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Chemical Compound Review

proctolin     (2S,3R)-2-[[(2S)-1-[(2S)-2- [[(2S)-2-[[(2S)...

Synonyms: Gut factor, CHEMBL295536, AG-G-04994, AC1L3XAD, AC1Q5JQC, ...
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Disease relevance of Arginyl-tyrosyl-leucyl-prolyl-threonyl

  • To study this issue in the crab Cancer borealis, we incubated exogenous proctolin (10(-5) M) with either the thoracic ganglion (TG) or with conditioned saline (CS) that had been preincubated with the TG [1].
  • In the hindleg extensor tibiae muscle of the locust, Schistocerca gregaria, the proctolin analogue [Afb (p-NO2)2]-proctolin is also able to potentiate neurally evoked contractions but is approximately 1,000-fold less effective in evoking contractures [2].
  • At the threshold concentration (1-10 pmol l(-1)), the neuropeptide hormones proctolin (PR) and the FLRFamide-like peptide (FLP) F(2) cause an increase in amplitude of electrically evoked contractions (each contraction is a brief tetanus) of lobster heart ostial muscle [3].

Psychiatry related information on Arginyl-tyrosyl-leucyl-prolyl-threonyl


High impact information on Arginyl-tyrosyl-leucyl-prolyl-threonyl

  • Thus, proctolin is a cardioactive peptide, a skeletal neuromuscular transmitter, a hindgut neuropeptide, a peptide of CNS interneurons (Keshishian & O'Shea 1984) and may have humoral roles [5].
  • Muscle contraction may be induced by a neuropeptide without depolarization of the muscle cells, for example see proctolin [5].
  • In competition-based studies, the CG6986 receptor binds proctolin with high affinity (IC(50) = 4 nM) [6].
  • Identification and characterization of a G protein-coupled receptor for the neuropeptide proctolin in Drosophilamelanogaster [6].
  • Proctolin is a bioactive neuropeptide that modulates interneuronal and neuromuscular synaptic transmission in a wide variety of arthropods [6].

Chemical compound and disease context of Arginyl-tyrosyl-leucyl-prolyl-threonyl

  • A comparison of the map for serotonin immunoreactivity with one generated for the pentapeptide transmitter proctolin suggests that the two systems overlap only in the suboesophageal ganglion and the tritocerebrum [7].
  • Both octopamine and proctolin have been found in Limulus cardiac ganglion [8].
  • In the isolated stomatogastric ganglion, red-pigment-concentrating hormone (RPCH), but not proctolin, activated the bursting activity in the inferior ventricular (IV) neurons that drives the cardiac sac pattern [9].
  • The results do not suggest that proctolin-like and dopamine-like immunoreactivity co-localize, but in the subesophageal ganglion there was a region of close proximity [10].
  • The enhancement of high K+-induced contractures by proctolin (1 micromol l-1) was mimicked upon application of the protein kinase C (PKC) activator phorbol-12-myristate 1-acetate (PMA) and was inhibited by the PKC inhibitor bisindolylmaleimide (BIM-1) [11].

Biological context of Arginyl-tyrosyl-leucyl-prolyl-threonyl


Anatomical context of Arginyl-tyrosyl-leucyl-prolyl-threonyl

  • Neuropeptide proctolin (H-Arg-Tyr-Leu-Pro-Thr-OH): immunological detection and neuronal localization in insect central nervous system [14].
  • Proctolin-like immunoreactivity is present in nearly every portion of the lobster nervous system; immunoreactivity is found in the brain, in each of the ganglia and connectives of the ventral nerve cord, and in many of the nerve roots that emerge from the cord [15].
  • Force measurements and current-clamp experiments revealed two actions of proctolin on the muscle fibers [12].
  • The neuropeptide proctolin acts as a neuromuscular co-transmitter in insect skeletal muscle [16].
  • The nerve endings in pericardial organs are capable of releasing proctolin-like material when depolarized in the presence of Ca++ [15].

Associations of Arginyl-tyrosyl-leucyl-prolyl-threonyl with other chemical compounds


Gene context of Arginyl-tyrosyl-leucyl-prolyl-threonyl


Analytical, diagnostic and therapeutic context of Arginyl-tyrosyl-leucyl-prolyl-threonyl


  1. Neuropeptide degradation produces functional inactivation in the crustacean nervous system. Coleman, M.J., Konstant, P.H., Rothman, B.S., Nusbaum, M.P. J. Neurosci. (1994) [Pubmed]
  2. Selective activity of a proctolin analogue reveals the existence of two receptor subtypes. Baines, R.A., Walther, C., Hinton, J.M., Osborne, R.H., Konopińska, D. J. Neurophysiol. (1996) [Pubmed]
  3. Sites and modes of action of proctolin and the FLP F2 on lobster cardiac muscle. Wilkens, J.L., Shinozaki, T., Yazawa, T., ter Keurs, H.E. J. Exp. Biol. (2005) [Pubmed]
  4. The insect neuropeptide proctolin can affect the CNS and the smooth=muscle of mammals. Schulz, H., Schwarzberg, H., Penzlin, H. Acta Biol. Med. Ger. (1981) [Pubmed]
  5. Neuropeptide function: the invertebrate contribution. O'Shea, M., Schaffer, M. Annu. Rev. Neurosci. (1985) [Pubmed]
  6. Identification and characterization of a G protein-coupled receptor for the neuropeptide proctolin in Drosophilamelanogaster. Johnson, E.C., Garczynski, S.F., Park, D., Crim, J.W., Nassel, D.R., Taghert, P.H. Proc. Natl. Acad. Sci. U.S.A. (2003) [Pubmed]
  7. Serotonin immunoreactive neurons in the central nervous system of an insect (Periplaneta americana). Bishop, C.A., O'Shea, M. J. Neurobiol. (1983) [Pubmed]
  8. Neuromuscular modulation in Limulus by both octopamine and proctolin. Rane, S.G., Gerlach, P.H., Wyse, G.A. J. Neurobiol. (1984) [Pubmed]
  9. Neurotransmitter interactions in the stomatogastric system of the spiny lobster: one peptide alters the response of a central pattern generator to a second peptide. Dickinson, P.S., Fairfield, W.P., Hetling, J.R., Hauptman, J. J. Neurophysiol. (1997) [Pubmed]
  10. Distribution of dopamine-like immunoreactivity suggests a role for dopamine in the courtship display behavior of the blue crab, Callinectes sapidus. Wood, D.E., Derby, C.D. Cell Tissue Res. (1996) [Pubmed]
  11. The neuropeptide proctolin potentiates contractions and reduces cGMP concentration via a PKC-dependent pathway. Philipp, B., Rogalla, N., Kreissl, S. J. Exp. Biol. (2006) [Pubmed]
  12. Effects of proctolin on contractions, membrane resistance, and non-voltage-dependent sarcolemmal ion channels in crustacean muscle fibers. Erxleben, C.F., deSantis, A., Rathmayer, W. J. Neurosci. (1995) [Pubmed]
  13. The acquisition and expression of a peptidergic phenotype in the grasshopper embryo. Keshishian, H., O'Shea, M. J. Neurosci. (1985) [Pubmed]
  14. Neuropeptide proctolin (H-Arg-Tyr-Leu-Pro-Thr-OH): immunological detection and neuronal localization in insect central nervous system. Bishop, C.A., O'Shea, M., Miller, R.J. Proc. Natl. Acad. Sci. U.S.A. (1981) [Pubmed]
  15. Proctolin in the lobster: the distribution, release, and chemical characterization of a likely neurohormone. Schwarz, T.L., Lee, G.M., Siwicki, K.K., Standaert, D.G., Kravitz, E.A. J. Neurosci. (1984) [Pubmed]
  16. Isolation and characterization of two myoactive neuropeptides: further evidence of an invertebrate peptide family. O'Shea, M., Witten, J., Schaffer, M. J. Neurosci. (1984) [Pubmed]
  17. Proctolin in identified serotonergic, dopaminergic, and cholinergic neurons in the lobster, Homarus americanus. Siwicki, K.K., Beltz, B.S., Kravitz, E.A. J. Neurosci. (1987) [Pubmed]
  18. Neuropeptide proctolin in postural motoneurons of the crayfish. Bishop, C.A., Wine, J.J., O'Shea, M. J. Neurosci. (1984) [Pubmed]
  19. Further observations on the behaviour of ouabain-insensitive sodium efflux towards proctolin in barnacle muscle fibres. Bittar, E.E., Nwoga, J. J. Physiol. (Lond.) (1989) [Pubmed]
  20. Gastric mill activity in the lobster. II. Proctolin and octopamine initiate and modulate chewing. Heinzel, H.G. J. Neurophysiol. (1988) [Pubmed]
  21. Vasopressin- and proctolin-like immunoreactive efferent neurons in blowfly abdominal ganglia: development and ultrastructure. Nässel, D.R., Holmqvist, B.I., Movérus, B.J. J. Comp. Neurol. (1989) [Pubmed]
  22. Immunohistochemical studies of the neurochemical markers, CGRP, enkephalin, galanin, gamma-MSH, NPY, PHI, proctolin, PTH, somatostatin, SP, VIP, tyrosine hydroxylase and neurofilament in nerves and cells of the human attached gingiva. Luthman, J., Johansson, O., Ahlström, U., Kvint, S. Arch. Oral Biol. (1988) [Pubmed]
  23. Characterization of a functionally expressed dipeptidyl aminopeptidase III from Drosophila melanogaster. Mazzocco, C., Fukasawa, K.M., Auguste, P., Puiroux, J. Eur. J. Biochem. (2003) [Pubmed]
  24. Purification, partial sequencing and characterization of an insect membrane dipeptidyl aminopeptidase that degrades the insect neuropeptide proctolin. Mazzocco, C., Fukasawa, K.M., Raymond, A.A., Puiroux, J. Eur. J. Biochem. (2001) [Pubmed]
  25. Distribution and action of some putative neurotransmitters in the stomatogastric nervous system of the earthworm, Eisenia fetida (Oligochaeta, Annelida). Barna, J., Csoknya, M., Lázár, Z., Barthó, L., Hámori, J., Elekes, K. J. Neurocytol. (2001) [Pubmed]
  26. Multiple peptide immunoreactivities in the nervous system of Aeschna cyanea (Insecta, Odonata). An immunohistochemical study using antisera to cholecystokinin octapeptide, somatoliberin, vasoactive intestinal peptide, motilin and proctolin. Andriès, J.C., Belemtougri, G., Tramu, G. Histochemistry (1991) [Pubmed]
  27. Neuropeptide proctolin associated with an identified skeletal motoneuron. O'Shea, M., Bishop, C.A. J. Neurosci. (1982) [Pubmed]
  28. The distribution of a peptide neurotransmitter in the postembryonic grasshopper central nervous system. Keshishian, H., O'Shea, M. J. Neurosci. (1985) [Pubmed]
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