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Peptides ; 106: 96-101, 2018 08.
Artigo em Inglês | MEDLINE | ID: mdl-30016700


For clinical use, it is essential to develop potent endomorphin (EM) analogs with reduced antinociceptive tolerance. In the present study, the antinociceptive activities and tolerance development of four potent EM-1 analogs with C-terminal oligoarginine-conjugation was evaluated and compared in the radiant heat paw withdrawal test. Following intracerebroventricular (i.c.v.) administration, all analogs 1-4 produced potent and prolonged antinociceptive effects. Notably, analogs 2 and 4 with the introduction of D-Ala in position 2 exhibited relatively higher analgesic potencies than those of analogs 1 and 3 with ß-Pro substitution, consistent with their µ-opioid binding characteristic. In addition, at a dose of 50 µmol/kg, endomorphin-1 (EM-1) failed to produce any significant antinociceptive activity after peripheral administration, whereas analogs 1-4 induced potent antinociceptive effects with an increased duration of action. Herein, our results indicated the development of antinociceptive tolerance to EM-1 and morphine at the supraspinal level on day 7. By contrast, analogs 1-4 decreased the antinociceptive tolerance. Furthermore, subcutaneous (s.c.) administration of morphine at 50 µmol/kg also developed the antinociceptive tolerance, whereas the extent of tolerance developed to analogs 1-4 was largely reduced. Especially, analog 4 exhibited non-tolerance-forming antinociception after peripheral administration. The present investigation gave the evidence that C-terminal conjugation of EM-1 with oligoarginine vector will facilitate the development of novel opioid analgesics with reduced opioid tolerance.

Analgésicos Opioides/farmacologia , Analgésicos/farmacologia , Arginina/química , Tolerância a Medicamentos , Oligopeptídeos/farmacologia , Animais , Membro Posterior/efeitos dos fármacos , Temperatura Alta/efeitos adversos , Masculino , Camundongos , Modelos Animais , Oligopeptídeos/síntese química , Oligopeptídeos/química , Dor/prevenção & controle , Receptores Opioides mu/efeitos dos fármacos
Zhongguo Zhen Jiu ; 30(10): 798-801, 2010 Oct.
Artigo em Chinês | MEDLINE | ID: mdl-21058472


OBJECTIVE: To select the best solution of immediate analgesia of migraine treated with acupuncture. METHODS: Taken 36 cases of migraine in attack stage as research objects, by means of orthogonal experimental design, applying the L9 (3(4)) orthogonal table, the therapeutic effect of immediate analgesia of acupuncture for migraine in attack stage was analyzed in four factors, which were effective acupoints combination, electroacupuncture therapy, auricular therapy and bloodletting therapy, and three levels of each factors. In the test procession, random approaches (stratified random and central random) and blinding experiment (the appraiser blind) were used. The time points of observation were before treatment, and 10, 20 minutes after treatment. Visual Analogue Scale (VAS) was used to evaluate therapeutic effect. RESULTS: Comparing with the headache before treatment, at the time points of 10 and 20 minutes after treatment, the best solution for headache relief was needling therapy (local and distal points and points selection according to the differentiation), auricular electroacupuncture therapy and bloodletting at Taiyang Zimai (Extra) or Taiyang (EX-HN 5)and Ashi points. CONCLUSION: In the attack stage of migraine, by the therapy combined with puncture on local and distal points and the points according to the differentiation, auricular electroacupuncture and bloodletting at Taiyang Zimai or Taiyang (EX-HN 5) and Ashi points, the favorable effects of immediate analgesia are received.

Analgesia por Acupuntura , Transtornos de Enxaqueca/terapia , Manejo da Dor , Pontos de Acupuntura , Adulto , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Adulto Jovem
Zhongguo Zhen Jiu ; 29(5): 421-3, 2009 May.
Artigo em Chinês | MEDLINE | ID: mdl-19489504


OBJECTIVE: To observe the therapeutic effect of Hwato never and muscle stimulator on peripheral facial paralysis. METHODS: Eighty-seven cases of peripheral facial paralysis were randomly divided into a Hwato never and muscle stimulator observation group (n=44) and a G 6805 electronic stimulator control group (n=43). The same acupoints, Hegu (LI 4), Sanyinjiao (SP 6), Taichong (LR 3) and local acupoints on the affected side were selected in the two groups. The therapeutic effects were compared between the two groups. RESULTS: Although the total effective rates were both 100.0% in the two groups, the cured rate was 90.9% in the observation group and 62.8% in the control group with a significant difference between the two groups (P < 0.05). There were no adverse effects in the two groups. CONCLUSION: The cured rate of Hwato never and muscle stimulator on peripheral facial paralysis is superior to that of G 6805 electronic stimulator.

Pontos de Acupuntura , Eletroacupuntura , Paralisia Facial/terapia , Adolescente , Adulto , Idoso , Criança , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Adulto Jovem