Contrasting Actions of Intrathecal U50, 488H, Morphine, or [D-Pen sup 2, D-Pen sup 5] Enkephalin or Intravenous U50, 488H on the Visceromotor Response to Colorectal Distension in the Rat

Harada, Yoshinori; Nishioka, Kengo; Kitahata, Luke M.; Nakatani, Keio; Collins, J. G.

doi:10.1097/00000542-199508000-00014

Cited by 43 publications

(34 citation statements)

References 19 publications

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“…This inhibition could not be completely antagonized by very high doses of naloxone or by two -opioid receptor-selective antagonists, nor-Binaltorphimine dihydrochloride (nor-BNI) and DIPPA. Furthermore, in experiments where the cloned rat -opioid receptor (KOR 1) was "knockeddown" at peripheral sites using antisense oligodeoxynucleotides, the dose-dependent inhibition of pelvic nerve afferent fiber responses to noxious CRD by -ORAs persisted (Joshi et al 2000). These results suggested that these peripheral, visceral -ORA actions are mediated by a nonopioid mechanism.…”

Section: Introductionmentioning

confidence: 97%

Sodium Channel Blocking Actions of the κ-Opioid Receptor Agonist U50,488 Contribute to Its Visceral Antinociceptive Effects

Joshi

Kardos

et al. 2002

Journal of Neurophysiology

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. Sodium channel blocking actions of the -opioid receptor agonist U50,488 contribute to its visceral antinociceptive effects. J Neurophysiol 87: 1271-1279, 2002; 10.1152/jn.00624.2001. The goal of the present study was to determine whether the -opioid receptor agonist (ORA) U50,488 attenuates behavioral and primary afferent nerve responses to noxious colorectal distension (CRD) by sodium channel blockade. We tested the analgesic -ORA (Ϯ)-trans U50,488, its enantiomers (Ϫ)-trans (1S,2S)-U50,488 and non -ORA (ϩ)-trans (1R,2R)-U50,488, and/or its diastereomer (Ϫ)-cis (1S,2R)-U50,488 for their ability to attenuate visceromotor and pelvic nerve afferent fiber responses to noxious CRD in vivo and voltage-activated sodium current in colon sensory neurons in vitro. In unanesthetized rats, subcutaneous administration of U50,488, (1S,2S)-U50,488, and (1R,2R)-U50,488 attenuated the behavioral visceromotor response to noxious CRD; the rank order of potency was: (1S,2S)-U50,488 Ͼ U50,488 Ͼ Ͼ (1R,2R)-U50,488. U50,488 and its stereoisomers also inhibited responses of decentralized pelvic nerve afferent fibers to noxious CRD in a dose-dependent manner. Cumulative doses of 16 mg/kg of (1S,2S)-U50,488, (1S,2R)-U50,488, and (1R,2R)-U50,488 reduced responses to a mean 29, 30, and 47% of control, respectively. The mean inhibitory doses of these drugs were not different (range: 6.6 -10.8 mg/kg). Sodium channel blockers mexiletine and carbamazepine mimicked the effect of U50,488. In contrast, the -ORAs dynorphin (1-13) and ICI 204,488 were ineffective in attenuating pelvic nerve activity. Perfusion of (1S,2S)-U50,488, (1S,2R)-U50,488, or (1R,2R)-U50,488 on colon sensory neurons in vitro decreased voltage-activated sodium currents. This inhibition by U50,488 and its stereoisomers was not opioid receptor-mediated because it could not be reversed by the opioid receptor antagonist naloxone and was also not a G protein-mediated effect. The results reported here suggest that the visceral antinociceptive effects of U50,488 and its stereoisomers are contributed to by their peripheral sodium channel blocking actions. I N T R O D U C T I O NThe mechanisms and modulation of visceral pain have been extensively examined using colorectal distension (CRD) as a noxious visceral stimulus. Previous studies employing CRD have documented the ability of -opioid receptor agonists (ORAs) like U50,488 to attenuate pseudaffective visceromotor and cardiovascular responses to noxious CRD following their systemic, but not intrathecal administration (Danzebrink et al. 1995; Harada et al. 1995a,b). A peripheral, visceral antinociceptive action of U50,488 has been demonstrated. U50,488 was shown to dose dependently inhibit responses of mechanosensitive pelvic nerve afferent fibers to noxious colorectal or urinary bladder distension in the rat Su et al. 1997a,b). This inhibition could not be completely antagonized by very high doses of naloxone or by two -opioid receptor-selective antagonists, nor-Binaltorphimine dihydrochloride (nor-BNI) and DIPPA. Furthermore, ...

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Section: Introductionmentioning

confidence: 97%

Sodium Channel Blocking Actions of the κ-Opioid Receptor Agonist U50,488 Contribute to Its Visceral Antinociceptive Effects

Joshi

Kardos

et al. 2002

Journal of Neurophysiology

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“…[ 9,10] Clinical efficacy of Intrathecal Clonidine to relieve visceral pain in well-established [11][12] but Clonidine is also associated with few side effects like bradycardia, hypotension and dry mouth. So, 50μg dose of Clonidine was chosen in our study, as higher doses (150ug) are also associated with significant risk of hypotension as reported by Chiari et, al.…”

Section: Discussionmentioning

confidence: 99%

Intrathecal Buprenorphine, Clonidine and Fentanyl as Adjuvants To 0.5% Hyperbaric Bupivacaine In Lower Abdominal Surgeries: A Prospective, Randomized And Comparative Study.

Krishnakumar¹,

Chandrasekaran²,

Nanthaprabu³

2016

IOSR

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“…Experimental studies have shown that opioids and  2 adrenergic agonist administered spinally are able to relieve visceral pain [13][14][15][16] . Clinical efficacy of intrathecal opioid to relieve visceral pain is well established [17][18] .…”

Section: Discussionmentioning

confidence: 99%

“…Clinical efficacy of intrathecal opioid to relieve visceral pain is well established [17][18] . Antinociceptive action of clonidine exist for both somatic and visceral pain 13,15,16 . In the present study, patients were randomly allocated in three groups: B, BF & BC.…”

Section: Discussionmentioning

confidence: 99%

“…Complains of chest pain was more in group B (36.66%) compared to group BF (13.33%) and group BC (6.66%). Less incidence of chest pain in group BC and BF may be due to action of spinally administered clonidine and fentanyl to relieve visceral pain [13][14][15][16] . Quality of anaesthesia was better in group BF and BC than control group B which was statistically significant (p=0.000).…”

Section: Discussionmentioning

confidence: 99%

See 1 more Smart Citation

Subarachnoid clonidine or fentanyl with low dose hyperbaric bupivacaine for elective caesarean section - A comparative study

Islam

Ali²,

Begum

et al. 2012

J. Dhaka Natl. Med. Coll. Hosp.

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Contrasting Actions of Intrathecal U50, 488H, Morphine, or [D-Pen sup 2, D-Pen sup 5] Enkephalin or Intravenous U50, 488H on the Visceromotor Response to Colorectal Distension in the Rat

Cited by 43 publications

References 19 publications

Sodium Channel Blocking Actions of the κ-Opioid Receptor Agonist U50,488 Contribute to Its Visceral Antinociceptive Effects

Sodium Channel Blocking Actions of the κ-Opioid Receptor Agonist U50,488 Contribute to Its Visceral Antinociceptive Effects

Intrathecal Buprenorphine, Clonidine and Fentanyl as Adjuvants To 0.5% Hyperbaric Bupivacaine In Lower Abdominal Surgeries: A Prospective, Randomized And Comparative Study.

Subarachnoid clonidine or fentanyl with low dose hyperbaric bupivacaine for elective caesarean section - A comparative study

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