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Two classes of structurally different antagonists display similar species preference for the human tachykinin neurokinin3 receptor.
Two classes of structurally different tachykinin neurokinin3 (NK3) antagonists were used to evaluate species difference in antagonist binding between human and rat NK3 receptors. In competitionExpand
PD 176252--the first high affinity non-peptide gastrin-releasing peptide (BB2) receptor antagonist.
In this paper we describe the development of a novel series of non-peptide, "balanced" neuromedin-B preferring (BB1)/gastrin-releasing peptide preferring (BB2) receptor ligands as exemplified by PDExpand
Bombesin Receptors as a Novel Anti-Anxiety Therapeutic Target: BB1 Receptor Actions on Anxiety through Alterations of Serotonin Activity
The effects of PD 176252 [3-(1H-indol-3-yl)-N-[1-(5-methoxy-pyridin-2-yl)-cyclohexylmethyl]-2-methyl-2-[3-(nitro-phenyl)ureido]propionamide], a nonpeptide bombesin (BB) BB1/BB2 receptor antagonist,Expand
PD 165929 — the first high affinity non-peptide neuromedin-B (NMB) receptor selective antagonist
Abstract In this paper we describe the development of a novel series of non-peptide neuromedin-B (NMB) receptor ligands as exemplified by PD 165929. PD 165929, which exhibits nanomolar affinity forExpand
[3H]PD 140376: a novel and highly selective antagonist radioligand for the cholecystokininB/gastrin receptor in guinea pig cerebral cortex and gastric mucosa.
The specific binding characteristics of the novel cholecystokinin (CCK)B/gastrin receptor-selective peptoid antagonist radioligand [3H]PD 140376 were investigated using membrane homogenates preparedExpand
Second generation "peptoid" CCK-B receptor antagonists: identification and development of N-(adamantyloxycarbonyl)-alpha-methyl-(R)-tryptophan derivative (CI-1015) with an improved pharmacokinetic
We have previously described the design and development of CI-988, a peptoid analogue of CCK-4 with excellent binding affinity and selectivity for the CCK-B receptor. Due to its anxiolytic profile inExpand
Rationally designed "dipeptoid" analogues of CCK. alpha-Methyltryptophan derivatives as highly selective and orally active gastrin and CCK-B antagonists with potent anxiolytic properties.
This paper describes the synthesis and structure-activity relationships (SAR) leading to the first rational design of "dipeptoid" analogues of the neuropeptide cholecystokinin (CCK). CompoundsExpand
Use of a dipeptide chemical library in the development of non-peptide tachykinin NK3 receptor selective antagonists.
The use of a dipeptide library as the source of a micromolar chemical lead compound for the human tachykinin NK3 receptor is described. The screening of a dipeptide library through a cloned human NK3Expand
Rational design of high affinity tachykinin NK1 receptor antagonists.
The rational design of a non-peptide tachykinin NK1 receptor antagonist, [(2-benzofuran)-CH2OCO]-(R)-alpha-MeTrp-(S)-NHCH(CH3)P h (28, PD 154075) is described. Compound 28 has a Ki = 9 and 0.35 nMExpand