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 |
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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 |
---|---|---|
Upregulation of immunoreactive angiotensin II release and angiotensinogen mRNA expression by high-frequency preganglionic stimulation at the canine cardiac sympathetic ganglia. | 2001 Jan 19 |
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Sympathetic blockade significantly improves cardiovascular alterations immediately after spinal cord injury in rats. | 2002 Feb 15 |
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Chronic central infusion of orexin-A increases arterial pressure in rats. | 2002 Mar 15 |
|
Central cardiovascular action of urotensin II in conscious rats. | 2003 Jan |
|
Ghrelin acts at the nucleus of the solitary tract to decrease arterial pressure in rats. | 2004 May |
|
Cardiovascular effects of noradrenaline microinjected into the dorsal periaqueductal gray area of unanaesthetized rats. | 2005 Dec |
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Pressor and tachycardic responses evoked by microinjections of L-glutamate into the medial prefrontal cortex of unanaesthetized rats. | 2005 May |
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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 |
|
Baroreceptor reflex stimulation does not induce cytomegalovirus promoter-driven transgene expression in the ventrolateral medulla in vivo. | 2006 Jun 30 |
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Effects of chronic treatment with 7-nitroindazole in hyperthyroid rats. | 2006 Nov |
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Levels of renal and extrarenal sympathetic drive in angiotensin II-induced hypertension. | 2008 Apr |
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Cardiovascular responses to noradrenaline microinjection in the ventrolateral periaqueductal gray of unanesthetized rats. | 2008 Feb 15 |
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Release of acetylcholine by syringin, an active principle of Eleutherococcus senticosus, to raise insulin secretion in Wistar rats. | 2008 Mar 28 |
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Neuronal source of plasma dopamine. | 2008 Nov |
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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 |
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Mechanisms involved in the pressor response to noradrenaline microinjection into the supraoptic nucleus of unanesthetized rats. | 2009 Jan 28 |
|
Role of N-methyl-D-aspartate and non-N-methyl-D-aspartate receptors in the cardiovascular effects of L-glutamate microinjection into the hypothalamic paraventricular nucleus of unanesthetized rats. | 2009 Jul |
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The role of nitric oxide in the development of neurogenic pulmonary edema in spinal cord-injured rats: the effect of preventive interventions. | 2009 Oct |
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Role of the sympathetic nervous system in Schlager genetically hypertensive mice. | 2009 Oct |
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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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Classification Tree | Code System | Code | ||
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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)