Pharmacological characterization of the novel ACh releaser α-tropanyl 2-(4-bromophenyl)propionate (PG-9)

CNS Drug Reviews

Volumn 6, Issue 1, 2000, Pages 63-78

  Ghelardini, C ^a,b   Galeotti, N ^a   Romanelli, M N ^a   Gualtieri, F ^a   Bartolini, A ^a  

^a UNIVERSITY OF FLORENCE   (Italy)

^b Department of Pharmacology ^*  (Italy)

Author keywords

Acetylcholine release; Analgesia; Antinociception; Cholinergic system; Learning; Memory; Pain; PG 9

Indexed keywords

2 (4 BROMOPHENYL)PROPIONIC ACID 3ALPHA TROPYL ESTER; ALPHA TROPANYL 2 (4 BROMOPHENYL)PROPIONATE; ANTINOCICEPTIVE AGENT; ATROPINE; HEMICHOLINIUM 3; METHOCTRAMINE; NEOSTIGMINE; NERVE GROWTH FACTOR; OTENZEPAD; PHYSOSTIGMINE; PILOCARPINE; UNCLASSIFIED DRUG;

AMNESIA; ANALGESIA; ANIMAL BEHAVIOR; ANIMAL EXPERIMENT; ANIMAL TISSUE; ANTINOCICEPTION; CONTROLLED STUDY; DRUG ACTIVITY; DRUG MECHANISM; DRUG RESEARCH; DRUG STRUCTURE; DRUG SYNTHESIS; INTESTINE MOTILITY; MOUSE; NONHUMAN; RAT; REVIEW;

EID: 0034112604     PISSN: 1080563X     EISSN: None     Source Type: Journal    
DOI: 10.1111/j.1527-3458.2000.tb00138.x     Document Type: Review

References (76)

1. Abbs CT, Wall AH. The effect of local anaesthetics on neuromuscular transmission in the rat phrenic nerve-diaphragm preparation. In: Ganguly JK, ed. Comparative Effect of Local Anaesthetics. London: Pergamon Press, 1981:22-31.
2. Aura J, Sirviö J, Riekkinen P, Jr. Methoctramine moderately improves memory but pirenzepine disrupts performance in delayed non-matching to position test. Eur J Pharmacol 1997;333:129-134.
3. Bartolini A, Galli A, Ghelardini C, et al. Antinociception induced by systemic administration of local anaesthetics depends on a cholinergic mechanism. Br J Pharmacol 1987;92:711-721.
4. Bartolini A, Ghelardini C, Gualtieri F, et al. I.c.v. AFDX 116 induces analgesia only when administered at very low doses. Trends Pharmacol Sci 1989;Suppl IV:99.
5. Bartolini A, Ghelardini C, Fantetti L, et al. Role of muscarinic receptor subtypes in central antinociception. Br J Pharmacol 1992;105:77-82.
6. Bartolini A, Ghelardini C, Galeotti N, Beneforti E, Zoppi M. Pharmacology of experimental analgesic drugs. Pain, Rheumatic Diseases and Quality of Life. October 1997. Florence, Italy; p. 48.
7. 3 agonists decrease acetylcholine efflux from the cerebral cortex of freely-moving guinea-pigs. Br J Pharmacol 1990;101:448-452.
8. Brown JH, Taylor P. Muscarinic receptor agonists and antagonists. In: Hardman JG, Limbird LE, eds. Goodman & Gilman's The Pharmacological Basis of Therapeutics. New York, NY: McGraw-Hill, 1996:141-160.
9. Bülbring E. Observations on the isolated phrenic nerve diaphragm preparation on the rat. Br J Pharmacol 1946;1:38-61.
10. 1 receptors. J Pharmacol Exp Ther 1995;273:637-642.
11. Chen C, Okayama H. High-efficiency transformation of mammalian cells by plasmid DNA. Mol Cell Biol 1987;7:2745-2752.
12. Chernov HI, Wilson DE, Fowler F, Plummer AJ. Non-specificity of the mouse writhing test. Arch Int Pharmacodyn 1967;167:171-178.
13. 3 receptor subtypes. Br J Pharmacol 1992;107:919-923.
14. 4 receptor stimulation facilitates acetylcholine release in frontal cortex. Neuroreport 1994;5:1230-1232.
15. Coyle JM. A cholinergic hypothesis for Alzheimer's disease. In: Meyer L, Nordeberg GH, eds. Learning and Memory Molecular Bases. London: Pergamon Press, 1995:1-32.
16. D'Amour FE, Smith DL. A method for determining loss of pain sensation. J Pharmacol Exp Ther 1941;72:74-79.
17. Dei S, Bellucci C, Gualtieri F, et al. Analgesic, antimuscarinic activity and enantioselectivity of the four isomers of 3-quiniclidinyl tropate as compared with the enantiomers of hyoscyamine. Il Farmaco 1995;50:303-309.
18. Doods H, Entzeroth M, Mayer N. Cardioselectivity of AQ-RA 741, a novel tricyclic antimuscarinic drug. Eur J Pharmacol 1991;192:147-152.
19. Dörje F, Friebe T, Tacke R, Mutschler E, Lambrecht G. Novel pharmacological profile of muscarinic receptors mediating contraction of the guinea-pig uterus. Naunyn Schmiedeberg's Arch Pharmacol 1990;342:284-289.
20. Dörje F, Wess J, Lambrecht G, Tacke R, Mutschler E, Brann MR. Antagonist binding profile of five cloned human muscarinic receptor subtypes. J Pharmacol Exp Ther 1991;256:727-733.
21. Eltze M, Gonne S, Riedel R, Schlotke B, Schudt C, Simon WA. Pharmacological evidence for selective inhibition of gastric acid secretion by telenzepine, a new antimuscarinic drug. Eur J Pharmacol 1985;112:211-224.
22. Eltze M, Figala V. Affinity and selectivity of biperiden enantiomers for muscarinic receptor subtypes. Eur J Pharmacol 1988;158:11-19.
23. 2 receptors mediating opposite effects on neuromuscular transmission in rabbit vas deferens. Eur J Pharmacol 1988;151:205-221.
24. Galeotti N, Ghelardini C, Bartolini A. Effect of pertussis toxin on morphine, diphenhydramine, baclofen, clomipramine and physostigmine antinociception. Eur J Pharmacol 1996;308(2):125-133.
25. 1A agonists induce central cholinergic antinociception. Pharmacol Biochem Behav 1997;57(4):835-841.
26. George R, Haslett WL, Jenden DJ. The central action of a metabolite of tremorine. Life Sci 1962;1:361-363.
27. Ghelardini C, Malmberg-Aiello P, Giotti A, Malcangio M, Bartolini A. Investigation into atropine-induced antinociception. Br J Pharmacol 1990;101:49-54.
28. 2 antagonist AQRA-741. 8th Camerino-Noordwijkerhout Symposium on "Trends in Receptors Research," September 1991. Camerino, Italy; Abstr P40, p. 160.
29. Ghelardini C, Giotti A, Gualtieri F, et al. Presynaptic auto- and heteroreceptors in the cholinergic regulation of pain. In: Angeli P, Gulini U, Quaglia W, eds. Trends in Receptor Research. Amsterdam: Elsevier Science Publisher BV, 1992:95-114.
30. Ghelardini C, Gualtieri F, Baldini M, et al. R-(+)-hyoscyamine: The first and selective antagonist for guinea-pig uterus muscarinic receptor subtype. Life Sci 1993;52:569.
31. 1A agonist 8-OH-DPAT induces antinociception through a cholinergic mechanism. Can J Physiol Pharmacol 1994;(Suppl IUPHAR):380.
32. 4 agonists: BIMU 1 and BIMU 8. Life Sci 1996;58:2297-2309.
33. Ghelardini C, Galeotti N, Gualtieri F, et al. R-(+)-hyoscyamine: A peripheral cholinergic amplifier. Phototherapy Res 1996;10:S62-S64.
34. Ghelardini C, Galeotti N, Bartolini A. Caffeine induces central cholinergic analgesia. Naunyn Schmiedeberg's Arch Pharmacol 1997;356:590-595.
35. Ghelardini C, Gualtieri F, Romanelli MN, et al. Stereoselective increase in cholinergic transmission by R-(+)-hyoscyamine. Neuropharmacology 1997;36:281-294.
36. Ghelardini C, Galeotti N, Bartolini A. Memory facilitation and stimulation of endogenous nerve growth factor synthesis by the ACh releaser PG-9. Jpn J Pharmacol 1998;73:245-251.
37. Ghelardini C, Galeotti N, Gualtieri F, et al. Antinociceptive and antiamnesic properties of the presynaptic cholinergic amplifier PG-9. J Pharmacol Exp Ther 1998;284:806-816.
38. 2 receptor antagonist. Life Sci 1986;38:1663-1672.
39. Giovannini MG, Casamenti F, Nistri A, Paoli F, Pepeu G. Effect of thyrotropin releasing hormone (TRH) on acetylcholine release from different brain areas investigated by microdialysis. Br J Pharmacol 1991;102:363-368.
40. Gorell JM, Czarnecki B. Pharmacological evidence for direct dopaminergic regulation of striatal acetylcholine release. Life Sci 1986;38:2239-2246.
41. Gouliaev AH, Senning A. Piracetam and other structurally related nootropics. Brain Res Rev 1994;19:180-222.
42. 2 antagonist methoctramine administered i.c.v. Trends Pharmacol Sci 1989;(Suppl IV):99.
43. Gualtieri F, Romanelli MN, Scapecchi S, et al. Muscarinic presynaptic autoreceptors and muscarinic postsynaptic receptors have opposite stereochemical requirements. Med Chem Res 1991;1:52-58.
44. Gualtieri F, Bottalico C, Calandrella A, et al. Presynaptic cholinergic modulators as potent cognition enhancers and analgesic drugs. II. 2-Phenoxy-, 2-(phenylthio)- and 2-(phenylamino) alkanoic acid esters. J Med Chem 1994;37:1712-1719.
45. Gualtieri F, Conti G, Dei S, et al. Presynaptic cholinergic modulators as potent cognition enhancer and analgesic drugs. Tropic and 2-phenylpropionic acid ester. J Med Chem 1994;37(11):1704-1711.
46. Haley TJ, McCormick WG. Pharmacological effects produced by intracerebral injection of drugs in the conscious mouse. Br J Pharmacol Chemother 1957;12:12-15.
47. Harris LS, Dewey WL, Howes JF, Kennedy JS, Pars H. Narcotic antagonists analgesics: Interaction with cholinergic system. J Pharmacol Exp Ther 1969;169:17-22.
48. Hendershot LC, Forsaith J. Antagonism of the frequency of phenylquinone-induced writhing in the mouse by weak analgesics and nonanalgesics. J Pharmacol Exp Ther 1959;125:237-240.
49. Herz A. Wirkungen des Arecolins auf das Zentralnervensystem. Arch Exp Path Pharmacokin 1962;242:414-429.
50. Hoehn K, Reid A, Sawynok J. Pertussis toxin inhibits antinociception produced by intrathecal injection of morphine, noradrenaline and baclofen. Eur J Pharmacol 1988;146:65-72.
51. 1 receptors. J Pharmacol Exp Ther 1993;266:557-562.
52. Jackisch R, Strittmatter H, Kasakov I, Hertting G. Endogenous adenosine as a modulator of hippocampal acetylcholine release. Naunyn Schmiedeberg's Arch Pharmacol 1984;327:319-325.
53. Koster R, Anderson M, De Beer EJ. Acetic acid for analgesic screening. Fed Proc 1959;18:412.
54. Kuribara H, Higuchi Y, Takadoro S. Effects of central depressants on rota-rod and traction performances in mice. Jpn J Pharmacol 1977;27:117-126.
55. 3H]AF-DX 116 and effect of AF-DX 116 on endogenous acetylcholine release from brain slices. Brain Res 1989;496:285-294.
56. Leighton GE, Rodriguez RE, Hill RG, Hughes J. K-Opioid agonists produce antinociception after i.v. and i.c.v. but not intrathecal administration in the rat. Br J Pharmacol 1988;93:553-560.
57. Lentz TL, Liley L, Michaelson U. Some actions of anticholinergic drugs. Br J Pharmacol 1969;32:156-162.
58. Malmberg-Aiello P, Lamberti C, Ghelardini C, Giotti A, Bartolini A. Role of histamine in rodent antinociception. Br J Pharmacol 1994;111:1269-1279.
59. McKinney M, Miller JH, Aagaard PJ. Pharmacological characterization of the rat hippocampal muscarinic autoreceptor. J Pharmacol Exp Ther 1993;264:74-78.
60. 2 muscarinic receptors. J Med Chem 1987;30:201-204.
61. B receptor blocker improves the cognitive performance of mice, rats and rhesus monkeys. Pharmacol Comm 1992;2:93-97.
62. O'Callaghan JP, Holtzman SG. Quantification of the analgesic activity of narcotic antagonists by a modified hot-plate procedure. J Pharmacol Exp Ther 1975;192:497-505.
63. Parenti M, Tirone F, Giagnoni G, Pecora N, Parolaro D. Pertussis toxin inhibits the antinociceptive action of morphine in the rat. Eur J Pharmacol 1986;124:357-359.
64. Paton WDM, Vizi ES. The inhibitory action of noradrenaline and acetylcholine output by guinea-pig longitudinal muscle strip. Br J Pharmacol 1969;35:10-28.
65. Pedigo NW, Dewey WL, Harris LS. Determination and characterization of the antinociceptive activity of intracerebroventricularly administered acetylcholine. J Pharmacol Exp Ther 1975;193:845-852.
66. Prado WA, Corrado AP. Cholinergic agonist and antagonist interactions on motor nerve endings of the rat -evidence for the involvement of presynaptic receptors in the regulation of acetylcholine release. Gen Pharmacol 1987;18:75-81.
67. Reynell PC, Spray GH. The simultaneous measurement of absorption and transit in the gastrointestinal tract of the rat. J Physiol 1956;131:452-462.
68. Romanelli MN, Bartolini A, Bertucci C, et al. Synthesis and enantioselectivity of the enantiomers of PG9 and SM21, new potent analgesic and cognition-enhancing drugs. Chirality 1996;8:225-233.
69. Sawynok J, Reid A. Role of G-proteins and adenylate cyclase in antinociception produced by intrathecal purines. Eur J Pharmacol 1988;156:25-34.
70. 1 dopamine receptors in dopaminergic control of striatal cholinergic transmission. Life Sci 1992;31:2883-2890.
71. Stillman MJ, Shukitt-Hale B, Kong RM, Levy A, Lieberman HR. Elevation of hippocampal extracellular acetylcholine levels by methoctramine. Brain Res Bull 1993;32:385-389.
72. Summers RW, Kent TH, Osborne JW. Effects of drugs, ileal obstruction, and irradiation on rat gastrointestinal propulsion. Gastroenterology 1970;59:731-739.
73. Tōrōcsik A, Vizi ES. Presynaptic effects of methoctramine on release of acetylcholine. Neuropharmacology 1991;30:293-298.
74. 2-receptors. Naunyn Schmiedeberg's Arch Pharmacol 1988;338:250-255.
75. 3H]-acetylcholine from a modified rat phrenic nerve - hemidiaphragm preparation. Naunyn Schmiedeberg's Arch Pharmacol 1986;334:357-364.
76. Wessler I, Diener A, Hoffermann M. Facilitatory and inhibitory muscarinic receptors on the rat phrenic nerve: Effects of pirenzepine and dicyclomine. Naunyn Schmiedeberg's Arch Pharmacol 1988;338:138-142.