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Chemical Compound Review:

AC1Q5YGV methyl(2S)-2-[[(2S)-2-[2- [[(2S)-2-[[(2S)...

Synonyms: CTK8D8786, AR-1J4262, AC1L3X8S, 8030-53-3, Methyl ester-SP, ...

Perren, M.J. et al., Shahbazian, A. et al., Guard, S. et al., Beattie, D.T. et al., Wienrich, M. et al., et al.

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High impact information on Methyl ester-substance P

Selective agonists at the NK-1 receptive site, substance P-methyl ester (SP-OME) and septide, mimicked the response to the natural neurokinins as did DiMe-C7, a selective NK-3 receptor agonist [1].
4. Co-administration of GR82334 (1 microM), a selective NK1 receptor antagonist, inhibited the vasodilatation produced by SPOMe (0.1 microM) but not that caused by calcitonin gene-related peptide (CGRP, 0.01 microM) [2].
2. In guinea-pig trachea, (+/-)-CP-96,345 produced antagonism of responses to the selective NK1 agonists [Sar9, Met(O2)11]SP and substance P-methyl ester that was apparently competitive in nature (pKB 7.0-7.5), while in guinea-pig ileum the antagonism was not surmountable [3].
The tachykinin NK1 receptor agonist substance P methyl ester (SPOME) impedes intestinal peristalsis by releasing nitric oxide (NO) from inhibitory motor neurones [4].
However, whilst NKA-evoked ventral root depolarization was completely abolished in the presence of staurosporine, SPOMe- and SP-induced depolarizations were unaffected [5].

Biological context of Methyl ester-substance P

CGRP8-37 (0.34 mumolkg-1) had no effect on decreases in carotid arterial vascular resistance produced by SPOMe, and CP99 994 (0.23 mumolkg-1 i.v.) had no effect on vasodilator responses produced by either alpha- or beta CGRP [6].

Anatomical context of Methyl ester-substance P

Since NK1 receptor agonists differ in their receptor interaction, we set out to compare a range of NK1 receptor agonists including SPOME, septide and GR-73 632 in their effects on propulsive peristalsis and circular muscle activity in the guinea-pig isolated small intestine [4].
The present study has investigated the effects of alpha and beta calcitonin gene-related peptide (CGRP), and the tachykinin neurokinin1 (NK1) receptor agonist, substance P methyl ester (SPOMe), on carotid vascular resistance, following their injection into the carotid artery bed of the anaesthetized rabbit [6].

References

Activation of substance P receptors leads to membrane potential responses in cultured astrocytes. Wienrich, M., Kettenmann, H. Glia (1989) [Pubmed]
Neurokinin-induced changes in pial artery diameter in the anaesthetized guinea-pig. Beattie, D.T., Stubbs, C.M., Connor, H.E., Feniuk, W. Br. J. Pharmacol. (1993) [Pubmed]
The interaction of the NK1 receptor antagonist CP-96,345 with L-type calcium channels and its functional consequences. Guard, S., Boyle, S.J., Tang, K.W., Watling, K.J., McKnight, A.T., Woodruff, G.N. Br. J. Pharmacol. (1993) [Pubmed]
Differences in circular muscle contraction and peristaltic motor inhibition caused by tachykinin NK1 receptor agonists in the guinea-pig small intestine. Shahbazian, A., Holzer, P. Neurogastroenterol. Motil. (2000) [Pubmed]
Tachykinin induced regulation of excitatory amino acid responses in the rat spinal cord in vitro. Urban, L., Naeem, S., Patel, I.A., Dray, A. Neurosci. Lett. (1994) [Pubmed]
NK1 and CGRP receptor-mediated dilatation of the carotid arterial bed of the anaesthetized rabbit. Perren, M.J., Connor, H.E., Beattie, D.T. Neuropeptides (1996) [Pubmed]

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