BIBP-3226

BIBP-3226
(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	5311023
Hemijski podaci
Formula	C27H31N5O3
Mol. masa	473.566 g/mol
SMILES	eMolekuli & PubHem
InChI
	InChI=1S/C27H31N5O3/c28-27(29)30-17-7-12-23(25(34)31-18-19-13-15-22(33)16-14-19)32-26(35)24(20-8-3-1-4-9-20)21-10-5-2-6-11-21/h1-6,8-11,13-16,23-24,33H,7,12,17-18H2,(H,31,34)(H,32,35)(H4,28,29,30)/t23-/m1/s1 ; Key: KUWBXRGRMQZCSS-HSZRJFAPSA-N
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

↑ 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. edit
↑ 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.

Spoljašnje veze

	Portal Medicina
	Portal Hemija

Šablon:Neuropeptidni ligandi

[1] 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. edit

[2] 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.

[pmid7705422-3] 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.

[pmid16762456-4] 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.

[pmid9723965-5] 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.

[pmid12034130-6] 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.

[pmid9802417-7] 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.

[pmid17463058-8] 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.

[pmid10915060-9] 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.

[pmid18851917-10] 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.

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