Naloxone-inaccessible sigma receptor in rat central nervous system.

Tam, S. William

doi:10.1073/pnas.80.21.6703

Cited by 182 publications

(116 citation statements)

References 18 publications

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“…These observations have led to the proposition that both a opioids and PCP exert their behavioural effects via a common receptor mechanism (Zukin et al, 1984 have presented preliminary evidence (Downes et al, 1985) that in the rat brain the a and PCP sites are not the same, (+ )-[3H]-SKFIO,047, the selective a ligand, and [3H]-PCP, binding to more than one site. These findings agree well with those of Tam (1983Tam ( , 1985 in rat spinal cord and guinea-pig membranes.…”

Section: Introductionsupporting

confidence: 82%

A comparison of the binding of σ opioids and phencyclidine, and the interaction with antipsychotic drugs in rat brain membranes

Downes¹,

Lewis²,

Stone³

1986

British J Pharmacology

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Section: Introductionsupporting

confidence: 82%

A comparison of the binding of σ opioids and phencyclidine, and the interaction with antipsychotic drugs in rat brain membranes

Downes¹,

Lewis²,

Stone³

1986

British J Pharmacology

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“…(+)-Pentazocine is a selective sigma receptor agonist, which binds both the naloxoneinaccessible and naloxone-sensitive sigma receptors (Tsao and Su, 1997;Tam, 1983;Tam and Cook, 1984;Martin et al, 1984). Thus, systemic administration of (+)-pentazocine will be like (+)-morphine to attenuate the (−)-morphine-produced antinociception via the activation of the naloxone-sensitive sigma receptors.…”

Section: (+)-Pentazocine Attenuates the (−)-Morphine-produced Antinocmentioning

confidence: 99%

Stereoselective action of (+)-morphine over (−)-morphine in attenuating the (−)-morphine-produced antinociception via the naloxone-sensitive sigma receptor in the mouse

Hong

Tseng

2007

European Journal of Pharmacology

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We have previously demonstrated that (+)-morphine and (−)-morphine given spinally stereoselectively attenuate the spinally-administered (−)-morphine-produced tail-flick inhibition in the mouse. The phenomenon has been defined as antianalgesia (Wu et al., 2005). Present studies were then undertaken to determine if the systemic administration of (+)-morphine and (−)-morphine also stereoselectively attenuates the systemic (−)-morphine-produced tail-flick inhibition and the effects of (+)-morphine and (−)-morphine are mediated by the naloxone-sensitive sigma receptor activation in male CD-1 mice. Pretreatment with (+)-morphine at a dose of 0.01-10 ng/kg given subcutaneously dose-dependently attenuated the tail-flick inhibition produced by subcutaneouslyadministered (−)-morphine (5 mg/kg). Pretreatment with (−)-morphine (0.01-1.0 mg/kg) given subcutaneously also attenuates the (−)-morphine-produced tail-flick inhibition. The ED 50 values for (+)-morphine and (−)-morphine for inhibiting the (−)-morphine-produced tail-flick inhibition were estimated to be 30.6 pg/kg and 97.5 µg/kg, respectively. The attenuation of the (−)-morphineproduced tail-flick inhibition induced by (+)-morphine or (−)-morphine pretreatment was reversed by the pretreatment with (+)-naloxone or by the sigma receptor antagonist BD1047 (N-[2-(3,4-dichlorophenyl)ethyl]-N-methyl-2-(dimethylamino)ethylamine dihydrobromide) given subcutaneously. Pretreatment with (+)-pentazocine, a selective sigma receptor agonist, (1-10 mg/ kg) given subcutaneously also attenuates (−)-morphine-produced tail-flick inhibition, which was restored by (+)-naloxone (4 mg/kg) or BD1047 (10 mg/kg) pretreated subcutaneously. It is concluded that (+)-morphine exhibits extremely high stereoselective action over (−)-morphine given systemically in attenuating the systemic (−)-morphine-produced antinociception and the antianalgesic effect of (+)-morphine and (−)-morphine is mediated by activation of the naloxonesensitive sigma receptor.

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“…The possible involvement of sigma receptors (σ receptors) in schizophrenia has been suggested, based on the psychotomimetic actions of σ receptor agonists [18], the density of σ receptors detected in various mesencephalic and limbic areas [19] [20], and the action of several receptor ligands on dopaminergic neurons [21]- [24]. In fact, there are reports showing a reduction of sigma-1 receptors in the brains of schizophrenic patients postmortem [19] [20] [25] and other link between sigma receptors and schizophrenia, is that the typical and extensively used antipsychotic haloperidol has a very high affinity for sigma-1 receptors [26] [27].…”

Section: Introductionmentioning

confidence: 99%

Differential Effect on Two Immobility Responses by Chronic Administration of 1,3-di-o-Tolyl-Guanidine (Sigma Receptor Agonist) in Rats with Neonatal Ventral Hippocampal Lesion

Jaramillo¹,

Cruz²,

Vargas³

et al. 2014

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The effect of chronic administration of the sigma agonist: 1,3-di-o-tolyl-guanidine (DTG), in neonatal ventral hippocampal lesioned (nVHL) rats, on the immobility by clamping and dorsal immobility, were investigated. The nVHL increases the duration of immobility by clamping, but does not affect the duration of the dorsal immobility. We found that DTG augments the duration of the dorsal immobility in the unlesioned rats, but does not modify the duration of immobility induced by clamping the neck. DTG also counteracts the increase in the duration of the immobility by clamping produced by nVHL. However, the increase in the duration of the dorsal immobility produced by DTG is counteracted by nVHL. These results are discussed with respect to the differential effect on the two immobility responses tested, suggesting that they are different forms of immobility mediated by different mechanisms although they behaviorally share common characteristics.

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Naloxone-inaccessible sigma receptor in rat central nervous system.

Abstract: It has been postulated that the psychotomimetic effects of opiates of the benzomorphan series are due to their activity at the v receptor. Therefore, the binding of (±) -

Cited by 182 publications

References 18 publications

A comparison of the binding of σ opioids and phencyclidine, and the interaction with antipsychotic drugs in rat brain membranes

A comparison of the binding of σ opioids and phencyclidine, and the interaction with antipsychotic drugs in rat brain membranes

Stereoselective action of (+)-morphine over (−)-morphine in attenuating the (−)-morphine-produced antinociception via the naloxone-sensitive sigma receptor in the mouse

Differential Effect on Two Immobility Responses by Chronic Administration of 1,3-di-o-Tolyl-Guanidine (Sigma Receptor Agonist) in Rats with Neonatal Ventral Hippocampal Lesion

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