ガラミン
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)』「2013/04/03 20:30:19」(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 |
AHFS/Drugs.com |
International Drug Names |
Pregnancy cat. |
? |
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
|
InChI
-
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]
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)
|
|
Peripherally acting
(primarily antinicotinic,
NMJ block) |
Non-depolarizing
|
Curare alkaloids
|
- Alcuronium
- Dimethyltubocurarine
- Tubocurarine
|
|
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)
|
|
|
Depolarizing
|
- Choline derivatives: Suxamethonium (Succinylcholine)
- Polyalkylene derivatives: Hexamethonium
|
|
ACh release inhibitors
|
|
|
|
Centrally acting |
Carbamic acid esters
|
- Carisoprodol
- Cyclarbamate
- Difebarbamate
- Febarbamate
- Meprobamate
- Methocarbamol
- Phenprobamate
- Styramate
- Tybamate
|
|
Benzodiazepines
|
- Bentazepam
- Diazepam
- Clonazepam
- Lorazepam
- Nitrazepam
- Tetrazepam
|
|
Anticholinergics (Antimuscarinics)
|
- Cyclobenzaprine
- Orphenadrine
|
|
Other
|
- Baclofen
- Chlormezanone
- Chlorphenesin
- Chlorzoxazone
- Donepezil
- Eperisone
- Fenyramidol
- Flopropione
- Mephenesin
- Mephenoxalone
- Metaxalone
- Pridinol
- Promoxolane
- Quinine
- Thiocolchicoside
- Tizanidine
- Tolperisone
- Trazadone
|
|
|
Directly acting |
|
|
|
anat (h/n, u, t/d, a/p, l)/phys/devp/hist
|
noco (m, s, c)/cong (d)/tumr, sysi/epon, injr
|
|
|
|
|
Cholinergics
|
|
Receptor ligands
|
|
mAChR
|
- 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.)
|
|
nAChR
|
- 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
- Dimethyltubocurarine/Metocurine
- Dipyrandium
- Dizocilpine/MK-801
- Doxacurium
- Duador
- 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
|
|
|
|
Reuptake inhibitors
|
|
Plasmalemmal
|
CHT Inhibitors
|
- Hemicholinium-3/Hemicholine
- Triethylcholine
|
|
|
Vesicular
|
|
|
|
|
Enzyme inhibitors
|
|
Anabolism
|
ChAT inhibitors
|
- 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
|
|
|
Catabolism
|
AChE inhibitors
|
|
|
BChE inhibitors
|
- Cymserine * Many of the acetylcholinesterase inhibitors listed above act as butyrylcholinesterase inhibitors.
|
|
|
|
|
Others
|
|
Precursors
|
- Choline (Lecithin)
- Citicoline
- Cyprodenate
- Dimethylethanolamine
- Glycerophosphocholine
- Meclofenoxate/Centrophenoxine
- Phosphatidylcholine
- Phosphatidylethanolamine
- Phosphorylcholine
- Pirisudanol
|
|
Cofactors
|
- Acetic acid
- Acetylcarnitine
- Acetyl-coA
- Vitamin B5 (Pantethine
- Pantetheine
- Panthenol)
|
|
Others
|
- Acetylcholine releasing agents: α-Latrotoxin
- β-Bungarotoxin; Acetylcholine release inhibitors: Botulinum toxin (Botox); Acetylcholinesterase reactivators: Asoxime
- Obidoxime
- Pralidoxime
|
|
|
|
UpToDate Contents
全文を閲覧するには購読必要です。 To read the full text you will need to subscribe.
English Journal
- 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
- Diadenosine tetraphosphate contributes to carbachol-induced tear secretion.
- Fonseca B1, Martínez-Águila A, Díaz-Hernández M, Pintor J.
- Purinergic signalling.Purinergic Signal.2015 Mar;11(1):87-93. doi: 10.1007/s11302-014-9434-3. Epub 2014 Nov 15.
- The purpose of this study is to investigate if the cholinergic stimulation by carbachol on tear secretion is a direct process or if it is also mediated by purinergic mechanisms. Experiments were performed in New Zealand male rabbits. The amount of tear secretion was measured with Schirmer's test and
- PMID 25398705
- Pharmacological evidence that 5-HT1A/1B/1D, α2-adrenoceptors and D2-like receptors mediate ergotamine-induced inhibition of the vasopressor sympathetic outflow in pithed rats.
- Villamil-Hernández MT1, Alcántara-Vázquez O1, Sánchez-López A1, Gutiérrez-Lara EJ1, Centurión D2.
- European journal of pharmacology.Eur J Pharmacol.2014 Oct 5;740:512-21. doi: 10.1016/j.ejphar.2014.06.036. Epub 2014 Jun 27.
- The sympathetic nervous system that innervates the peripheral circulation is regulated by several mechanisms/receptors. It has been reported that prejunctional 5-HT1A, 5-HT1B, 5-HT1D, D2-like receptors and α2-adrenoceptors mediate the inhibition of the vasopressor sympathetic outflow in pithed rats
- PMID 24975101
Japanese Journal
- 魚類の水晶体筋収縮に関与するムスカリン性受容体サブタイプの生理学的検討
- Chemically Modified Carbon Paste Electrode for Iodide Determination on the Basis of Cetyltrimethylammonium Iodide Ion-Pair.
- Application of a high-performance liquid chromatographic assay for the neuromuscular blocker gallamine to analysis of rat plasma, muscle and microdialysate samples
- Journal of chromatography. B, Biomedical sciences and applications 754(2), 467-475, 2001-04-25
- NAID 10012262862
Related Links
- Identification Name Gallamine Triethiodide Accession Number DB00483 (APRD00712) Type Small Molecule Groups Approved Description A synthetic nondepolarizing blocking drug. The actions of gallamine triethiodide are similar to ...
- Group: non-depolarizing muscle relaxant Injection: 40 mg (triethiodide)/ml in 2-ml ampoule General information Gallamine is a synthetic non-depolarizing neuromuscular blocking agent. Its effect becomes apparent within 2 minutes of ...
★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
[★]
ガラミントリエチオジド
- 関
- gallamine