Literature DB >> 24190666

Spantide III, a superior tachykinin antagonist with high potency and negligible neurotoxicity.

K Folkers1, R Hakanson, D M Feng, J C Xu, A Janecka, Z Y Wang.   

Abstract

Five new antagonists of Substance P were designed and synthesized toward increasing potency and safety. One of them was more effective than Spantide II, which was the basis for the design. It was named Spantide III and has the structure: D-NicLys,Pro,Pal,Pro,D-Cl2Phe,Asn,D-Trp,Phe,D-Pal,Leu, NleNH2.

Entities:  

Year:  1993        PMID: 24190666     DOI: 10.1007/BF00805985

Source DB:  PubMed          Journal:  Amino Acids        ISSN: 0939-4451            Impact factor:   3.520


  15 in total

1.  Activity of spantide I and II at various tachykinin receptors and NK-2 tachykinin receptor subtypes.

Authors:  C A Maggi; R Patacchini; D M Feng; K Folkers
Journal:  Eur J Pharmacol       Date:  1991-06-18       Impact factor: 4.432

2.  Design, synthesis and bioassays of antagonists of LHRH which have high antiovulatory activity and release negligible histamine.

Authors:  A Ljungqvist; D M Feng; P F Tang; M Kubota; T Okamoto; Y W Zhang; C Y Bowers; W A Hook; K Folkers
Journal:  Biochem Biophys Res Commun       Date:  1987-10-29       Impact factor: 3.575

3.  Substance P antagonists showing some selectivity for different receptor types.

Authors:  D Regoli; J Mizrahi; P D'Orléans-Juste; S Dion; G Drapeau; E Escher
Journal:  Eur J Pharmacol       Date:  1985-02-12       Impact factor: 4.432

4.  Spantide II, an effective tachykinin antagonist having high potency and negligible neurotoxicity.

Authors:  K Folkers; D M Feng; N Asano; R Håkanson; Z Weisenfeld-Hallin; S Leander
Journal:  Proc Natl Acad Sci U S A       Date:  1990-06       Impact factor: 11.205

5.  Antinociceptive and substance P antagonistic effects of intrathecally injected spantide II in rat: no signs of motor impairment or neurotoxicity.

Authors:  Z Wiesenfeld-Hallin; X J Xu; K Kristensson; R Håkanson; D M Feng; K Folkers
Journal:  Regul Pept       Date:  1990-06

6.  Comparison of spantide II and CP-96,345 for blockade of tachykinin-evoked contractions of smooth muscle.

Authors:  R Håkanson; Z Y Wang; K Folkers
Journal:  Biochem Biophys Res Commun       Date:  1991-07-15       Impact factor: 3.575

7.  Antinociceptive and neurotoxic actions of substance P analogues in the rat's spinal cord after intrathecal administration.

Authors:  C Post; I Paulsson
Journal:  Neurosci Lett       Date:  1985-06-12       Impact factor: 3.046

8.  The effects of substance P on histamine and 5-hydroxytryptamine release in the rat.

Authors:  C M Fewtrell; J C Foreman; C C Jordan; P Oehme; H Renner; J M Stewart
Journal:  J Physiol       Date:  1982-09       Impact factor: 5.182

Review 9.  Substance P--structure-activity studies and the development of antagonists.

Authors:  D Regoli; E Escher; J Mizrahi
Journal:  Pharmacology       Date:  1984       Impact factor: 2.547

10.  Biological evaluation of substance P antagonists.

Authors:  K Folkers; R Håkanson; J Hörig; J C Xu; S Leander
Journal:  Br J Pharmacol       Date:  1984-10       Impact factor: 8.739

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