Detail of "86917-57-9"

Reference

Receptors for substance P

Receptors for substance P. III. Classification by competitive antagonists. Regoli, Domenico; Escher, Emanuel; Drapeau, Guy; D'Orleans-Juste, Pedro; Mizrahi, Jacques (Med. Sch., Univ. Sherbrooke, Sherbrooke, PQ J1H 5N4, Can.Several substances are used for example 89430-35-3 and 81039-85-2 which are their cas registry numbers.). Eur. J. Pharmacol., 97(3-4), 179-89 (English) 1984. CODEN: EJPHAZ. ISSN: 0014-2999. DOCUMENT TYPE: Journal CA Section: 2 (Mammalian Hormones) A series of octa- and undecapeptide antagonists of substance P (SP) [33507-63-0] were tested in isolated smooth muscle prepns. to characterize the receptors mediating the SP-induced contractions of the guinea pig ileum (G.P.I), the guinea pig trachea (G.P.T), and the rabbit mesenteric vein (R.M.V) and the relaxation of the dog carotid artery (D.C.A). Indirect effects by SP and related peptides, mediated by acetylcholine or prostaglandins, reduce the affinity of [Pro4 D-Trp7,9,10]SP (4-11) [86917-57-9] only in the G.P.I. Octapeptide antagonists are specific for SP, have no agonistic activities, and exert a competitive antagonism against SP, its homologs, and its fragments. Undecapeptide antagonists are weaker than the octapeptides in the G.P.I and G.P.T. and slightly stronger in the D.C.A. and R.M.V. However these compds. still have variable degrees of agonistic activity in some tissues. Affinity of octapeptide antagonists bearing the basic structure [D-Pro4, D-Trp7,9]SP-(4-11) [81039-85-2] is increased by the addnl. replacement of leucine-10 with D-tryptophan or of methionine-11 with leucine, norleucine, or phenylalanine, but it is slightly reduced by substituting phenylalanine-8 with valine. Antagonists contg. aliph. residues at the C-terminal end, for instance (L-2 Pro4,D-2 Trp7,9,Nle11]SP-(4-11) [89430-34-2] are more potent than others in the R.M.V., and those with arom. residues, for instance (D-2 Pro4,D-2 Trp,7,9,10]SP-(4-11) are weak on the R.M.V. but fairly active on the G.P.T. These antagonists do not show any selectivity on the G.P.I. and the D.C.A. Comparison of antagonists affinities for receptor characterization suggest the existence of 3 different functional sites for SP-related peptides: the site of the G.P.I and D.C.A., which accepts both the antagonists contg. arom. or aliph. groups at the C-terminal end; the site of the G.P.T. which prefers the arom. residues and that of the R.M.V. which shows high affinity for aliph. residues. The receptor classification from data obtained with antagonists is compared with the classifications of the literature and with those based on the order of potencies of SP homologs and fragments. .

The substance P receptor on rat mast cells and in human skin

The substance P receptor on rat mast cells and in human skin. Piotrowski, W.; Devoy, M. A.In this study， 33507-63-0 and 51-45-6 are also used. B.; Jordan, C. C.; Foreman, J. C. (Dep. Pharmacol., Univ. Coll. London, London WC1E 6BT, UK). Agents Actions, 14(3-4), 420-4 (English) 1984. CODEN: AGACBH. ISSN: 0065-4299. DOCUMENT TYPE: Journal CA Section: 2 (Mammalian Hormones) (D-Pro4,D-Trp7,9,10) substance P(4-11) (SPA) [86917-57-9] was a competitive antagonist of the histamine [51-45-6] releasing action of substance P [33507-63-0] in rat peritoneal mast cells. Antagonist activity of SPA is expressed in the concn. range 1-10 mM, but at higher concns. SPA releases histamine. SPA inhibits the flare response induced by substance P in human skin, but is without effect on the wheal response. Up to 12.5 pmol SPA produces neither wheal nor flare response by itself. The structurally related peptide, kassinin [63968-82-1], does not cause histamine release from rat mast cells at concns. up to 10 mM whereas the Me ester of substance P [76260-78-1] was 1.6-fold more active than substance P in this respect. The findings are discussed in terms of the classification of substance P receptors and the mechanism of wheal and flare in human skin. .