Tìm theo
Mecamylamine
Các tên gọi khác (1) :
  • Versamine
Thuốc Gốc
Small Molecule
CAS: 60-40-2
ATC: C02BB01
ĐG : Layton Bioscience Inc.
CTHH: C11H21N
PTK: 167.2911
A nicotinic antagonist that is well absorbed from the gastrointestinal tract and crosses the blood-brain barrier. Mecamylamine has been used as a ganglionic blocker in treating hypertension, but, like most ganglionic blockers, is more often used now as a research tool. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
Phân tử khối
167.2911
Monoisotopic mass
167.167399677
InChI
InChI=1S/C11H21N/c1-10(2)8-5-6-9(7-8)11(10,3)12-4/h8-9,12H,5-7H2,1-4H3
InChI Key
InChIKey=IMYZQPCYWPFTAG-UHFFFAOYSA-N
IUPAC Name
N,2,3,3-tetramethylbicyclo[2.2.1]heptan-2-amine
Traditional IUPAC Name
mecamylamine
SMILES
CNC1(C)C2CCC(C2)C1(C)C
Độ tan chảy
249 with decomposition
Độ sôi
72 °C at 4.00E+00 mm Hg
Độ hòa tan
1.24e-01 g/l
logP
2.7
logS
-3.1
pKa (Strongest Basic)
10.88
PSA
12.03 Å2
Refractivity
51.83 m3·mol-1
Polarizability
20.74 Å3
Rotatable Bond Count
1
H Bond Acceptor Count
1
H Bond Donor Count
1
Physiological Charge
1
Number of Rings
2
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Mecamylamine is a potent, oral antihypertensive agent and ganglion blocker, and is a secondary amine. Mecamylamine is indicated for the management of moderately severe to severe essential hypertension and in uncomplicated cases of malignant hypertension. Mecamylamine reduces blood pressure in both normotensive and hypertensive individuals. A small oral dosage often produces a smooth and predictable reduction of blood pressure. Although this antihypertensive effect is predominantly orthostatic, the supine blood pressure is also significantly reduced. Mecamylamine crosses the blood-brain and placental barriers.
Cơ Chế Tác Dụng : A nicotinic antagonist that is well absorbed from the gastrointestinal tract and crosses the blood-brain barrier. Mecamylamine has been used as a ganglionic blocker in treating hypertension, but, like most ganglionic blockers, is more often used now as a research tool. [PubChem] Mecamylamine is a ganglionic blocker which prevents stimulation of postsynaptic receptors by acetylcholine released from presynaptic nerve endings. The hypotensive effect of Mecamylamine is attributed to reduction in sympathetic tone, vasodilation, and reduced cardiac output, and is primarily postural.
Dược Động Học :
▧ Absorption :
Mecamylamine is almost completely absorbed from the gastrointestinal tract
▧ Protein binding :
40%
▧ Route of Elimination :
Mecamylamine is excreted slowly in the urine in the unchanged form. The rate of its renal elimination is influenced markedly by urinary pH. Alkalinization of the urine reduces, and acidification promotes, renal excretion of mecamylamine. Mecamylamine crosses the blood-brain and placental barriers.
Chỉ Định : For the treatment of moderately severe to severe essential hypertension and in uncomplicated cases of malignant hypertension
Liều Lượng & Cách Dùng : Tablet - Oral
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty : Targacept
    Sản phẩm biệt dược : Inversine
  • Công ty :
    Sản phẩm biệt dược : Vecamyl
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