Abstract
The degradation of [3H]-substance P was monitored in guinea-pig ileum and rat vas deferens. Substantial and rapid metabolism occurred in both tissues within the time course of the pharmacological responses; for example, after 1 min more than 50% of the extracted tritium from both tissues was present in the form of metabolites. [3H]-inulin was used to estimate the rate of equilibration of the extracellular space of guinea-pig ileum longitudinal muscle and rat vas deferens with the bath fluid; half-lives of 30 s and 5 min respectively were observed. These two factors combine to give different concentrations of substance P in the biophase of the tissues. The peak concentration of substance P reached in the guinea-pig ileum longitudinal muscle was approximately five times higher than in the rat vas deferens. An analogue of substance P, [3H]-DiMe-C7, was found to be stable in both tissues. These results are discussed in the light of the suggested existence of multiple receptors for substance P, based on agonist potency differences.
Full text
PDFSelected References
These references are in PubMed. This may not be the complete list of references from this article.
- Allen M. C., Brundish D. E., Wade R., Sandberg B. E., Hanley M. R., Iversen L. L. Tritiated peptides. 12. Synthesis and biological activity of [4-3H-Phe8]substance P. J Med Chem. 1982 Oct;25(10):1209–1213. doi: 10.1021/jm00352a022. [DOI] [PubMed] [Google Scholar]
- Egan S. M., Graham J. D., Lewis M. J. The uptake of tritiated delta 1-tetrahydrocannabinol by the isolated vas deferens of the rat. Br J Pharmacol. 1976 Apr;56(4):413–416. doi: 10.1111/j.1476-5381.1976.tb07451.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Eison A. S., Iversen S. D., Sandberg B. E., Watson S. P., Hanley M. R., Iversen L. L. Substance P analog, DiMe-C7: evidence for stability in rat brain and prolonged central actions. Science. 1982 Jan 8;215(4529):188–190. doi: 10.1126/science.6171884. [DOI] [PubMed] [Google Scholar]
- Erspamer G. F., Erspamer V., Piccinelli D. Parallel bioassay of physalaemin and kassinin, a tachykinin dodecapeptide from the skin of the African frog Kassina senegalensis. Naunyn Schmiedebergs Arch Pharmacol. 1980 Feb;311(1):61–65. doi: 10.1007/BF00500303. [DOI] [PubMed] [Google Scholar]
- Gater P. R., Jordan C. C., Owen D. G. Relative activities of substance P-related peptides in the guinea-pig ileum and rat parotid gland, in vitro. Br J Pharmacol. 1982 Feb;75(2):341–351. doi: 10.1111/j.1476-5381.1982.tb08792.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Goto K., Masuda Y., Kasuya Y. The effect of denervation on the synchronization of contraction of the rat vas deferens. Eur J Pharmacol. 1976 Apr;36(2):395–404. doi: 10.1016/0014-2999(76)90093-5. [DOI] [PubMed] [Google Scholar]
- Holzer P., Emson P. C., Iversen L. L., Sharman D. F. Regional differences in the response to substance P on the longitudinal muscle and the concentration of substance P in the digestive tract of the guinea-pig. Neuroscience. 1981;6(7):1433–1441. doi: 10.1016/0306-4522(81)90198-6. [DOI] [PubMed] [Google Scholar]
- Lee C. M., Iversen L. L., Hanley M. R., Sandberg B. E. The possible existence of multiple receptors for substance P. Naunyn Schmiedebergs Arch Pharmacol. 1982 Mar;318(4):281–287. doi: 10.1007/BF00501166. [DOI] [PubMed] [Google Scholar]
- Piercey M. F., Dobry P. J., Einspahr F. J., Schroeder L. A., Masiques N. Use of substance P fragments to differentiate substance P receptors of different tissues. Regul Pept. 1982 May;3(5-6):337–349. doi: 10.1016/0167-0115(82)90057-x. [DOI] [PubMed] [Google Scholar]
- RANG H. P. STIMULANT ACTIONS OF VOLATILE ANAESTHETICS ON SMOOTH MUSCLE. Br J Pharmacol Chemother. 1964 Apr;22:356–365. doi: 10.1111/j.1476-5381.1964.tb02040.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Sandberg B. E., Hanley M. R., Watson S. P., Brundish D. E., Wade R., Eison A. S. Synthesis and metabolic stability of a tritium-labelled substance P analogue. FEBS Lett. 1982 Jan 25;137(2):236–240. doi: 10.1016/0014-5793(82)80357-8. [DOI] [PubMed] [Google Scholar]
- Sandberg B. E., Iversen L. L. Substance P. J Med Chem. 1982 Sep;25(9):1009–1015. doi: 10.1021/jm00351a001. [DOI] [PubMed] [Google Scholar]
- Sandberg B. E., Lee C. M., Hanley M. R., Iversen L. L. Synthesis and biological properties of enzyme-resistant analogues of substance P. Eur J Biochem. 1981 Feb;114(2):329–337. doi: 10.1111/j.1432-1033.1981.tb05152.x. [DOI] [PubMed] [Google Scholar]
- Schnieden H., Small R. C. Spasmolytic effects of cadmium and zinc ions upon the guinea-pig isolated ileum preparation. Br J Pharmacol. 1971 Mar;41(3):488–499. doi: 10.1111/j.1476-5381.1971.tb08046.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Teichberg V. I., Cohen S., Blumberg S. Distinct classes of substance P receptors revealed by a comparison of the activities of substance P and some of its segments. Regul Pept. 1981 Feb;1(5):327–333. doi: 10.1016/0167-0115(81)90056-2. [DOI] [PubMed] [Google Scholar]
- Watson S. P., Sandberg B. E., Hanley M. R., Iversen L. L. Tissue selectivity of substance P alkyl esters: suggesting multiple receptors. Eur J Pharmacol. 1983 Jan 28;87(1):77–84. doi: 10.1016/0014-2999(83)90052-3. [DOI] [PubMed] [Google Scholar]