水蛭Retzius神经元上谷氨酸兴奋性受体的构效关系研究。
Structure-activity studies on an excitatory receptor for glutamate on leech Retzius neurones.
作者信息
James V A, Walker R J, Wheal H V
出版信息
Br J Pharmacol. 1980 Apr;68(4):711-7. doi: 10.1111/j.1476-5381.1980.tb10864.x.
Abstract
1 Intracellular recordings were made from Retzius cells from the segmental ganglia of Hirudo medicinalis and Haemopis sanguisuga. Glutamate had a direct excitatory effect on the leech Retzius cells. 2 L-Glutamate was 25 times more potent than D-glutamate. 3 L-Glutamate was approximately equipotent with ibotenic acid and 11.2 times more potent than L-aspartic acid. 4 Quisqualic acid and kainic acid were both approximately 100 times more potent than L-glutamate. DL-1-Amino-cis-1-3-dicarboxyclyclopentane was approximately 5 times more potent than L-glutamate, while the trans isomer was 105 times less potent. 5 alpha-NH2-pimelic acid and beta-CH3-glutamic acid reduced the response to L-glutamate. 6 It is suggested that glutamic acid may interact with the Retzius cell glutamate receptor in an extended conformation.
摘要
- 从医用水蛭和红蛭的节段神经节中的雷丘斯细胞进行细胞内记录。谷氨酸对水蛭雷丘斯细胞有直接兴奋作用。2. L-谷氨酸的效力比D-谷氨酸强25倍。3. L-谷氨酸与鹅膏蕈氨酸效力大致相当，比L-天冬氨酸强11.2倍。4. quisqualic酸和海人藻酸的效力均比L-谷氨酸强约100倍。DL-1-氨基-顺-1,3-二羧基环戊烷的效力比L-谷氨酸强约5倍，而反式异构体的效力则弱105倍。5. α-氨基庚二酸和β-甲基谷氨酸降低了对L-谷氨酸的反应。6. 提示谷氨酸可能以伸展构象与雷丘斯细胞谷氨酸受体相互作用。
相似文献
1
Structure-activity studies on an excitatory receptor for glutamate on leech Retzius neurones.水蛭Retzius神经元上谷氨酸兴奋性受体的构效关系研究。
Br J Pharmacol. 1980 Apr;68(4):711-7. doi: 10.1111/j.1476-5381.1980.tb10864.x.
2
The ionic mechanisms associated with the excitatory response of kainate, L-glutamate, quisqualate, ibotenate, AMPA and methyltetrahydrofolate on leech Retzius cells.与红藻氨酸、L-谷氨酸、quisqualate、鹅膏蕈氨酸、AMPA和甲基四氢叶酸对水蛭Retzius细胞的兴奋性反应相关的离子机制。
Comp Biochem Physiol C Comp Pharmacol Toxicol. 1984;77(1):115-26. doi: 10.1016/0742-8413(84)90139-7.
3
Comparison of effects of endogenous and exogenous excitatory amino acids on Retzius nerve cells of the leech.内源性和外源性兴奋性氨基酸对水蛭Retzius神经细胞作用的比较。
Folia Biol (Krakow). 2009;57(1-2):83-90. doi: 10.3409/fb57_1-2.83-90.
4
Actions of glutamate, kainate, dihydrokainate and analogues on leech neurone acidic amino acid receptors.
Eur J Pharmacol. 1980 Mar 7;62(1):35-9. doi: 10.1016/0014-2999(80)90478-1.
5
Neuropharmacological studies on the receptors mediating responses to carbachol, amino acids and octopamine on Limulus and Hirudo central neurons.关于鲎和水蛭中枢神经元中介导对卡巴胆碱、氨基酸和章鱼胺反应的受体的神经药理学研究。
Comp Biochem Physiol C Comp Pharmacol Toxicol. 1984;77(2):371-80. doi: 10.1016/0742-8413(84)90031-8.
6
The halomethylketone derivative L-Glu-gamma-DL-Ala-CH2Cl and N-methyl-D-aspartate as selective antagonists against L-glutamate and kainate excitation respectively on Retzius cells of the leech, Hirudo medicinalis.卤代甲基酮衍生物L-谷氨酸-γ-DL-丙氨酸-CH₂Cl和N-甲基-D-天冬氨酸分别作为针对水蛭（药用水蛭）Retzius细胞上L-谷氨酸和红藻氨酸兴奋作用的选择性拮抗剂。
Comp Biochem Physiol C Comp Pharmacol Toxicol. 1984;77(2):385-98. doi: 10.1016/0742-8413(84)90033-1.
7
Two distinct electrophysiological mechanisms underlie extensive depolarization elicited by 2,4 diaminobutyric acid in leech Retzius neurons.两种不同的电生理机制为 2,4-二氨基丁酸在水蛭 Retzius 神经元中引起广泛去极化提供了基础。
Aquat Toxicol. 2020 Mar;220:105398. doi: 10.1016/j.aquatox.2019.105398. Epub 2019 Dec 26.
8
gamma-D-glutamylglycine as an antagonist of kainic acid on leech Retzius neurones.γ-D-谷氨酰甘氨酸作为红藻氨酸对水蛭瑞氏神经元的拮抗剂。
Neuropharmacology. 1982 Dec;21(12):1245-9. doi: 10.1016/0028-3908(82)90128-9.
9
Effects of glutamic acid analogues on identifiable giant neurones, sensitive to beta-hydroxy-L-glutamic acid, of an African giant snail (Achatina fulica Férussac).谷氨酸类似物对非洲大蜗牛（Achatina fulica Férussac）中对β-羟基-L-谷氨酸敏感的可识别巨型神经元的影响。
Br J Pharmacol. 1985 Nov;86(3):645-54. doi: 10.1111/j.1476-5381.1985.tb08941.x.
10
Extensive depolarization and lack of recovery of leech Retzius neurons caused by 2,4 diaminobutyric acid.2,4-二氨基丁酸导致水蛭 Retzius 神经元广泛去极化和无法恢复。
Aquat Toxicol. 2018 Jun;199:269-275. doi: 10.1016/j.aquatox.2018.03.036. Epub 2018 Mar 31.
引用本文的文献
1
Mechanism of inhibition of the GluA2 AMPA receptor channel opening by talampanel and its enantiomer: the stereochemistry of the 4-methyl group on the diazepine ring of 2,3-benzodiazepine derivatives.噻加宾及对映体抑制 GluA2 AMPA 受体通道开放的作用机制：2,3-苯并二氮䓬衍生物的二氮杂环庚烷环上 4-甲基的立体化学。
ACS Chem Neurosci. 2013 Apr 17;4(4):635-44. doi: 10.1021/cn3002398. Epub 2013 Feb 12.
2
Molecular identification and expression of the NMDA receptor NR1 subunit in the leech.水蛭中N-甲基-D-天冬氨酸受体NR1亚基的分子鉴定与表达
Invert Neurosci. 2009 Mar;9(1):11-20. doi: 10.1007/s10158-008-0085-3. Epub 2009 Jan 14.
3
Glutamate as a transmitter in the sensory pathway from prostomial lip to serotonergic Retzius neurons in the medicinal leech Hirudo.谷氨酸作为从药用水蛭（医蛭）的口前叶唇部到5-羟色胺能雷悌氏神经元的感觉通路中的一种神经递质。
Invert Neurosci. 1996 Sep;2(2):121-8. doi: 10.1007/BF02214115.
4
Effects of glutamic acid analogues on identifiable giant neurones, sensitive to beta-hydroxy-L-glutamic acid, of an African giant snail (Achatina fulica Férussac).谷氨酸类似物对非洲大蜗牛（Achatina fulica Férussac）中对β-羟基-L-谷氨酸敏感的可识别巨型神经元的影响。
Br J Pharmacol. 1985 Nov;86(3):645-54. doi: 10.1111/j.1476-5381.1985.tb08941.x.
本文引用的文献
1
EXTRACELLULAR SPACE AS A PATHWAY FOR EXCHANGE BETWEEN BLOOD AND NEURONS IN THE CENTRAL NERVOUS SYSTEM OF THE LEECH: IONIC COMPOSITION OF GLIAL CELLS AND NEURONS.水蛭中枢神经系统中细胞外空间作为血液与神经元之间交换的途径：神经胶质细胞和神经元的离子组成
J Neurophysiol. 1964 Jul;27:645-71. doi: 10.1152/jn.1964.27.4.645.
2
THE EFFECT ON CRAYFISH MUSCLE OF IONTOPHORETICALLY APPLIED GLUTAMATE.离子电渗法施加谷氨酸对小龙虾肌肉的影响
J Physiol. 1964 Mar;170(2):296-317. doi: 10.1113/jphysiol.1964.sp007332.
3
Crayfish vas deferens: contractions in response to L-glutamate and gamma-aminobutyrate.小龙虾输精管：对L-谷氨酸和γ-氨基丁酸的反应性收缩
Comp Gen Pharmacol. 1971 Mar;2(5):93-8. doi: 10.1016/0010-4035(71)90073-5.
4
5
Spinal interneurone excitation by conformationally restricted analogues of L-glutamic acid.L-谷氨酸构象受限类似物对脊髓中间神经元的兴奋作用。
Nature. 1974 Apr 26;248(5451):804-5. doi: 10.1038/248804a0.
6
Glutamate antagonists at a crayfish neuromuscular junction.小龙虾神经肌肉接头处的谷氨酸拮抗剂。
Nature. 1974 Apr 5;248(448):533-5. doi: 10.1038/248533a0.
7
The site of action of ibotenic acid and the identification of two populations of glutamate receptors on insect muscle-fibres.鹅膏蕈氨酸的作用位点以及昆虫肌纤维上两类谷氨酸受体的鉴定。
Comp Gen Pharmacol. 1973 Dec;4(16):333-50. doi: 10.1016/0010-4035(73)90045-1.
8
A new potent excitant, quisqualic acid: effects on crayfish neuromuscular junction.一种新的强效兴奋剂——喹啉酸：对小龙虾神经肌肉接头的影响。
Neuropharmacology. 1974 Jul;13(7):665-72. doi: 10.1016/0028-3908(74)90056-2.
9
Chemical transmission in invertebrate central nervous systems and neuromuscular junctions.无脊椎动物中枢神经系统和神经肌肉接头中的化学传递。
Physiol Rev. 1973 Jan;53(1):1-119. doi: 10.1152/physrev.1973.53.1.1.
10
Pharmacological studies on a locust neuromuscular preparation.蝗虫神经肌肉标本的药理学研究。
J Exp Biol. 1974 Oct;61(2):421-42. doi: 10.1242/jeb.61.2.421.
Zotero 插件