Tìm theo
Cyclopentolate
Các tên gọi khác (14 ) :
  • (+-)-Cyclopentolate
  • (±)-cyclopentolate
  • 1-Hydroxy-alpha-phenylcyclopentaneacetic acid 2-(dimethylamino)ethyl ester
  • 2-(dimethylamino)Ethyl 1-hydroxy-alpha-phenylcyclopentaneacetate
  • 2-(dimethylamino)Ethyl 2-(1-hydroxycyclopentyl)-2-phenylacetate
  • 2-Phenyl-2-(1-hydroxycyclopentyl)ethanoic acid beta-(dimethylamino)ethyl ester
  • alpha-(1-Hydroxycyclopentyl)benzeneacetic acid 2-(dimethylamino)ethyl ester
  • beta-(dimethylamino)Ethyl (1-hydroxycyclopentyl)phenylacetate
  • beta-Dimethylaminoethyl (1-hydroxycyclopentyl)phenylacetate
  • Ciclopentolato
  • Cyclopentolate
  • Cyclopentolatum
  • α-(1-hydroxycyclopentyl)benzeneacetic acid 2-(dimethylamino)ethyl ester
  • β-dimethylaminoethyl (1-hydroxycyclopentyl)phenylacetate
muscarinic antagonists, parasympatholytics, mydriatics
Thuốc Gốc
Small Molecule
CAS: 512-15-2
ATC: S01FA04
ĐG : Akorn Inc. , http://www.akorn.com
CTHH: C17H25NO3
PTK: 291.3853
A parasympatholytic anticholinergic used solely to obtain mydriasis or cycloplegia. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
Phân tử khối
291.3853
Monoisotopic mass
291.183443671
InChI
InChI=1S/C17H25NO3/c1-18(2)12-13-21-16(19)15(14-8-4-3-5-9-14)17(20)10-6-7-11-17/h3-5,8-9,15,20H,6-7,10-13H2,1-2H3
InChI Key
InChIKey=SKYSRIRYMSLOIN-UHFFFAOYSA-N
IUPAC Name
2-(dimethylamino)ethyl 2-(1-hydroxycyclopentyl)-2-phenylacetate
Traditional IUPAC Name
(+-)-cyclopentolate
SMILES
CN(C)CCOC(=O)C(C1=CC=CC=C1)C1(O)CCCC1
Độ tan chảy
134-136
Độ hòa tan
1.50e+00 g/l
logP
2.4
logS
-2.3
pKa (strongest acidic)
14.19
pKa (Strongest Basic)
8.42
PSA
49.77 Å2
Refractivity
82.81 m3·mol-1
Polarizability
32.51 Å3
Rotatable Bond Count
7
H Bond Acceptor Count
3
H Bond Donor Count
1
Physiological Charge
1
Number of Rings
2
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Cyclopentolate is an anti-muscarinic in the same class as atropine and scopolamine. Cyclopentolate blocks the receptors in the muscles of the eye (muscarinic receptors). These receptors are involved controlling the pupil size and the shape of the lens. Cyclopentolate thus induces relaxation of the sphincter of the iris and the ciliary muscles. When applied topically to the eyes, it causes a rapid, intense cycloplegic and mydriatic effect that is maximal in 15 to 60 minutes; recovery usually occurs within 24 hours. The cycloplegic and mydriatic effects are slower in onset and longer in duration in patients who have dark pigmented irises.
Cơ Chế Tác Dụng : A parasympatholytic anticholinergic used solely to obtain mydriasis or cycloplegia. [PubChem] By blocking muscarinic receptors, cyclopentolate produces dilatation of the pupil (mydriasis) and prevents the eye from accommodating for near vision (cycloplegia).
Dược Động Học :
▧ Absorption :
Absorbed following ophthalmic administration.
Độc Tính : Oral LD50 in the rat is 4000 mg/kg and 960 mg/kg in the mouse. Symptoms of overdose include tachycardia, dizziness, dry mouth, behavioral disturbances, uncoordination and drowsiness.
Chỉ Định : Used mainly to produce mydriasis and cycloplegia for diagnostic purposes.
Tương Tác Thuốc :
  • Tacrine The therapeutic effects of the central acetylcholinesterase inhibitor, Tacrine, and/or the anticholinergic, Cyclopentolate, may be reduced due to antagonism. The interaction may be beneficial when the anticholinergic action is a side effect. Monitor for decreased efficacy of both agents.
  • Triprolidine Triprolidine and Cyclopentolate, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Trospium Trospium and Cyclopentolate, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Liều Lượng & Cách Dùng : Liquid - Ophthalmic
Solution - Ophthalmic
Solution / drops - Ophthalmic
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
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