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Substance P binding in gastrointestinal tract of nondiabetic BB rat and changes in diabetic BB rat over time.
Dig Dis Sci
April 1999
Department of Medicine, University of Pennsylvania, Philadelphia, USA.
Our aim was to determine sites of substance P binding in the gut of the BB rat and examine changes in SP binding in the diabetic rat, over time. Specific binding of [125I]substance P was localized in sections of nondiabetic gut using emulsion autoradiography and quantitated in diabetic and nondiabetic gut using film autoradiography. High levels of SP binding were located in esophageal muscularis mucosa, circular muscle of the stomach and colon, deep muscular plexus, and in the circular muscle adjacent to the plexus in the ileum.
View Article and Find Full Text PDFStructural optimization affording 2-(R)-(1-(R)-3, 5-bis(trifluoromethyl)phenylethoxy)-3-(S)-(4-fluoro)phenyl-4- (3-oxo-1,2,4-triazol-5-yl)methylmorpholine, a potent, orally active, long-acting morpholine acetal human NK-1 receptor antagonist.
J Med Chem
November 1998
Merck Research Laboratories, P.O. Box 2000, Rahway, New Jersey 07065, USA.
Structural modifications requiring novel synthetic chemistry were made to the morpholine acetal human neurokinin-1 (hNK-1) receptor antagonist 4, and this resulted in the discovery of 2-(R)-(1-(R)-3, 5-bis(trifluoromethyl)phenylethoxy)-3-(S)-(4-fluoro)phenyl-4-(3-ox o-1 ,2,4-triazol-5-yl)methyl morpholine (17). This modified compound is a potent, long-acting hNK-1 receptor antagonist as evidenced by its ability to displace [125I]Substance P from hNK-1 receptors stably expressed in CHO cells (IC50 = 0.09 +/- 0.
View Article and Find Full Text PDFDifferential distribution of substance P binding sites in guinea-pig sympathetic ganglia.
J Auton Nerv Syst
April 1998
Department of Anatomy and Histology, and Centre for Neuroscience, Flinders University of South Australia, Adelaide, Australia.
We have used a combination of autoradiographic and immunohistochemical techniques to investigate the distribution of binding sites for substance P in relation to the distribution of substance P-immunoreactive nerve fibres and specific functional populations of neurons in the sympathetic ganglia of guinea-pigs. There was considerable heterogeneity in the density of binding sites for Bolton Hunter labelled 125I - substance P (BHSP). Binding sites were more dense in the prevertebral ganglia, such as the coeliac and inferior mesenteric ganglia, than in the paravertebral ganglia, such as the superior cervical or lumbar chain ganglia.
View Article and Find Full Text PDFDistribution of substance P receptor binding in dorsal column nuclei of rat, cat, monkey and human.
Brain Res
March 1998
Department of Biological Sciences, University of North Texas, P.O. Box 305220, Denton, TX 76203-5220, USA.
In the present study, substance P receptor binding was localized in the dorsal column nuclei (DCN) of the rat, cat, monkey, and human. Bolton-Hunter-labeled [125I]substance P binding was most concentrated in the cell nests of the core region, but was present throughout the DCN of each species. The distribution of substance P receptors may reconcile apparent mismatches between the widespread responsiveness of DCN neurons to substance P and the restricted distribution of substance P containing afferents.
View Article and Find Full Text PDFCharacterization of the binding and activity of a high affinity, pseudoirreversible morpholino tachykinin NK1 receptor antagonist.
Eur J Pharmacol
May 1997
Department of Molecular Pharmacology, Merck Research Laboratories, Rahway, NJ 07065, USA.
2(S)-((3,5-Bis(trifluoromethyl)benzyl)-oxy)-3(S)-phenyl-4-((3-oxo-1,2,4- triazol-5-yl)methyl)morpholine (L-742,694) is a selective morpholino tachykinin NK1 receptor antagonist that inhibits the binding of 125I-substance P to the human tachykinin NK1 receptor with a Kd = 37 pM. Increasing concentrations of L-742,694 added to cells 15 min prior to agonist progressively increase the apparent EC50 of substance P for inducing the synthesis of inositol phosphate in Chinese hamster ovary (CHO) cells expressing human tachykinin NK1 receptor and decrease the maximal level of stimulation observed. In contrast, addition of substance P and L-742,694 to the cells at the same time results in an increase in the EC50 for substance P with no decrease in the maximal level of stimulation.
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