Tìm theo
Bupranolol
Các tên gọi khác (5 ) :
  • b-1312 [As hydrochloride]
  • Bupranol
  • Bupranolol
  • Bupranolol hcl
  • KL-255 [as hydrochloride]
antihypertensive agents, anti arrhythmia agents, adrenergic beta antagonists
Thuốc Gốc
Small Molecule
CAS: 23284-25-5
ATC: C07AA19
CTHH: C14H22ClNO2
PTK: 271.783
Bupranolol is a non-selective beta blocker without intrinsic sympathomimetic activity (ISA), but with strong membrane stabilizing activity. Its potency is similar to "propranolol":http://www.drugbank.ca/drugs/DB00571.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C14H22ClNO2
Phân tử khối
271.783
Monoisotopic mass
271.13390666
InChI
InChI=1S/C14H22ClNO2/c1-10-5-6-12(15)13(7-10)18-9-11(17)8-16-14(2,3)4/h5-7,11,16-17H,8-9H2,1-4H3
InChI Key
InChIKey=HQIRNZOQPUAHHV-UHFFFAOYSA-N
IUPAC Name
tert-butyl[3-(2-chloro-5-methylphenoxy)-2-hydroxypropyl]amine
Traditional IUPAC Name
bupranolol
SMILES
CC1=CC(OCC(O)CNC(C)(C)C)=C(Cl)C=C1
Độ hòa tan
1.43e-01 g/l
logP
2.99
logS
-3.3
pKa (strongest acidic)
14.09
pKa (Strongest Basic)
9.76
PSA
41.49 Å2
Refractivity
74.86 m3·mol-1
Polarizability
30.35 Å3
Rotatable Bond Count
6
H Bond Acceptor Count
3
H Bond Donor Count
2
Physiological Charge
1
Number of Rings
1
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Bupranolol is a competitive, nonselective beta-blocker similar to propanolol without intrinsic sympathomimetic activity.
Cơ Chế Tác Dụng : Bupranolol is a non-selective beta blocker without intrinsic sympathomimetic activity (ISA), but with strong membrane stabilizing activity. Its potency is similar to "propranolol":http://www.drugbank.ca/drugs/DB00571. Bupranolol competes with sympathomimetic neurotransmitters such as catecholamines for binding at beta(1)-adrenergic receptors in the heart, inhibiting sympathetic stimulation. This results in a reduction in resting heart rate, cardiac output, systolic and diastolic blood pressure, and reflex orthostatic hypotension.
Dược Động Học :
▧ Absorption :
Quickly and completely absorbed from the gut with less than 10% oral bioavailability.
▧ Protein binding :
76%
▧ Metabolism :
Over 90% undergo first-pass metabolism. The main metabolite is carboxybupranolol, 4-chloro-3-[3-(1,1-dimethylethylamino)-2-hydroxy-propyloxy]benzoic acid, of which 88% are eliminated renally within 24 hours.
▧ Half Life :
2-4 hours
Độc Tính : Symptoms of overdose include bradycardia, cardiac failure, hypotension, and brochospasm.
Chỉ Định : Used to manage hypertension and tachycardia. Also used to treat glaucoma.
Liều Lượng & Cách Dùng : Solution - Ophthalmic
Tablet - Oral
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty : Desma
    Sản phẩm biệt dược : Betadrenol
  • Công ty : Winzer (Germany)
    Sản phẩm biệt dược : Ophtorenin
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB08808
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D07590
ChemSpider
http://www.chemspider.com/Chemical-Structure.2381.html
PharmGKB
http://www.pharmgkb.org/drug/PA165958426
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