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In Vitro Properties of a High Affinity Selective Antagonist of the VIP1 Receptor
A selective high affinity VIP1 receptor antagonist [Acetyl-His1, D-Phe2, Lys15, Arg16, Leu17] VIP(3-7)/GRF(8-27) or PG 97-269 was synthesized, by analogy with recently obtained selective VIP1Expand
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Molecular cloning and functional characterization of a human VIP receptor from SUP-T1 lymphoblasts.
We have cloned and sequenced a cDNA isolated from a human SUP-T1 lymphoblast cell line library. It encoded a 457 amino acids protein having 87% identity with the rat PACAP type II, VIP2 receptor.Expand
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Binding of selective antagonists to four muscarinic receptors (M1 to M4) in rat forebrain.
To compare the proportions of four muscarinic receptors in different rat brain regions, we used competition curves with four selective antagonists, at 1-[N-methyl-3H]scopolamine methyl chloride [(Expand
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Ghrelin degradation by serum and tissue homogenates: identification of the cleavage sites.
The endogenous ligand for the GH secretagogue receptor is ghrelin, a peptide recently purified from the stomach. Ghrelin is n-octanoylated on the Ser(3) residue, and this modification is essentialExpand
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Techniques: promiscuous Galpha proteins in basic research and drug discovery.
Assay technologies that measure the activation of heterotrimeric (alphabetagamma) G proteins by G-protein-coupled receptors (GPCRs) are well established within the pharmaceutical industry, either forExpand
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Techniques: Promiscuous Gα proteins in basic research and drug discovery
Assay technologies that measure the activation of heterotrimeric (αβγ) G proteins by G-protein-coupled receptors (GPCRs) are well established within the pharmaceutical industry, either forExpand
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Interaction of growth hormone-releasing factor (GRF) and 14 GRF analogs with vasoactive intestinal peptide (VIP) receptors of rat pancreas. Discovery of (N-Ac-Tyr1,D-Phe2)-GRF(1-29)-NH2 as a VIP
Adenylate cyclase stimulation by GH-releasing factor (GRF) and 14 GRF analogs (modified in the N-terminal part) was compared to the capacity of the same peptides to inhibit [125I]iodo-vasoactiveExpand
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Two Basic Residues of the h-VPAC1 Receptor Second Transmembrane Helix Are Essential for Ligand Binding and Signal Transduction*
We mutated the vasoactive intestinal peptide (VIP) Asp3 residue and two VPAC1receptor second transmembrane helix basic residues (Arg188and Lys195). VIP had a lower affinity for R188Q, R188L, K195Q,Expand
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Propiverine and metabolites: differences in binding to muscarinic receptors and in functional models of detrusor contraction
Propiverine is a commonly used antimuscarinic drug used as therapy for symptoms of an overactive bladder. Propiverine is extensively biotransformed into several metabolites that could contribute toExpand
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A new type of functional VIP receptor has an affinity for helodermin in human SUP‐T1 lymphoblasts
A new type of VIP receptor was characterized in human SUP‐T1 lymphoblasts. The order of potency of unlabeled peptides in the presence of [125I]helodermin, was: helodermin(1–35)‐NH2 =Expand
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