BIBP-3226

BIBP-3226
IUPAC ime
	(2R)-5-(diaminomethylideneamino)-2-([2,2-diphenylacetyl]amino)-N-[(4-hydroxyphenyl)methyl]pentanamide
Identifikatori
CAS broj	159013-54-4
PubChem	CID 5311023
IUPHAR/BPS	1485
Sinonimi	BIBP-3226
Hemijski podaci
Formula	C27H31N5O3
Molarna masa	473.566 g/mol
	SMILES C1=CC=C(C=C1)C(C2=CC=CC=C2)C(=O)N[C@H](CCCN=C(N)N)C(=O)NCC3=CC=C(C=C3)O; ;

BIBP-3226 je lek koji se koristi u naučnim istraživanjima. On deluje kao potentan i selektivan antagonist neuropeptidnog Y receptora Y₁^[1] kao i neuropeptidnog FF receptora.^[2] 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^[3] i anksioznost,^[4] i BIBP-3226 ima anksiogeno^[5] i anoreksno dejstvo, kao i sposobnost blokiranja Y₁-posredovanog oslobađanja kortikotropin oslobađajućeg hormona.^[6] On je takođe bio korišten kao vodeće jedinjenje u razvoju brojnih novijih i potentnijih Y₁ antagonista.^[7]^[8]

Reference

^ Rudolf K, Eberlein W, Engel W, Wieland HA, Willim KD, Entzeroth M, Wienen W, Beck-Sickinger AG, Doods HN (1994). „The first highly potent and selective non-peptide neuropeptide Y Y1 receptor antagonist: BIBP3226”. European Journal of Pharmacology. 271 (2-3): R11—3. PMID 7705422. doi:10.1016/0014-2999(94)90822-2.
^ Fang Q, Guo J, He F, Peng YL, Chang M, Wang R (2006). „In vivo inhibition of neuropeptide FF agonism by BIBP3226, an NPY Y1 receptor antagonist”. Peptides. 27 (9): 2207—13. PMID 16762456. doi:10.1016/j.peptides.2006.04.002.
^ Kask A, Rägo L, Harro J (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. PMC 1565528 . PMID 9723965. doi:10.1038/sj.bjp.0701969.
^ Kask A, Harro J, von Hörsten S, Redrobe JP, Dumont Y, Quirion R (2002). „The neurocircuitry and receptor subtypes mediating anxiolytic-like effects of neuropeptide Y”. Neuroscience and Biobehavioral Reviews. 26 (3): 259—83. PMID 12034130. doi:10.1016/S0149-7634(01)00066-5.
^ Kask A, Rägo L, Harro J (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. PMID 9802417. doi:10.1016/S0167-0115(98)00076-7.
^ Dimitrov EL, DeJoseph MR, Brownfield MS, Urban JH (2007). „Involvement of neuropeptide Y Y1 receptors in the regulation of neuroendocrine corticotropin-releasing hormone neuronal activity”. Endocrinology. 148 (8): 3666—73. PMID 17463058. doi:10.1210/en.2006-1730.
^ Aiglstorfer I, Hendrich I, Moser C, Bernhardt G, Dove S, Buschauer A (2000). „Structure-activity relationships of neuropeptide Y Y1 receptor antagonists related to BIBP 3226”. Bioorganic & Medicinal Chemistry Letters. 10 (14): 1597—600. PMID 10915060. doi:10.1016/S0960-894X(00)00292-4.
^ Weiss S, Keller M, Bernhardt G, Buschauer A, König B (2008). „Modular synthesis of non-peptidic bivalent NPY Y1 receptor antagonists”. Bioorganic & Medicinal Chemistry. 16 (22): 9858—66. PMID 18851917. doi:10.1016/j.bmc.2008.09.033.

Spoljašnje veze

Molimo Vas, obratite pažnju na važno upozorenje
u vezi sa temama iz oblasti medicine (zdravlja).

[pmid7705422-1] Rudolf K, Eberlein W, Engel W, Wieland HA, Willim KD, Entzeroth M, Wienen W, Beck-Sickinger AG, Doods HN (1994). „The first highly potent and selective non-peptide neuropeptide Y Y1 receptor antagonist: BIBP3226”. European Journal of Pharmacology. 271 (2-3): R11—3. PMID 7705422. doi:10.1016/0014-2999(94)90822-2.

[pmid16762456-2] Fang Q, Guo J, He F, Peng YL, Chang M, Wang R (2006). „In vivo inhibition of neuropeptide FF agonism by BIBP3226, an NPY Y1 receptor antagonist”. Peptides. 27 (9): 2207—13. PMID 16762456. doi:10.1016/j.peptides.2006.04.002.

[pmid9723965-3] Kask A, Rägo L, Harro J (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. PMC 1565528 . PMID 9723965. doi:10.1038/sj.bjp.0701969.

[pmid12034130-4] Kask A, Harro J, von Hörsten S, Redrobe JP, Dumont Y, Quirion R (2002). „The neurocircuitry and receptor subtypes mediating anxiolytic-like effects of neuropeptide Y”. Neuroscience and Biobehavioral Reviews. 26 (3): 259—83. PMID 12034130. doi:10.1016/S0149-7634(01)00066-5.

[pmid9802417-5] Kask A, Rägo L, Harro J (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. PMID 9802417. doi:10.1016/S0167-0115(98)00076-7.

[pmid17463058-6] Dimitrov EL, DeJoseph MR, Brownfield MS, Urban JH (2007). „Involvement of neuropeptide Y Y1 receptors in the regulation of neuroendocrine corticotropin-releasing hormone neuronal activity”. Endocrinology. 148 (8): 3666—73. PMID 17463058. doi:10.1210/en.2006-1730.

[pmid10915060-7] Aiglstorfer I, Hendrich I, Moser C, Bernhardt G, Dove S, Buschauer A (2000). „Structure-activity relationships of neuropeptide Y Y1 receptor antagonists related to BIBP 3226”. Bioorganic & Medicinal Chemistry Letters. 10 (14): 1597—600. PMID 10915060. doi:10.1016/S0960-894X(00)00292-4.

[pmid18851917-8] Weiss S, Keller M, Bernhardt G, Buschauer A, König B (2008). „Modular synthesis of non-peptidic bivalent NPY Y1 receptor antagonists”. Bioorganic & Medicinal Chemistry. 16 (22): 9858—66. PMID 18851917. doi:10.1016/j.bmc.2008.09.033.

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