Multiple Tachykinin Binding Sites in Rat Brain and Peripheral Tissues
Based on the different rank order of potencies as well as the lack of complete cross-tachyphylaxis observed among different tachykinins and their analogues in several biological assays, we have previously proposed the existence of multiple subtypes of SP receptors in different tissues [1–3]. For the SP-P subtype, both physalaemin (PHY) and SP are active at nanomolar concentrations with eledoisin (E) and kassinin (KAS) more or less equipotent. On the other hand, for the SP-E subtype, KAS, E and neurokinin A (NKA) are active at nanomolar concentrations and they are several hundred times more active than PHY or SP. The distinction between SP-P and SP-E system was further delineated by the development of a SP-P selective agonist, SP-O-methyl ester (SPOMe), which is 100–1000 times less potent than substance P on SP-E systems .
KeywordsNanomolar Concentration Tachykinin Receptor Substance Preceptor Dohme Research Laboratory Distinct Pharmacological Profile
Unable to display preview. Download preview PDF.
- 2.Iversen L L, Hanley M R, Sandberg B E B, Lee C M, Pinnock R D, Watson S P (1982) Substance P receptors in the nervous system and the possible existence of multiple receptor subtypes. In: Ciba Foundation Symposium Vol.91, Substance P in the Nervous System London: Pitman Medical Ltd. pp 186–195.Google Scholar
- 3.Iversen L L (1985) Multiple receptors for tachykinins. In: Hakanson Rand Sundler F (eds) Tachykinin Antagonists, 8th Eric K. Fernstrom Symposium. Amsterdam: Elsevier pp 291–304.Google Scholar
- 7.Cascieri M A, Chicchi G G, Liang T (1985) Demonstration of two distinct tachykinin receptors in rat brain cortex, J. BioI. Chem., 260, 1501–1507.Google Scholar
- 11.Lee C M, Campbell N J, Williams B J, Iversen L L (1986) Multiple tachykinin binding sites in perpheral tissues and in brain. Eur.J. Pharmacol. (in press).Google Scholar