Tìm theo
Carfentanil
Thuốc Gốc
Small Molecule
CAS: 59708-52-0
CTHH: C24H30N2O3
PTK: 394.5066
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C24H30N2O3
Phân tử khối
394.5066
Monoisotopic mass
394.225642836
InChI
InChI=1S/C24H30N2O3/c1-3-22(27)26(21-12-8-5-9-13-21)24(23(28)29-2)15-18-25(19-16-24)17-14-20-10-6-4-7-11-20/h4-13H,3,14-19H2,1-2H3
InChI Key
InChIKey=YDSDEBIZUNNPOB-UHFFFAOYSA-N
IUPAC Name
methyl 1-(2-phenylethyl)-4-(N-phenylpropanamido)piperidine-4-carboxylate
Traditional IUPAC Name
carfentanil
SMILES
CCC(=O)N(C1=CC=CC=C1)C1(CCN(CCC2=CC=CC=C2)CC1)C(=O)OC
Độ hòa tan
2.59e-02 g/l
logP
3.67
logS
-4.2
pKa (Strongest Basic)
8.05
PSA
49.85 Å2
Refractivity
114.38 m3·mol-1
Polarizability
44.6 Å3
Rotatable Bond Count
8
H Bond Acceptor Count
3
H Bond Donor Count
0
Physiological Charge
1
Number of Rings
3
Bioavailability
1
Rule of Five
true
Ghose Filter
true
MDDR-Like Rule
true
Dược Lực Học : Carfentanil acts primarily on the mu (some kappa and delta) opioid receptors as an agonist. It will induce similar effects of analgesia as other opioids, however, due to its potency, it will also induce strong side effects such as sedation. Consequently, that is why it is used as a tranquilizer for large animals. Carfentanil interacts predominately with the opioid mu-receptor. These mu-binding sites are discretely distributed in the brain, spinal cord, and other tissues. It exerts its principal pharmacologic effects on the central nervous system. Its primary actions of therapeutic value are analgesia and sedation. Carfentanil also depresses the respiratory centers, depresses the cough reflex, and constricts the pupils.
Cơ Chế Tác Dụng : Carfentanil binds very strongly to mu opioid receptors and acts as a competitive agonist. Opiate receptors are coupled with G-protein receptors and function as both positive and negative regulators of synaptic transmission via G-proteins that activate effector proteins. Binding of the opiate stimulates the exchange of GTP for GDP on the G-protein complex. As the effector system is adenylate cyclase and cAMP located at the inner surface of the plasma membrane, opioids decrease intracellular cAMP by inhibiting adenylate cyclase. Subsequently, the release of nociceptive neurotransmitters such as substance P, GABA, dopamine, acetylcholine and noradrenaline is inhibited. Opioids also inhibit the release of vasopressin, somatostatin, insulin and glucagon. Opioids close N-type voltage-operated calcium channels (OP2-receptor agonist) and open calcium-dependent inwardly rectifying potassium channels (OP3 and OP1 receptor agonist). This results in hyperpolarization and reduced neuronal excitability.
Chỉ Định : Carfentanil is similar (but more potent) to the opioid analgesic fentanyl. It is used as a tranquilizer for large animals.
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01535
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=62156
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46505501
ChemSpider
http://www.chemspider.com/Chemical-Structure.55986.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50012477
Wikipedia
http://en.wikipedia.org/wiki/Carfentanil
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