• Title/Summary/Keyword: Cholinergic

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Assessment of antinociceptive property of Cynara scolymus L. and possible mechanism of action in the formalin and writhing models of nociception in mice

  • Pegah Yaghooti;Samad Alimoahmmadi
    • The Korean Journal of Pain
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    • v.37 no.3
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    • pp.218-232
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    • 2024
  • Background: Cynara scolymus has bioactive constituents and has been used for therapeutic actions. The present study was undertaken to investigate the mechanisms underlying pain-relieving effects of the hydroethanolic extract of C. scolymus (HECS). Methods: The antinociceptive activity of HECS was assessed through formalin and acetic acid-induced writhing tests at doses of 50, 100 and 200 mg/kg intraperitoneally. Additionally, naloxone (non-selective opioid receptors antagonist, 2 mg/kg), atropine (non-selective muscarinic receptors antagonist, 1 mg/kg), chlorpheniramine (histamine H1-receptor antagonist, 20 mg/kg), cimetidine (histamine H2-receptor antagonist, 12.5 mg/kg), flumazenil (GABAA/BDZ receptor antagonist, 5 mg/kg) and cyproheptadine (serotonin receptor antagonist, 4 mg/kg) were used to determine the systems implicated in HECS-induced analgesia. Impact of HECS on locomotor activity was executed by open-field test. Determination of total phenolic content (TPC) and total flavonoid content (TFC) was done. Evaluation of antioxidant activity was conducted employing 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radical scavenging assay. Results: HECS (50, 100 and 200 mg/kg) significantly indicated dose dependent antinociceptive activity against pain-related behavior induced by formalin and acetic acid (P < 0.001). Pretreatment with naloxone, atropine and flumazenil significantly reversed HECS-induced analgesia. Antinociceptive effect of HECS remained unaffected by chlorpheniramine, cimetidine and cyproheptadine. Locomotor activity was not affected by HECS. TPC and TFC of HECS were 59.49 ± 5.57 mgGAE/g dry extract and 93.39 ± 17.16 mgRE/g dry extract, respectively. DPPH free radical scavenging activity (IC50) of HECS was 161.32 ± 0.03 ㎍/mL. Conclusions: HECS possesses antinociceptive activity which is mediated via opioidergic, cholinergic and GABAergic pathways.

Effects of Electrolytes and Drugs on the Inhibitory Junction Potentials Recorded from the Antrum of Guinea-pig Stomach (기니피그 유문동에서 기록되는 억제성 접합부 전압에 미치는 전해질과 약물의 효과)

  • Goo, Yong-Sook;Suh, Suk-Hyo;Lee, Suk-Ho;Hwang, Sang-Ik;Kim, Ki-Whan
    • The Korean Journal of Physiology
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    • v.24 no.1
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    • pp.1-13
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    • 1990
  • The effects of electrolytes, adenosine, ATP, 5-hydroxytryptamine (5-HT, serotonin) and ketanserin on the inhibitory junction potentials (IJPs) were investigated to clarify the interactions of these drugs with the neurotransmitters released from non-adrenergic, non-cholinergic nerves in the antrum of guinea-pig stomach. Electrical responses of antral circular muscle cells were recorded intracellularly using glass capillary microelectrode filled with 3 M KCI. All experiments were performed in Tris-buffered Tyrode soluition which was aerated with 100% $O_{2}$ and kept at $35^{\circ}C$. The results obtained were as follows: 1) Inhibitory junction potential (IJP) was recorded in antral strip, while excitatory junction potential (EJP) was recorded in fundic strip. 2) IJP recorded in antral strip was not influenced by atropine $(10^{-6}\;M)$ and guanethidine $(5{\times}10^{-6})$. 3) The amplitude of IJP increased in high $Ca^{2+}$ solution, while that of IJP decreased in high $Mg^{2+}$ solution or by $Ca^{2+}$ antagonist (verapamil). Apamin, $Ca^{2+}$-activated $K^{+}$ channel blocker blocked IJP completely. 4) ATP and adenosine decreased the amplitude of IJP. 5) 5-HT decreased the amplitude of IJP with no change of the amplitude of slow waves, while ketanserin (5-HT type 2 blocker) decreased the amplitude of slow waves markedly with no change in that of IJP. From the above results, the following conclusions could be made. 1) IJP recorded in antral strip is resulted from neurotransmitters released from non-adrenergic, non-cholinergic nerves. 2) An increase in the concentration of external $Ca^{2+}$ enhances the release of neurotransmitters from non-adrenergic, non-cholinergic nerves which activate the $Ca^{2+}$-dependent $K^{+}$ channel.

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Pharmacological studies on aggressive behavior induced by lesions of the nucleus accumbens septi in rats

  • Lee, Soon-Chul;Ueki, Showa
    • Archives of Pharmacal Research
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    • v.9 no.3
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    • pp.169-174
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    • 1986
  • Bilateral lesion of nucleus accumbens septi (N, AB), one of the mesolimbic nuclei, resulted in hyperirritability and muricide including mouse eating behavior in rats. The effects of various drugs on hyperirritability and muricide induced by NAB lesion were investigated in rats. Hyperirritability in NAB rats were significantly reduced by L-DOPA L-5-HTP major and minor tranquilizers but not reduced by MA, ATP and imipriamine-like antidepressants. On the other hand, muricide in NAB rats was significantly suppressed by L-DOPA, L-5-HTP, major and minor tranquilizers, furthermore, selectively suppressed by MA, ATP and antidepressants. These results suggested that the neural mechanism for inducing muricide is distinct from for hyperirritability in NAB rats, and that muricide in NAB rats is resulted from the increasing of cholinergic activity and reduction of dopaminergic and serotonergic activity.

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The Influence of guanethidine on the renal function of the rabbit (Guanethidine이 가토의 신장기능에 미치는 영향)

  • 고석태;김성원
    • YAKHAK HOEJI
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    • v.17 no.1
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    • pp.31-39
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    • 1973
  • The influence of guanethidine on the renal function was investigated in the rabbit. Guanethidine, 1-10mg/kg, i.v., produced no marked change in the renal function, while second and successive doses of guanethidine elicited a significant increase in urine flow and electrolyte excretion as well as renal plasma flow and glomerular filtration rate. It was suggested that the diuretic action was brought about by improvement of hemodynamic state in the kidney ; increased filtration as a result of increased renal perfusion. Atropine alone did not significantly influence the renal function but pretreatment of animals with atropine, 4 mg/kg i.v., completely abolished the diuretic action of guanethidine. It is suggested that guanethidine influences the renal function by activating parasympathetic nervous system or some cholinergic mechanism in the kidney.

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Selaginella tamariscina Extract Improves Scopolamine-induced Learning and Memory Dificits in Rats (부처손 추출물의 치매개선 효과 및 기전탐색)

  • Chu, Soon-Ju;Heo, Jin-Sun;Sohn, Kie-ho
    • Korean Journal of Pharmacognosy
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    • v.47 no.4
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    • pp.319-326
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    • 2016
  • We investigated the effect of Selaginella tamariscina extract on the learning and memory impairments in scopolamine-induced (5 mg/kg, i.p.) dementia rats. Rats treated with oral tacrin (20 mg/kg, p.o.) as positive control group and S. tamariscina extract 100, 200mg/kg, p. o. (SME 100, SME 200) as experimental group had significantly reduced scopolamine-induced memory deficits in the passive avoidance test. The acetylcholine content were paralleled the results of the behavior experiment. The acetylcholine contents of the experimental groups (SME 200 group) was higher than that of control group. We also evaluated expression of VAchT, vesicular acetylcholine transporter. SME was significantly increased VAchT expression on hippocampus of scopolamine-induced dementia rats. We suggest that S. tamariscina might exert a significantly neuro-protective effect on cognitive impairment.

Central Anticholinergic Syndrome by the Use of Scopolamine Patch -A case report- (수술후 통증관리 환자에서 Scopolamine Patch에 의해 발생한 중추항콜린성증후군 -증례 보고-)

  • Cho, Chong-Duk
    • The Korean Journal of Pain
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    • v.12 no.2
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    • pp.250-252
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    • 1999
  • A 77-year-old male patient was admitted to the hospital with acute appendicitis and underwent emergency appendectomy under inhalation anesthesia without any complications. After the operation, the patient was placed on epidural analgesia with the mixture of fentanyl-bupivacaine and scopolamine patch for nausea and vomiting. The patient experienced central anticholinergic syndrome (CAS) with hallucination, confusion, somnolence, dysarthria and delirium at 20 hours after patch placement and recovered from all symptoms of CAS in 24 hours after the removal of the patch. The CAS occurs when central cholinergic sites are occupied by specific drugs and also as a result of an insufficient release of acetylcholine. The diagnosis of CAS is often determined by a process of exclusion and not actually made until a positive therapeutic response to physostigmine, a centrally active anticholiesterase agent, has taken place. Treatment of CAS includes prompt removal of the patch, cleansing of the area, and physostigmine administration. The scopolamine patch should be used with extreme caution in elderly patient.

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Rat의 실험적 건망 모델에 있어 항치매 효과 물질의 약효 검색에 관한 연구

  • 이영근;류항묵;김옥희;양지선;이숙영;노응남;강석연
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 1994.04a
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    • pp.291-291
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    • 1994
  • Ibotonic acid와 FeCl$_3$ 투여군은 phosphate buffered saline을 투여한 대조군에 비해 흰쥐의 능동적 회피학습 습득율을 감소시켰고 해마영역의 과산화지질 형성도를 유의하게 증가시켰으며 acetylcholinesterase의 활성을 감소시켰으나 acetylcholine의 농도에는 별영향을 주지 못하였다. 이들 약물은 신경세포 지질막등에 작용하여 노인성 치매에서와 유사한 cholinergic신경계통에 neuronal degeneration을 유발하여 학습능력 감소를 유발한 것으로 보인다. 4,결론 중추 Cholinergic성 신경계활성의 변화와 뇌내 과산화지질의 과다 형성이 학습능력 감소 및 노인성치매의 원인이라고 말할수는 없지만 이러한 뇌내의 변화률이 치매과정과 연관성을 갖는 것으로 보여진다.

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Cholinergic involvement of spatial memory impairment in $\mu$-opioid receptor knockout mice

  • Yoo, Ji-Hoon;Yang, Eun-Mi;Kim, Kyung-In;Lee, Seok-Yong;Jang, Choon-Gon
    • Proceedings of the PSK Conference
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    • 2002.10a
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    • pp.304.3-305
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    • 2002
  • The present study investigated the passive avoidance and spatial learning in the ${\mu}$-opioid receptor gene knockout mice and wild type mice. In the step-through passive avoidance task. the ${\mu}$-opioid receptor knockout mice did not differ from the wild type mice. In Morris water maze. however. the ${\mu}$-opioid receptor knockout mice showed significant memory deficit compared to wild type mice. (omitted)

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