Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Monoisotopic mass
213.147726867
InChI
InChI=1S/C10H19N3O2/c11-9(12)13-6-8-7-14-10(15-8)4-2-1-3-5-10/h8H,1-7H2,(H4,11,12,13)
InChI Key
InChIKey=HPBNRIOWIXYZFK-UHFFFAOYSA-N
IUPAC Name
2-{1,4-dioxaspiro[4.5]decan-2-ylmethyl}guanidine
Traditional IUPAC Name
guanadrel
SMILES
NC(N)=NCC1COC2(CCCCC2)O1
pKa (strongest acidic)
19.85
pKa (Strongest Basic)
12.56
Refractivity
56.54 m3·mol-1
Dược Lực Học :
High blood pressure adds to the work load of the heart and arteries. If it continues for a long time, the heart and arteries may not function properly. This can damage the blood vessels of the brain, heart, and kidneys resulting in a stroke, heart failure, or kidney failure. High blood pressure may also increase the risk of heart attacks. These problems may be less likely to occur if blood pressure is controlled. Guanadrel works by controlling nerve impulses along certain nerve pathways. As a result, it relaxes the blood vessels so that blood passes through them more easily. This helps to lower blood pressure.
Cơ Chế Tác Dụng :
Guanadrel is a postganglionic adrenergic blocking agent. Uptake of guanadrel and storage in sympathetic neurons occurs via the norepinephrine pump or transporter.
Guanadrel is a postganglionic adrenergic blocking agent. Uptake of guanadrel and storage in sympathetic neurons occurs via the norepinephrine pump or transporter. Guanadrel slowly displaces norepinephrine from its storage in nerve endings and thereby blocks the release of norepinephrine normally produced by nerve stimulation. The reduction in neurotransmitter release in response to sympathetic nerve stimulation, as a result of catecholamine depletion, leads to reduced arteriolar vasoconstriction, especially the reflex increase in sympathetic tone that occurs with a change in position.
Dược Động Học :
▧ Absorption :
Rapidly and readily absorbed from the gastrointestinal tract.
▧ Protein binding :
Low, approximately 20%
▧ Metabolism :
Primarily hepatic
▧ Half Life :
10 hours
Độc Tính :
Side effects include dizziness, drowsiness, headache, constipation, diarrhea, gas pains, loss of appetite, fatigue, and nasal congestion.
Chỉ Định :
Used to treat and control hypertension.