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
Molecular Formula | C15H32N2 |
Molecular Weight | 240.428 |
Charge | 2 |
Count |
|
Stereochemistry | MIXED |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
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 |
---|---|---|---|---|
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 |
---|---|---|
Blood pressure, heart rate, and behavioral responses to psychological "novelty" stress in freely moving rats. | 2001 May |
|
Sympathetic blockade significantly improves cardiovascular alterations immediately after spinal cord injury in rats. | 2002 Feb 15 |
|
Altered balance of main vasopressor and vasodepressor systems in rats with genetic hypertension and hypertriglyceridaemia. | 2002 Mar |
|
Release of acetylcholine by Die-Huang-Wan to enhance insulin secretion for lowering plasma glucose in Wistar rats. | 2002 Sep 30 |
|
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 |
|
Vasoactive systems in L-NAME hypertension: the role of inducible nitric oxide synthase. | 2004 Jan |
|
Role of bradykinin B2-receptor in the sympathoadrenal effects of 'new pressor protein' related to human blood coagulation factor XII fragment. | 2004 Jun |
|
Ghrelin acts at the nucleus of the solitary tract to decrease arterial pressure in rats. | 2004 May |
|
Peptide YY administration into the posterior hypothalamic nucleus of the rat evokes cardiovascular changes by non-adrenergic, non-cholinergic mechanisms. | 2005 Apr |
|
Cardiovascular effects of noradrenaline microinjected into the dorsal periaqueductal gray area of unanaesthetized rats. | 2005 Dec |
|
Pressor and tachycardic responses evoked by microinjections of L-glutamate into the medial prefrontal cortex of unanaesthetized rats. | 2005 May |
|
Release of acetylcholine by Hon-Chi to raise insulin secretion in Wistar rats. | 2006 Aug 14 |
|
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 |
|
Antihypertensive mechanisms of chronic captopril or N-acetylcysteine treatment in L-NAME hypertensive rats. | 2006 Dec |
|
Increase of insulin secretion by ginsenoside Rh2 to lower plasma glucose in Wistar rats. | 2006 Jan-Feb |
|
Baroreceptor reflex stimulation does not induce cytomegalovirus promoter-driven transgene expression in the ventrolateral medulla in vivo. | 2006 Jun 30 |
|
Effects of chronic treatment with 7-nitroindazole in hyperthyroid rats. | 2006 Nov |
|
Pressor effects of noradrenaline injected into the lateral septal area of unanesthetized rats. | 2006 Nov 29 |
|
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 |
|
Total peripheral resistance responsiveness during the development of secondary renal hypertension in dogs. | 2007 Mar |
|
The participation of brain NO synthase in blood pressure control of adult spontaneously hypertensive rats. | 2007 Mar |
|
Cardiovascular effects of L-glutamate microinjection in the supraoptic nucleus of unanaesthetized rats. | 2007 May |
|
Cardiovascular effects of noradrenaline microinjection in the bed nucleus of the stria terminalis of the rat brain. | 2007 May 15 |
|
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 |
|
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 |
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
Substance Class |
Chemical
Created
by
admin
on
Edited
Fri Dec 15 16:12:11 GMT 2023
by
admin
on
Fri Dec 15 16:12:11 GMT 2023
|
Record UNII |
ULL76WPU5X
|
Record Status |
Validated (UNII)
|
Record Version |
|
-
Download
Name | Type | Language | ||
---|---|---|---|---|
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English |
Classification Tree | Code System | Code | ||
---|---|---|---|---|
|
NCI_THESAURUS |
C66886
Created by
admin on Fri Dec 15 16:12:11 GMT 2023 , Edited by admin on Fri Dec 15 16:12:11 GMT 2023
|
Code System | Code | Type | Description | ||
---|---|---|---|---|---|
|
2096
Created by
admin on Fri Dec 15 16:12:11 GMT 2023 , Edited by admin on Fri Dec 15 16:12:11 GMT 2023
|
PRIMARY | |||
|
Pentolinium
Created by
admin on Fri Dec 15 16:12:11 GMT 2023 , Edited by admin on Fri Dec 15 16:12:11 GMT 2023
|
PRIMARY | |||
|
347401
Created by
admin on Fri Dec 15 16:12:11 GMT 2023 , Edited by admin on Fri Dec 15 16:12:11 GMT 2023
|
PRIMARY | |||
|
SUB03692MIG
Created by
admin on Fri Dec 15 16:12:11 GMT 2023 , Edited by admin on Fri Dec 15 16:12:11 GMT 2023
|
PRIMARY | |||
|
DTXSID5048554
Created by
admin on Fri Dec 15 16:12:11 GMT 2023 , Edited by admin on Fri Dec 15 16:12:11 GMT 2023
|
PRIMARY | |||
|
144-44-5
Created by
admin on Fri Dec 15 16:12:11 GMT 2023 , Edited by admin on Fri Dec 15 16:12:11 GMT 2023
|
PRIMARY | |||
|
5850
Created by
admin on Fri Dec 15 16:12:11 GMT 2023 , Edited by admin on Fri Dec 15 16:12:11 GMT 2023
|
PRIMARY | |||
|
C77367
Created by
admin on Fri Dec 15 16:12:11 GMT 2023 , Edited by admin on Fri Dec 15 16:12:11 GMT 2023
|
PRIMARY | |||
|
100000085527
Created by
admin on Fri Dec 15 16:12:11 GMT 2023 , Edited by admin on Fri Dec 15 16:12:11 GMT 2023
|
PRIMARY | |||
|
DB01090
Created by
admin on Fri Dec 15 16:12:11 GMT 2023 , Edited by admin on Fri Dec 15 16:12:11 GMT 2023
|
PRIMARY | |||
|
ULL76WPU5X
Created by
admin on Fri Dec 15 16:12:11 GMT 2023 , Edited by admin on Fri Dec 15 16:12:11 GMT 2023
|
PRIMARY |
Related Record | Type | Details | ||
---|---|---|---|---|
|
SALT/SOLVATE -> PARENT |
Related Record | Type | Details | ||
---|---|---|---|---|
|
ACTIVE MOIETY |