113209990167. PMID 23862615.
- ^ a b c Burnette EM, Nieto SJ, Grodin EN, Meredith LR, Hurley B, Miotto K, et al. (February 2022). "Novel Agents for the Pharmacological Treatment of Alcohol Use Disorder". review. Drugs. 82 (3): 251–274. doi:10.1007/s40265-021-01670-3. PMC 8888464. PMID 35133639.
- ^ a b Haass-Koffler CL, Goodyear K, Loche A, Long VM, Lobina C, Tran HH, et al. (February 2018). "Administration of the metabotropic glutamate receptor subtype 5 allosteric modulator GET 73 with alcohol: A translational study in rats and humans". Journal of Psychopharmacology (Oxford, England). 32 (2): 163–173. doi:10.1177/0269881117746904. PMC 7014573. PMID 29361897.
- ^ Mihov Y, Hasler G (July 2016). "Negative Allosteric Modulators of Metabotropic Glutamate Receptors Subtype 5 in Addiction: a Therapeutic Window". The International Journal of Neuropsychopharmacology. 19 (7): pyw002. doi:10.1093/ijnp/pyw002. PMC 4966271. PMID 26802568.
- ^ Haass-Koffler CL, Perciballi R, Magill M, Loche A, Cacciaglia R, Leggio L, et al. (January 2022). "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. doi:10.1007/s00213-021-06008-1. PMC 8865311. PMID 34731268.
- ^ "GET-73". Synapse. PatSnap.
Further reading
[edit]- Beggiato S, Borelli AC, Tomasini MC, Castelli MP, Pintori N, Cacciaglia R, et al. (5 April 2018). "In Vitro Functional Characterization of GET73 as Possible Negative Allosteric Modulator of Metabotropic Glutamate Receptor 5". Frontiers in Pharmacology. 9: 327. doi:10.3389/fphar.2018.00327. PMC 5895880. PMID 29674969.
- Haass-Koffler CL, Perciballi R, Magill M, Loche A, Cacciaglia R, Leggio L, et al. (January 2022). "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. doi:10.1007/s00213-021-06008-1. PMC 8865311. PMID 34731268.
- Witkin JM, Pandey KP, Smith JL (September 2022). "Clinical investigations of compounds targeting metabotropic glutamate receptors". review. Pharmacology, Biochemistry, and Behavior. 219: 173446. doi:10.1016/j.pbb.2022.173446. PMID 35987339.
