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Guanadrel

From Wikipedia, the free encyclopedia
Guanadrel
Names
IUPAC name
2-(1,4-Dioxaspiro[4.5]decan-2-ylmethyl)guanidine
Identifiers
3D model (JSmol)
ChEBI
ChEMBL
ChemSpider
KEGG
MeSHC004945
UNII
  • 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) ☒N
    Key: HPBNRIOWIXYZFK-UHFFFAOYSA-N ☒N
  • InChI=1/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)
    Key: HPBNRIOWIXYZFK-UHFFFAOYAB
  • C1CCC2(CC1)OCC(O2)CN=C(N)N
Properties
C10H19N3O2
Molar mass213.281 g·mol−1
Except where otherwise noted, data are given for materials in theirstandard state (at 25 °C [77 °F], 100 kPa).
☒N verify (what is checkY☒N ?)
Chemical compound

Guanadrel is anantihypertensive agent.[1] It is used in the form of itssulfate.

Mechanism of action

[edit]

Guanadrel is a postganglionic adrenergic blocking agent. Uptake of guanadrel and storage in sympathetic neurons occurs via thenorepinephrine pump; 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 tosympathetic nerve stimulation, as a result ofcatecholamine depletion, leads to reduced arteriolarvasoconstriction, especially the reflex increase in sympathetic tone that occurs with a change in position. Guanadrel is rapidly and well absorbed from gastrointestinal tract.[2]

In 1981 theJAMA reported guanadrel as an effective step II or step III treatment of hypertension.[3]

References

[edit]
  1. ^Oren A, Rotmensch HH, Vlasses PH, et al. (1985)."A dose-titration trial of guanadrel as step-two therapy in essential hypertension".J Clin Pharmacol.25 (5):343–6.doi:10.1002/j.1552-4604.1985.tb02852.x.PMID 4031111.[permanent dead link]
  2. ^Guanadrel, from Pharmacogenetics Knowledge Base
  3. ^M. I. Dunn and J. L. Dunlap (1981). "Guanadrel. A new antihypertensive drug".JAMA.245 (16):1639–42.doi:10.1001/jama.1981.03310410017019.PMID 7206175.

External links

[edit]
Sympatholytic (and closely related)antihypertensives (C02)
Sympatholytics
(antagonizeα-adrenergic
vasoconstriction)
Central
α2-Adrenergic receptor agonists
Adrenergic release inhibitors
Imidazoline receptor agonists
Ganglion-blocking/nicotinic antagonists
Peripheral
Indirect
Monoamine oxidase inhibitors
VMAT inhibitors
Tyrosine hydroxylase inhibitors
Direct
α1-Adrenergic receptor blockers
Non-selective α-adrenergic receptor blockers
Otherantagonists
Serotonin receptor antagonists
Endothelin receptor antagonists (forPHTooltip Pulmonary hypertension)
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