Antagonists of substance P

Caranikas, Stephanos; Mizrahi, Jacques; D’Orléans-Juste, Pedro; Regoli, Doménico

doi:10.1016/0014-2999(82)90023-1

Cited by 44 publications

(12 citation statements)

References 3 publications

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“…Analogs of Uru‐TKs and mammalian tachykinins were synthesized by a solid‐phase peptide synthesizer (PE Biosystems Japan Model 433A, Tokyo, Japan) using the FastMoc method. A SP antagonist, [ D ‐Pro 4 , D ‐Trp 7,9 ]SP (4‐11), D ‐Pro‐Gln‐Gln‐ D ‐Trp‐Phe‐ D ‐Trp‐Leu‐Met‐NH 2 [12] and its C‐terminal Arg analog were also synthesized. The peptides and analogs are shown in Fig.…”

Section: Methodsmentioning

confidence: 99%

The importance of C‐terminal residues of vertebrate and invertebrate tachykinins for their contractile activities in gut tissues

1999

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The C-terminal residues of mammalian tachykinins and urechistachykinins (Uru-TKs), tachykinin-related peptides of echiuroid worm origin, were substituted for each other. Their contractile effects were assayed on the cockroach hindgut and the guinea pig ileum. [Met 10 ] substitution of Uru-TKs caused a 1000 times lower activity on the hindgut, but a 1000 times higher activity on the ileum. In contrast, [Arg 11 ]substance P (SP) was 100 times more and 400 times less potent than SP on the hindgut and ileum, respectively. A SP antagonist blocked these Uru-TK activities on the hindgut. These results demonstrated that the C-terminal Met-NH 2 is necessary for ileum contraction and the Arg-NH 2 is required for hindgut contraction, which was caused by binding to the cockroach's neurokinin-like receptor.z 1999 Federation of European Biochemical Societies.

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Section: Methodsmentioning

confidence: 99%

The importance of C‐terminal residues of vertebrate and invertebrate tachykinins for their contractile activities in gut tissues

1999

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“…Furthermore, by using compounds which antagonize the effects of histamine or serotonin and which block the synthesis of prostaglandins, we have also demonstrated that SP did not exert its ino tropic effect by stimulating the intramural synthesis and/or the release of naturally oc curring autacoids. In addition, the existence of specific receptors for SP on the rat portal vein has been confirmed by using the SP antagonists (pro2, phe7, trp9)-SP [Leander et al, 1981] and (pro4, trp7-9)-SP 4-11 [Caranikas et al, 1982].…”

Section: Introductionmentioning

confidence: 93%

“…Two analogues of SP, the undecapeptide (pro2, phe7, trp9)-SP and the octapeptide (pro4, trp7' 9)-SP 4-11, described as specific antagonists of SP receptors by Leander et al [1981] and Caranikas et al [1982] respec tively, were tested on the rat portal vein. These compounds were added to the medium 10 min before the first SP application.…”

Section: )-Sp 4-11mentioning

confidence: 99%

Postjunctional Localization of Substance P Receptors on the Rat Portal Vein

Mastrangelo¹,

Mathison²,

Huggel³

1983

Pharmacology

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A dose-dependent contractile effect of substance P (SP) on the isolated, everted rat portal vein was competitively inhibited by two selective SP antagonists (pro², phe⁷, trp⁹)-SP and (pro⁴, trp^7,9)-SP 4–11. Phentolamine, atropine, methysergide, mepyramine, cimetidine, Sar¹, Ile⁸-angiotensin II, Leu⁸, des-Arg⁹-bradykinin and indomethacin did not block the action of SP. However, some of these antagonists differentially reduced SP responses, but such inhibitory effects were shown to be nonspecific. The results suggest that the SP-induced contractions of the rat portal vein were directly mediated by specific receptors localized on the smooth muscle cells. In addition, the response to SP appeared to be independent of prostaglandin biosynthesis.

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“…; 2Present address: Clinical Pharmacology, Centre Block, Southampton General Hospital, Southampton S09 4XY; 3Present address: Department of Neuropharmacology, Glaxo Group Research Ltd, Ware, Hertfordshire SG120DJ; 4Author for correspondence. tachykinin antagonists (Folkers et al, 1981;Caranikas et al, 1982) and findings with some of the earlier examples have been reviewed by Rosell & Folkers (1982). Many of these earlier analogues, however, still retained agonist activity in smooth muscle.…”

Section: Introductionmentioning

confidence: 99%

“…One of the earliest attempts to alter the activity of a tachykinin by this method was with a seven amino acid analogue of eledoisin (Schroder et al, 1965), before the structure of substance P (SP) had been elucidated (Chang et al, 1971 tachykinin antagonists (Folkers et al, 1981;Caranikas et al, 1982) and findings with some of the earlier examples have been reviewed by Rosell & Folkers (1982). Many of these earlier analogues, however, still retained agonist activity in smooth muscle.…”

Section: Introductionmentioning

confidence: 99%

An examination of the pharmacology of two substance P antagonists and the evidence for tachykinin receptor subtypes

Bailey

Featherstone

Jordan

et al. 1986

British J Pharmacology

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1 The potencies of two tachykinin antagonists ) and Trp7'9, Leull]-SP(,II1) against four tachykinins were examined in a range of smooth muscle preparations, including guinea-pig ileum and bladder and rat colon muscularis mucosae and duodenum. 2 Parallel shifts in the log dose-response curves of all the tachykinins tested were observed in all tissues, except in the case of the guinea-pig bladder where [D-Pro4, D-Trp7'9" 0-SP(4, ] was without effect at concentrations up to 32 jaM. 3 The slopes of the Schild plots for the two antagonists did not differ significantly from unity, with the exception of [D-Pro4, D-Trp7'9"0I-SP(4 11) in the rat duodenum, which may indicate a heterogeneous receptor population in this tissue. The antagonists displayed agonist selectivity in the case of the guinea-pig ileum where log dose-response curves to substance P and physalaemin were shifted less than those to eledoisin and kassinin. 4 Rank orders of potency for eledoisin, kassinin, physalaemin and substance P in the five preparations studied allowed classification of the tissues by the predominant receptor type according to the 'SP-P' and 'SP-E' scheme.

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Antagonists of substance P

Cited by 44 publications

References 3 publications

The importance of C‐terminal residues of vertebrate and invertebrate tachykinins for their contractile activities in gut tissues

The importance of C‐terminal residues of vertebrate and invertebrate tachykinins for their contractile activities in gut tissues

Postjunctional Localization of Substance P Receptors on the Rat Portal Vein

An examination of the pharmacology of two substance P antagonists and the evidence for tachykinin receptor subtypes

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