Details
Stereochemistry | ACHIRAL |
Molecular Formula | C15H32N2 |
Molecular Weight | 240.428 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 2 |
SHOW SMILES / InChI
SMILES
C[N+]2(CCCCC[N+]1(C)CCCC1)CCCC2
InChI
InChIKey=XSBSKEQEUFOSDD-UHFFFAOYSA-N
InChI=1S/C15H32N2/c1-16(12-6-7-13-16)10-4-3-5-11-17(2)14-8-9-15-17/h3-15H2,1-2H3/q+2
Pentolinium (brand name Ansolysen) is a ganglionic cholinergic antagonist, acting on alpha 3 beta 4 neuronal nicotinic acetylcholine receptors (nAChRs). It was used as an antihypertensive drug during surgery or to control hypertensive crises, but Ansolysen was discontinued. Pentolinium inhibits release of adrenaline and noradrenaline from adrenergic nerves.
Originator
Sources: https://www.ncbi.nlm.nih.gov/pubmed/13316673
Curator's Comment: In 1952, Libman, Pain and Slack in the laboratories of May & Baker, London
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL1907594 Sources: https://www.ncbi.nlm.nih.gov/pubmed/7761270 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
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Primary | ANSOLYSEN Approved UseUnknown |
Doses
Dose | Population | Adverse events |
---|---|---|
80 mg 3 times / day multiple, intravenous Dose: 80 mg, 3 times / day Route: intravenous Route: multiple Dose: 80 mg, 3 times / day Sources: |
unhealthy, 58 years n = 1 Health Status: unhealthy Condition: hypertension Age Group: 58 years Sex: M Population Size: 1 Sources: |
Other AEs: Dizziness, Constipation... Other AEs: Dizziness Sources: Constipation Vomiting Paralytic ileus (grade 5) |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Constipation | 80 mg 3 times / day multiple, intravenous Dose: 80 mg, 3 times / day Route: intravenous Route: multiple Dose: 80 mg, 3 times / day Sources: |
unhealthy, 58 years n = 1 Health Status: unhealthy Condition: hypertension Age Group: 58 years Sex: M Population Size: 1 Sources: |
|
Dizziness | 80 mg 3 times / day multiple, intravenous Dose: 80 mg, 3 times / day Route: intravenous Route: multiple Dose: 80 mg, 3 times / day Sources: |
unhealthy, 58 years n = 1 Health Status: unhealthy Condition: hypertension Age Group: 58 years Sex: M Population Size: 1 Sources: |
|
Vomiting | 80 mg 3 times / day multiple, intravenous Dose: 80 mg, 3 times / day Route: intravenous Route: multiple Dose: 80 mg, 3 times / day Sources: |
unhealthy, 58 years n = 1 Health Status: unhealthy Condition: hypertension Age Group: 58 years Sex: M Population Size: 1 Sources: |
|
Paralytic ileus | grade 5 | 80 mg 3 times / day multiple, intravenous Dose: 80 mg, 3 times / day Route: intravenous Route: multiple Dose: 80 mg, 3 times / day Sources: |
unhealthy, 58 years n = 1 Health Status: unhealthy Condition: hypertension Age Group: 58 years Sex: M Population Size: 1 Sources: |
PubMed
Title | Date | PubMed |
---|---|---|
Noradrenaline and the kidney: friends or foes? | 2001 Dec |
|
Short exposure of maturing, bone marrow-derived dendritic cells to norepinephrine: impact on kinetics of cytokine production and Th development. | 2002 Aug |
|
Sympathetic blockade significantly improves cardiovascular alterations immediately after spinal cord injury in rats. | 2002 Feb 15 |
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Altered balance of main vasopressor and vasodepressor systems in rats with genetic hypertension and hypertriglyceridaemia. | 2002 Mar |
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The altered balance between sympathetic nervous system and nitric oxide in salt hypertensive Dahl rats: ontogenetic and F2 hybrid studies. | 2002 May |
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In vivo effects of fenoldopam on autonomic nervous system after inhibition or activation of ganglionic transmission. | 2002 May 31 |
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Human coagulation factor XII-related "new pressor protein": role of PACAP in its cardiovascular and sympathoadrenal effects. | 2002 Oct |
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Release of acetylcholine by Die-Huang-Wan to enhance insulin secretion for lowering plasma glucose in Wistar rats. | 2002 Sep 30 |
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Resolving the composite trait of hypertension into its pharmacogenetic determinants by acute pharmacological modulation of blood pressure regulatory systems. | 2003 Jan |
|
The role of renal sympathetic nervous system in the pathogenesis of ischemic acute renal failure. | 2003 Nov 28 |
|
Fenfluramine-induced hypothermia is associated with cutaneous dilation in conscious rats. | 2004 Feb |
|
Role of bradykinin B2-receptor in the sympathoadrenal effects of 'new pressor protein' related to human blood coagulation factor XII fragment. | 2004 Jun |
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Release of acetylcholine by Hon-Chi to raise insulin secretion in Wistar rats. | 2006 Aug 14 |
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Release of acetylcholine to raise insulin secretion in Wistar rats by oleanolic acid, one of the active principles contained in Cornus officinalis. | 2006 Aug 14 |
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Increase of insulin secretion by ginsenoside Rh2 to lower plasma glucose in Wistar rats. | 2006 Jan-Feb |
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Effects of chronic treatment with 7-nitroindazole in hyperthyroid rats. | 2006 Nov |
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Cardiovascular effects of carbachol microinjected into the bed nucleus of the stria terminalis of the rat brain. | 2007 Apr 27 |
|
Vasorelaxant activity of some oxime derivatives. | 2007 Dec 1 |
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Angiotensin II-based hypertension and the sympathetic nervous system: the role of dose and increased dietary salt in rabbits. | 2007 Sep |
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Levels of renal and extrarenal sympathetic drive in angiotensin II-induced hypertension. | 2008 Apr |
|
Angiotensin converting enzyme-regulated, noncholinergic sympathoadrenal catecholamine release mediates the cardiovascular actions of human 'new pressor protein' related to coagulation beta-factor XIIa. | 2009 Apr |
|
The role of nitric oxide in the development of neurogenic pulmonary edema in spinal cord-injured rats: the effect of preventive interventions. | 2009 Oct |
|
Role of the sympathetic nervous system in Schlager genetically hypertensive mice. | 2009 Oct |
|
Role of sympathetic tone in BSO-induced hypertension in mice. | 2010 Aug |
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/13316673
intramuscularly: 1 to 2 0.25-mg ampoules
Ansolysen must be used with caution. The initial dose is from 20-40 mg., taken 15 to 20 minutes before each meal and at bedtime, to ensure an even digestive absorption. Each dose is increased by 20-40 mg. four times a day at intervals of five to seven days until the desired hvpotensive effect is obtained. The maintenance dose varies generally between 160 and 800 mg. a day.
Route of Administration:
Other
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NCI_THESAURUS |
C66886
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2096
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Pentolinium
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347401
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SUB03692MIG
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DTXSID5048554
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144-44-5
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5850
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C77367
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100000085527
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DB01090
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ULL76WPU5X
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ACTIVE MOIETY
SALT/SOLVATE (PARENT)