Tìm theo
Anileridine
Các tên gọi khác (9 ) :
  • 1-[2-(4-Aminophenyl)ethyl]-4-phenyl-4-piperidinecarboxlic acid ethyl ester
  • Anileridina
  • Anileridinum
  • Ethyl 1-(2-(4-aminophenyl)ethyl)-4-phenyl-4-piperidinecarboxylate
  • ethyl 1-(4-aminophenethyl)-4-phenylisonipecotate
  • Ethyl 1-(P-aminophenethyl)-4-phenylisonipecotate
  • N-(beta-(P-Aminophenyl)ethyl)-4-phenyl-4-carbethoxypiperidine
  • N-beta-(P-Aminophenyl)ethylnormeperidine
  • N-β-(p-aminophenyl)ethylnormeperidine
Thuốc Gốc
Small Molecule
CAS: 144-14-9
ATC: N01AH05
CTHH: C22H28N2O2
PTK: 352.4699
Anileridine is a synthetic opioid and strong analgesic medication. It is a narcotic pain reliever used to treat moderate to severe pain. Narcotic analgesics act in the central nervous system (CNS) to relieve pain. Some of their side effects are also caused by actions in the CNS.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C22H28N2O2
Phân tử khối
352.4699
Monoisotopic mass
352.21507815
InChI
InChI=1S/C22H28N2O2/c1-2-26-21(25)22(19-6-4-3-5-7-19)13-16-24(17-14-22)15-12-18-8-10-20(23)11-9-18/h3-11H,2,12-17,23H2,1H3
InChI Key
InChIKey=LKYQLAWMNBFNJT-UHFFFAOYSA-N
IUPAC Name
ethyl 1-[2-(4-aminophenyl)ethyl]-4-phenylpiperidine-4-carboxylate
Traditional IUPAC Name
anileridine
SMILES
CCOC(=O)C1(CCN(CCC2=CC=C(N)C=C2)CC1)C1=CC=CC=C1
Độ tan chảy
275-277
Độ hòa tan
1.24e-02 g/l
logP
3.7
logS
-4.5
pKa (Strongest Basic)
8.88
PSA
55.56 Å2
Refractivity
106.55 m3·mol-1
Polarizability
40.98 Å3
Rotatable Bond Count
7
H Bond Acceptor Count
3
H Bond Donor Count
1
Physiological Charge
1
Number of Rings
3
Bioavailability
1
Rule of Five
true
Ghose Filter
true
MDDR-Like Rule
true
Dược Lực Học : Anileridine, a potent analgesic, is an analog of pethidine. Anileridine is useful for the relief of moderate to severe pain. It may also be used as an analgesic adjunct in general anesthesia in the same manner as meperidine to reduce the amount of anesthetic needed, to facilitate relaxation, and to reduce laryngospasm. In addition, anileridine exerts mild antihistaminic, spasmolytic and antitussive effects. Anileridine's main pharmacologic action is exerted on the CNS. Respiratory depression, when it occurs, is of shorter duration than that seen with morphine or meperidine when equipotent analgesic doses are used.
Cơ Chế Tác Dụng : Anileridine is a synthetic opioid and strong analgesic medication. It is a narcotic pain reliever used to treat moderate to severe pain. Narcotic analgesics act in the central nervous system (CNS) to relieve pain. Some of their side effects are also caused by actions in the CNS. 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 such as anileridine 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.
Dược Động Học :
▧ Absorption :
Anileridine is absorbed by all routes of administration.
▧ Protein binding :
> 95%
▧ Metabolism :
Hepatic
Độc Tính : Symptoms of overexposure include dizziness, perspiration, a feeling of warmth, dry mouth, visual difficulty, itching, euphoria, restlessness, nervousness and excitement have been reported.
Chỉ Định : For treatment and management of pain (systemic) and for use as an anesthesia adjunct.
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Sản phẩm biệt dược : Apodol
  • Công ty : Merck
    Sản phẩm biệt dược : Leritine
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00913
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=8944
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46505199
ChemSpider
http://www.chemspider.com/Chemical-Structure.8600.html
PharmGKB
http://www.pharmgkb.org/drug/PA164768817
Wikipedia
http://en.wikipedia.org/wiki/Anileridine
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