55-65-2 Usage
Description
Guanethidine is used for severe hypertension when the use of the more generally
accepted drugs turns out to be unsuccessful. It is a powerful, long-lasting antihypertensive
drug; however, it affects a patient’s blood pressure only in the orthostatic position, and not
when lying down.
Guanethidine is a very powerful and long-lasting drug, and its action often lasts 2–3
days after its use has been stopped.
Originator
Ismelin,Ciba,US,1960
Uses
Antihypertensive.
Definition
ChEBI: A member of the class of guanidines in which one of the hydrogens of the amino group has been replaced by a 2-azocan-1-ylethyl group.
Manufacturing Process
13.6 grams of chloroacetyl guanide is added while stirring to a solution of
22.6 grams of heptamethylene imine in 200 ml of benzene. After warming for
1 hour, and then cooling, the solution is filtered and the filtrate concentrated
under reduced pressure. The residue, containing the 2-(1-N,N-heptamethylene-imino)-aceticacid guanide, is suspended in tetrahydrofuran
and added to a refluxing solution of 6 grams of lithium aluminum hydride in
tetrahydrofuran. After completion of the reaction, the excess of lithium
aluminum hydride is decomposed by adding water, then aqueous sodium
hydroxide. The solid material is filtered off, the filtrate is acidified with sulfuric
acid and the 2-(1-N,N-heptamethylene-imino)-ethyl-guanidine sulfate can be
recovered and recrystallized from aqueous ethanol, MP 276° to 281°C (with
decomposition).
Brand name
Ismelin (Novartis).
Therapeutic Function
Antihypertensive
Biological Functions
Guanethidine (Ismelin) is a powerful antihypertensive
agent that is quite effective in the treatment of moderate
to severe hypertension. It is most frequently used in
the treatment of severe hypertension that is resistant to
other agents.
Guanethidine exerts its effects at peripheral sympathetic
nerve endings following its active transport into the
nerve varicosities by the neuronal amine transport system.
This is the same uptake system that transports norepinephrine
into the varicosity).The accumulation
of guanethidine in adrenergic neurons,
through an as yet unexplained mechanism, disrupts the
process by which action potentials trigger the release of
stored norepinephrine and other cotransmitters from
nerve terminals. It is this action of guanethidine that is
primarily responsible for its antihypertensive properties.
Parasympathetic function is not altered, a fact that
distinguishes guanethidine from the ganglionic blocking
agent.
Guanethidine is suitable for oral use, and this is its
usual route of administration. However, absorption
from the gastrointestinal tract is variable. The half-life
of guanethidine is 5 days, with about one-seventh of the
total administered dose eliminated per day. The slow
elimination contributes to the cumulative and prolonged
effects of the drug.
Guanethidine reduces blood pressure by its ability
to diminish vascular tone; both the arterial and venous
sides of the circulatory system are involved. The resulting
venous pooling contributes to orthostatic hypotension,
a prominent feature of guanethidine treatment.
The reduction in blood pressure is more prominent
when the patient is standing than recumbent.
General Description
Different sources of media describe the General Description of 55-65-2 differently. You can refer to the following data:
1. Guanethidine or guanethidinesulfate [C10H22N4·H2SO4].
2. Guanethidinehas been classified traditionally as an adrenergic blockingagent because it can prevent the release of norepinephrinefrom postganglionic neurons in response to adrenergic stimulation.Guanethidine and other compounds discussed in thissection have other actions on catecholamine metabolism andcan cause significant depletion of these amines in adrenergicneurons. They do not interfere with release of epinephrinefrom the adrenal medulla.
Side effects
Guanethidine may aggravate congestive heart failure
or actually precipitate failure in patients with marginal
cardiac reserve, owing to its ability to produce vascular
volume expansion, edema, and a reduced
effectiveness of sympathetic cardiac stimulation.
Guanethidine is contraindicated in patients with
pheochromocytoma because the drug may release catecholamines
from the tumor. The concomitant use of
monoamine oxidase (MAO) inhibitors and guanethidine
is also to be avoided, since this combined drug
treatment eliminates two of the principal mechanisms
for terminating the actions of the catecholamines and
certain other adrenomimetic drugs, that is, biotransformation
and neuronal uptake. Dangerously high concentrations
of catecholamines at receptor sites are possible.
Check Digit Verification of cas no
The CAS Registry Mumber 55-65-2 includes 5 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 2 digits, 5 and 5 respectively; the second part has 2 digits, 6 and 5 respectively.
Calculate Digit Verification of CAS Registry Number 55-65:
(4*5)+(3*5)+(2*6)+(1*5)=52
52 % 10 = 2
So 55-65-2 is a valid CAS Registry Number.
InChI:InChI=1/C10H22N4.H2O4S/c11-10(12)13-6-9-14-7-4-2-1-3-5-8-14;1-5(2,3)4/h1-9H2,(H4,11,12,13);(H2,1,2,3,4)
55-65-2Relevant articles and documents
COMPOSITIONS AND METHODS FOR DIAGNOSING AND TREATING SALT SENSITIVITY OF BLOOD PRESSURE
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, (2015/02/05)
To characterize the urinary exosome miRNome, microarrays were used to identify the miRNA spectrum present within urinary exosomes from ten individuals that were previously classified for their salt sensitivity status. The present application discloses distinct patterns of selected exosomal miRNA expression that were different between salt-sensitive (SS), salt-resistant (SR), and inverse salt-sensitive (ISS) individuals. These miRNAs can be useful as biomarkers either individually or as panels comprising multiple miRNAs. The present invention provides compositions and methods for identifying, diagnosing, monitoring, and treating subjects with salt sensitivity of blood pressure. The applications discloses panels of miRNAs useful for comparing profiles, and in some cases one or more of the miRNAs in a panel can be used. The miRNAs useful for distinguishing SS and SR or ISS and SR subjects. One or more of the 45 miRNAs can be used. Some of the miRNAs have not been previously reported to be circulating. See those miRNAs with asterisks in FIG. 1 and below. The present invention encompasses the use of one or more of these markers for identifying and diagnosing SR, SS, and ISS subjects.
