Tìm theo
Dapoxetine
Các tên gọi khác (2) :
  • Dapoxetina
  • Dapoxetinum
serotonin uptake inhibitors
Thuốc Gốc
Small Molecule
CAS: 119356-77-3
CTHH: C21H23NO
PTK: 305.4134
Dapoxetine is a selective serotonin reuptake inhibitor, for the treatment of premature ejaculation. In a phase II proof-of-concept study conducted by PPD, dapoxetine demonstrated a statistically significant increase in ejaculatory latency when compared to placebo. Alza submitted a NDA to the FDA for dapoxetine for the treatment of premature ejaculation in December 2004. In October 2005, the company received a FDA Non-Approvable letter from the FDA, at which time they planned to work with regulators to address outstanding questions.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C21H23NO
Phân tử khối
305.4134
Monoisotopic mass
305.177964363
InChI
InChI=1S/C21H23NO/c1-22(2)20(18-10-4-3-5-11-18)15-16-23-21-14-8-12-17-9-6-7-13-19(17)21/h3-14,20H,15-16H2,1-2H3/t20-/m0/s1
InChI Key
InChIKey=USRHYDPUVLEVMC-FQEVSTJZSA-N
IUPAC Name
dimethyl[(1S)-3-(naphthalen-1-yloxy)-1-phenylpropyl]amine
Traditional IUPAC Name
dapoxetine
SMILES
CN(C)[C@@H](CCOC1=CC=CC2=CC=CC=C12)C1=CC=CC=C1
Độ hòa tan
8.37e-04 g/l
logP
4.67
logS
-5.6
pKa (Strongest Basic)
9.04
PSA
12.47 Å2
Refractivity
96.14 m3·mol-1
Polarizability
35 Å3
Rotatable Bond Count
6
H Bond Acceptor Count
2
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 : Dapoxetine is a selective serotonin reuptake inhibitor currently undergoing trials through Alza (under license from GenuPro, a collaboration between Eli Lilly and PPD). Dapoxetine is a short-acting SSRI drug currently being considered for approval by the Food and Drug Administration (FDA) for the treatment of premature ejaculation in men, which would make it the first drug approved for such treatment. Despite two clinical trials finished in 2006, experts doubt it will be approved by the FDA soon because SSRIs come with undesirable side-effects after long-term use, such as psychiatric problems, dermatological reactions, increase in body weight, lower sex-drive, nausea, headache, upset stomach and weakness, thus not significantly outweighing the benefit of premature ejaculation medication versus the risks. By contrast with SSRIs approved for depression, which take 2 weeks or longer to reach steady-state concentration, dapoxetine has a unique pharmacokinetic profile, with a short time to maximum serum concentration (about 1 h) and rapid elimination (initial half-life of 1-2 h).
Cơ Chế Tác Dụng : Dapoxetine is a selective serotonin reuptake inhibitor, for the treatment of premature ejaculation. In a phase II proof-of-concept study conducted by PPD, dapoxetine demonstrated a statistically significant increase in ejaculatory latency when compared to placebo. Alza submitted a NDA to the FDA for dapoxetine for the treatment of premature ejaculation in December 2004. In October 2005, the company received a FDA Non-Approvable letter from the FDA, at which time they planned to work with regulators to address outstanding questions. The drug's mechanism of action is thought to be related to inhibition of neuronal reuptake of serotonin and subsequent potentiation of serotonin activity. The central ejaculatory neural circuit comprises spinal and cerebral areas that form a highly interconnected network. The sympathetic, parasympathetic, and somatic spinal centers, under the influence of sensory genital and cerebral stimuli integrated and processed at the spinal cord level, act in synergy to command physiologic events occurring during ejaculation. Experimental evidence indicates that serotonin (5-HT), throughout brain descending pathways, exerts an inhibitory role on ejaculation. To date, three 5-HT receptor subtypes (5-HT(1A), 5-HT(1B), and 5-HT(2C)) have been postulated to mediate 5-HT's modulating activity on ejaculation.
Dược Động Học :
▧ Absorption :
Rapidly absorbed.
▧ Half Life :
Initial half-life of 1-2 hours.
Chỉ Định : For the treatment of premature ejaculation.
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB04884
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=71353
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=14849767
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D03649
ChemSpider
http://www.chemspider.com/Chemical-Structure.64453.html
Wikipedia
http://en.wikipedia.org/wiki/Dapoxetine
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