Tìm theo
Procyclidine
Các tên gọi khác (7 ) :
  • 1-cyclohexyl-1-phenyl-3-pyrrolidin-1-yl-propan-1-ol hydrochloride
  • 1-Cyclohexyl-1-phenyl-3-pyrrolidino-1-propanol
  • Prociclidina
  • Procyclidin
  • Procyclidine
  • Procyclidinum
  • Tricyclamol
Thuốc chống Parkinson
Thuốc Gốc
Small Molecule
CAS: 77-37-2
ATC: N04AA04
CTHH: C19H29NO
PTK: 287.4397
A muscarinic antagonist that crosses the blood-brain barrier and is used in the treatment of drug-induced extrapyramidal disorders and in parkinsonism. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
Phân tử khối
287.4397
Monoisotopic mass
287.224914555
InChI
InChI=1S/C19H29NO/c21-19(17-9-3-1-4-10-17,18-11-5-2-6-12-18)13-16-20-14-7-8-15-20/h1,3-4,9-10,18,21H,2,5-8,11-16H2
InChI Key
InChIKey=WYDUSKDSKCASEF-UHFFFAOYSA-N
IUPAC Name
1-cyclohexyl-1-phenyl-3-(pyrrolidin-1-yl)propan-1-ol
Traditional IUPAC Name
procyclidine
SMILES
OC(CCN1CCCC1)(C1CCCCC1)C1=CC=CC=C1
Độ tan chảy
86 °C
Độ hòa tan
Moderately soluble in water, ~ 30 mg/ml
logP
4.2
logS
-4.5
pKa (strongest acidic)
13.84
pKa (Strongest Basic)
9.45
PSA
23.47 Å2
Refractivity
88.6 m3·mol-1
Polarizability
34.43 Å3
Rotatable Bond Count
5
H Bond Acceptor Count
2
H Bond Donor Count
1
Physiological Charge
1
Number of Rings
3
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Procyclidine has an atropine-like action on parasympathetic-innervated peripheral structures including smooth muscle. It's antispasmodic effects are thought to be related to the blockage of central cholinergic receptors M1, M2 and M4. It is used to treat symptomatic Parkinsonism and extrapyramidal dysfunction caused by antipsychotic agents.
Cơ Chế Tác Dụng : A muscarinic antagonist that crosses the blood-brain barrier and is used in the treatment of drug-induced extrapyramidal disorders and in parkinsonism. [PubChem] The mechanism of action is unknown. It is thought that Procyclidine acts by blocking central cholinergic receptors, and thus balancing cholinergic and dopaminergic activity in the basal ganglia. Many of its effects are due to its pharmacologic similarities with atropine. Procyclidine exerts an antispasmodic effect on smooth muscle, and may produce mydriasis and reduction in salivation.
Dược Động Học :

▧ Protein binding :
Approximately 100% bound to albumin.
Độc Tính : LD50=60 mg/kg (IV in mice)
Chỉ Định : For the treatment of all forms of Parkinson's Disease, as well as control of extrapyramidal reactions induced by antipsychotic agents.
Tương Tác Thuốc :
  • Donepezil Possible antagonism of action
  • Galantamine Possible antagonism of action
  • Haloperidol The anticholinergic increases the risk of psychosis and tardive dyskinesia
  • Tacrine The therapeutic effects of the central acetylcholinesterase inhibitor, Tacrine, and/or the anticholinergic, Procyclidine, 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.
  • Trimethobenzamide Trimethobenzamide and Procyclidine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Triprolidine Triprolidine and Procyclidine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Trospium Trospium and Procyclidine, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Liều Lượng & Cách Dùng : Elixir - Oral
Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
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