SNAP-7941

SNAP-7941
Klinički podaci
Identifikatori
ATC kod	nije dodeljen
ChEMBL	CHEMBL185271
Hemijski podaci
Formula	C33H41F2N5O6
Mol. masa	641,704
SMILES	eMolekuli & PubHem
InChI
	InChI=1S/C33H41F2N5O6/c1-20(2)30(41)37-24-8-5-7-22(17-24)21-11-15-39(16-12-21)14-6-13-36-32(43)40-29(23-9-10-25(34)26(35)18-23)28(31(42)46-4)27(19-45-3)38-33(40)44/h5,7-10,17-18,20-21,29H,6,11-16,19H2,1-4H3,(H,36,43)(H,37,41)(H,38,44) ; Key: SDJGJNOAZSCFSF-UHFFFAOYSA-N
Farmakoinformacioni podaci
Trudnoća	?
Pravni status

SNAP-7941 je lek koji se koristi u naučnim istraživanjima. On je selektivni nepeptidni antagonist melanin-koncentrirajućeg hormonskog receptora MCH₁. U životinjskim studijama je pokazano da proizvodi anksiolitičke, antidepresivne i anoreksne efekte.^[2]^[3] Međutim, rezultati kliničkih ispitivanja su bili razoračaravajući.^[4] SNAP-7941 je značajan kao vodeće jedinjenje iz kojeg su potentniji i selektivniji antagonist i razvijeni, poput SNAP-94847,^[5]^[6] mada se ovo jedinjenje i dalje koristi u istraživanjima funkcija MCH₁ receptora.^[7]^[8]

Reference

↑ Gaulton A, Bellis LJ, Bento AP, Chambers J, Davies M, Hersey A, Light Y, McGlinchey S, Michalovich D, Al-Lazikani B, Overington JP. (2012). „ChEMBL: a large-scale bioactivity database for drug discovery”. Nucleic Acids Res 40 (Database issue): D1100-7. DOI:10.1093/nar/gkr777. PMID 21948594. edit
↑ Borowsky B, Durkin MM, Ogozalek K, Marzabadi MR, DeLeon J, Lagu B, Heurich R, Lichtblau H, Shaposhnik Z, Daniewska I, Blackburn TP, Branchek TA, Gerald C, Vaysse PJ, Forray C (August 2002). „Antidepressant, anxiolytic and anorectic effects of a melanin-concentrating hormone-1 receptor antagonist”. Nature Medicine 8 (8): 825–30. DOI:10.1038/nm741. PMID 12118247.
↑ Doggrell SA (June 2003). „Does the melanin-concentrating hormone antagonist SNAP-7941 deserve 3As?”. Expert Opinion on Investigational Drugs 12 (6): 1035–8. DOI:10.1517/13543784.12.6.1035. PMID 12783607.
↑ Basso AM, Bratcher NA, Gallagher KB, Cowart MD, Zhao C, Sun M, Esbenshade TA, Brune ME, Fox GB, Schmidt M, Collins CA, Souers AJ, Iyengar R, Vasudevan A, Kym PR, Hancock AA, Rueter LE (July 2006). „Lack of efficacy of melanin-concentrating hormone-1 receptor antagonists in models of depression and anxiety”. European Journal of Pharmacology 540 (1-3): 115–20. DOI:10.1016/j.ejphar.2006.04.043. PMID 16765941.
↑ Jiang Y, Chen CA, Lu K, Daniewska I, De Leon J, Kong R, Forray C, Li B, Hegde LG, Wolinsky TD, Craig DA, Wetzel JM, Andersen K, Marzabadi MR (August 2007). „Synthesis and SAR investigations for novel melanin-concentrating hormone 1 receptor (MCH1) antagonists Part 1. The discovery of arylacetamides as viable replacements for the dihydropyrimidinone moiety of an HTS hit”. Journal of Medicinal Chemistry 50 (16): 3870–82. DOI:10.1021/jm060381c. PMID 17668921.
↑ Chen CA, Jiang Y, Lu K, Daniewska I, Mazza CG, Negron L, Forray C, Parola T, Li B, Hegde LG, Wolinsky TD, Craig DA, Kong R, Wetzel JM, Andersen K, Marzabadi MR (August 2007). „Synthesis and SAR investigations for novel melanin-concentrating hormone 1 receptor (MCH1) antagonists part 2: A hybrid strategy combining key fragments of HTS hits”. Journal of Medicinal Chemistry 50 (16): 3883–90. DOI:10.1021/jm060383x. PMID 17668922.
↑ Millan MJ, Gobert A, Panayi F, Rivet JM, Dekeyne A, Brocco M, Ortuno JC, Di Cara B (December 2008). „The melanin-concentrating hormone1 receptor antagonists, SNAP-7941 and GW3430, enhance social recognition and dialysate levels of acetylcholine in the frontal cortex of rats”. The International Journal of Neuropsychopharmacology / Official Scientific Journal of the Collegium Internationale Neuropsychopharmacologicum (CINP) 11 (8): 1105–22. DOI:10.1017/S1461145708008894. PMID 18466669.
↑ Hegde LG, Ping XL, Jochnowitz N, Craig DA (January 2009). „The role of melanin-concentrating hormone-1 receptors in the voiding reflex in rats”. The Journal of Pharmacology and Experimental Therapeutics 328 (1): 165–73. DOI:10.1124/jpet.108.143495. PMID 18849359.

Spoljašnje veze

	Portal Medicina
	Portal Hemija

Šablon:Neuropeptidni ligandi

[1] Gaulton A, Bellis LJ, Bento AP, Chambers J, Davies M, Hersey A, Light Y, McGlinchey S, Michalovich D, Al-Lazikani B, Overington JP. (2012). „ChEMBL: a large-scale bioactivity database for drug discovery”. Nucleic Acids Res 40 (Database issue): D1100-7. DOI:10.1093/nar/gkr777. PMID 21948594. edit

[pmid12118247-2] Borowsky B, Durkin MM, Ogozalek K, Marzabadi MR, DeLeon J, Lagu B, Heurich R, Lichtblau H, Shaposhnik Z, Daniewska I, Blackburn TP, Branchek TA, Gerald C, Vaysse PJ, Forray C (August 2002). „Antidepressant, anxiolytic and anorectic effects of a melanin-concentrating hormone-1 receptor antagonist”. Nature Medicine 8 (8): 825–30. DOI:10.1038/nm741. PMID 12118247.

[pmid12783607-3] Doggrell SA (June 2003). „Does the melanin-concentrating hormone antagonist SNAP-7941 deserve 3As?”. Expert Opinion on Investigational Drugs 12 (6): 1035–8. DOI:10.1517/13543784.12.6.1035. PMID 12783607.

[pmid16765941-4] Basso AM, Bratcher NA, Gallagher KB, Cowart MD, Zhao C, Sun M, Esbenshade TA, Brune ME, Fox GB, Schmidt M, Collins CA, Souers AJ, Iyengar R, Vasudevan A, Kym PR, Hancock AA, Rueter LE (July 2006). „Lack of efficacy of melanin-concentrating hormone-1 receptor antagonists in models of depression and anxiety”. European Journal of Pharmacology 540 (1-3): 115–20. DOI:10.1016/j.ejphar.2006.04.043. PMID 16765941.

[pmid17668921-5] Jiang Y, Chen CA, Lu K, Daniewska I, De Leon J, Kong R, Forray C, Li B, Hegde LG, Wolinsky TD, Craig DA, Wetzel JM, Andersen K, Marzabadi MR (August 2007). „Synthesis and SAR investigations for novel melanin-concentrating hormone 1 receptor (MCH1) antagonists Part 1. The discovery of arylacetamides as viable replacements for the dihydropyrimidinone moiety of an HTS hit”. Journal of Medicinal Chemistry 50 (16): 3870–82. DOI:10.1021/jm060381c. PMID 17668921.

[pmid17668922-6] Chen CA, Jiang Y, Lu K, Daniewska I, Mazza CG, Negron L, Forray C, Parola T, Li B, Hegde LG, Wolinsky TD, Craig DA, Kong R, Wetzel JM, Andersen K, Marzabadi MR (August 2007). „Synthesis and SAR investigations for novel melanin-concentrating hormone 1 receptor (MCH1) antagonists part 2: A hybrid strategy combining key fragments of HTS hits”. Journal of Medicinal Chemistry 50 (16): 3883–90. DOI:10.1021/jm060383x. PMID 17668922.

[pmid18466669-7] Millan MJ, Gobert A, Panayi F, Rivet JM, Dekeyne A, Brocco M, Ortuno JC, Di Cara B (December 2008). „The melanin-concentrating hormone1 receptor antagonists, SNAP-7941 and GW3430, enhance social recognition and dialysate levels of acetylcholine in the frontal cortex of rats”. The International Journal of Neuropsychopharmacology / Official Scientific Journal of the Collegium Internationale Neuropsychopharmacologicum (CINP) 11 (8): 1105–22. DOI:10.1017/S1461145708008894. PMID 18466669.

[pmid18849359-8] Hegde LG, Ping XL, Jochnowitz N, Craig DA (January 2009). „The role of melanin-concentrating hormone-1 receptors in the voiding reflex in rats”. The Journal of Pharmacology and Experimental Therapeutics 328 (1): 165–73. DOI:10.1124/jpet.108.143495. PMID 18849359.

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