Tìm theo
Reserpine
Các tên gọi khác (8 ) :
  • (-)-Reserpine
  • (−)-reserpine
  • (3beta,16beta,17alpha,18beta,20alpha)-11,17-Dimethoxy-18-[(3,4,5-trimethoxybenzoyl)oxy]yohimban-16-carboxylic acid methyl ester
  • 3,4,5-trimethoxybenzoyl methyl reserpate
  • Apoplon
  • Reserpin
  • Reserpine
  • Serpalan
antihypertensive agents, adrenergic uptake inhibitors, antipsychotic agents, adrenergic antagonists
Thuốc Gốc
Small Molecule
CAS: 50-55-5
ATC: C02AA02
ĐG : Apotheca Inc.
CTHH: C33H40N2O9
PTK: 608.6787
An alkaloid found in the roots of Rauwolfia serpentina and R. vomitoria. Reserpine inhibits the uptake of norepinephrine into storage vesicles resulting in depletion of catecholamines and serotonin from central and peripheral axon terminals. It has been used as an antihypertensive and an antipsychotic as well as a research tool, but its adverse effects limit its clinical use. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
Phân tử khối
608.6787
Monoisotopic mass
608.273380888
InChI
InChI=1S/C33H40N2O9/c1-38-19-7-8-20-21-9-10-35-16-18-13-27(44-32(36)17-11-25(39-2)30(41-4)26(12-17)40-3)31(42-5)28(33(37)43-6)22(18)15-24(35)29(21)34-23(20)14-19/h7-8,11-12,14,18,22,24,27-28,31,34H,9-10,13,15-16H2,1-6H3/t18-,22+,24-,27-,28+,31+/m1/s1
InChI Key
InChIKey=QEVHRUUCFGRFIF-MDEJGZGSSA-N
IUPAC Name
methyl (1R,15S,17R,18R,19S,20S)-6,18-dimethoxy-17-[(3,4,5-trimethoxyphenyl)carbonyloxy]-3,13-diazapentacyclo[11.8.0.0^{2,10}.0^{4,9}.0^{15,20}]henicosa-2(10),4,6,8-tetraene-19-carboxylate
Traditional IUPAC Name
reserpine
SMILES
[H][[email protected]]12C[[email protected]@H](OC(=O)C3=CC(OC)=C(OC)C(OC)=C3)[[email protected]](OC)[[email protected]@H](C(=O)OC)[[email protected]@]1([H])C[[email protected]@]1([H])N(CCC3=C1NC1=C3C=CC(OC)=C1)C2
Độ tan chảy
264.5 °C
Độ hòa tan
73 mg/L (at 30 °C)
logP
3.2
logS
-4.7
pKa (strongest acidic)
16.29
pKa (Strongest Basic)
7.56
PSA
117.78 Å2
Refractivity
161.42 m3·mol-1
Polarizability
66.05 Å3
Rotatable Bond Count
10
H Bond Acceptor Count
8
H Bond Donor Count
1
Physiological Charge
1
Number of Rings
6
Bioavailability
1
MDDR-Like Rule
true
pKa
6.6
Dược Lực Học : Reserpine is an adrenergic blocking agent used to treat mild to moderate hypertension via the disruption of norepinephrine vesicular storage. The antihypertensive actions of Reserpine are a result of its ability to deplete catecholamines from peripheral sympathetic nerve endings. These substances are normally involved in controlling heart rate, force of cardiac contraction and peripheral resistance.
Cơ Chế Tác Dụng : An alkaloid found in the roots of Rauwolfia serpentina and R. vomitoria. Reserpine inhibits the uptake of norepinephrine into storage vesicles resulting in depletion of catecholamines and serotonin from central and peripheral axon terminals. It has been used as an antihypertensive and an antipsychotic as well as a research tool, but its adverse effects limit its clinical use. [PubChem] Reserpine's mechanism of action is through inhibition of the ATP/Mg2+ pump responsible for the sequestering of neurotransmitters into storage vesicles located in the presynaptic neuron. The neurotransmitters that are not sequestered in the storage vesicle are readily metabolized by monoamine oxidase (MAO) causing a reduction in catecholamines.
Dược Động Học :

▧ Protein binding :
62%
▧ Route of Elimination :
Reserpine is extensively metabolized to inactive compounds. It is slowly excreted via the urine and feces.
Độc Tính : Possible human carcinogen. May cause reproductive harm. ORL-RAT LD50 420 mg/kg; IPR-RAT LD50 44 mg/kg; IVN-RAT LD50 15 mg/kg; ORL-MUS LD50 200 mg/kg; SCU-MUS LD50 52 mg/kg; IPR-RBT LD50 7 mg/kg
Chỉ Định : Foe the treatment of hypertension
Tương Tác Thuốc :
  • Dobutamine Increased arterial pressure
  • Dopamine Increased arterial pressure
  • Ephedra Increased arterial pressure
  • Ephedrine Increased arterial pressure
  • Epinephrine Increased arterial pressure
  • Fenoterol Increased arterial pressure
  • Iobenguane May diminish the therapeutic effect and increase chances of producing a false negative imaging result of Iobenguane as it depletes or inhibit reuptake of noradrenaline stores
  • Isoprenaline Increased arterial pressure
  • Mephentermine Increased arterial pressure
  • Metaraminol Increased arterial pressure
  • Methoxamine Increased arterial pressure
  • Norepinephrine Increased arterial pressure
  • Orciprenaline Increased arterial pressure
  • Phenylephrine Increased arterial pressure
  • Phenylpropanolamine Increased arterial pressure
  • Pirbuterol Increased arterial pressure
  • Procaterol Increased arterial pressure
  • Pseudoephedrine Increased arterial pressure
  • Salbutamol Increased arterial pressure
  • Terbutaline Increased arterial pressure
  • Tetrabenazine Reserpine may increase the adverse/toxic effects of tetrabenazine as they have similar pharmacologic properties. Concomitant therapy is contraindicated.
  • Topotecan The p-glycoprotein inhibitor, Reserpine, may increase the bioavailability of oral Topotecan. A clinically significant effect is also expected with IV Topotecan. Concomitant therapy should be avoided.
  • Tranylcypromine Addition of Reserpine to Tranylcypromine therapy may induce paradoxical Reserpine effects, including peripheral hypertension and central exciation. Close monitoring for adverse effects is required. Addition of Tranylcypromine to Reserpine therapy may be less of a concern.
  • Treprostinil Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
  • Triprolidine The CNS depressants, Triprolidine and Reserpine, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy.
Liều Lượng & Cách Dùng : Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Apoplon
  • Công ty :
    Sản phẩm biệt dược : Hiserpia
  • Công ty :
    Sản phẩm biệt dược : Novoreserpine
  • Công ty :
    Sản phẩm biệt dược : Reserfia
  • Công ty :
    Sản phẩm biệt dược : Serpalan
  • Công ty :
    Sản phẩm biệt dược : Serpanray
  • Công ty :
    Sản phẩm biệt dược : Serpasil
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