Localized injections of the mu antagonist CTOP into intracisternal (i.c.) or intracerebroventricular (i.c.v.) sites altered the behavior of 1-day-old rat pups during continuous exposure to an artificial nipple. Blockade of mu opioid receptors by i.c. injection decreased oral responsiveness to the nipple, while blockade of receptors by i.c.v. injection of CTOP increased oral responsiveness. The injection of CTOP into the i.c. site produced a transient reduction in body weight gain in pups suckling from their mother, while injection into the i.c.v. site had no effect. When cesarean-delivered pups were tested prior to suckling, injection of CTOP into the i.c. site increased latency of the first nipple attachment and decreased total time attached to a surrogate nipple providing milk. Injection of CTOP into the i.c.v. site decreased latency to the first nipple attachment. The results indicate that there is a caudal population of opioid receptors that is involved in the initiation of suckling behavior and a rostral population that plays a role in decreasing responsiveness at the nipple.
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http://dx.doi.org/10.1016/s0031-9384(98)00228-5 | DOI Listing |
Objective: To observe the effect of "Shugan Tiaoshen"(liver-soothing and mind-regulating) acupuncture on behavior reactions, opioid receptor expressions in the anterior cingulate cortex tissue and inflammatory factors in the serum in migraine rats, in order to explore its mechanism underlying improvement of migraine.
Methods: In the first part of this study, forty male Wistar rats were randomized into control, model, routine acupuncture and "Shugan Tiaoshen" acupuncture groups (=10/group), and in the second part, other 40 more male Wistar rats were randomized into low, medium and high dosage of blocker of μopioid receptor (OPRM)CTOP5 and PBS groups (=10/group, for validating the involvement of opioid receptor in the effect of "Shugan Tiaoshen"). The migraine model was established by subcutaneous injection of glyceryl trinitrate.
Front Neurosci
April 2022
Graduate Programme in Health Sciences, Federal University of Ceará, Sobral, Brazil.
Objective: possesses multiple biological effects and the 4-[(4'--acetyl-α-L- rhamnosyloxy) benzyl] isothiocyanate accounts for them. Based on the original isothiocyanate molecule we obtained a semisynthetic derivative, named 4-[(2',3',4'--triacetyl-α-L-rhamnosyloxy) -benzyl] hydrazine carbothioamide (MC-H) which was safe and effective in a temporomandibular joint (TMJ) inflammatory hypernociception in rats. Therefore, considering that there is still a gap in the knowledge concerning the mechanisms of action through which the MC-H effects are mediated, this study aimed to investigate the involvement of the adhesion molecules (ICAM-1, CD55), the pathways heme oxygenase-1 (HO-1) and NO/cGMP/PKG/K , and the central opioid receptors in the efficacy of the MC-H in a pre-clinical study of TMJ pain.
View Article and Find Full Text PDFJ Neurosci Res
January 2022
Department of Anesthesiology and Perioperative Medicine, Pittsburgh Center for Pain Research, Pittsburgh Project to End Opioid Misuse, University of Pittsburgh, Pittsburgh, PA, USA.
Tissue injury induces a long-lasting latent sensitization (LS) of spinal nociceptive signaling that is kept in remission by an opposing µ-opioid receptor (MOR) constitutive activity. To test the hypothesis that supraspinal sites become engaged, we induced hindpaw inflammation, waited 3 weeks for mechanical hypersensitivity to resolve, and then injected the opioid receptor inhibitors naltrexone, CTOP or β-funaltrexamine subcutaneously, and/or into the cerebral ventricles. Intracerebroventricular injection of each inhibitor reinstated hypersensitivity and produced somatic signs of withdrawal, indicative of LS and endogenous opioid dependence, respectively.
View Article and Find Full Text PDFBiochemistry
May 2021
Department of Medicinal Chemistry, College of Pharmacy, University of Minnesota, Minneapolis, Minnesota 55455, United States.
This report describes the unique pharmacological profile of FBNTI, a potent DOR antagonist that acts as a MOR agonist via an allosteric mechanism. Binding of FBNTI to opioid receptors expressed in HEK 293 cells revealed a 190-fold greater affinity for DOR ( = 0.84 nM) over MOR ( = 160 nM).
View Article and Find Full Text PDFBiomed Pharmacother
November 2020
Department of Pain and Analgesia, Beritashvili Center for Experimental Biomedicine, Tbilisi, Georgia; Department of Physiology, Tbilisi State Medial University, Tbilisi, Georgia. Electronic address:
Pain sensation is characterized as a complex experience, dependent on sensory processes as well as the activation of limbic brain areas involved in emotion, among them anterior insula. This cortical area is involved in the perception and response to painful stimuli. We investigated if this area contributes to antinociception produced by NSAIDs, and underlying mechanisms.
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