Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C15H32N2.2C4H5O6 |
| Molecular Weight | 538.5858 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 4 / 4 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
O[C@H]([C@@H](O)C([O-])=O)C(O)=O.O[C@H]([C@@H](O)C([O-])=O)C(O)=O.C[N+]2(CCCCC[N+]1(C)CCCC1)CCCC2
InChI
InChIKey=HSMKTIKKPMTUQH-WBPXWQEISA-L
InChI=1S/C15H32N2.2C4H6O6/c1-16(12-6-7-13-16)10-4-3-5-11-17(2)14-8-9-15-17;2*5-1(3(7)8)2(6)4(9)10/h3-15H2,1-2H3;2*1-2,5-6H,(H,7,8)(H,9,10)/q+2;;/p-2/t;2*1-,2-/m.11/s1
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.
Approval Year
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 |
|
| Receptor protection studies to characterize neuronal nicotinic receptors: tubocurarine prevents alkylation of adrenal nicotinic receptors. | 2001 Feb 9 |
|
| Upregulation of immunoreactive angiotensin II release and angiotensinogen mRNA expression by high-frequency preganglionic stimulation at the canine cardiac sympathetic ganglia. | 2001 Jan 19 |
|
| Central orexin-A augments sympathoadrenal outflow in conscious rabbits. | 2001 Jun |
|
| Altered balance of main vasopressor and vasodepressor systems in rats with genetic hypertension and hypertriglyceridaemia. | 2002 Mar |
|
| Chronic central infusion of orexin-A increases arterial pressure in rats. | 2002 Mar 15 |
|
| In vivo effects of fenoldopam on autonomic nervous system after inhibition or activation of ganglionic transmission. | 2002 May 31 |
|
| Human coagulation factor XII-related "new pressor protein": role of PACAP in its cardiovascular and sympathoadrenal effects. | 2002 Oct |
|
| Release of acetylcholine by Die-Huang-Wan to enhance insulin secretion for lowering plasma glucose in Wistar rats. | 2002 Sep 30 |
|
| Gender-specific genetic determinants of blood pressure and organ weight: pharmacogenetic approach. | 2003 |
|
| Catecholamine and oxytocin cells respond to hypovolaemia as well as hypotension. | 2003 Aug 6 |
|
| Resolving the composite trait of hypertension into its pharmacogenetic determinants by acute pharmacological modulation of blood pressure regulatory systems. | 2003 Jan |
|
| Central cardiovascular action of urotensin II in conscious rats. | 2003 Jan |
|
| Fenfluramine-induced hypothermia is associated with cutaneous dilation in conscious rats. | 2004 Feb |
|
| Cardiovascular effects of noradrenaline microinjected into the dorsal periaqueductal gray area of unanaesthetized rats. | 2005 Dec |
|
| Antihypertensive mechanisms of chronic captopril or N-acetylcysteine treatment in L-NAME hypertensive rats. | 2006 Dec |
|
| Baroreceptor reflex stimulation does not induce cytomegalovirus promoter-driven transgene expression in the ventrolateral medulla in vivo. | 2006 Jun 30 |
|
| Vasorelaxant activity of some oxime derivatives. | 2007 Dec 1 |
|
| Angiotensin II-based hypertension and the sympathetic nervous system: the role of dose and increased dietary salt in rabbits. | 2007 Sep |
|
| Cardiovascular responses to noradrenaline microinjection in the ventrolateral periaqueductal gray of unanesthetized rats. | 2008 Feb 15 |
|
| Neuronal source of plasma dopamine. | 2008 Nov |
|
| 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 |
|
| 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 |
|
| 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 |
|
| Enhanced responses to ganglion blockade do not reflect sympathetic nervous system contribution to angiotensin II-induced hypertension. | 2009 Sep |
|
| Cardiovascular effects of noradrenaline microinjection into the medial part of the superior colliculus of unanesthetized rats. | 2009 Sep 22 |
|
| Role of sympathetic tone in BSO-induced hypertension in mice. | 2010 Aug |
Sample Use Guides
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 |
C270
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C66886
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759890
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953357GACY
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5849
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SUB09700MIG
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m8515
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DTXSID5045542
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C66345
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DBSALT000236
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D010425
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55326
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52-62-0
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100000082536
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200-146-7
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CHEMBL1271
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330
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ACTIVE MOIETY
PARENT (SALT/SOLVATE)
SUBSTANCE RECORD
