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Alessandro Bartolini - One of the best experts on this subject based on the ideXlab platform.

  • antiamnesic effect of the two novel κ opioid agonists va 100 and va 101 in the mouse Passive Avoidance Test
    Drug Development Research, 2001
    Co-Authors: Carla Ghelardini, Nicoletta Galeotti, Lorenzo Di Cesare Mannelli, Andrea Cappelli, Maurizio Anzini, Alessandro Bartolini
    Abstract:

    The effects of the administration of the two novel κ-opioid agonists (VA-100, VA-101) on memory processes were evaluated with the mouse Passive Avoidance Test. The administration of VA-100 (50–100 mg kg–1 p.o.) and VA-101 (100 mg kg–1 p.o.) administered 20 min before the training session prevented nor-binaltorphimine (4.9 μg per mouse i.c.v.), scopolamine (1.5 mg kg–1 i.p.), mecamylamine (20 mg kg–1 i.p.), diphenhydramine (20 mg kg–1 i.p.), and baclofen (2 mg kg–1 i.p.) amnesia. At the highest effective doses, none of the drugs impaired motor coordination, as revealed by the rota-rod Test, nor modified spontaneous motility and inspection activity, as revealed by the hole board Test. The antiamnesic effect induced by VA-100 and VA-101 was comparable to that exerted by the κ-opioid agonist U-50,488H, as well as that induced by the nootropic drug piracetam and the cholinesterase inhibitor physostigmine. These results suggest that the activation of κ-opioid receptors plays an important role in the prevention of memory impairment. On these bases, κ-opioid receptor agonists could represent a useful symptomatic treatment for cognitive deficits. Drug Dev. Res. 54:12–18, 2001. © 2001 Wiley-Liss, Inc.

  • Antiamnesic effect of the two novel κ‐opioid agonists, VA‐100 and VA‐101, in the mouse Passive Avoidance Test
    Drug Development Research, 2001
    Co-Authors: Carla Ghelardini, Nicoletta Galeotti, Lorenzo Di Cesare Mannelli, Andrea Cappelli, Maurizio Anzini, Alessandro Bartolini
    Abstract:

    The effects of the administration of the two novel κ-opioid agonists (VA-100, VA-101) on memory processes were evaluated with the mouse Passive Avoidance Test. The administration of VA-100 (50–100 mg kg–1 p.o.) and VA-101 (100 mg kg–1 p.o.) administered 20 min before the training session prevented nor-binaltorphimine (4.9 μg per mouse i.c.v.), scopolamine (1.5 mg kg–1 i.p.), mecamylamine (20 mg kg–1 i.p.), diphenhydramine (20 mg kg–1 i.p.), and baclofen (2 mg kg–1 i.p.) amnesia. At the highest effective doses, none of the drugs impaired motor coordination, as revealed by the rota-rod Test, nor modified spontaneous motility and inspection activity, as revealed by the hole board Test. The antiamnesic effect induced by VA-100 and VA-101 was comparable to that exerted by the κ-opioid agonist U-50,488H, as well as that induced by the nootropic drug piracetam and the cholinesterase inhibitor physostigmine. These results suggest that the activation of κ-opioid receptors plays an important role in the prevention of memory impairment. On these bases, κ-opioid receptor agonists could represent a useful symptomatic treatment for cognitive deficits. Drug Dev. Res. 54:12–18, 2001. © 2001 Wiley-Liss, Inc.

  • Antiamnesic effect of metoprine and of selective histamine H1 receptor agonists in a modified mouse Passive Avoidance Test
    Neuroscience Letters, 2000
    Co-Authors: Petra Malmberg-aiello, Alessandro Bartolini, Alessandra Ipponi, Walter Schunack
    Abstract:

    The aim of this study was to elucidate the effect caused by the inhibition of histamine catabolism by means of metoprine and the activation of histamine H(1) receptors by selective agonists on learning and memory processes, using a modified method of the mouse Passive Avoidance Test. The administration of scopolamine 1 mg/kg (i. p.) immediately after the training session caused statistically-significant amnesia during the retention trial performed 24 h later. Piracetam (30 mg/kg (i.p.)), used as a positive control, and administered 20 min before the training session, prevented scopolamine-induced memory impairment. The histamine-N-methyltransferase inhibitor, metoprine, (2 and 5 mg/kg (s.c.)) had effects similar to those of this nootropic drug. The highly-selective H(1) receptor agonist, 2-(3-trifluoromethylphenyl)histamine (FMPH) (2.65 and 6.5 microg/mouse (i.c.v.)) and the less selective agonist, 2-thiazolylethylamine (2-TEA) (0.1 and 0.3 microg/mouse (i.c.v.)) both antagonized the scopolamine-induced amnesia significantly and in a dose-related manner. The selective H(1) receptor antagonist, pyrilamine (20 mg/kg (i.p.)), revealed no effect by itself, but significantly prevented the antiamnesic action both that of the H(1) receptor agonists, and that of endogenous histamine, released by metoprine, thus suggesting a cognitive improvement via the activation of H(1) receptors.

  • Improvement of cognitive functions by the acetylcholine releaser SM 21
    Drug Development Research, 1999
    Co-Authors: Carla Ghelardini, Nicoletta Galeotti, Fulvio Gualtieri, Serena Scapecchi, Alessandro Bartolini
    Abstract:

    The effect of administration of SM 21 on memory processes was evaluated in the mouse Passive Avoidance and in the rat social learning Tests. SM 21 (10–20 mg kg−1 i.p.) prevented amnesia induced by scopolamine and dicyclomine as Tested by the mouse Passive Avoidance Test and prevented memory disruption by AF-64A and benehexol ascertained by the rat Passive Avoidance Test. Both SM 21 enantiomers were able to abolish dicyclomine-induced amnesia in mice. SM 21, starting from the dose of 10 mg kg−1 i.p., antagonized the memory impairment produced by mecamylamine, baclofen, and diphenhydramine in mice, as well as amnesia induced by diazepam in rats. SM 21, at doses ranging between 10 and 30 mg kg−1 i.p., prevented memory reduction in mice by hypoxia in the Passive Avoidance Test. In the social learning Test, SM 21 (10 mg kg−1 i.p.) injected in adult rats reduced the duration of active exploration of a familiar partner in the second session of the Test. SM 21 prevented amnesia in both mice and rats comparable to that of the cholinesterase inhibitor physostigmine (0.2 mg kg−1 i.p.), the M1 selective agonist AF-102B (10 mg kg−1 i.p.), and the nootropic drug piracetam (30 mg kg−1 i.p.). These results demonstrated the ability of SM 21 to modulate memory functions and suggests that SM 21 could be useful in the treatment of cognitive deficits. Drug Dev. Res. 47:118–126, 1999. © 1999 Wiley-Liss, Inc.

  • Role of 5-HT4 Receptors in the Mouse Passive Avoidance Test
    Journal of Pharmacology and Experimental Therapeutics, 1998
    Co-Authors: Nicoletta Galeotti, Carla Ghelardini, Alessandro Bartolini
    Abstract:

    The effects of the administration of different 5-HT4receptor antagonists (SDZ 205557, GR 125487) and 5-HT4receptor agonists (BIMU 1, BIMU 8) on memory processes were evaluated in the mouse Passive Avoidance Test. The administration of SDZ 205557 (10 mg kg−1 i.p.) and GR 125487 (10 mg kg−1i.p.) immediately after termination of the training session produced an amnesic effect. BIMU 1 (20 mg kg−1 i.p.) and BIMU 8 (30 mg kg−1 i.p.), administered 20 min before the training session, prevented the 5-HT4 receptor antagonist-induced amnesia. In the same experimental conditions BIMU 1 (10 mg kg−1 i.p.; 25 μg/mouse intracerebroventricularly) and BIMU 8 (30 mg kg−1 i.p.; 30 μg per mouse intracerebroventricularly) prevented scopolamine (1 mg kg−1 i.p.) and dicyclomine (2 mg kg−1 i.p.) amnesia and, at the dose of 10 and 30 mg kg−1 i.p. respectively, prevented amnesia induced by exposure to a hypoxic environment. At the highest effective doses, none of the drugs impaired motor coordination, as revealed by the rota rod Test, or modified spontaneous motility and inspection activity, as revealed by the hole board and Animex Tests. The 5-HT3 antagonist ondansetron (0.1–1 mg kg−1 i.p.) was unable to prevent scopolamine-, 5-HT4 antagonist- and hypoxia-induced amnesia. These results suggest that the modulation of 5-HT4 receptors plays an important role in the regulation of memory processes. On these bases, the 5-HT4 receptor agonists could be useful in the treatment of cognitive deficits although 5-HT4 receptor antagonists may represent pharmacological tools for investigation of new potential antiamnesic drugs.

Carla Ghelardini - One of the best experts on this subject based on the ideXlab platform.

  • Design, synthesis and nootropic activity of new analogues of sunifiram and sapunifiram, two potent cognition-enhancers.
    Bioorganic & Medicinal Chemistry, 2009
    Co-Authors: Elisabetta Martini, Carla Ghelardini, Alberto Salvicchi, Dina Manetti, Silvia Dei, Luca Guandalini, Cecilia Martelli, Michele Melchiorre, Cristina Cellai, Serena Scapecchi
    Abstract:

    A series of amides and sulfonamides, structurally related to DM235 (sunifiram) and MN19 (sapunifiram), derived by ring expansion or contraction, or by inversion of the exocyclic amide function, have been synthesized and Tested for cognition-enhancing activity in the mouse Passive-Avoidance Test. Some of the compounds display good antiamnesic and procognitive activity, with higher potency than piracetam, and with a potency similar to the parent compounds.

  • antiamnesic effect of the two novel κ opioid agonists va 100 and va 101 in the mouse Passive Avoidance Test
    Drug Development Research, 2001
    Co-Authors: Carla Ghelardini, Nicoletta Galeotti, Lorenzo Di Cesare Mannelli, Andrea Cappelli, Maurizio Anzini, Alessandro Bartolini
    Abstract:

    The effects of the administration of the two novel κ-opioid agonists (VA-100, VA-101) on memory processes were evaluated with the mouse Passive Avoidance Test. The administration of VA-100 (50–100 mg kg–1 p.o.) and VA-101 (100 mg kg–1 p.o.) administered 20 min before the training session prevented nor-binaltorphimine (4.9 μg per mouse i.c.v.), scopolamine (1.5 mg kg–1 i.p.), mecamylamine (20 mg kg–1 i.p.), diphenhydramine (20 mg kg–1 i.p.), and baclofen (2 mg kg–1 i.p.) amnesia. At the highest effective doses, none of the drugs impaired motor coordination, as revealed by the rota-rod Test, nor modified spontaneous motility and inspection activity, as revealed by the hole board Test. The antiamnesic effect induced by VA-100 and VA-101 was comparable to that exerted by the κ-opioid agonist U-50,488H, as well as that induced by the nootropic drug piracetam and the cholinesterase inhibitor physostigmine. These results suggest that the activation of κ-opioid receptors plays an important role in the prevention of memory impairment. On these bases, κ-opioid receptor agonists could represent a useful symptomatic treatment for cognitive deficits. Drug Dev. Res. 54:12–18, 2001. © 2001 Wiley-Liss, Inc.

  • Antiamnesic effect of the two novel κ‐opioid agonists, VA‐100 and VA‐101, in the mouse Passive Avoidance Test
    Drug Development Research, 2001
    Co-Authors: Carla Ghelardini, Nicoletta Galeotti, Lorenzo Di Cesare Mannelli, Andrea Cappelli, Maurizio Anzini, Alessandro Bartolini
    Abstract:

    The effects of the administration of the two novel κ-opioid agonists (VA-100, VA-101) on memory processes were evaluated with the mouse Passive Avoidance Test. The administration of VA-100 (50–100 mg kg–1 p.o.) and VA-101 (100 mg kg–1 p.o.) administered 20 min before the training session prevented nor-binaltorphimine (4.9 μg per mouse i.c.v.), scopolamine (1.5 mg kg–1 i.p.), mecamylamine (20 mg kg–1 i.p.), diphenhydramine (20 mg kg–1 i.p.), and baclofen (2 mg kg–1 i.p.) amnesia. At the highest effective doses, none of the drugs impaired motor coordination, as revealed by the rota-rod Test, nor modified spontaneous motility and inspection activity, as revealed by the hole board Test. The antiamnesic effect induced by VA-100 and VA-101 was comparable to that exerted by the κ-opioid agonist U-50,488H, as well as that induced by the nootropic drug piracetam and the cholinesterase inhibitor physostigmine. These results suggest that the activation of κ-opioid receptors plays an important role in the prevention of memory impairment. On these bases, κ-opioid receptor agonists could represent a useful symptomatic treatment for cognitive deficits. Drug Dev. Res. 54:12–18, 2001. © 2001 Wiley-Liss, Inc.

  • Improvement of cognitive functions by the acetylcholine releaser SM 21
    Drug Development Research, 1999
    Co-Authors: Carla Ghelardini, Nicoletta Galeotti, Fulvio Gualtieri, Serena Scapecchi, Alessandro Bartolini
    Abstract:

    The effect of administration of SM 21 on memory processes was evaluated in the mouse Passive Avoidance and in the rat social learning Tests. SM 21 (10–20 mg kg−1 i.p.) prevented amnesia induced by scopolamine and dicyclomine as Tested by the mouse Passive Avoidance Test and prevented memory disruption by AF-64A and benehexol ascertained by the rat Passive Avoidance Test. Both SM 21 enantiomers were able to abolish dicyclomine-induced amnesia in mice. SM 21, starting from the dose of 10 mg kg−1 i.p., antagonized the memory impairment produced by mecamylamine, baclofen, and diphenhydramine in mice, as well as amnesia induced by diazepam in rats. SM 21, at doses ranging between 10 and 30 mg kg−1 i.p., prevented memory reduction in mice by hypoxia in the Passive Avoidance Test. In the social learning Test, SM 21 (10 mg kg−1 i.p.) injected in adult rats reduced the duration of active exploration of a familiar partner in the second session of the Test. SM 21 prevented amnesia in both mice and rats comparable to that of the cholinesterase inhibitor physostigmine (0.2 mg kg−1 i.p.), the M1 selective agonist AF-102B (10 mg kg−1 i.p.), and the nootropic drug piracetam (30 mg kg−1 i.p.). These results demonstrated the ability of SM 21 to modulate memory functions and suggests that SM 21 could be useful in the treatment of cognitive deficits. Drug Dev. Res. 47:118–126, 1999. © 1999 Wiley-Liss, Inc.

  • Role of 5-HT4 Receptors in the Mouse Passive Avoidance Test
    Journal of Pharmacology and Experimental Therapeutics, 1998
    Co-Authors: Nicoletta Galeotti, Carla Ghelardini, Alessandro Bartolini
    Abstract:

    The effects of the administration of different 5-HT4receptor antagonists (SDZ 205557, GR 125487) and 5-HT4receptor agonists (BIMU 1, BIMU 8) on memory processes were evaluated in the mouse Passive Avoidance Test. The administration of SDZ 205557 (10 mg kg−1 i.p.) and GR 125487 (10 mg kg−1i.p.) immediately after termination of the training session produced an amnesic effect. BIMU 1 (20 mg kg−1 i.p.) and BIMU 8 (30 mg kg−1 i.p.), administered 20 min before the training session, prevented the 5-HT4 receptor antagonist-induced amnesia. In the same experimental conditions BIMU 1 (10 mg kg−1 i.p.; 25 μg/mouse intracerebroventricularly) and BIMU 8 (30 mg kg−1 i.p.; 30 μg per mouse intracerebroventricularly) prevented scopolamine (1 mg kg−1 i.p.) and dicyclomine (2 mg kg−1 i.p.) amnesia and, at the dose of 10 and 30 mg kg−1 i.p. respectively, prevented amnesia induced by exposure to a hypoxic environment. At the highest effective doses, none of the drugs impaired motor coordination, as revealed by the rota rod Test, or modified spontaneous motility and inspection activity, as revealed by the hole board and Animex Tests. The 5-HT3 antagonist ondansetron (0.1–1 mg kg−1 i.p.) was unable to prevent scopolamine-, 5-HT4 antagonist- and hypoxia-induced amnesia. These results suggest that the modulation of 5-HT4 receptors plays an important role in the regulation of memory processes. On these bases, the 5-HT4 receptor agonists could be useful in the treatment of cognitive deficits although 5-HT4 receptor antagonists may represent pharmacological tools for investigation of new potential antiamnesic drugs.

Lorenzo Di Cesare Mannelli - One of the best experts on this subject based on the ideXlab platform.

  • antiamnesic effect of the two novel κ opioid agonists va 100 and va 101 in the mouse Passive Avoidance Test
    Drug Development Research, 2001
    Co-Authors: Carla Ghelardini, Nicoletta Galeotti, Lorenzo Di Cesare Mannelli, Andrea Cappelli, Maurizio Anzini, Alessandro Bartolini
    Abstract:

    The effects of the administration of the two novel κ-opioid agonists (VA-100, VA-101) on memory processes were evaluated with the mouse Passive Avoidance Test. The administration of VA-100 (50–100 mg kg–1 p.o.) and VA-101 (100 mg kg–1 p.o.) administered 20 min before the training session prevented nor-binaltorphimine (4.9 μg per mouse i.c.v.), scopolamine (1.5 mg kg–1 i.p.), mecamylamine (20 mg kg–1 i.p.), diphenhydramine (20 mg kg–1 i.p.), and baclofen (2 mg kg–1 i.p.) amnesia. At the highest effective doses, none of the drugs impaired motor coordination, as revealed by the rota-rod Test, nor modified spontaneous motility and inspection activity, as revealed by the hole board Test. The antiamnesic effect induced by VA-100 and VA-101 was comparable to that exerted by the κ-opioid agonist U-50,488H, as well as that induced by the nootropic drug piracetam and the cholinesterase inhibitor physostigmine. These results suggest that the activation of κ-opioid receptors plays an important role in the prevention of memory impairment. On these bases, κ-opioid receptor agonists could represent a useful symptomatic treatment for cognitive deficits. Drug Dev. Res. 54:12–18, 2001. © 2001 Wiley-Liss, Inc.

  • Antiamnesic effect of the two novel κ‐opioid agonists, VA‐100 and VA‐101, in the mouse Passive Avoidance Test
    Drug Development Research, 2001
    Co-Authors: Carla Ghelardini, Nicoletta Galeotti, Lorenzo Di Cesare Mannelli, Andrea Cappelli, Maurizio Anzini, Alessandro Bartolini
    Abstract:

    The effects of the administration of the two novel κ-opioid agonists (VA-100, VA-101) on memory processes were evaluated with the mouse Passive Avoidance Test. The administration of VA-100 (50–100 mg kg–1 p.o.) and VA-101 (100 mg kg–1 p.o.) administered 20 min before the training session prevented nor-binaltorphimine (4.9 μg per mouse i.c.v.), scopolamine (1.5 mg kg–1 i.p.), mecamylamine (20 mg kg–1 i.p.), diphenhydramine (20 mg kg–1 i.p.), and baclofen (2 mg kg–1 i.p.) amnesia. At the highest effective doses, none of the drugs impaired motor coordination, as revealed by the rota-rod Test, nor modified spontaneous motility and inspection activity, as revealed by the hole board Test. The antiamnesic effect induced by VA-100 and VA-101 was comparable to that exerted by the κ-opioid agonist U-50,488H, as well as that induced by the nootropic drug piracetam and the cholinesterase inhibitor physostigmine. These results suggest that the activation of κ-opioid receptors plays an important role in the prevention of memory impairment. On these bases, κ-opioid receptor agonists could represent a useful symptomatic treatment for cognitive deficits. Drug Dev. Res. 54:12–18, 2001. © 2001 Wiley-Liss, Inc.

Maurizio Anzini - One of the best experts on this subject based on the ideXlab platform.

  • antiamnesic effect of the two novel κ opioid agonists va 100 and va 101 in the mouse Passive Avoidance Test
    Drug Development Research, 2001
    Co-Authors: Carla Ghelardini, Nicoletta Galeotti, Lorenzo Di Cesare Mannelli, Andrea Cappelli, Maurizio Anzini, Alessandro Bartolini
    Abstract:

    The effects of the administration of the two novel κ-opioid agonists (VA-100, VA-101) on memory processes were evaluated with the mouse Passive Avoidance Test. The administration of VA-100 (50–100 mg kg–1 p.o.) and VA-101 (100 mg kg–1 p.o.) administered 20 min before the training session prevented nor-binaltorphimine (4.9 μg per mouse i.c.v.), scopolamine (1.5 mg kg–1 i.p.), mecamylamine (20 mg kg–1 i.p.), diphenhydramine (20 mg kg–1 i.p.), and baclofen (2 mg kg–1 i.p.) amnesia. At the highest effective doses, none of the drugs impaired motor coordination, as revealed by the rota-rod Test, nor modified spontaneous motility and inspection activity, as revealed by the hole board Test. The antiamnesic effect induced by VA-100 and VA-101 was comparable to that exerted by the κ-opioid agonist U-50,488H, as well as that induced by the nootropic drug piracetam and the cholinesterase inhibitor physostigmine. These results suggest that the activation of κ-opioid receptors plays an important role in the prevention of memory impairment. On these bases, κ-opioid receptor agonists could represent a useful symptomatic treatment for cognitive deficits. Drug Dev. Res. 54:12–18, 2001. © 2001 Wiley-Liss, Inc.

  • Antiamnesic effect of the two novel κ‐opioid agonists, VA‐100 and VA‐101, in the mouse Passive Avoidance Test
    Drug Development Research, 2001
    Co-Authors: Carla Ghelardini, Nicoletta Galeotti, Lorenzo Di Cesare Mannelli, Andrea Cappelli, Maurizio Anzini, Alessandro Bartolini
    Abstract:

    The effects of the administration of the two novel κ-opioid agonists (VA-100, VA-101) on memory processes were evaluated with the mouse Passive Avoidance Test. The administration of VA-100 (50–100 mg kg–1 p.o.) and VA-101 (100 mg kg–1 p.o.) administered 20 min before the training session prevented nor-binaltorphimine (4.9 μg per mouse i.c.v.), scopolamine (1.5 mg kg–1 i.p.), mecamylamine (20 mg kg–1 i.p.), diphenhydramine (20 mg kg–1 i.p.), and baclofen (2 mg kg–1 i.p.) amnesia. At the highest effective doses, none of the drugs impaired motor coordination, as revealed by the rota-rod Test, nor modified spontaneous motility and inspection activity, as revealed by the hole board Test. The antiamnesic effect induced by VA-100 and VA-101 was comparable to that exerted by the κ-opioid agonist U-50,488H, as well as that induced by the nootropic drug piracetam and the cholinesterase inhibitor physostigmine. These results suggest that the activation of κ-opioid receptors plays an important role in the prevention of memory impairment. On these bases, κ-opioid receptor agonists could represent a useful symptomatic treatment for cognitive deficits. Drug Dev. Res. 54:12–18, 2001. © 2001 Wiley-Liss, Inc.

Andrea Cappelli - One of the best experts on this subject based on the ideXlab platform.

  • antiamnesic effect of the two novel κ opioid agonists va 100 and va 101 in the mouse Passive Avoidance Test
    Drug Development Research, 2001
    Co-Authors: Carla Ghelardini, Nicoletta Galeotti, Lorenzo Di Cesare Mannelli, Andrea Cappelli, Maurizio Anzini, Alessandro Bartolini
    Abstract:

    The effects of the administration of the two novel κ-opioid agonists (VA-100, VA-101) on memory processes were evaluated with the mouse Passive Avoidance Test. The administration of VA-100 (50–100 mg kg–1 p.o.) and VA-101 (100 mg kg–1 p.o.) administered 20 min before the training session prevented nor-binaltorphimine (4.9 μg per mouse i.c.v.), scopolamine (1.5 mg kg–1 i.p.), mecamylamine (20 mg kg–1 i.p.), diphenhydramine (20 mg kg–1 i.p.), and baclofen (2 mg kg–1 i.p.) amnesia. At the highest effective doses, none of the drugs impaired motor coordination, as revealed by the rota-rod Test, nor modified spontaneous motility and inspection activity, as revealed by the hole board Test. The antiamnesic effect induced by VA-100 and VA-101 was comparable to that exerted by the κ-opioid agonist U-50,488H, as well as that induced by the nootropic drug piracetam and the cholinesterase inhibitor physostigmine. These results suggest that the activation of κ-opioid receptors plays an important role in the prevention of memory impairment. On these bases, κ-opioid receptor agonists could represent a useful symptomatic treatment for cognitive deficits. Drug Dev. Res. 54:12–18, 2001. © 2001 Wiley-Liss, Inc.

  • Antiamnesic effect of the two novel κ‐opioid agonists, VA‐100 and VA‐101, in the mouse Passive Avoidance Test
    Drug Development Research, 2001
    Co-Authors: Carla Ghelardini, Nicoletta Galeotti, Lorenzo Di Cesare Mannelli, Andrea Cappelli, Maurizio Anzini, Alessandro Bartolini
    Abstract:

    The effects of the administration of the two novel κ-opioid agonists (VA-100, VA-101) on memory processes were evaluated with the mouse Passive Avoidance Test. The administration of VA-100 (50–100 mg kg–1 p.o.) and VA-101 (100 mg kg–1 p.o.) administered 20 min before the training session prevented nor-binaltorphimine (4.9 μg per mouse i.c.v.), scopolamine (1.5 mg kg–1 i.p.), mecamylamine (20 mg kg–1 i.p.), diphenhydramine (20 mg kg–1 i.p.), and baclofen (2 mg kg–1 i.p.) amnesia. At the highest effective doses, none of the drugs impaired motor coordination, as revealed by the rota-rod Test, nor modified spontaneous motility and inspection activity, as revealed by the hole board Test. The antiamnesic effect induced by VA-100 and VA-101 was comparable to that exerted by the κ-opioid agonist U-50,488H, as well as that induced by the nootropic drug piracetam and the cholinesterase inhibitor physostigmine. These results suggest that the activation of κ-opioid receptors plays an important role in the prevention of memory impairment. On these bases, κ-opioid receptor agonists could represent a useful symptomatic treatment for cognitive deficits. Drug Dev. Res. 54:12–18, 2001. © 2001 Wiley-Liss, Inc.