The world's first wiki where authorship really matters (Nature Genetics, 2008). Due credit and reputation for authors. Imagine a global collaborative knowledge base for original thoughts. Search thousands of articles and collaborate with scientists around the globe.

wikigene or wiki gene protein drug chemical gene disease author authorship tracking collaborative publishing evolutionary knowledge reputation system wiki2.0 global collaboration genes proteins drugs chemicals diseases compound
Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)
Chemical Compound Review

AC1NSJUK     (2R)-5- (diaminomethylideneamino)-2- (2,2...

Synonyms: BIBP-3226, BIBP3226, CHEMBL332347, SureCN650331, B174_SIGMA, ...
Welcome! If you are familiar with the subject of this article, you can contribute to this open access knowledge base by deleting incorrect information, restructuring or completely rewriting any text. Read more.

Disease relevance of BIBP3226

  • This decrease was blocked by BIBP3226, a Y(1) receptor antagonist, or by pertussis toxin, in agreement with Y(1) receptor activation [1].
  • Although there was no major difference in the hemodynamic parameters among the groups, injection of [Leu(31),Pro(34)]-neuropeptide Y tended to further reduce cerebral perfusion during ischemia, while injection of BIBP3226 at 15 microg/kg appeared to have the opposite effect [2].
  • The binding of tritium-labelled BIBP3226, N2-(diphenylacetyl)-N-[(4-hydroxy-phenyl)methyl]-D-arginine amide, to human neuroblastoma SK-N-MC cells was investigated [3].
  • This effect of BIBP3226 on the gonadotrope axis occurred without apparent toxicity, but was accompanied by a transient decrease in body weight gain on the first day of treatment, suggesting an effect on appetite [4].
  • BIBP3226 (N2-(diphenylacetyl)-N-[4-hydroxyphenyl)methyl]-D-arginine amide) has been used to examine the presence of neuropeptide Y Y1 receptors in 3 gastrointestinal epithelial preparations, namely the rat jejunum and descending colon mucosae and a human colonic adenocarcinoma cell line [5].

Psychiatry related information on BIBP3226


High impact information on BIBP3226

  • QRFP-induced food intake was abolished by preadministration of BIBP3226, a specific antagonist for the Y1 neuropeptide Y receptor [8].
  • Assays performed by using [125I][Leu31,Pro34]PYY in the presence of 1 microM BIBP3226 to block the Y1 receptor subtype revealed a pharmacological profile highly similar to the cloned Y5 receptor [9].
  • These similarities together with the finding that BIBP3226, an anorexigenic Y1 receptor ligand, also binds to NPFF1 suggest a potential role for NPFF1 in feeding [10].
  • Hindlimb vascular conductance was measured during infusion of BIBP3226 (Y(1)-receptor antagonist; 100 microg kg(-1)), prazosin (alpha(1)-receptor antagonist; 20 microg kg(-1)), and combined blockade [11].
  • The effects of 100 nM NPY, but not PYY, were antagonized partially by the Y1 receptor selective antagonist BIBP3226 (0.1 micro M) [12].

Chemical compound and disease context of BIBP3226


Biological context of BIBP3226

  • Additionally, [125I][Leu31,Pro34]PYY/BIBP3226-insensitive binding sites were not clearly detected in the vervet and human brains [14].
  • BIBP3226, but not rauwolscine (a selective alpha2-adrenoceptor antagonist), abolished periarterial nerve stimulation-induced enhancement of angiotensin II-mediated renal vasoconstriction [15].
  • BIBP3226, the selective Y1 antagonist, potently displaces [125I]NPY from its binding site IC50 = 1.91 x 10(-9) M [16].
  • It is concluded that, at moderately high concentrations, the NPY Y1 receptor antagonist BIBP3226 and its entantiomer BIBP3435 are able to increase the [Ca2+ ]i in CHO cells either by stimulating another receptor or by directly affecting cellular mechanisms that are involved in calcium homeostasis [17].
  • The selective Y1 receptor antagonist (1 microM BIBP3226) had no significant effect upon either peptide YY (PYY) responses or on electric field stimulated changes in electrogenic ion transport in rat jejunum mucosa [5].

Anatomical context of BIBP3226

  • This stimulation was resistant to BIBP3226 a non-peptidergic antagonist at Y1 receptors, but it was significantly reduced in membranes treated with selective antibodies against the Gialpha subunits [18].
  • Intracerebroventricular injection of a neuropeptide Y-Y1 receptor agonist increases while BIBP3226, a Y1 antagonist, reduces the infarct volume following transient middle cerebral artery occlusion in rats [2].
  • NPY Y(1) antagonist BIBP3226 and mixed Y(1) antagonist/Y(4) agonist GR231118 are able to displace with low affinity, 50 -- 100 nM, the specific binding on NPFF receptors expressed in CHO cells as well as in rat dorsal spinal cord, an affinity however superior to those determined against Y(2), Y(4) or Y(5) receptors [19].
  • Results from the present study showed that microinjection of the D1 receptor agonist SKF-38393 into the nucleus accumbens shell induced a suppression of NK activity that was reversed by BIBP3226 [20].
  • Because cardiac myocytes express both Y1 and Y2 NPY receptors, we repeated the experiments in the presence of the receptor blockers, BIBP3226 and BIIE0246 [21].

Associations of BIBP3226 with other chemical compounds

  • However, pretreatment with BIBO3304 or BIBP3226 significantly blocked the anti-immobility effects of NPY [22].
  • Treatment with BIBP3226 was found to completely prevent NPY amplification of LHRH-induced LH surges in pentobarbital-blocked, proestrous rats, thus confirming a pituitary locus of action of the drug [23].
  • Furthermore, BIBP3226 which is unable to inhibit the forskolin-stimulated cyclic AMP production mediated by NPFF(2) receptors, antagonizes the effect of NPFF, revealing the first antagonist of NPFF receptors [19].
  • BIBP3226 {(R)-N2-(diphenylacetyl)-N-[(4-hydroxyphenyl)-methyl]-argininamide} was recently shown to display relatively high affinities for neuropeptide FF (NPFF) receptors and exhibit antagonist activities towards NPFF receptors in vitro [24].
  • Effect of BIBP3226 on inositol phosphate accumulation and cytosolic calcium level in control and NPY Y1 receptor expressing CHO-K1 cells [25].

Gene context of BIBP3226

  • BIBP3226, a nonpeptide Y1 receptor antagonist, as well as its opposite enantiomer, BIBP3435, which is inactive at Y1 receptors, blocked feeding elicited by NPY, [Leu31Pro34], or PYY at doses that did not cause overt behavioral dysfunction [26].
  • 4. Y(1) receptor antagonists, BIBP3226 and BIBO3304 both increased basal I(sc) levels per se and inhibited subsequent PYY and Pro(34)PYY but not hPP or PYY(3 - 36) responses [27].
  • NPY 2-36 was much less potent than NPY itself and pretreatment with BIBP3226 did not affect the inhibitory response [28].
  • Pretreatment with the Y1 receptor-selective antagonist BIBP3226 (1 microM) failed to prevent the NPY-induced inhibition [29].
  • BIBP3226 alone did not alter CRF release from hypothalamic explants [30].

Analytical, diagnostic and therapeutic context of BIBP3226

  • Emulsion receptor autoradiography using a newly developed ligand, [(125)I]GR231118 in the presence of PYY, hPP or BIBP3226 (1 microM), pharmacologically established the Y(1) nature of these receptors [31].
  • As one of the recently cloned Y5 receptors is synthesized in these regions, as shown by in-situ hybridization techniques, we suggest that the small population of [125I]PYY(3-36) binding sites which are sensitive to human PP and [Leu31,Pro34]NPY, but insensitive to BIBP3226, may represent binding to Y5 receptors [32].
  • BIBP3226 potently blocked (pA2 = 7.36) the contractile effect of neuropeptide Y in the rabbit saphenous vein, a Y1 receptor bioassay and demonstrated nM affinity for Y1/[125I][Leu31,Pro34]peptide YY binding sites [33].
  • When compared to the vehicle-treated control group, treatment with NPY or [Leu31,Pro34]-NPY (Y1 agonist) reduced viability of cultured SK-N-MC (Y1-expressing) human neuronal cells at 24 h after 1 h of OGD, while BIBP3226 (Y1 antagonist) improved viability [34].


  1. Rapid internalization and recycling of the human neuropeptide Y Y(1) receptor. Gicquiaux, H., Lecat, S., Gaire, M., Dieterlen, A., Mély, Y., Takeda, K., Bucher, B., Galzi, J.L. J. Biol. Chem. (2002) [Pubmed]
  2. Intracerebroventricular injection of a neuropeptide Y-Y1 receptor agonist increases while BIBP3226, a Y1 antagonist, reduces the infarct volume following transient middle cerebral artery occlusion in rats. Chen, S.H., Cheung, R.T. Neuroscience (2003) [Pubmed]
  3. Labeling of neuropeptide Y receptors in SK-N-MC cells using the novel, nonpeptide Y1 receptor-selective antagonist [3H]BIBP3226. Entzeroth, M., Braunger, H., Eberlein, W., Engel, W., Rudolf, K., Wienen, W., Wieland, H.A., Willim, K.D., Doods, H.N. Eur. J. Pharmacol. (1995) [Pubmed]
  4. Acceleration of pubertal development following central blockade of the Y1 subtype of neuropeptide Y receptors. Pralong, F.P., Voirol, M., Giacomini, M., Gaillard, R.C., Grouzmann, E. Regul. Pept. (2000) [Pubmed]
  5. Selective inhibition of neuropeptide Y Y1 receptors by BIBP3226 in rat and human epithelial preparations. Tough, I.R., Cox, H.M. Eur. J. Pharmacol. (1996) [Pubmed]
  6. Anxiogenic-like effect of the neuropeptide Y Y1 receptor antagonist BIBP3226: antagonism with diazepam. Kask, A., Rägo, L., Harro, J. Eur. J. Pharmacol. (1996) [Pubmed]
  7. NPY Y1 receptors in the dorsal periaqueductal gray matter regulate anxiety in the social interaction test. Kask, A., Rägo, L., Harro, J. Neuroreport (1998) [Pubmed]
  8. A neuropeptide ligand of the G protein-coupled receptor GPR103 regulates feeding, behavioral arousal, and blood pressure in mice. Takayasu, S., Sakurai, T., Iwasaki, S., Teranishi, H., Yamanaka, A., Williams, S.C., Iguchi, H., Kawasawa, Y.I., Ikeda, Y., Sakakibara, I., Ohno, K., Ioka, R.X., Murakami, S., Dohmae, N., Xie, J., Suda, T., Motoike, T., Ohuchi, T., Yanagisawa, M., Sakai, J. Proc. Natl. Acad. Sci. U.S.A. (2006) [Pubmed]
  9. Expression and characterization of the neuropeptide Y Y5 receptor subtype in the rat brain. Dumont, Y., Fournier, A., Quirion, R. J. Neurosci. (1998) [Pubmed]
  10. Identification and characterization of two G protein-coupled receptors for neuropeptide FF. Bonini, J.A., Jones, K.A., Adham, N., Forray, C., Artymyshyn, R., Durkin, M.M., Smith, K.E., Tamm, J.A., Boteju, L.W., Lakhlani, P.P., Raddatz, R., Yao, W.J., Ogozalek, K.L., Boyle, N., Kouranova, E.V., Quan, Y., Vaysse, P.J., Wetzel, J.M., Branchek, T.A., Gerald, C., Borowsky, B. J. Biol. Chem. (2000) [Pubmed]
  11. Gender-modulated endogenous baseline neuropeptide Y Y1-receptor activation in the hindlimb of Sprague-Dawley rats. Jackson, D.N., Milne, K.J., Noble, E.G., Shoemaker, J.K. J. Physiol. (Lond.) (2005) [Pubmed]
  12. Neuropeptide Y and peptide YY inhibit excitatory synaptic transmission in the rat dorsal motor nucleus of the vagus. Browning, K.N., Travagli, R.A. J. Physiol. (Lond.) (2003) [Pubmed]
  13. Antagonism of neuropeptide YY1 receptors does not inhibit ethanol's effects on cortical EEG and ERPs in Wistar rats. Slawecki, C.J., Thorsell, A., Ehlers, C.L. J. Stud. Alcohol (2005) [Pubmed]
  14. Species differences in the expression and distribution of the neuropeptide Y Y1, Y2, Y4, and Y5 receptors in rodents, guinea pig, and primates brains. Dumont, Y., Jacques, D., Bouchard, P., Quirion, R. J. Comp. Neurol. (1998) [Pubmed]
  15. Role of renal sympathetic nerves in regulating renovascular responses to angiotensin II in spontaneously hypertensive rats. Dubinion, J.H., Mi, Z., Jackson, E.K. J. Pharmacol. Exp. Ther. (2006) [Pubmed]
  16. Identification of an NPY-Y1 receptor subtype in bovine chromaffin cells. Zhang, P., Zheng, J., Vorce, R.L., Hexum, T.D. Regul. Pept. (2000) [Pubmed]
  17. Effects of BIBP3226 and BIBP3435 on cytosolic calcium in neuropeptide Y Y1 receptor-transfected Chinese hamster ovary cells and wild type CHO-K1 cells. Van Liefde, n.u.l.l., Vanderheyden, P.M., De Backer, J.P., Ebinger, G., Vauquelin, G. J. Recept. Signal Transduct. Res. (2001) [Pubmed]
  18. The direct stimulation of Gi proteins by neuropeptide Y (NPY) in the rat left ventricle. Raimondi, L., Banchelli, G., Matucci, R., Stillitano, F., Pirisino, R. Biochem. Pharmacol. (2002) [Pubmed]
  19. Agonist and antagonist activities on human NPFF(2) receptors of the NPY ligands GR231118 and BIBP3226. Mollereau, C., Gouardères, C., Dumont, Y., Kotani, M., Detheux, M., Doods, H., Parmentier, M., Quirion, R., Zajac, J.M. Br. J. Pharmacol. (2001) [Pubmed]
  20. Neuropeptide Y Y1 receptors mediate morphine-induced reductions of natural killer cell activity. Saurer, T.B., Ijames, S.G., Lysle, D.T. J. Neuroimmunol. (2006) [Pubmed]
  21. Neuropeptide Y rapidly enhances [Ca2+]i transients and Ca2+ sparks in adult rat ventricular myocytes through Y1 receptor and PLC activation. Heredia, M.d.e.l. .P., Delgado, C., Pereira, L., Perrier, R., Richard, S., Vassort, G., Bénitah, J.P., Gómez, A.M. J. Mol. Cell. Cardiol. (2005) [Pubmed]
  22. The neuropeptide Y (NPY) Y1 receptor subtype mediates NPY-induced antidepressant-like activity in the mouse forced swimming test. Redrobe, J.P., Dumont, Y., Fournier, A., Quirion, R. Neuropsychopharmacology (2002) [Pubmed]
  23. Neuropeptide Y Y1-receptor stimulation is required for physiological amplification of preovulatory luteinizing hormone surges. Leupen, S.M., Besecke, L.M., Levine, J.E. Endocrinology (1997) [Pubmed]
  24. In vivo inhibition of neuropeptide FF agonism by BIBP3226, an NPY Y1 receptor antagonist. Fang, Q., Guo, J., He, F., Peng, Y.L., Chang, M., Wang, R. Peptides (2006) [Pubmed]
  25. Effect of BIBP3226 on inositol phosphate accumulation and cytosolic calcium level in control and NPY Y1 receptor expressing CHO-K1 cells. Vanderheyden, P.M., Van Liefde, I., DeBacker, J.P., Ebinger, G., Vauquelin, G. Regul. Pept. (1998) [Pubmed]
  26. Characterization of neuropeptide Y-induced feeding in mice: do Y1-Y6 receptor subtypes mediate feeding? Iyengar, S., Li, D.L., Simmons, R.M. J. Pharmacol. Exp. Ther. (1999) [Pubmed]
  27. Neuropeptide Y, Y1, Y2 and Y4 receptors mediate Y agonist responses in isolated human colon mucosa. Cox, H.M., Tough, I.R. Br. J. Pharmacol. (2002) [Pubmed]
  28. Suppression of sensory C fiber-mediated contractions by neuropeptide Y Y1 receptors in the guinea pig bronchi. Grundemar, L. Regul. Pept. (1998) [Pubmed]
  29. Characterization of the receptor response for the neuropeptide Y-evoked suppression of parasympathetically-mediated contractions in the guinea pig trachea. Grundemar, L. Regul. Pept. (1997) [Pubmed]
  30. The central effects of orexin-A in the hypothalamic-pituitary-adrenal axis in vivo and in vitro in male rats. Russell, S.H., Small, C.J., Dakin, C.L., Abbott, C.R., Morgan, D.G., Ghatei, M.A., Bloom, S.R. J. Neuroendocrinol. (2001) [Pubmed]
  31. Sub-population of cultured hippocampal astrocytes expresses neuropeptide Y Y(1) receptors. St-Pierre, J.A., Nouel, D., Dumont, Y., Beaudet, A., Quirion, R. Glia (2000) [Pubmed]
  32. Distribution of [Leu31,Pro34]NPY-sensitive, BIBP3226-insensitive [125I]PYY(3-36) binding sites in rat brain: possible relationship to Y5 NPY receptors. Widdowson, P.S., Buckingham, R., Williams, G. Brain Res. (1997) [Pubmed]
  33. Apparent affinity and potency of BIBP3226, a non-peptide neuropeptide Y receptor antagonist, on purported neuropeptide Y Y1, Y2 and Y3 receptors. Jacques, D., Cadieux, A., Dumont, Y., Quirion, R. Eur. J. Pharmacol. (1995) [Pubmed]
  34. Neuropeptide Y-Y1 receptor agonist worsens while antagonist improves survival of cultured Y1-expressing neuronal cells following oxygen and glucose deprivation. Chen, S.H., Cheung, R.T. J. Biomed. Sci. (2004) [Pubmed]
WikiGenes - Universities