BIBP-3226
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| |||
| (IUPAC) ime | |||
|---|---|---|---|
| (2R)-5-(diaminomethylideneamino)-2-([2,2-diphenylacetyl]amino)-N-[(4-hydroxyphenyl)methyl]pentanamide | |||
| Klinički podaci | |||
| Identifikatori | |||
| CAS broj | 159013-54-4 | ||
| ATC kod | ? | ||
| PubChem[1][2] | 5311023 | ||
| Hemijski podaci | |||
| Formula | C27H31N5O3 | ||
| Mol. masa | 473.566 g/mol | ||
| SMILES | eMolekuli & PubHem | ||
| |||
| Sinonimi | BIBP-3226 | ||
| Farmakoinformacioni podaci | |||
| Trudnoća | ? | ||
| Pravni status | |||
BIBP-3226 je lek koji se koristi u naučnim istraživanjima. On deluje kao potentan i selektivan antagonist neuropeptidnog Y receptora Y1[3] kao i neuropeptidnog FF receptora.[4] On je bio prvi ne-peptidni antagonist razvijen za Y1 receptor i bio je široko korišten za određivanje funkcije tog receptora u telu. Za Y1 aktivaciju se smatra da učestvuje u funkcijama kao što su regulacija apetita[5] i anksioznost,[6] i BIBP-3226 ima anksiogeno[7] i anoreksno dejstvo, kao i sposobnost blokiranja Y1-posredovanog oslobađanja kortikotropin oslobađajućeg hormona.[8] On je takođe bio korišten kao vodeće jedinjenje u razvoju brojnih novijih i potentnijih Y1 antagonista.[9][10]
Referece[uredi | uredi kod]
- ↑ Li Q, Cheng T, Wang Y, Bryant SH (2010). „PubChem as a public resource for drug discovery.”. Drug Discov Today 15 (23-24): 1052-7. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519.
- ↑ Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). „Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities”. Annual Reports in Computational Chemistry 4: 217-241. DOI:10.1016/S1574-1400(08)00012-1.
- ↑ Rudolf K, Eberlein W, Engel W, Wieland HA, Willim KD, Entzeroth M, Wienen W, Beck-Sickinger AG, Doods HN (December 1994). „The first highly potent and selective non-peptide neuropeptide Y Y1 receptor antagonist: BIBP3226”. European Journal of Pharmacology 271 (2-3): R11–3. DOI:10.1016/0014-2999(94)90822-2. PMID 7705422.
- ↑ Fang Q, Guo J, He F, Peng YL, Chang M, Wang R (September 2006). „In vivo inhibition of neuropeptide FF agonism by BIBP3226, an NPY Y1 receptor antagonist”. Peptides 27 (9): 2207–13. DOI:10.1016/j.peptides.2006.04.002. PMID 16762456.
- ↑ Kask A, Rägo L, Harro J (August 1998). „Evidence for involvement of neuropeptide Y receptors in the regulation of food intake: studies with Y1-selective antagonist BIBP3226”. British Journal of Pharmacology 124 (7): 1507–15. DOI:10.1038/sj.bjp.0701969. PMC 1565528. PMID 9723965.
- ↑ Kask A, Harro J, von Hörsten S, Redrobe JP, Dumont Y, Quirion R (May 2002). „The neurocircuitry and receptor subtypes mediating anxiolytic-like effects of neuropeptide Y”. Neuroscience and Biobehavioral Reviews 26 (3): 259–83. DOI:10.1016/S0149-7634(01)00066-5. PMID 12034130.
- ↑ Kask A, Rägo L, Harro J (September 1998). „Anxiogenic-like effect of the NPY Y1 receptor antagonist BIBP3226 administered into the dorsal periaqueductal gray matter in rats”. Regulatory Peptides 75-76: 255–62. DOI:10.1016/S0167-0115(98)00076-7. PMID 9802417.
- ↑ Dimitrov EL, DeJoseph MR, Brownfield MS, Urban JH (August 2007). „Involvement of neuropeptide Y Y1 receptors in the regulation of neuroendocrine corticotropin-releasing hormone neuronal activity”. Endocrinology 148 (8): 3666–73. DOI:10.1210/en.2006-1730. PMID 17463058.
- ↑ Aiglstorfer I, Hendrich I, Moser C, Bernhardt G, Dove S, Buschauer A (July 2000). „Structure-activity relationships of neuropeptide Y Y1 receptor antagonists related to BIBP 3226”. Bioorganic & Medicinal Chemistry Letters 10 (14): 1597–600. DOI:10.1016/S0960-894X(00)00292-4. PMID 10915060.
- ↑ Weiss S, Keller M, Bernhardt G, Buschauer A, König B (November 2008). „Modular synthesis of non-peptidic bivalent NPY Y1 receptor antagonists”. Bioorganic & Medicinal Chemistry 16 (22): 9858–66. DOI:10.1016/j.bmc.2008.09.033. PMID 18851917.
