Anxiolytic activity of glycine-B antagonists and partial agonists—No relation to intrinsic activity in the patch clamp

Karcz-Kubicha, Marzena; Jessa, Maria; Nazar, Maciej; Płaźnik, Adam; Hartmann, Sabine; Parsons, Chris G.; Danysz, Wojciech

doi:10.1016/s0028-3908(97)00130-5

Cited by 63 publications

(37 citation statements)

References 52 publications

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“…CGP 37849 significantly increased the number of shocks in VCT at the dose (0.6 mg/kg, i.p.) which is in line with previously published data [21,31].…”

Section: Discussionsupporting

confidence: 94%

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NMDA/glutamate mechanism of anxiolytic-like action of zinc in Vogel conflict test in mice

Abdel-Maksoud¹

2012

iosrphr

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Abstract--The objective of our study is to investigate the possible anxiolytic-like effect of zinc using one of the most useful animal models of anxiety, which is the Vogel conflict test (VCT) and to investigate the possible involvement of the glutamatergic system and NMDA receptors in this postulated effect. The anxiolytic-like effect of ZnCl 2 (20 mg/kg, i.p.) in the VCT was abolished by the pretreatment of animals with N-methyl-D-Aspartic acid (75 mg/kg, i.p., NMDA receptor agonist) that per se produced no effect in VCT. Moreover, the treatment of mice with CGP37849 (0.3 mg/kg, i.p., a competitive NMDA receptor antagonist) or MK-801 (0.05 mg/kg, i.p., a non-competitive NMDA receptor antagonist) was able to potentiate the action of sub-effective dose of ZnCl 2 (10 mg/kg, i.p.). Overall results indicate that zinc induces the anxiolytic-like effect in mice without development of tolerance and inhibition of the NMDA receptor activity is involved in the mechanism of this effect.

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“…CGP 37849 significantly increased the number of shocks in VCT at the dose (0.6 mg/kg, i.p.) which is in line with previously published data [21,31].…”

Section: Discussionsupporting

confidence: 94%

“…MK-801 significantly increased the number of shocks in VCT at the dose (0.1 mg/kg, i.p.) which is in line with previously published data [21,31].All these results indicate that inhibition of the NMDA receptor activity by either competitive or non-competitive antagonists is involved in the mechanism of anxiolytic activity.…”

Section: Discussionsupporting

confidence: 93%

NMDA/glutamate mechanism of anxiolytic-like action of zinc in Vogel conflict test in mice

Abdel-Maksoud¹

2012

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“…D-cycloserine and (+R)-HA-966 are partial agonists at the glycine B site with different levels of intrinsic activity of 57% and 14% respectively in cultured hippocampal neurons 384 . Although these systemically active partial agonists do not induce receptor desensitization [384][385][386] , they have favorable therapeutic profiles in some in vivo models 387,388 .…”

Section: ) Glycinementioning

confidence: 99%

“…Although these systemically active partial agonists do not induce receptor desensitization [384][385][386] , they have favorable therapeutic profiles in some in vivo models 387,388 . In part this positive effect may be due to their own intrinsic activity as agonists at the glycine B site, which would serve to preserve a certain level of NMDA receptor function even at very high concentrations [389][390][391] .…”

Section: ) Glycinementioning

confidence: 99%

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A Review of Glutamate Receptors I: Current Understanding of Their Biology

Rousseaux

2008

J Toxicol Pathol

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Seventy years ago it was discovered that glutamate is abundant in the brain and that it plays a central role in brain metabolism. However, it took the scientific community a long time to realize that glutamate also acts as a neurotransmitter. Glutamate is an amino acid and brain tissue contains as much as 5 -15 mM glutamate per kg depending on the region, which is more than of any other amino acid. The main motivation for the ongoing research on glutamate is due to the role of glutamate in the signal transduction in the nervous systems of apparently all complex living organisms, including man. Glutamate is considered to be the major mediator of excitatory signals in the mammalian central nervous system and is involved in most aspects of normal brain function including cognition, memory and learning. In this review, the basic biology of the excitatory amino acids glutamate, glutamate receptors, GABA, and glycine will first be explored. In the second part of this review, the known pathophysiology and pathology will be described. (J Toxicol Pathol 2008; 21: 25-51)

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Excitatory Amino Acid Neurotransmission

Parsons

Danysz

Zieglgänsberger

Anxiety and Anxiolytic Drugs

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Anxiolytic activity of glycine-B antagonists and partial agonists—No relation to intrinsic activity in the patch clamp

Cited by 63 publications

References 52 publications

NMDA/glutamate mechanism of anxiolytic-like action of zinc in Vogel conflict test in mice

NMDA/glutamate mechanism of anxiolytic-like action of zinc in Vogel conflict test in mice

A Review of Glutamate Receptors I: Current Understanding of Their Biology

Excitatory Amino Acid Neurotransmission

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