ガラミントリエチオジド
- 関
- gallamine
WordNet
- neuromuscular blocking agent (trade name Flaxedil) used as a muscle relaxant in the administration of anesthesia (同)Flaxedil
Wikipedia preview
出典(authority):フリー百科事典『ウィキペディア(Wikipedia)』「2014/06/10 15:15:23」(JST)
[Wiki en表示]
Gallamine triethiodide
|
Systematic (IUPAC) name |
2,2’,2’’-[benzene-1,2,3-triyltris(oxy)]tris(N,N,N-triethylethanaminium) triiodide |
Clinical data |
Trade names |
Flaxedil |
AHFS/Drugs.com |
International Drug Names |
Legal status |
? |
Identifiers |
CAS number |
65-29-2 Y |
ATC code |
M03AC02 |
PubChem |
CID 6172 |
IUPHAR ligand |
356 |
DrugBank |
DB00483 |
ChemSpider |
5937 N |
UNII |
Q3254X40X2 Y |
KEGG |
D02292 Y |
ChEBI |
CHEBI:503442 Y |
ChEMBL |
CHEMBL1200993 N |
Chemical data |
Formula |
C30H60N3O3+3 · 3 I- (gallamine triethiodide)
C24H45N3O3 (gallamine) |
Mol. mass |
891.529 g/mol (gallamine triethiodide)
423.633 g/mol
(gallamine) |
SMILES
- [I-].[I-].[I-].O(c1c(OCC[N+](CC)(CC)CC)cccc1OCC[N+](CC)(CC)CC)CC[N+](CC)(CC)CC
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InChI
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InChI=1S/C24H45N3O3/c1-7-25(8-2)16-19-28-22-14-13-15-23(29-20-17-26(9-3)10-4)24(22)30-21-18-27(11-5)12-6/h13-15H,7-12,16-21H2,1-6H3 Y
Key:ICLWTJIMXVISSR-UHFFFAOYSA-N Y
|
N (what is this?) (verify) |
Gallamine triethiodide (Flaxedil) is a non-depolarising muscle relaxant.[1] It acts by combining with the cholinergic receptor sites in muscle and competitively blocking the transmitter action of acetylcholine.[2] Gallamine triethiodide has a parasympatholytic effect on the cardiac vagus nerve which causes tachycardia and occasionally hypertension. Very high doses cause histamine release.
Gallamine triethiodide is commonly used to stabilize muscle contractions during surgical procedures.
It was developed by Daniel Bovet in 1947.[3]
The pharmaceutical is no longer marketed in the United States, according to the FDA Orange Book.
References
- ^ "Webster's Online Dictionary - Flaxedil". Retrieved 2008-12-15.
- ^ "RxMed: Pharmaceutical Information - FLAXEDIL". Retrieved 2008-12-15.
- ^ Raghavendra T (July 2002). "Neuromuscular blocking drugs: discovery and development". J R Soc Med 95 (7): 363–7. doi:10.1258/jrsm.95.7.363. PMC 1279945. PMID 12091515.
Skeletal muscle relaxants (M03)
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|
Peripherally acting
(primarily antinicotinic,
NMJ block) |
Non-depolarizing
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Curare alkaloids
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- Alcuronium
- Dimethyltubocurarine
- Tubocurarine
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4° ammonium agents
|
- ultra-short duration: Gantacurium
- short duration: Mivacurium
- Chandonium
- intermediate duration: Atracurium
- Cisatracurium
- Fazadinium
- Rocuronium
- Vecuronium
- long duration: Doxacurium
- Dimethyltubocurarine
- Pancuronium
- Pipecuronium
- Laudexium
- Gallamine
- unsorted: Hexafluronium (Hexafluorenium)
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Depolarizing
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- Choline derivatives: Suxamethonium (Succinylcholine)
- Polyalkylene derivatives: Hexamethonium
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ACh release inhibitors
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Centrally acting |
Carbamic acid esters
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- Carisoprodol
- Cyclarbamate
- Difebarbamate
- Febarbamate
- Meprobamate
- Methocarbamol
- Phenprobamate
- Styramate
- Tybamate
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Benzodiazepines
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- Bromazepam
- Diazepam
- Clonazepam
- Flunitrazepam
- Lorazepam
- Nitrazepam
- Temazepam
- Tetrazepam
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Nonbenzodiazepines
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Thienodiazepines
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Quinazolines
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Anticholinergics (Antimuscarinics)
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- Cyclobenzaprine
- Orphenadrine
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Other
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- Arbaclofen placarbil
- Baclofen
- Chlormezanone
- Chlorphenesin
- Chlorzoxazone
- Donepezil
- Eperisone
- Fenyramidol
- Flopropione
- Gabapentin
- GHB
- Mephenesin
- Mephenoxalone
- Metaxalone
- Phenibut
- Pregabalin
- Pridinol
- Promoxolane
- Quinine
- Thiocolchicoside
- Tizanidine
- Tolperisone
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Directly acting |
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anat (h/n, u, t/d, a/p, l)/phys/devp/hist
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noco (m, s, c)/cong (d)/tumr, sysi/epon, injr
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Cholinergics
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Receptor ligands
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mAChR
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- Agonists: 77-LH-28-1
- AC-42
- AC-260,584
- Aceclidine
- Acetylcholine
- AF30
- AF150(S)
- AF267B
- AFDX-384
- Alvameline
- AQRA-741
- Arecoline
- Bethanechol
- Butyrylcholine
- Carbachol
- CDD-0034
- CDD-0078
- CDD-0097
- CDD-0098
- CDD-0102
- Cevimeline
- Choline
- cis-Dioxolane
- Ethoxysebacylcholine
- LY-593,039
- L-689,660
- LY-2,033,298
- McNA343
- Methacholine
- Milameline
- Muscarine
- NGX-267
- Ocvimeline
- Oxotremorine
- PD-151,832
- Pilocarpine
- RS86
- Sabcomeline
- SDZ 210-086
- Sebacylcholine
- Suberylcholine
- Talsaclidine
- Tazomeline
- Thiopilocarpine
- Vedaclidine
- VU-0029767
- VU-0090157
- VU-0152099
- VU-0152100
- VU-0238429
- WAY-132,983
- Xanomeline
- YM-796
Antagonists: 3-Quinuclidinyl Benzilate
- 4-DAMP
- Aclidinium Bromide
- Anisodamine
- Anisodine
- Atropine
- Atropine Methonitrate
- Benactyzine
- Benzatropine/Benztropine
- Benzydamine
- BIBN 99
- Biperiden
- Bornaprine
- CAR-226,086
- CAR-301,060
- CAR-302,196
- CAR-302,282
- CAR-302,368
- CAR-302,537
- CAR-302,668
- CS-27349
- Cyclobenzaprine
- Cyclopentolate
- Darifenacin
- DAU-5884
- Dimethindene
- Dexetimide
- DIBD
- Dicyclomine/Dicycloverine
- Ditran
- EA-3167
- EA-3443
- EA-3580
- EA-3834
- Etanautine
- Etybenzatropine/Ethylbenztropine
- Flavoxate
- Himbacine
- HL-031,120
- Ipratropium bromide
- J-104,129
- Hyoscyamine
- Mamba Toxin 3
- Mamba Toxin 7
- Mazaticol
- Mebeverine
- Methoctramine
- Metixene
- N-Ethyl-3-Piperidyl Benzilate
- N-Methyl-3-Piperidyl Benzilate
- Orphenadrine
- Otenzepad
- Oxybutynin
- PBID
- PD-102,807
- PD-0298029
- Phenglutarimide
- Phenyltoloxamine
- Pirenzepine
- Piroheptine
- Procyclidine
- Profenamine
- RU-47,213
- SCH-57,790
- SCH-72,788
- SCH-217,443
- Scopolamine/Hyoscine
- Solifenacin
- Telenzepine
- Tiotropium bromide
- Tolterodine
- Trihexyphenidyl
- Tripitamine
- Tropatepine
- Tropicamide
- WIN-2299
- Xanomeline
- Zamifenacin; Others: 1st Generation Antihistamines (Brompheniramine
- chlorphenamine
- cyproheptadine
- dimenhydrinate
- diphenhydramine
- doxylamine
- mepyramine/pyrilamine
- phenindamine
- pheniramine
- tripelennamine
- triprolidine, etc)
- Tricyclic Antidepressants (Amitriptyline
- doxepin
- trimipramine, etc)
- Tetracyclic Antidepressants (Amoxapine
- maprotiline, etc)
- Typical Antipsychotics (Chlorpromazine
- thioridazine, etc)
- Atypical Antipsychotics (Clozapine
- olanzapine, etc.)
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nAChR
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- Agonists: 5-HIAA
- A-84,543
- A-366,833
- A-582,941
- A-867,744
- ABT-202
- ABT-418
- ABT-560
- ABT-894
- Acetylcholine
- Altinicline
- Anabasine
- Anatoxin-a
- AR-R17779
- Butinoline
- Butyrylcholine
- Carbachol
- Choline
- Cotinine
- Cytisine
- Decamethonium
- Desformylflustrabromine
- Dianicline
- Dimethylphenylpiperazinium
- Epibatidine
- Epiboxidine
- Ethanol
- Ethoxysebacylcholine
- EVP-4473
- EVP-6124
- Galantamine
- GTS-21
- Ispronicline
- Lobeline
- MEM-63,908/RG-3487
- Nicotine
- NS-1738
- PHA-543,613
- PHA-709,829
- PNU-120,596
- PNU-282,987
- Pozanicline
- Rivanicline
- RJR-2429
- Sazetidine A
- Sebacylcholine
- SIB-1508Y
- SIB-1553A
- SSR-180,711
- Suberylcholine
- Suxamethonium/Succinylcholine
- TC-1698
- TC-1734
- TC-1827
- TC-2216
- TC-5214
- TC-5619
- TC-6683
- Tebanicline
- Tropisetron
- UB-165
- Varenicline
- WAY-317,538
- XY-4083
Antagonists: 18-Methoxycoronaridine
- α-Bungarotoxin
- α-Conotoxin
- Alcuronium
- Amantadine
- Anatruxonium
- Atracurium
- Bupropion
- Chandonium
- Chlorisondamine
- Cisatracurium
- Coclaurine
- Coronaridine
- Dacuronium
- Decamethonium
- Dextromethorphan
- Dextropropoxyphene
- Dextrorphan
- Diadonium
- DHβE
- Dihydrochandonium
- Dimethyltubocurarine/Metocurine
- Dipyrandium
- Dizocilpine/MK-801
- Doxacurium
- Esketamine
- Fazadinium
- Gallamine
- Hexafluronium
- Hexamethonium/Benzohexonium
- Ibogaine
- Isoflurane
- Ketamine
- Kynurenic acid
- Laudexium/Laudolissin
- Levacetylmethadol
- Malouetine
- Mecamylamine
- Memantine
- Methadone (Levomethadone)
- Methorphan/Racemethorphan
- Methyllycaconitine
- Metocurine
- Mivacurium
- Morphanol/Racemorphan
- Neramexane
- Nitrous Oxide
- Pancuronium
- Pempidine
- Pentamine
- Pentolinium
- Phencyclidine
- Pipecuronium
- Radafaxine
- Rapacuronium
- Rocuronium
- Surugatoxin
- Thiocolchicoside
- Toxiferine
- Trimethaphan
- Tropeinium
- Tubocurarine
- Vecuronium
- Xenon
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Reuptake inhibitors
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Plasmalemmal
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CHT Inhibitors
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- Hemicholinium-3/Hemicholine
- Triethylcholine
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Vesicular
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Enzyme inhibitors
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Anabolism
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ChAT inhibitors
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- 1-(-Benzoylethyl)pyridinium
- 2-(α-Naphthoyl)ethyltrimethylammonium
- 3-Chloro-4-stillbazole
- 4-(1-Naphthylvinyl)pyridine
- Acetylseco hemicholinium-3
- Acryloylcholine
- AF64A
- B115
- BETA
- CM-54,903
- N,N-Dimethylaminoethylacrylate
- N,N-Dimethylaminoethylchloroacetate
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Catabolism
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AChE inhibitors
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BChE inhibitors
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- Cymserine * Many of the acetylcholinesterase inhibitors listed above act as butyrylcholinesterase inhibitors.
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Others
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Precursors
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- Choline (Lecithin)
- Citicoline
- Cyprodenate
- Dimethylethanolamine
- Glycerophosphocholine
- Meclofenoxate/Centrophenoxine
- Phosphatidylcholine
- Phosphatidylethanolamine
- Phosphorylcholine
- Pirisudanol
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Cofactors
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- Acetic acid
- Acetylcarnitine
- Acetyl-coA
- Vitamin B5 (Pantethine
- Pantetheine
- Panthenol)
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Others
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- Acetylcholine releasing agents: α-Latrotoxin
- β-Bungarotoxin; Acetylcholine release inhibitors: Botulinum toxin (Botox); Acetylcholinesterase reactivators: Asoxime
- Obidoxime
- Pralidoxime
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English Journal
- Carbachol dimers as homobivalent modulators of muscarinic receptors.
- Matucci R1, Nesi M2, Martino MV3, Bellucci C3, Manetti D3, Ciuti E2, Mazzolari A4, Dei S3, Guandalini L3, Teodori E3, Vistoli G4, Romanelli MN3.
- Biochemical pharmacology.Biochem Pharmacol.2016 Mar 17. pii: S0006-2952(16)00179-9. doi: 10.1016/j.bcp.2016.03.012. [Epub ahead of print]
- A series of homodimers of the well-known cholinergic agonist carbachol have been synthesized, showing the two agonist units symmetrically connected through a methylene chain of variable length. The new compounds have been tested on the five cloned muscarinic receptors (hM1-5) expressed in CHO cells
- PMID 26996304
- Further evidence for the role of histamine H3, but not H1, H2 or H4, receptors in immepip-induced inhibition of the rat cardioaccelerator sympathetic outflow.
- Pinacho-García M1, Marichal-Cancino BA2, Villalón CM3.
- European journal of pharmacology.Eur J Pharmacol.2016 Feb 15;773:85-92. doi: 10.1016/j.ejphar.2016.01.014. Epub 2016 Jan 27.
- Since histamine H3 and H4 receptors are coupled to heterotrimeric Gi/o proteins, a signal transduction pathway associated with inhibition of neurotransmitter release, the present study has investigated the inhibition of the rat cardioaccelerator sympathetic outflow induced by the H3/H4 receptor agon
- PMID 26826593
- Pharmacological evidence that histamine H3 receptors inhibit the vasodepressor responses by selective stimulation of the rat perivascular sensory CGRPergic outflow.
- Manrique-Maldonado G1, Altamirano-Espinoza AH2, Marichal-Cancino BA3, Rivera-Mancilla E4, Avilés-Rosas V5, Villalón CM6.
- European journal of pharmacology.Eur J Pharmacol.2015 May 5;754:25-31. doi: 10.1016/j.ejphar.2015.02.017. Epub 2015 Feb 19.
- This study has investigated whether pharmacological activation of Gi/o coupled histamine H3/H4 receptors inhibits the rat vasodepressor sensory outflow. For this purpose, 100 male Wistar rats were pithed, artificially ventilated and pretreated (i.v.) with: 25mg/kg gallamine, 2mg/kg/min hexamethonium
- PMID 25704614
Japanese Journal
- 橋呼吸調節中枢の機能 ―特に延髄腹側呼吸性ニューロン群(VRG)の橋への軸索投射様式について―
- 小林 信義
- 1990-08-01
- … Adult cats were anesthetized with pentobarbital and immobilized with gallamine triethiodide. …
- NAID 120001796782
- Two Types of Gastric Excitatory Responses to Stimulation of the Vagal Trunk in Cats: Efferent and Afferent Responses
- TSUBOMURA Tatsuyuki,KURAHASHI Kazuyoshi,OKAMOTO Toshihiro,FUJIWARA Motohatsu
- The Japanese Journal of Pharmacology 47(2), 115-122, 1988
- … Experiments were performed on cats anesthetized with pentobarbital sodium and gallamine triethiodide. …
- NAID 130000832188
Related Links
- Gallamine triethiodide (Flaxedil) is a non-depolarising muscle relaxant. It acts by combining with the cholinergic receptor sites in muscle and competitively blocking the transmitter action of acetylcholine. Gallamine triethiodide has a ...
- 化学式, C30H60N3O3+3 · 3 I- (gallamine triethiodide) C24H45N3O3 (gallamine). ガラミン(英:gallamine)とは筋弛緩薬の1つ。終板のニコチン受容体へのアセチルコリン の結合を競合的に拮抗することにより脱分極を阻害する。その結果、活動電位が発生 ...
Related Pictures
★リンクテーブル★
[★]
- 英
- gallamine、gallamine triethiodide
- 関
- ガラミントリエチオジド、三ヨウ化エチルガラミン
[★]
- 英
- gallamine triethiodide
- 関
- ガラミン