Similar ameliorating effects of benzomorphans and 5-HT2 antagonists on drug-induced impairment of passive avoidance response in mice: comparison with acetylcholinesterase inhibitors

Matsuno, Kiyoshi; Senda, Toshihiko; Matsunaga, Keiko; Mita, Shiro; Kaneto, Hiroshi

doi:10.1007/bf02247374

Cited by 46 publications

(22 citation statements)

References 60 publications

(61 reference statements)

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“…Sig-1R modulate neurotransmitter release (37), synaptic activity (38), contraction of cardiac myocytes (27,28), and learning and In the presence of a Sig-1R agonist, such as (ϩ)PTZ, cocaine, or certain steroids, the Sig-1R͞ankyrin B complex dissociates from IP 3R-3 on the ER perhaps as a transport vesicle. As a result, IP3 binding to IP3R-3 increases and the Ca 2ϩ efflux is enhanced.…”

Section: Discussionmentioning

confidence: 99%

Regulating ankyrin dynamics: Roles of sigma-1 receptors

Hayashi

2001

Proc. Natl. Acad. Sci. U.S.A.

256

105

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Section: Discussionmentioning

confidence: 99%

Regulating ankyrin dynamics: Roles of sigma-1 receptors

Hayashi

2001

Proc. Natl. Acad. Sci. U.S.A.

256

105

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“…Using microdialysis techniques, Matsuno's group also reported an increased release of acetycholine in the frontal cortex of rat brain after administration of sigma-1 receptor agonists [66]. Horan et al.…”

Section: Cellular and Biochemical Studiesmentioning

confidence: 99%

Understanding the Molecular Mechanism of Sigma-1 Receptors: Towards A Hypothesis that Sigma-1 Receptors are Intracellular Amplifiers for Signal Transduction

Su¹,

Hayashi²

2003

Current Medicinal Chemistry

181

156

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Although sigma receptors were discovered in 1982, the biochemical and physiological roles of sigma receptors have just begun to unveil. Sigma receptors are non-opioid, non-phencyclidine receptors that contain two subtypes: sigma-1 and sigma-2 receptors. The sigma-1 receptor has been cloned and its sequence does not resemble that of any mammalian protein. Sigma-2 receptors have not been cloned. The focus of this review will be on sigma-1 receptors. Sigma-1 receptors contain 223 amino acids and reside primarily at the endoplasmic reticulum. Sigma-1 receptors exist mainly in the central nervous system, but also in the periphery. Sigma-1 receptor ligands include cocaine, (+)-benzomorphans like (+)-pentazocine and (+)N-allyl-normetazocine (or (+)-SKF-10047), and endogenous neurosteroids like progesterone and pregnenolone sulfate. Many pharmacological and physiological actions have been attributed to sigma-1 receptors. These include the regulation of IP3 receptors and calcium signaling at the endoplasmic reticulum, mobilization of cytoskeletal adaptor proteins, modulation of nerve growth factor-induced neurite sprouting, modulation of neurotransmitter release and neuronal firing, modulation of potassium channels as a regulatory subunit, alteration of psychostimulant-induced gene expression, and blockade of spreading depression. Behaviorally, sigma-1 receptors are involved in learning and memory, psychostimulant-induced sensitization, cocaine-induced conditioned place preference, and pain perception. Notably, in almost all the aforementioned biochemical and behavioral tests, sigma-1 agonists, while having no effects by themselves, caused the amplification of signal transductions incurred upon the stimulation of the glutamatergic, dopaminergic, IP3-related metabotropic, or nerve growth factor-related systems. Thus, it is hypothesized that sigma-1 receptors, at least in part, are intracellular amplifiers creating a supersensitized state for signal transduction in the biological system. HISTORY AND INTRODUCTIONOriginally intending to identify a subtype of opioid receptors, the sigma/opioid receptors as proposed by Martin et al.. [1], Su [2] used the tritiated prototypic sigma/opioid receptor ligand SKF-10047 (N-allyl-normetazocine) in binding assays and identified a protein that has a nanomolar affinity for SKF-10047. Surprisingly though, the protein had no affinity for the opioid antagonist naloxone. This raised a possibility that the protein identified by Su [2] may not be the sigma/opioid receptor proposed by Martin et al..[1] but may represent a new receptor at which SKF-10047 has an affinity. The protein identified by Su [2] was later termed "sigma receptor", with the word "opioid" dropped to differentiate it from the sigma/opioid receptor and the word "sigma" retained for it being identified with the labeled ligand SKF-10047. So far, the sigma/opioid receptor proposed by Martin et al.. has not been clearly identified.The sigma receptor has several peculiarities in its ligand binding profile and its distri...

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“…The antiamnesic effects of SA4503 were blocked after sigma-1 receptor antisense administration, but not after administration of a mismatch oligodeoxynucleotide [79,80,81,93,139]. Thus, activation of the sigma-1 receptor is involved in the improvement of cognition, and sigma-1 agonists have potential for the treatment of amnesia resulting from cholinergic dysfunction.…”

Section: Sigma Ligands Improve Cognition In Animal Models Of Cognitivmentioning

confidence: 99%

The cholinergic system, sigma-1 receptors and cognition

Waarde

Ramakrishnan

Rybczynska

et al. 2011

Behavioural Brain Research

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a b s t r a c tThis article provides an overview of present knowledge regarding the relationship between the cholinergic system and sigma-1 receptors, and discusses potential applications of sigma-1 receptor agonists in the treatment of memory deficits and cognitive disorders. Sigma-1 receptors, initially considered as a subtype of the opioid family, are unique ligand-regulated molecular chaperones in the endoplasmatic reticulum playing a modulatory role in intracellular calcium signaling and in the activity of several neurotransmitter systems, particularly the cholinergic and glutamatergic pathways. Several central nervous system (CNS) drugs show high to moderate affinities for sigma-1 receptors, including acetylcholinesterase inhibitors (donepezil), antipsychotics (haloperidol, rimcazole), selective serotonin reuptake inhibitors (fluvoxamine, sertraline) and monoamine oxidase inhibitors (clorgyline). These compounds can influence cognitive functions both via their primary targets and by activating sigma-1 receptors in the CNS. Sigma-1 agonists show powerful anti-amnesic and neuroprotective effects in a large variety of animal models of cognitive dysfunction involving, among others (i) pharmacologic target blockade (with muscarinic or NMDA receptor antagonists or p-chloroamphetamine); (ii) selective lesioning of cholinergic neurons; (iii) CNS administration of ␤-amyloid peptides; (iv) aging-induced memory loss, both in normal and senescentaccelerated rodents; (v) neurodegeneration induced by toxic compounds (CO, trimethyltin, cocaine), and (vi) prenatal restraint stress.

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Similar ameliorating effects of benzomorphans and 5-HT2 antagonists on drug-induced impairment of passive avoidance response in mice: comparison with acetylcholinesterase inhibitors

Cited by 46 publications

References 60 publications

Regulating ankyrin dynamics: Roles of sigma-1 receptors

Regulating ankyrin dynamics: Roles of sigma-1 receptors

Understanding the Molecular Mechanism of Sigma-1 Receptors: Towards A Hypothesis that Sigma-1 Receptors are Intracellular Amplifiers for Signal Transduction

The cholinergic system, sigma-1 receptors and cognition

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