In vitro properties of a high affinity selective antagonist of the VIP1 receptor

P Gourlet, P De Neef, J Cnudde, M Waelbroeck… - Peptides, 1997 - Elsevier
… interaction with two types of high affinity receptors that have been … absence of high affinity
antagonists with known affinities for the … of a new highly selective VIP 1 receptor antagonist. …

A novel high-affinity peptide antagonist to the insulin receptor

L Schäffer, CL Brand, BF Hansen, U Ribel… - Biochemical and …, 2008 - Elsevier
… In conclusion, the insulin receptor antagonists S661 and S961 exhibit high affinity and
selectivity for the insulin receptor and can be used to unravel the role of insulin receptor signaling …

8-Cyclopentyl-1,3-dipropylxanthine (DPCPX) — a selective high affinity antagonist radioligand for A1 adenosine receptors

MJ Lohse, KN Klotz, J Lindenborn-Fotinos… - Naunyn-Schmiedeberg's …, 1987 - Springer
… Thus, 8-cyclopentyltheophylline has a 1,000-fold higher affinity and a 30-fold higher … an
antagonist with enhanced affinity and selectivity for At adenosine receptors. Such an antagonist

Conversion of human interleukin‐4 into a high affinity antagonist by a single amino acid replacement.

N Kruse, HP Tony, W Sebald - The EMBO Journal, 1992 - embopress.org
… These results demonstrate that high affinity binding and signal … time, that a powerful antagonist
acting on the IL4 receptor … forward identification of high affinity antagonists in both systems …

Pharmacological actions of a novel, high-affinity, and selective human dopamine D3 receptor antagonist, SB-277011-A

C Reavill, SG Taylor, MD Wood, T Ashmeade… - … of Pharmacology and …, 2000 - ASPET
… In summary, SB-277011-A is a dopamine D 3 receptor antagonist with high affinity and
selectivity for D 3 receptors in human and rat with good bioavailability and CNS penetration. SB-…

BIIE0246: a selective and high affinity neuropeptide Y Y2 receptor antagonist

H Doods, W Gaida, HA Wieland, H Dollinger… - European journal of …, 1999 - Elsevier
… Y 2 antagonist T4-[neuropeptide Y (33–36)] 4 . In addition to its high affinity to the neuropeptide
YY 2 receptor we could also show that BIIE0246 has virtually no affinity for neuropeptide …

GR113808: a novel, selective antagonist with high affinity at the 5‐HT4 receptor

JD Gale, CJ Grossman, JWF Whitehead… - British journal of …, 1994 - Wiley Online Library
… be a specific antagonist with high affinity for the 5-HT4 receptor in guinea-pig isolated
ascending colon and rat isolated oesophagus. It behaved as a surmountable antagonist in both pre…

RS‐127445: a selective, high affinity, orally bioavailable 5‐HT2B receptor antagonist

DW Bonhaus, LA Flippin… - British journal of …, 1999 - Wiley Online Library
… In conclusion, RS-127445 is a selective, high affinity 5-HT 2B receptor antagonist
suitable for use in vivo. The therapeutic potential of this molecule is being further evaluated. …

High-affinity neuropeptide Y receptor antagonists.

AJ Daniels, JE Matthews, RJ Slepetis… - Proceedings of the …, 1995 - National Acad Sciences
… of specific high-affinity receptor antagonists. Three potent NPY receptor antagonists were …
At least two NPY receptor subtypes have been described based on the relative affinity of …

[HTML][HTML] Characterization of a powerful high affinity antagonist that inhibits biological activities of human interleukin-13

Y Oshima, RK Puri - Journal of Biological Chemistry, 2001 - ASBMB
… We hypothesized that an IL-13 antagonist may have profound … , IL-13E13K, bound with 4-fold
higher affinity to the IL-13 receptor … These results demonstrate that high affinity binding and …