GET-73

GET-73
Identifiers
	IUPAC name 4-methoxy-N-[[4-(trifluoromethyl)phenyl]methyl]butanamide;
CAS Number	202402-01-5;
PubChem CID	10221200;
PubChem SID	8396692;
DrugBank	DB12928;
UNII	U5CLZ223FH;
KEGG	D84113;
ChEMBL	ChEMBL4297543;
E number	{{#property:P628}}
ECHA InfoCard	{{#property:P2566}}
Chemical and physical data
Formula	C13H16F3NO2
Molar mass	275.271 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES COCCCC(=O)NCC1=CC=C(C=C1)C(F)(F)F;
	InChI InChI=InChI=1S/C13H16F3NO2/c1-19-8-2-3-12(18)17-9-10-4-6-11(7-5-10)13(14,15)16/h4-7H,2-3,8-9H2,1H3,(H,17,18); Key:QLZOWJNFLXSDSH-UHFFFAOYSA-N;

GET 73 is an investigational new drug developed by Laboratorio Farmaceutico CT SRL, primarily investigated for its potential in 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]^[5]

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.^[4] It has also been evaluated in early-phase human trials for safety and potential efficacy in reducing alcohol craving and consumption.^[3]

GET 73 is a more structurally complex analog of GHB.^[6]

References

↑ Ferraro L, Loche A, Beggiato S, Tomasini MC, Antonelli T, Colombo G, Lobina C, Carai MA, Porcu A, Castelli MP, Clerici F, Borelli AC, Cacciaglia R, Tanganelli S (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". Current Medicinal Chemistry. 20 (27): 3339–57. doi:10.2174/09298673113209990167. PMID 23862615.
↑ Beggiato S, Borelli AC, Tomasini MC, Castelli MP, Pintori N, Cacciaglia R, Loche A, Ferraro L (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.
↑ ^3.0 ^3.1 Haass-Koffler CL, Perciballi R, Magill M, Loche A, Cacciaglia R, Leggio L, Swift RM (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 Check |pmc= value (help). PMID 34731268 Check |pmid= value (help).
↑ ^4.0 ^4.1 Haass-Koffler CL, Goodyear K, Loche A, Long VM, Lobina C, Tran HH, Cacciaglia R, Swift RM, Colombo G, Leggio L (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 Check |pmc= value (help). 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.
↑ "GET-73". Synapse. PatSnap.

Burnette EM, Nieto SJ, Grodin EN, Meredith LR, Hurley B, Miotto K, Gillis AJ, Ray LA (February 2022). "Novel Agents for the Pharmacological Treatment of Alcohol Use Disorder". Drugs. 82 (3): 251–274. doi:10.1007/s40265-021-01670-3. PMC 8888464 Check |pmc= value (help). PMID 35133639 Check |pmid= value (help).
Witkin JM, Pandey KP, Smith JL (September 2022). "Clinical investigations of compounds targeting metabotropic glutamate receptors". Pharmacology, Biochemistry, and Behavior. 219: 173446. doi:10.1016/j.pbb.2022.173446. PMID 35987339 Check |pmid= value (help).

Template:Drugs used in addictive disorders

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[Ferraro_2013-1] Ferraro L, Loche A, Beggiato S, Tomasini MC, Antonelli T, Colombo G, Lobina C, Carai MA, Porcu A, Castelli MP, Clerici F, Borelli AC, Cacciaglia R, Tanganelli S (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". Current Medicinal Chemistry. 20 (27): 3339–57. doi:10.2174/09298673113209990167. PMID 23862615.

[Beggiato_2018-2] Beggiato S, Borelli AC, Tomasini MC, Castelli MP, Pintori N, Cacciaglia R, Loche A, Ferraro L (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_2022-3] 3.0 ^3.1 Haass-Koffler CL, Perciballi R, Magill M, Loche A, Cacciaglia R, Leggio L, Swift RM (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 Check |pmc= value (help). PMID 34731268 Check |pmid= value (help).

[Haass-Koffler_2018-4] 4.0 ^4.1 Haass-Koffler CL, Goodyear K, Loche A, Long VM, Lobina C, Tran HH, Cacciaglia R, Swift RM, Colombo G, Leggio L (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 Check |pmc= value (help). PMID 29361897.

[Mihov_2016-5] 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.

[synapse-6] "GET-73". Synapse. PatSnap.

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GET-73

References

Further reading

📰 Article(s) of the same category(ies)[edit]

Identifiers

IUPAC name 4-methoxy-N-[[4-(trifluoromethyl)phenyl]methyl]butanamide
CAS Number	202402-01-5
PubChem CID	10221200
PubChem SID	8396692
DrugBank	DB12928
UNII	U5CLZ223FH
KEGG	D84113
ChEMBL	ChEMBL4297543
E number	{{#property:P628}}
ECHA InfoCard	{{#property:P2566}}
Chemical and physical data
Formula	C₁₃H₁₆F₃NO₂
Molar mass	275.271 g·mol⁻¹
3D model (JSmol)	Interactive image
SMILES COCCCC(=O)NCC1=CC=C(C=C1)C(F)(F)F
InChI InChI=InChI=1S/C13H16F3NO2/c1-19-8-2-3-12(18)17-9-10-4-6-11(7-5-10)13(14,15)16/h4-7H,2-3,8-9H2,1H3,(H,17,18) Key:QLZOWJNFLXSDSH-UHFFFAOYSA-N