지원사업
학술연구/단체지원/교육 등 연구자 활동을 지속하도록 DBpia가 지원하고 있어요.
커뮤니티
연구자들이 자신의 연구와 전문성을 널리 알리고, 새로운 협력의 기회를 만들 수 있는 네트워킹 공간이에요.
논문 기본 정보
- 자료유형
- 학술저널
- 저자정보
- 저널정보
- 대한약리학회 The Korean Journal of Physiology & Pharmacology The Korean Journal of Physiology & Pharmacology 제22권 제5호
- 발행연도
- 2018.9
- 수록면
- 585 - 595 (11page)
- DOI
- https://doi.org/10.4196/kjpp.2018.22.5.585
이용수
초록· 키워드
오류제보하기
Amitriptyline, a tricyclic antidepressant, is commonly used to treat depression and neuropathic pain, but its mechanism is still unclear. We tested the effect of amitriptyline on 5-hydroxytryptamine 3 (5-HT3) receptor currents and studied its blocking mechanism because the clinical applications of amitriptyline overlapped with 5-HT3 receptor therapeutic potentials. Using a whole-cell voltage clamp method, we recorded the currents of the 5-HT3 receptor when 5-HT was applied alone or co-applied with amitriptyline in cultured NCB-20 neuroblastoma cells known to express 5-HT3 receptors. To elucidate the mechanism of amitriptyline, we simulated the 5-HT3 receptor currents using Berkeley Madonna® software and calculated the rate constants of the agonist binding and receptor transition steps. The 5-HT3 receptor currents were inhibited by amitriptyline in a concentration-dependent, voltage-independent manner, and a competitive mode. Amitriptyline accelerated the desensitization of the 5-HT3 receptor. When amitriptyline was applied before 5-HT treatment, the currents rose slowly until the end of 5-HT treatment. When amitriptyline was coapplied with 5-HT, currents rose and decayed rapidly. Peak current amplitudes were decreased in both applications. All macroscopic currents recorded in whole cell voltage clamping experiments were reproduced by simulation and the changes of rate constants by amitriptyline were correlated with macroscopic current recording data.
These results suggest that amitriptyline blocks the 5-HT3 receptor by close and open state blocking mechanisms, in a competitive manner. We could expand an understanding of pharmacological mechanisms of amitriptyline related to the modulation of a 5-HT3 receptor, a potential target of neurologic and psychiatric diseases through this study.
목차
등록된 정보가 없습니다.
참고문헌 (45)
참고문헌 신청
Barnes NM / 2009 / The 5-HT3 receptor--the relationship between structure and function / Neuropharmacology 56:273~284
Maricq AV / 1991 / Primary structure and functional expression of the 5HT3 receptor, a serotonin-gated ion channel / Science 254:432~437
Sugita S / 1992 / 5-hydroxytryptamine is a fast excitatory transmitter at 5-HT3 receptors in rat amygdala / Neuron 8:199~203
Katsurabayashi S / 2003 / A distinct distribution of functional presynaptic 5-HT receptor subtypes on GABAergic nerve terminals projecting to single hippocampal CA1 pyramidal neurons / Neuropharmacology 44:1022~1030
Thompson AJ / 2006 / 5-HT3 receptors / Curr Pharm Des 12:3615~3630
Maricq AV / 1991 / Primary structure and functional expression of the 5HT3 receptor, a serotonin-gated ion channel / Science 254:432~437
Sugita S / 1992 / 5-hydroxytryptamine is a fast excitatory transmitter at 5-HT3 receptors in rat amygdala / Neuron 8:199~203
Katsurabayashi S / 2003 / A distinct distribution of functional presynaptic 5-HT receptor subtypes on GABAergic nerve terminals projecting to single hippocampal CA1 pyramidal neurons / Neuropharmacology 44:1022~1030
Thompson AJ / 2006 / 5-HT3 receptors / Curr Pharm Des 12:3615~3630
함께 읽어보면 좋을 논문
논문 유사도에 따라 DBpia 가 추천하는 논문입니다. 함께 보면 좋을 연관 논문을 확인해보세요!
-
Gastroprokinetic agent, mosapride inhibits 5-HT3 receptor currents in NCB-20 cells
The Korean Journal of Physiology & Pharmacology
2019 .01
-
Distribution of 5-HT3, 5-HT4, and 5-HT7 Receptors Along the Human Colon
Journal of Neurogastroenterology and Motility (JNM)
2015 .01
-
Lamotrigine, an antiepileptic drug, inhibits 5-HT3 receptor currents in NCB-20 neuroblastoma cells
The Korean Journal of Physiology & Pharmacology
2017 .03
-
Potentiation of the glycine response by serotonin on the substantia gelatinosa neurons of the trigeminal subnucleus caudalis in mice
The Korean Journal of Physiology & Pharmacology
2019 .01
-
Omission of chemotherapy for hormone receptor-positive and human epidermal growth factor receptor 2-negative breast cancer: patterns of treatment and outcomes from the Korean Breast Cancer Society Registry
Annals of Surgical Treatment and Research
2022 .12
-
Stress-Induced Depression Is Alleviated by Aerobic Exercise Through Up-Regulation of 5-Hydroxytryptamine 1A Receptors in Rats
International Neurourology Journal
2015 .01
-
Suboptimal control status of young hypertensive population
Clinical Hypertension
2023 .01
-
Effects of 5HT1A Activation on Depression Profile Following 5-HT Depletion in Rats Lacking Social Attachment Since Weanling
PSYCHIATRY INVESTIGATION
2018 .01
-
Ketanserin and Naftopidil Enhance the Potentiating Effect of Alpha-Methyl-Serotonin on the Neurally-Induced Contraction of Human Isolated Urinary Bladder Muscle Strips
International Neurourology Journal
2017 .01
-
Schisandrin C interact with V225A and V288Y on serotonin receptor
한국실험동물학회 학술발표대회 논문집
2022 .07
-
Selective serotonin reuptake inhibitor escitalopram inhibits 5-HT3 receptor currents in NCB-20 cells
The Korean Journal of Physiology & Pharmacology
2019 .01
-
Evaluation of anti-cancer effects of M60 as a novel 5-HT2A antagonist in colorectal cancer
한국실험동물학회 학술발표대회 논문집
2022 .01
-
Effects of triterpenoid Alisol-F on human 5-hydroxytryptamine 3A and nicotinic acetylcholine receptor channel activity
한국실험동물학회 학술발표대회 논문집
2021 .07
-
Effects of 5HT1A Activation on Gating Profile Following 5HT Depletion in Rats Lacking Social Attachment Since Weanling
PSYCHIATRY INVESTIGATION
2018 .01
-
Serotonergic Regulation of Hepatic Energy Metabolism
Endocrinology and Metabolism
2021 .12
-
염산/에탄올로 유도된 위손상 동물모델에서 HT074의 항궤양 효과
대한본초학회지(본초분과학회지)
2018 .01
-
Sedative-Hypnotic and Receptor Binding Studies of Fermented Marine Organisms
Biomolecules & Therapeutics(구 응용약물학회지)
2015 .01
-
Antidepressant Effects of Cynanchum wilfordii Hemsley, Phlomis umbrosa Turcz, and Angelica gigas Nakai via Inhibition of 5-HT6 Receptor-mediated cyclic AMP Activity
동의생리병리학회지
2018 .01
-
Layer-specific serotonergic induction of long-term depression in the prefrontal cortex of rats
The Korean Journal of Physiology & Pharmacology
2020 .01
-
Expression of the spinal 5-HT7 receptor and p-ERK pathway in the carrageenan inflammatory pain of rats
Korean Journal of Anesthesiology
2015 .01
이 논문의 저자 정보
최근 본 자료
댓글(0)
0