Tìm theo
Metocurine Iodide
Các tên gọi khác (10 ) :
  • (+)-O,O'-Dimethylchondrocurarine Di-iodide
  • Dimethyl Tubocurarine Iodide
  • Dimethyltubocurarine Iodide
  • Dimetiltubocurarinio, ioduro de
  • Metocurine iodide
  • Metocurini Iodidum
  • Metokuriinijodidi
  • Metokurinjodid
  • Metubine iodide
  • Trimethyltubocurarine Iodide
Thuốc Gốc
Small Molecule
CAS: 7601-55-0
ATC: M03AA04
CTHH: C40H48I2N2O6
PTK: 906.6279
Metocurine iodide is a benzylisoquinolinium competitive nondepolarizing neuromuscular blocking agent. It is used as an anesthesia adjunct to induce skeletal muscle relaxation and to reduce the intensity of muscle contractions in convulsive therapy Metocurine iodide has a moderate risk of inducing histamine release and has some ganglion blocking activity. Metocurine iodide can be used most advantageously if muscle twitch response to peripheral nerve stimulation is monitored to assess degree of muscle relaxation. Metocurine Iodide is no longer available on the US market.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C40H48I2N2O6
Phân tử khối
906.6279
Monoisotopic mass
906.160174118
InChI
InChI=1S/C40H48N2O6.2HI/c1-41(2)17-15-27-22-34(44-6)36-24-30(27)31(41)19-25-9-12-29(13-10-25)47-40-38-28(23-37(45-7)39(40)46-8)16-18-42(3,4)32(38)20-26-11-14-33(43-5)35(21-26)48-36;;/h9-14,21-24,31-32H,15-20H2,1-8H3;2*1H/q+2;;/p-2/t31-,32+;;/m0../s1
InChI Key
InChIKey=DIGFQJFCDPKEPF-OIUSMDOTSA-L
IUPAC Name
(1S,16R)-9,10,21,25-tetramethoxy-15,15,30,30-tetramethyl-7,23-dioxa-15,30-diazaheptacyclo[22.6.2.2^{3,6}.1^{8,12}.1^{18,22}.0^{27,31}.0^{16,34}]hexatriaconta-3,5,8,10,12(34),18(33),19,21,24(32),25,27(31),35-dodecaene-15,30-diium diiodide
Traditional IUPAC Name
(1S,16R)-9,10,21,25-tetramethoxy-15,15,30,30-tetramethyl-7,23-dioxa-15,30-diazaheptacyclo[22.6.2.2^{3,6}.1^{8,12}.1^{18,22}.0^{27,31}.0^{16,34}]hexatriaconta-3,5,8,10,12(34),18(33),19,21,24(32),25,27(31),35-dodecaene-15,30-diium diiodide
SMILES
[I-].[I-].[H][C@@]12CC3=CC=C(OC4=C5C(CC[N+](C)(C)[C@]5([H])CC5=CC(OC6=C(OC)C=C(CC[N+]1(C)C)C2=C6)=C(OC)C=C5)=CC(OC)=C4OC)C=C3
Độ tan chảy
267-270
Độ hòa tan
1.23e-04 g/l
logP
-1.8
logS
-6.9
pKa (strongest acidic)
12.99
pKa (Strongest Basic)
-4.3
PSA
55.38 Å2
Refractivity
211.94 m3·mol-1
Polarizability
73.46 Å3
Rotatable Bond Count
4
H Bond Acceptor Count
4
H Bond Donor Count
0
Physiological Charge
2
Number of Rings
7
Bioavailability
1
Dược Lực Học : Metocurine iodide is a benzylisoquinolinium competitive nondepolarizing neuromuscular blocking agent. Metocurine iodide has a moderate risk of inducing histamine release and has some ganglion blocking activity. Metocurine iodide can be used most advantageously if muscle twitch response to peripheral nerve stimulation is monitored to assess degree of muscle relaxation. As with other nondepolarizing neuromuscular blockers, the time to onset of paralysis decreases and the duration of maximum effect increases with increasing doses of metocurine iodide. Repeated administration of maintenance doses of metocurine iodide has no cumulative effect on the duration of neuromuscular block if recovery is allowed to begin prior to repeat dosing. Moreover, the time needed to recover from repeat doses does not change with additional doses. Repeat doses can therefore be administered at relatively regular intervals with predictable results.
Cơ Chế Tác Dụng : Metocurine iodide is a benzylisoquinolinium competitive nondepolarizing neuromuscular blocking agent. It is used as an anesthesia adjunct to induce skeletal muscle relaxation and to reduce the intensity of muscle contractions in convulsive therapy Metocurine iodide has a moderate risk of inducing histamine release and has some ganglion blocking activity. Metocurine iodide can be used most advantageously if muscle twitch response to peripheral nerve stimulation is monitored to assess degree of muscle relaxation. Metocurine Iodide is no longer available on the US market. Metocurine iodide antagonizes the neurotransmitter action of acetylcholine by binding competitively with cholinergic receptor sites on the motor end-plate. This antagonism is inhibited, and neuromuscular block reversed, by acetylcholinesterase inhibitors such as neostigmine, edrophonium, and pyridostigmine.
Dược Động Học :

▧ Protein binding :
35% in plasma
▧ Half Life :
3 to 4 hours
Độc Tính : Excessive doses can be expected to produce enhanced pharmacological effects. Overdosage may increase the risk of histamine release and cardiovascular effects, especially hypotension.
Chỉ Định : For use as an anesthesia adjunct to induce skeletal muscle relaxation and to reduce the intensity of muscle contractions in convulsive therapy.
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00416
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=24244
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46507773
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00761
ChemSpider
http://www.chemspider.com/Chemical-Structure.22666.html
PharmGKB
http://www.pharmgkb.org/drug/PA164749507
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