Eur J Pharmacol. 1999 Nov 19;384(2-3):R3-5.

BIIE0246: a selective and high affinity neuropeptide Y Y(2) receptor antagonist.

Doods H, Gaida W, Wieland HA, Dollinger H, Schnorrenberg G, Esser F, Engel W, Eberlein W, Rudolf K.

Source

Boehringer Ingelheim Pharma, Birkendorfer Str. 65, D-88397, Biberach, Germany. henri.doods@bc.boehringer-ingelheim.com

Abstract

The in vitro biological characterisation of the first potent and selective non-peptide neuropeptide Y Y(2) receptor antagonist, (S)-N(2)-[[1-[2-[4-[(R,S)-5,11-dihydro-6(6h)-oxodibenz[b, e]azepin-11-yl]-1-piperazinyl]-2-oxoethyl] cylopentyl] acetyl]-N-[2-[1,2-dihydro-3,5(4H)-dioxo-1,2-diphenyl-3H-1,2, 4-triazol-4-yl]ethyl]-argininamid (BIIE0246) is reported. BIIE0246 displaced [125I]neuropeptide Y with high affinity (IC(50)=3.3 nM) from the human neuropeptide Y Y(2) receptor and proved to be highly selective. BIIE0246 displayed antagonistic properties and thus represents the first selective non-peptide neuropeptide Y Y(2) receptor antagonist.

PMID:: 10611450; [PubMed - indexed for MEDLINE]

LinkOut - more resources

Full Text Sources

Other Literature Sources

Labome Researcher Resource - ExactAntigen/Labome

Molecular Biology Databases

Libraries

LinkOut Holdings

Supplemental Content

Save items

Related citations in PubMed

Effects of the neuropeptide Y Y(2) receptor antagonist BIIE0246 on presynaptic inhibition by neuropeptide Y in rat hippocampal slices. [Eur J Pharmacol. 2000]
Effects of the neuropeptide Y Y(2) receptor antagonist BIIE0246 on presynaptic inhibition by neuropeptide Y in rat hippocampal slices.
Weiser T, Wieland HA, Doods HN. Eur J Pharmacol. 2000 Sep 15; 404(1-2):133-6.
Effect of a selective neuropeptide Y Y(2) receptor antagonist, BIIE0246 on neuropeptide Y release. [Eur J Pharmacol. 2000]
Effect of a selective neuropeptide Y Y(2) receptor antagonist, BIIE0246 on neuropeptide Y release.
King PJ, Williams G, Doods H, Widdowson PS. Eur J Pharmacol. 2000 May 12; 396(1):R1-3.
Existence of both neuropeptide Y, Y1 and Y2 receptors in pig spleen: evidence using subtype-selective antagonists in vivo. [Life Sci. 2001]
Existence of both neuropeptide Y, Y1 and Y2 receptors in pig spleen: evidence using subtype-selective antagonists in vivo.
Malmström RE. Life Sci. 2001 Sep 14; 69(17):1999-2005.
Review Apparent affinity and potency of BIBP3226, a non-peptide neuropeptide Y receptor antagonist, on purported neuropeptide Y Y1, Y2 and Y3 receptors. [Eur J Pharmacol. 1995]
Review 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 May 4; 278(1):R3-5.
Review High-affinity analogues of neuropeptide Y containing conformationally restricted non-proteinogenic amino acids. [Biochem Soc Trans. 1994]
Review High-affinity analogues of neuropeptide Y containing conformationally restricted non-proteinogenic amino acids.
Beck-Sickinger AG, Hoffmann E, Paulini K, Reissig HU, Willim KD, Wieland HA, Jung G. Biochem Soc Trans. 1994 Feb; 22(1):145-9.

See reviews... See all...

Cited by 24 PubMed Central articles

Salivary PYY: a putative bypass to satiety. [PLoS One. 2011]
Salivary PYY: a putative bypass to satiety.
Acosta A, Hurtado MD, Gorbatyuk O, La Sala M, Duncan D, Aslanidi G, Campbell-Thompson M, Zhang L, Herzog H, Voutetakis A, et al. PLoS One. 2011; 6(10):e26137. Epub 2011 Oct 10.
Neuropeptide Y inhibits cholangiocarcinoma cell growth and invasion. [Am J Physiol Cell Physiol. 2011]
Neuropeptide Y inhibits cholangiocarcinoma cell growth and invasion.
DeMorrow S, Onori P, Venter J, Invernizzi P, Frampton G, White M, Franchitto A, Kopriva S, Bernuzzi F, Francis H, et al. Am J Physiol Cell Physiol. 2011 May; 300(5):C1078-89. Epub 2011 Jan 26.
Peripheral peptide YY inhibits propulsive colonic motor function through Y2 receptor in conscious mice. [Am J Physiol Gastrointest Live...]
Peripheral peptide YY inhibits propulsive colonic motor function through Y2 receptor in conscious mice.
Wang L, Gourcerol G, Yuan PQ, Wu SV, Million M, Larauche M, Taché Y. Am J Physiol Gastrointest Liver Physiol. 2010 Jan; 298(1):G45-56. Epub 2009 Nov 5.

See all...

Related information

Related Citations
Calculated set of PubMed citations closely related to the selected article(s) retrieved using a word weight algorithm. Related articles are displayed in ranked order from most to least relevant, with the “linked from” citation displayed first.
Compound
PubChem chemical compound records that cite the current articles. These references are taken from those provided on submitted PubChem chemical substance records. Multiple substance records may contribute to the PubChem compound record.
Compound (MeSH Keyword)
PubChem chemical compound records that are classified under the same Medical Subject Headings (MeSH) controlled vocabulary as the current articles.
Substance
PubChem chemical substance records that cite the current articles. These references are taken from those provided on submitted PubChem chemical substance records.
Substance (MeSH Keyword)
PubChem chemical substance (submitted) records that are classified under the same Medical Subject Headings (MeSH) controlled vocabulary as the current articles.
Cited in PMC
Full-text articles in the PubMed Central Database that cite the current articles.

Recent activity

Clear Turn Off Turn On

BIIE0246: a selective and high affinity neuropeptide Y Y(2) receptor antagonist.
BIIE0246: a selective and high affinity neuropeptide Y Y(2) receptor antagonist.
Eur J Pharmacol. 1999 Nov 19 ;384(2-3):R3-5.

PubMed
Separation of inner and outer membranes of Rickettsia prowazeki and characteriza...
Separation of inner and outer membranes of Rickettsia prowazeki and characterization of their polypeptide compositions.
J Bacteriol. 1979 Feb ;137(2):963-71.

PubMed
Falls prevention over 2 years: a randomized controlled trial in women 80 years a...
Falls prevention over 2 years: a randomized controlled trial in women 80 years and older.
Age Ageing. 1999 Oct ;28(6):513-8.

PubMed
Effect of temporal fluctuation of selection coefficient on gene frequency in a p...
Effect of temporal fluctuation of selection coefficient on gene frequency in a population.
Proc Natl Acad Sci U S A. 1975 Nov ;72(11):4541-5.

PubMed
Stress-associated endoplasmic reticulum protein 1 (SERP1)/Ribosome-associated me...
Stress-associated endoplasmic reticulum protein 1 (SERP1)/Ribosome-associated membrane protein 4 (RAMP4) stabilizes membrane proteins during stress and facilitates subsequent glycosylation.
J Cell Biol. 1999 Dec 13 ;147(6):1195-204.

PubMed

Your browsing activity is empty.

Activity recording is turned off.

Turn recording back on

PubMed

Result Filters

Display Settings:

Send to:

BIIE0246: a selective and high affinity neuropeptide Y Y(2) receptor antagonist.

Source

Abstract

MeSH Terms, Substances

MeSH Terms

Substances

LinkOut - more resources

Full Text Sources

Other Literature Sources

Molecular Biology Databases

Libraries

Supplemental Content

Save items

Related citations in PubMed

Cited by 24 PubMed Central articles

Related information

Recent activity

Simple NCBI Directory

Getting Started

Resources

Popular

Featured

NCBI Information