The effect of nociceptin on Ca<sup>2+</sup> channel current and intracellular Ca<sup>2+</sup> in the SH‐SY5Y human neuroblastoma cell line

Connor, Mark; Yoe, Alison; Henderson, Graeme

doi:10.1111/j.1476-5381.1996.tb15387.x

Cited by 202 publications

(115 citation statements)

References 9 publications

(8 reference statements)

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“…Interestingly, this fourth member of the opioid receptor family is also coupled to the same second messenger systems [9,10,22,42,57,61,66,70,78,97]. Thus, activation of the ORL-1 receptor leads to inhibition of the enzyme adenylate cyclase [61,78] and calcium channel conductance [10,42,57].…”

Section: Introductionmentioning

confidence: 99%

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Buprenorphine: A Unique Drug with Complex Pharmacology

Lutfy

Cowan²

2004

275

232

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Buprenorphine, an opioid with mixed agonist-antagonist activity at classical opioid receptors, has been approved recently for the treatment of opioid dependency. Buprenorphine is also used as an analgesic. The buprenorphine dose-response curve is sometimes submaximal, or even bell-shaped, in nociceptive assays, depending upon the nature and intensity of the noxious stimulus. Moreover, buprenorphine, when administered with full agonists, such as morphine, antagonizes the action of these drugs. Partial agonism at the mu opioid receptor and, in some cases, antagonism at the kappa or delta opioid receptor have been considered as possible underlying mechanisms for the ceiling effect and bell-shaped dose-response curve of buprenorphine. While ceiling effects can be explained by partial agonist activity of buprenorphine, the bell-shaped dose-response curve cannot be a consequence of this property of the drug. Recently, buprenorphine has been shown to activate the opioid receptor-like (ORL-1; also known as NOP) receptor. Supraspinal activation of the ORL-1 receptor counteracts the antinociceptive and rewarding actions of morphine, raising the possibility that these actions of buprenorphine can also be altered by its ability to concomitantly activate the ORL-1 receptor. The use of molecular biological techniques has advanced our knowledge regarding the role of opioid receptors in modulation of pain and reward. In particular, generation of opioid receptor knockout mice has proven useful in this regard. Indeed, using knockout mice, we have recently shown that the antinociceptive effect of buprenorphine mediated primarily by the mu opioid receptor is attenuated by the ability of the drug to activate the ORL-1 receptor. Thus, the goal of this review is to provide evidence demonstrating that the ORL-1 receptor plays a functional role not only in the antinociceptive effect of buprenorphine but also in other actions of the drug as well.

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Section: Introductionmentioning

confidence: 99%

“…Thus, activation of the ORL-1 receptor leads to inhibition of the enzyme adenylate cyclase [61,78] and calcium channel conductance [10,42,57]. Stimulation of the ORL-1 receptor also activates inwardly rectifying potassium channels [9,97].…”

Section: Introductionmentioning

confidence: 99%

Buprenorphine: A Unique Drug with Complex Pharmacology

Lutfy

Cowan²

2004

275

232

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“…Despite these observations, the cellular actions of NC are similar to those of opioids. NC activates the NC-receptor to either inhibit adenylyl cyclase (Meunier et al, 1995;Reinscheid et al, 1995) and/or voltage-gated calcium channels (Connor et al, 1996b;Abdulla & Smith, 1997) or to stimulate an inwardly rectifying potassium conductance (Matthes et al, 1996;Connor et al, 1996a;Vaughan & Christie, 1996). These actions are expected to reduce neuronal excitability and neurotransmitter release.…”

Section: Introductionmentioning

confidence: 99%

Comparison of the effects of [Phe¹Ψ(CH₂‐NH)Gly²]Nociceptin (1–13)NH₂ in rat brain, rat vas deferens and CHO cells expressing recombinant human nociceptin receptors

Okawa

Nicol

Bigoni

et al. 1999

British J Pharmacology

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Nociceptin(NC) is the endogenous ligand for the opioid receptor like‐1 receptor (NC‐receptor). [Phe1ΨC(CH2‐NH)Gly2]Nociceptin(1–13)NH2 ([F/G]NC(1–13)NH2) has been reported to antagonize NC actions in peripheral guinea‐pig and mouse tissues. In this study, we investigated the effects of a range of NC C‐terminal truncated fragments and [F/G]NC(1–13)NH2 on NC receptor binding, glutamate release from rat cerebrocortical slices (rCX), inhibition of cyclic AMP accumulation in CHO cells expressing the NC receptor (CHONCR) and electrically evoked contractions of the rat vas deferens (rVD). In radioligand binding assays, a range of ligands inhibited [125I]‐Tyr14‐NC binding in membranes from rCX and CHONCR cells. As the peptide was truncated there was a general decline in pKi. [F/G]NC(1–13)NH2 was as potent as NC(1–13)NH2. The order of potency for NC fragments to inhibit cyclic AMP accumulation in whole CHONCR cells was NCNH2NC=NC(1–13)NH2>NC(1–12)NH2>>NC(1–11)NH2. [F/G]NC(1–13)NH2 was a full agonist with a pEC50 value of 8.65. NCNH2 and [F/G]NC(1–13)NH2 both inhibited K+ evoked glutamate release from rCX with pEC50 and maximum inhibition of 8.16, 48.5±4.9% and 7.39, 58.9±6.8% respectively. In rVD NC inhibited electrically evoked contractions with a pEC50 of 6.63. Although [F/G]NC(1–13)NH2, displayed a small (instrinsic activity α=0.19) but consistent residual agonist activity, it acted as a competitive antagonist (pA2 6.76) in the rVD. The differences between [F/G]NC(1–13)NH2 action on central and peripheral NC signalling could be explained if [F/G]NC(1–13)NH2 was a partial agonist with high strength of coupling in the CNS and low in the periphery. An alternative explanation could be the existence of central and peripheral receptor isoforms. British Journal of Pharmacology (1999) 127, 123–130; doi:10.1038/sj.bjp.0702539

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“…Many novel NOPreceptor ligands have been obtained by N/OFQsequence modifications and have been synthesized in the past few years [7,12,13,32]. In a previous investigation [31], we tested the effects of N/OFQ(1-13) NH 2 The aim of the current study was to investigate the possible correlation between the affinity, antioxidant activity (in free radical generating systems and in brain and liver) and putative toxicity (damage and viability) of the previously synthesized peptides in a neuroblastoma cell-line SH-SY5Y, expressing "orphan" opioid receptor [6,40]). …”

Section: Introductionmentioning

confidence: 99%

Study of the cytotoxicity and antioxidant capacity of N/OFQ(1–13)NH2 and its structural analogues

Kirkova

Zamfirova

Leśkiewicz

et al. 2009

Pharmacological Reports

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Abstract:The effect of side-chain shortening of N/OFQ(1-13)NH 2 at position 9 ([Orn 9 ]N/OFQ(1-13)NH 2 , [Dab 9 ]N/OFQ(1-13)NH 2 , [Dap 9 ]N/OFQ(1-13)NH 2 ) was studied regarding potential toxicity and antioxidant capacity. Staurosporine-and H 2 O 2 -induced damage of SH-SY5Y neuroblastoma cells was not changed in the presence of N/OFQ(1-13)NH 2 and [Orn 9 ]N/OFQ(1-13)NH 2 , but was strongly enhanced in the presence of [Dab 9 ]N/OFQ(1-13)NH 2 and [Dap 9 ]N/OFQ(1-13)NH 2 . Moreover, treatment of cells with the latter two analogues alone led to cell injury. Neuropeptide-dependent differences in the viability of SH-SY5Y cells were also observed, i.e., a cytoprotective effect was observed only in the presence of N/OFQ(1-13)NH 2 and [Orn 9 ]N/OFQ(1-13)NH 2 . Compared to [Dab 9 ]N/OFQ(1-13)NH 2 and [Dap 9 ]N/OFQ(1-13)NH 2 , the effects of N/OFQ(1-13)NH 2 and [Orn 9 ]N/OFQ(1-13)NH 2 were more beneficial in systems generating free oxygen radicals (O 2 -and . OH), as well as on the antioxidant status of rat brain and liver. Taken together, our findings show that N/OFQ(1-13)NH 2 and its structural analogue [Orn 9 ]N/OFQ(1-13)NH 2 possess more favorable profiles than the other two nociceptin (N/OFQ) analogues. The present results suggest that shortening of the side-chain of N/OFQ(1-13)NH 2 might increase cell damage and reduce the viability of SH-SY5Y neuroblastoma cells. Moreover, such alterations may lead to changes in free-oxygen generating systems and in antioxidant status in animal tissues.

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The effect of nociceptin on Ca²⁺ channel current and intracellular Ca²⁺ in the SH‐SY5Y human neuroblastoma cell line

Cited by 202 publications

References 9 publications

Buprenorphine: A Unique Drug with Complex Pharmacology

Buprenorphine: A Unique Drug with Complex Pharmacology

Comparison of the effects of [Phe¹Ψ(CH₂‐NH)Gly²]Nociceptin (1–13)NH₂ in rat brain, rat vas deferens and CHO cells expressing recombinant human nociceptin receptors

Study of the cytotoxicity and antioxidant capacity of N/OFQ(1–13)NH2 and its structural analogues

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The effect of nociceptin on Ca2+ channel current and intracellular Ca2+ in the SH‐SY5Y human neuroblastoma cell line

Cited by 202 publications

References 9 publications

Buprenorphine: A Unique Drug with Complex Pharmacology

Buprenorphine: A Unique Drug with Complex Pharmacology

Comparison of the effects of [Phe1Ψ(CH2‐NH)Gly2]Nociceptin (1–13)NH2 in rat brain, rat vas deferens and CHO cells expressing recombinant human nociceptin receptors

Study of the cytotoxicity and antioxidant capacity of N/OFQ(1–13)NH2 and its structural analogues

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The effect of nociceptin on Ca²⁺ channel current and intracellular Ca²⁺ in the SH‐SY5Y human neuroblastoma cell line

Comparison of the effects of [Phe¹Ψ(CH₂‐NH)Gly²]Nociceptin (1–13)NH₂ in rat brain, rat vas deferens and CHO cells expressing recombinant human nociceptin receptors