ArticleBritish journal of pharmacology1993
2-Naphthalenesulphonyl L-aspartyl-(2-phenethyl)amide (2-NAP)--a selective cholecystokinin CCKA-receptor antagonist.
Article in British journal of pharmacology, 1993. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 papers.
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Who cites it
9 citing papers in PubMed, 35 citations in OpenAlex.
- PEGylated cholecystokinin is more potent in inducing anorexia than conditioned taste aversion in rats.British journal of pharmacology · 2008Article
- PEGylated cholecystokinin prolongs satiation in rats: dose dependency and receptor involvement.British journal of pharmacology · 2007Article
- Unexpected relationship between plasma protein binding and the pharmacodynamics of 2-NAP, a CCK1-receptor antagonist.British journal of clinical pharmacology · 2007Article
- Molecular cloning, expression and pharmacological characterization of the canine cholecystokinin 1 receptor.British journal of pharmacology · 2005Article
- Pharmacological evidence for putative CCK(1) receptor heterogeneity in human colon smooth muscle.British journal of pharmacology · 2002Article
- Effect of three nonpeptide cholecystokinin antagonists on human isolated gallbladder.Digestive diseases and sciences · 2001Article
- Characterization of the binding of a novel radioligand to CCKB/gastrin receptors in membranes from rat cerebral cortex.British journal of pharmacology · 1999Article
- Analysis of variation in L-365,260 competition curves in radioligand binding assays.British journal of pharmacology · 1996Article
- 2-Naphthalenesulphanyl-L-aspartyl-2-(phenethyl) amide (2-NAP) and food intake in rats: evidence that endogenous peripheral CCK does not play a major role as a satiety factor.British journal of pharmacology · 1995Article
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5 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
1. The in vitro pharmacological characterization of the sodium salt of 2-naphthalenesulphonyl 1-aspartyl-(2-phenethyl)amide [2-NAP], a hydrophilic compound derived from the C-terminal aspartate-phenylalanine dipeptide of cholecystokinin (CCK), is described. 2. 2-NAP behaved as a competitive antagonist of sulphated cholecystokinin octapeptide (CCK-8) at CCKA-receptors in both intact tissue bioassays (guinea-pig gall bladder, pancreas and ileum, human and rabbit gall bladder) and a radioligand displacement assay (guinea-pig pancreatic cells). The mean pKB, over assays, was 6.5. 3. Compared to the other assays, the rabbit gall bladder assay gave a significantly higher pKB estimate [7.0] for 2-NAP and a significantly lower estimate [8.9] for devazepide (formerly L-364,718 and MK-329), a well-characterized CCKA-receptor antagonist; these anomalous results suggest that a different class of CCKA-receptors may be involved. 4. 2-NAP, was found to be highly selective, having at least 300 fold greater affinity for CCKA-receptors than for 50 other pharmacological loci, including gastrin/CCKB, as estimated by bioassay or radioligand displacement.
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