LY-2183240

LY-2183240
Nama
	Nama IUPAC N,N-dimethyl-5-[(4-biphenyl)methyl]tetrazole-1-carboxamide
Pengecam
No. Pendaftaran CAS	874902-19-9;
Imej model 3D Jmol	Imej berinteraktif;
ChemSpider	9682599;
ECHA InfoCard	100.189.657
PubChem CID	11507802;
UNII	2WBU91OKM7 ;
	InChI InChI=1S/C17H17N5O/c1-21(2)17(23)22-16(18-19-20-22)12-13-8-10-15(11-9-13)14-6-4-3-5-7-14/h3-11H,12H2,1-2H3 Key: GZNIYOXWFCDBBJ-UHFFFAOYSA-N; InChI=1/C17H17N5O/c1-21(2)17(23)22-16(18-19-20-22)12-13-8-10-15(11-9-13)14-6-4-3-5-7-14/h3-11H,12H2,1-2H3 Key: GZNIYOXWFCDBBJ-UHFFFAOYAF;
	SMILES CN(C)C(=O)n1nnnc1Cc2ccc(cc2)-c3ccccc3;
Sifat
Formula kimia	C17H17N5O
Jisim molar	307.349
	Kecuali jika dinyatakan sebaliknya, data diberikan untuk bahan-bahan dalam keadaan piawainya (pada 25 °C [77 °F], 100 kPa).
	Rujukan kotak info

LY-2183240 ialah sebuah ubat yang bertindak sebagai perencat kuat pengambilan semula anandamide endokannabinoid dan sebagai perencat asid lemak amide hydrolase (FAAH), enzim utama yang bertanggungjawab untuk merendahkan anandamide. Ini membawa kepada paras anandamide yang meningkat dengan ketara dalam otak, dan LY-2183240 telah ditunjukkan untuk menghasilkan kesan analgesik dan anxiolytic dalam model haiwan.^[1]^[2]^[3] Walaupun LY-2183240 adalah perencat kuat FAAH, ia mempunyai keupayaan selektiviti yang agak lemah dan juga boleh menghalang beberapa sasaran sampingan enzim lain.^[4] Akibatnya, ia tidak pernah dibangunkan untuk kegunaan klinikal, walaupun ia masih digunakan secara meluas dalam penyelidikan, dan juga telah dijual sebagai ubat pereka.^[5]

Lihat juga[sunting | sunting sumber]

Inhibitor pengambilan semula endokannabinoid
perencat FAAH
- BIA 10-2474
- PF-04457845
- URB-597

Rujukan[sunting | sunting sumber]

^ Dickason-Chesterfield AK, Kidd SR, Moore SA, Schaus JM, Liu B, Nomikos GG, Felder CC (2006). "Pharmacological characterization of endocannabinoid transport and fatty acid amide hydrolase inhibitors". Cellular and Molecular Neurobiology. 26 (4–6): 407–23. doi:10.1007/s10571-006-9072-6. PMID 16736384.CS1 maint: multiple names: authors list (link)
^ Maione S, Morera E, Marabese I, Ligresti A, Luongo L, Ortar G, Di Marzo V (Nov 2008). "Antinociceptive effects of tetrazole inhibitors of endocannabinoid inactivation: cannabinoid and non-cannabinoid receptor-mediated mechanisms". British Journal of Pharmacology. 155 (5): 775–82. doi:10.1038/bjp.2008.308. PMC 2584918. PMID 18660824.CS1 maint: multiple names: authors list (link)
^ Powers MS, Barrenha GD, Mlinac NS, Barker EL, Chester JA (Dec 2010). "Effects of the novel endocannabinoid uptake inhibitor, LY2183240, on fear-potentiated startle and alcohol-seeking behaviors in mice selectively bred for high alcohol preference". Psychopharmacology. 212 (4): 571–83. doi:10.1007/s00213-010-1997-2. PMC 2982902. PMID 20838777.CS1 maint: multiple names: authors list (link)
^ Alexander JP, Cravatt BF (Aug 2006). "The putative endocannabinoid transport blocker LY2183240 is a potent inhibitor of FAAH and several other brain serine hydrolases". Journal of the American Chemical Society. 128 (30): 9699–704. doi:10.1021/ja062999h. PMID 16866524.
^ Uchiyama N, Matsuda S, Kawamura M, Shimokawa Y, Kikura-Hanajiri R, Aritake K, Urade Y, Goda Y (2014). "Characterization of four new designer drugs, 5-chloro-NNEI, NNEI indazole analog, α-PHPP and α-POP, with 11 newly distributed designer drugs in illegal products". Forensic Sci Int. 243: 1–13. doi:10.1016/j.forsciint.2014.03.013. PMID 24769262.CS1 maint: multiple names: authors list (link)

Bacaan lanjut[sunting | sunting sumber]

Moore, S. A.; Nomikos, G. G.; Dickason-Chesterfield, A. K.; Schober, D. A.; Schaus, J. M.; Ying, B. P.; Xu, Y. C.; Phebus, L; Simmons, R. M. (2005). "Identification of a high-affinity binding site involved in the transport of endocannabinoids". Proceedings of the National Academy of Sciences. 102 (49): 17852–7. doi:10.1073/pnas.0507470102. PMC 1295594. PMID 16314570.Templat:Cannabinoids Templat:Cannabinoidergics

[1] Dickason-Chesterfield AK, Kidd SR, Moore SA, Schaus JM, Liu B, Nomikos GG, Felder CC (2006). "Pharmacological characterization of endocannabinoid transport and fatty acid amide hydrolase inhibitors". Cellular and Molecular Neurobiology. 26 (4–6): 407–23. doi:10.1007/s10571-006-9072-6. PMID 16736384.CS1 maint: multiple names: authors list (link)

[2] Maione S, Morera E, Marabese I, Ligresti A, Luongo L, Ortar G, Di Marzo V (Nov 2008). "Antinociceptive effects of tetrazole inhibitors of endocannabinoid inactivation: cannabinoid and non-cannabinoid receptor-mediated mechanisms". British Journal of Pharmacology. 155 (5): 775–82. doi:10.1038/bjp.2008.308. PMC 2584918. PMID 18660824.CS1 maint: multiple names: authors list (link)

[3] Powers MS, Barrenha GD, Mlinac NS, Barker EL, Chester JA (Dec 2010). "Effects of the novel endocannabinoid uptake inhibitor, LY2183240, on fear-potentiated startle and alcohol-seeking behaviors in mice selectively bred for high alcohol preference". Psychopharmacology. 212 (4): 571–83. doi:10.1007/s00213-010-1997-2. PMC 2982902. PMID 20838777.CS1 maint: multiple names: authors list (link)

[4] Alexander JP, Cravatt BF (Aug 2006). "The putative endocannabinoid transport blocker LY2183240 is a potent inhibitor of FAAH and several other brain serine hydrolases". Journal of the American Chemical Society. 128 (30): 9699–704. doi:10.1021/ja062999h. PMID 16866524.

[5] Uchiyama N, Matsuda S, Kawamura M, Shimokawa Y, Kikura-Hanajiri R, Aritake K, Urade Y, Goda Y (2014). "Characterization of four new designer drugs, 5-chloro-NNEI, NNEI indazole analog, α-PHPP and α-POP, with 11 newly distributed designer drugs in illegal products". Forensic Sci Int. 243: 1–13. doi:10.1016/j.forsciint.2014.03.013. PMID 24769262.CS1 maint: multiple names: authors list (link)

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