Non‐peptide antagonists, CP‐96,345 and RP 67580, distinguish species variants in tachykinin NK<sub>1</sub> receptors

Barr, Alastair J.; Watson, Steve P.

doi:10.1111/j.1476-5381.1993.tb13466.x

Cited by 46 publications

(22 citation statements)

References 28 publications

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“…Moreover, RP 67580 exhibited higher affinity versus NK, receptors in the mouse and rat than in the dog, guinea-pig and man. In contrast, CP-96,345, another recently described non-peptide NK, receptor antagonist (Snider et al, 1991) displayed higher affinity versus NK, receptors present in the latter group of species (Fardin et al, 1992;Barr & Watson, 1993). In the present study, we have examined the pharmacological profile of RP 67580 in the neonatal rat spinal cord and its effects on a primary afferent-evoked slow VRP.…”

Section: Introductionmentioning

confidence: 74%

Effects of RP 67580, a tachykinin NK₁ receptor antagonist, on a primary afferent‐evoked response of ventral roots in the neonatal rat spinal cord

Hosoki

Yanagisawa

Guo

et al. 1994

British J Pharmacology

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Section: Introductionmentioning

confidence: 74%

Effects of RP 67580, a tachykinin NK₁ receptor antagonist, on a primary afferent‐evoked response of ventral roots in the neonatal rat spinal cord

Hosoki

Yanagisawa

Guo

et al. 1994

British J Pharmacology

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“…In particular, NK1r, NK2r and NK3r have the highest affinity to SP, NKA and NKB, respectively [56][57][58]. Moreover, in the ileum of mouse, rat and guineapig, species-dependent variations in the affinity of these receptors have been demonstrated by pharmacology [56,57,59,60] and in amino acid sequence by molecular biology [61].…”

Section: Neurokinin Receptorsmentioning

confidence: 99%

Relationships between neurokinin receptor‐expressing interstitial cells of Cajal and tachykininergic nerves in the gut

Faussone–Pellegrini

2006

J Cellular Molecular Medi

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The so-called interstitial cells of Cajal (ICC) are distributed throughout the muscle coat of the alimentary tract with characteristic intramural location and species-variations in structure and staining. Several ICC sub-types have been identified: ICC-DMP, ICC-MP, ICC-IM, ICC-SM. Gut motility is regulated by ICC and each sub-type is responsible for the electrical activities typical of each gut region and/or muscle layer. The interstitial position of the ICC between nerve endings and smooth muscle cells has been extensively considered. Some of these nerve endings contain tachykinins. Three distinct tachykinin receptors (NK1r, NK2r and NK3r) have been demonstrated by molecular biology. Each of them binds with different affinities to a series of tachykinins (SP, NKA and NKB). In the ileum, SP-immunoreactive (SP-IR) nerve fibers form a rich plexus at the deep muscular plexus (DMP), distributed around SP-negative cells, and ICC-DMP intensely express the SP-preferred receptor NK1r; conversely a faint NK1r-IR is detected on the ICC-MP and mainly after receptor internalization was induced by agonists. ICC-IM are never stained in laboratory mammals, while those of the human antrum are NK1r-IR. RT-PCR conducted on isolated ileal ICC-MP and gastric ICC-IM showed that these cells express NK1r and NK3r. Colonic ICC, except those in humans, do not express NK1r-IR, at least in resting conditions. Outside the gut, NK1r-IR cells were seen in the arterial wall and exocrine pancreas. In the mouse gut only, NK1r-IR is present in non-neuronal cells located within the intestinal villi, so-called myoid cells, which are c-kit-negative and α-smooth muscle actin-positive. Immunohistochemistry and functional studies confirmed that ICC receive input from SP-IR terminals, with differences between ICC sub-types. In the rat, very early after birth, NK1r is expressed by the ICC-DMP and SP by the related nerve varicosities. Studies on pathological conditions are few and those on mutant strains practically absent. It has only been reported that in the inflamed ileum of rats the NK1r-IR ICC-DMP disappear and that at the peak of inflammatory conditions ICC-MP are NK1r-IR. In the ileum of mice with a mutation in the W locus, ICC-DMP were seen to express c-kit-IR but not NK1-IR, and SP-IR innervation seems unchanged. In summary, there are distinct ICC populations, each of them under a different tachykininergic control and, likely, having different functions. Further studies are recommended at the aim of understanding ICC involvement in modulating/transmitting tachykininergic inputs.

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“…The nonpeptide antagonist, (± )-CP 96,345 (Snider et al, 1991) is about 100 times more potent at NKI receptor expressed in e.g. man and guinea-pigs than rats or mice (Gitter et al, 1991;Patacchini et al, 1992;Barr & Watson, 1993), while the nonpeptide antagonist, RP 67,580 (Garret et al, 1991) is more potent at rat than guinea-pig or human NKI receptors. For NK2-receptors, certain peptide (e.g.…”

Section: Introductionmentioning

confidence: 99%

Comparison of tachykinin NK₁ and NK₂ receptors in the circular muscle of the guinea‐pig ileum and proximal colon

Maggi

Patacchini

Meini

et al. 1994

British J Pharmacology

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1 The aim of this study was the pharmacological characterization of tachykinin NKI and NK2 receptors mediating contraction in the circular muscle of the guinea-pig ileum and proximal colon. The action of substance P (SP), neurokinin A (NKA) and of the synthetic agonists [ Furthermore, an intraspecies heterogeneity of the NK2 receptor in the circular muscle of the guinea-pig ileum and colon is suggested.

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Non‐peptide antagonists, CP‐96,345 and RP 67580, distinguish species variants in tachykinin NK₁ receptors

Cited by 46 publications

References 28 publications

Effects of RP 67580, a tachykinin NK₁ receptor antagonist, on a primary afferent‐evoked response of ventral roots in the neonatal rat spinal cord

Effects of RP 67580, a tachykinin NK₁ receptor antagonist, on a primary afferent‐evoked response of ventral roots in the neonatal rat spinal cord

Relationships between neurokinin receptor‐expressing interstitial cells of Cajal and tachykininergic nerves in the gut

Comparison of tachykinin NK₁ and NK₂ receptors in the circular muscle of the guinea‐pig ileum and proximal colon

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Non‐peptide antagonists, CP‐96,345 and RP 67580, distinguish species variants in tachykinin NK1 receptors

Cited by 46 publications

References 28 publications

Effects of RP 67580, a tachykinin NK1 receptor antagonist, on a primary afferent‐evoked response of ventral roots in the neonatal rat spinal cord

Effects of RP 67580, a tachykinin NK1 receptor antagonist, on a primary afferent‐evoked response of ventral roots in the neonatal rat spinal cord

Relationships between neurokinin receptor‐expressing interstitial cells of Cajal and tachykininergic nerves in the gut

Comparison of tachykinin NK1 and NK2 receptors in the circular muscle of the guinea‐pig ileum and proximal colon

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Non‐peptide antagonists, CP‐96,345 and RP 67580, distinguish species variants in tachykinin NK₁ receptors

Effects of RP 67580, a tachykinin NK₁ receptor antagonist, on a primary afferent‐evoked response of ventral roots in the neonatal rat spinal cord

Effects of RP 67580, a tachykinin NK₁ receptor antagonist, on a primary afferent‐evoked response of ventral roots in the neonatal rat spinal cord

Comparison of tachykinin NK₁ and NK₂ receptors in the circular muscle of the guinea‐pig ileum and proximal colon