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Chemical Compound Review

Physalemin     4-[2-[[1-[[5-amino-1-[[1-[[1- [[1-[(1...

Synonyms: Physalaemin, AGN-PC-002851, LS-187047, LS-187659, AC1L29NZ, ...
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Disease relevance of Physalemin


Psychiatry related information on Physalemin

  • The present findings suggest that in adult rats central eledoisin and physalaemin exert a selective suppressive effect on drinking behavior without affecting feeding [3].

High impact information on Physalemin

  • Substance P (SP), first identified by bioassay as early as 1931 but sequenced only in 1971, several years after the elucidation of the structure of eledoisin from molluscan tissues and of physalaemin from amphibian skin, may be considered as a prototype of the tachykinins [4].
  • Both physalaemin and the tumor peptide produced a contractile response of isolated guinea pig ileum at threshold concentrations of approximately 100 to 150 picograms per milliliter [1].
  • The disulfide bridge constraints have been designed on the basis of conformational studies on SP and physalaemin indicating an alpha-helical structure for the core of these two tachykinins (group I) and a folding of the C-terminal carboxamide towards the side chains of the glutamines 5 and 6 (group II) [5].
  • These results indicate that dispersed acini from guinea pig pancreas possess a single class of receptors that interact with physalaemin, substance P, and eledoisin and that occupation of 45% of these receptors will cause a maximal biological response [6].
  • Binding of 125I-labeled physalaemin was saturable, temperature-dependent, and reversible and reflected interaction of the labeled peptide with a single class of binding sites on the plasma membrane of pancreatic acinar cells [6].

Biological context of Physalemin


Anatomical context of Physalemin


Associations of Physalemin with other chemical compounds


Gene context of Physalemin

  • Of these SP analogues, [D-Arg1,D-Pro2,4,D-Phe7,D-His9]SP attenuated selectively the behavioural responses produced by NK-1 receptor agonists such as SP and physalaemin [21].
  • These immunoconjugates, composed of IL-1 beta, IL-2, TNF-alpha, physalaemin, leukotriene B4, histamine, and bradykinin chemically linked to TNT-1, a murine monoclonal antibody that binds necrotic regions in tumors, have been tested for their effects on antibody uptake in vivo [22].
  • The tachykinins neurokinin A and physalaemin stimulate murine thymocyte proliferation [23].
  • The receptor for SP is particularly sensitive to SP and physalaemin and shows higher affinity for the whole natural peptides (SP, NKA) than for their C-terminal fragments [24].
  • SP proved to be the most efficient IL-2 inducer, exerting its maximal effect at concentrations that were 4 to 5 orders of magnitude lower than the optimal stimulatory concentrations of physalaemin, NKA, or NKB [25].

Analytical, diagnostic and therapeutic context of Physalemin

  • Thus, we developed a rapid physalaemin-specific radioimmunoassay that led to the initial discovery of a substance in mammalian tissues with an immunoreactivity resembling that of the original amphibian peptide [26].
  • SK, kassinin and eledoisin were more potent than SP and physalaemin in increasing respiratory insufflation pressure [27].
  • Equimolar amounts of the related peptides physalaemin and eledoisin-related peptide also caused analgesia, but the SP N-terminal fragment (1-9) was inactive [28].
  • Bombesin, GRP, SP, physalaemin and eledoisin contracted the smooth muscle and potentiated the response to electrical stimulation [29].
  • Substance P, P-octapeptide, physalaemin and eledoisin, and eledoisin related peptide were found to be potent miotics on these preparations, yielding ED50 values in the range of 8 to 95 nM and complete pupillary constriction in the range of 100 to 1000 nM [30].


  1. Physalaemin: an amphibian tachykinin in human lung small-cell carcinoma. Lazarus, L.H., DiAugustine, R.P., Jahnke, G.D., Hernandez, O. Science (1983) [Pubmed]
  2. Comparative toxicity of amyloid beta-peptide in neuroblastoma cell lines: effects of albumin and physalaemin. Zhao, X., Valantas, J.A., Vyas, S., Duffy, L.K. Comp. Biochem. Physiol. C, Comp. Pharmacol. Toxicol. (1993) [Pubmed]
  3. Suppression of drinking but not feeding by central eledoisin and physalaemin in the rat. Massi, M., Micossi, L.G., de Caro, G., Epstein, A.N. Appetite. (1986) [Pubmed]
  4. The tachykinin peptide family. Severini, C., Improta, G., Falconieri-Erspamer, G., Salvadori, S., Erspamer, V. Pharmacol. Rev. (2002) [Pubmed]
  5. Interaction of tachykinins with their receptors studied with cyclic analogues of substance P and neurokinin B. Ploux, O., Lavielle, S., Chassaing, G., Julien, S., Marquet, A., d'Orléans-Juste, P., Dion, S., Regoli, D., Beaujouan, J.C., Bergström, L. Proc. Natl. Acad. Sci. U.S.A. (1987) [Pubmed]
  6. Interaction of physalaemin, substance P, and eledoisin with specific membrane receptors on pancreatic acinar cells. Jensen, R.T., Gardner, J.D. Proc. Natl. Acad. Sci. U.S.A. (1979) [Pubmed]
  7. Characterization and segmental distribution of 125I-Bolton-Hunter-labeled substance P binding sites in rat spinal cord. Charlton, C.G., Helke, C.J. J. Neurosci. (1985) [Pubmed]
  8. Modifications of drinking behaviour and of arterial blood pressure induced by tachykinins in rats and pigeons. de Caro, G., Massi, M., Micossi, L.G. Psychopharmacology (Berl.) (1980) [Pubmed]
  9. Specific binding of a 125I-labeled substance P analog to rat submaxillary gland. Bahouth, S.W., Stewart, J.M., Musacchio, J.M. J. Pharmacol. Exp. Ther. (1984) [Pubmed]
  10. Ultrastructural localization and afferent sources of substance P in the rat parabrachial region. Milner, T.A., Pickel, V.M. Neuroscience (1986) [Pubmed]
  11. In vitro growth inhibition of human small cell lung cancer by physalaemin. Bepler, G., Carney, D.N., Gazdar, A.F., Minna, J.D. Cancer Res. (1987) [Pubmed]
  12. Human skin mast cells: their dispersion, purification, and secretory characterization. Benyon, R.C., Lowman, M.A., Church, M.K. J. Immunol. (1987) [Pubmed]
  13. Effects of streptozocin-induced diabetes on sympathetic and parasympathetic stimulation of parotid salivary gland function in rats. Anderson, L.C., Garrett, J.R., Thulin, A., Proctor, G.B. Diabetes (1989) [Pubmed]
  14. Salivary secretion induced by substance P. Yu, J.H., Burns, S.M., Schneyer, C.A. Proc. Soc. Exp. Biol. Med. (1983) [Pubmed]
  15. Characterization and autoradiographic localization of multiple tachykinin binding sites in gastrointestinal tract and bladder. Burcher, E., Buck, S.H., Lovenberg, W., O'Donohue, T.L. J. Pharmacol. Exp. Ther. (1986) [Pubmed]
  16. Bombesin-related peptides induce calcium mobilization in a subset of human small cell lung cancer cell lines. Heikkila, R., Trepel, J.B., Cuttitta, F., Neckers, L.M., Sausville, E.A. J. Biol. Chem. (1987) [Pubmed]
  17. NK-1 receptor mediation of neurogenic plasma extravasation in rat skin. Andrews, P.V., Helme, R.D., Thomas, K.L. Br. J. Pharmacol. (1989) [Pubmed]
  18. Biological evaluation of substance P antagonists. Folkers, K., Håkanson, R., Hörig, J., Xu, J.C., Leander, S. Br. J. Pharmacol. (1984) [Pubmed]
  19. Contractile effects of substance P and other tachykinins on the mouse isolated distal colon. Fontaine, J., Lebrun, P. Br. J. Pharmacol. (1989) [Pubmed]
  20. A study of [D-Pro2, D-Phe7, D-Trp9]-substance P and [D-Trp7,9]-substance P as tachykinin partial agonists in the rat colon. Bailey, S.J., Jordan, C.C. Br. J. Pharmacol. (1984) [Pubmed]
  21. Substance P analogues containing D-histidine antagonize the behavioural effects of intrathecally co-administered substance P in mice. Sakurada, T., Yamada, T., Sakurada, S., Kisara, K., Ohba, M. Eur. J. Pharmacol. (1989) [Pubmed]
  22. Effect of seven new vasoactive immunoconjugates on the enhancement of monoclonal antibody uptake in tumors. Khawli, L.A., Miller, G.K., Epstein, A.L. Cancer (1994) [Pubmed]
  23. The tachykinins neurokinin A and physalaemin stimulate murine thymocyte proliferation. Söder, O., Hellström, P.M. Int. Arch. Allergy Appl. Immunol. (1989) [Pubmed]
  24. Receptors for substance P and related neurokinins. Regoli, D., Drapeau, G., Dion, S., D'Orléans-Juste, P. Pharmacology (1989) [Pubmed]
  25. Stimulation of IL-2 production in murine lymphocytes by substance P and related tachykinins. Rameshwar, P., Gascon, P., Ganea, D. J. Immunol. (1993) [Pubmed]
  26. A neuropeptide in mammalian tissues with physalaemin-like immunoreactivity. Lazarus, L.H., Linnoila, R.I., Hernandez, O., DiAugustine, R.P. Nature (1980) [Pubmed]
  27. Comparison of cardiovascular and bronchoconstrictor effects of substance P, substance K and other tachykinins. Hua, X., Lundberg, J.M., Theodorsson-Norheim, E., Brodin, E. Naunyn Schmiedebergs Arch. Pharmacol. (1984) [Pubmed]
  28. Analgesic and cardiovascular effects of centrally administered substance P. Clint, B.D., Lipton, J.M., Giesecke, A.H. Peptides (1988) [Pubmed]
  29. Immunohistochemical localization of substance P, vasoactive intestinal polypeptide and gastrin-releasing peptide in vas deferens and seminal vesicle, and the effect of these and eight other neuropeptides on resting tension and neurally evoked contractile activity. Stjernquist, M., Håkanson, R., Leander, S., Owman, C., Sundler, F., Uddman, R. Regul. Pept. (1983) [Pubmed]
  30. The mechanism of peptidergic miosis. I. The structural basis of miotic potency among biologically active polypeptides. Bito, L.Z., Baroody, R.A., Backerman, A. Curr. Eye Res. (1981) [Pubmed]
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