Analgesic properties of chimeric peptide based on morphiceptin and PFRTic-amide

Li, Meixing; Zhou, Lei; Ma, Guoliang; Dong, Shouliang

doi:10.1016/j.regpep.2012.08.008

Cited by 13 publications

(19 citation statements)

References 37 publications

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“…Chimeric MCRT produced quite remarkable analgesia (i.c.v., ED 50 = 29.8 pmol/mouse) in tail‐withdrawal test . Figure demonstrated that high doses of MCRT (3 and 10 nmol/mouse) significantly inhibited gastric emptying and intestinal transit, while 1 nmol/mouse was inactive.…”

Section: Discussionmentioning

confidence: 92%

“…As Figures showed, MCRT‐induced gastrointestinal dysfunction could be blocked completely by naloxone and naltrindole, but not affected by cyprodime, suggesting the involvement of DOR rather than MOR. Therefore, there seems to be a discrepancy that cyprodime significantly blocked MCRT‐induced analgesia, but not mediated its motility disorders (Figure ).…”

Section: Discussionmentioning

confidence: 97%

“…PFRTic‐NH 2 was speculated to be a NPFF antagonist based on the successful cases of the designed novel antagonists with Tic . Accumulative evidences confirmed that PFRTic‐NH 2 exerted opposite actions from NPFF in the morphine withdrawal syndromes, supraspinal pain and cardiovascular regulation . However, in‐vitro contractility study and intrathecal pain regulation etc.…”

Section: Discussionmentioning

confidence: 99%

“…Major efforts were made to develop compounds that possessed more efficacious analgesic property with relatively less side effects. Chimeric MCRT, a bifunctional ligand of MOR and δ‐opioid receptors (DOR), produced potent analgesia (ED 50 = 29.8 pmol/mouse) in tail‐withdrawal test . Thus, we attempted to preliminarily evaluate the potential of MCRT served as the analgesic through examining its influence on gastrointestinal motility.…”

Section: Introductionmentioning

confidence: 99%

“…MCRT (YPFPFRTic-NH 2 ), a chimeric heptapeptide based on morphiceptin (YPFP-NH 2 ) and a neuropeptide FF (NPFF) derivative (PFRTic-NH 2 ), was designed and synthesized via an overlapping proline. [1][2][3] Parent peptide morphiceptin, which was isolated from the enzymatic digest of bovine b-casein, showed the high selectivity for l-opioid receptor (MOR). [4] In-vitro contractility studies, morphiceptin at 10 À6 mol/l concentration completely blocked the neostigmine-induced colon contractions.…”

Section: Introductionmentioning

confidence: 99%

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Supraspinal inhibitory effects of chimeric peptide MCRT on gastrointestinal motility in mice

Zhang

et al. 2017

Journal of Pharmacy and Pharmacology

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(1) Morphiceptin and PFRTic-NH played important roles in the regulation of gastrointestinal motility; (2) MCRT possessed higher bioactivity of pain relief than gastrointestinal regulation, suggesting its promising analgesic property; (3) MCRT-induced motility disorders were sensitive to DOR but not to MOR blockade, indicating the pain-relieving specificity of speculated MOR subtype or splice variant or MOR-DOR heterodimer.

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Section: Discussionmentioning

confidence: 92%

Section: Discussionmentioning

confidence: 97%

Section: Discussionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

See 3 more Smart Citations

Supraspinal inhibitory effects of chimeric peptide MCRT on gastrointestinal motility in mice

Zhang

et al. 2017

Journal of Pharmacy and Pharmacology

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Cyclic derivatives of morphiceptin possess anti-transit effect in the gastrointestinal tract and alleviate abdominal pain in mice

Szymaszkiewicz

Włodarczyk

Mazur³

et al. 2020

Pharmacol. Rep

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Background Irritable bowel syndrome (IBS) is a chronic condition with recurring gastrointestinal (GI) symptoms: altered motility and abdominal pain. As endogenous opioid system participates in pain perception and in the control of GI peristalsis, opioids have been proposed as a promising therapy in IBS. In a previous study, we observed that morphiceptin derivative, P-317 (Dmt-cyclo-(d-Lys-Phe-d-Pro-Asp)-NH 2), presents promising features to be applied in IBS. In this project, we tested whether modifications in cyclic morphiceptin-based structure: fluorination (compound 1) or peptide bond reduction (compound 2) improve pharmacological effect. Methods We evaluated tested derivatives in the mouse GI system under physiological (GI transit) and pathophysiological (castor oil diarrhea, stress-induced hypermotility, visceral pain) conditions. Results Both compounds prolonged GI transit. Compound 1 and P-317 inhibited upper GI transit and motility of the colon; compound 2 remained inactive. Compound 1 and P-317 inhibited hypermotility in stressed mice and delayed the acute diarrhea in comparison to control. Only P-317 exerted antinociceptive effect. None of tested derivatives, similar to P-317, affected locomotor activity. Conclusions Compound 1 is equally effective as P-317 in the mouse GI tract. The peptide bond reduction decreased the activity of compound 2. Fluorination appears to be an efficient way to increase the effects of morphiceptin analogs in the GI tract.

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MCRT, a chimeric peptide based on morphiceptin and PFRTic-NH2, regulates the depressor effects induced by endokinin A/B

Zhang¹,

He²,

Pi³

et al. 2016

European Journal of Pharmacology

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Analgesic properties of chimeric peptide based on morphiceptin and PFRTic-amide

Cited by 13 publications

References 37 publications

Supraspinal inhibitory effects of chimeric peptide MCRT on gastrointestinal motility in mice

Supraspinal inhibitory effects of chimeric peptide MCRT on gastrointestinal motility in mice

Cyclic derivatives of morphiceptin possess anti-transit effect in the gastrointestinal tract and alleviate abdominal pain in mice

MCRT, a chimeric peptide based on morphiceptin and PFRTic-NH2, regulates the depressor effects induced by endokinin A/B

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