Page last updated: 2024-09-20

chlorisondamine

Description

Chlorisondamine: A nicotinic antagonist used primarily as a ganglionic blocker in animal research. It has been used as an antihypertensive agent but has been supplanted by more specific drugs in most clinical applications. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID6244
CHEMBL ID1398654
CHEBI ID135514
SCHEMBL ID14340042
MeSH IDM0004145

Synonyms (26)

Synonym
chlorisondamine
PDSP1_000172
PDSP2_000171
NCGC00024930-01
tocris-1001
NCGC00163230-01
CHEBI:135514
NCGC00024930-02
7701-62-4
4,5,6,7-tetrachloro-2-methyl-2-(2-(trimethylammonio)ethyl)isoindolinium
unii-jd3m24f66i
isoindolinium, 4,5,6,7-tetrachloro-2-methyl-2-(2-(trimethylammonio)ethyl)-
jd3m24f66i ,
cas_6243
bdbm84948
nsc_6243
CHEMBL1398654
chlorisondamine ion
chlorisondamine cation
isoindolinium, 4,5,6,7-tetrachloro-2-methyl-2-(2- (trimethylammonio)ethyl)-
chlorisondamine [who-dd]
1h-isoindolium, 4,5,6,7-tetrachloro-2,3-dihydro-2-methyl-2-(2- (trimethylammonio)ethyl)-
SCHEMBL14340042
DTXSID0048395
Q5102966
chlorisondamine-diiodide

Research Excerpts

Overview

ExcerptReference
"Chlorisondamine is a charged molecule that acts as long-acting nicotinic antagonist in many species, including pigeon. "( Chadman, KK; Stitzel, J; Woods, JH, 2007)

Effects

ExcerptReference
"Chlorisondamine (CSD) has been used to assess the neurogenic contribution to blood pressure (BP) and vasomotor sympathetic tone in animal models. "( Cooper, SG; Feng Earley, Y; Souza, LA; Thakore, P; Worker, CJ, 2021)

Actions

ExcerptReference
"3. Chlorisondamine failed to lower heart rate significantly in 4 or 7 day old rats, but lowered the rate by 50 to 80 beats per min in the older animals and eliminated the difference in rate between 16 day old and the other ages; atropine had little or no effect on heart rate."( Seidler, FJ; Slotkin, TA, 1979)
"Chlorisondamine inhibited the increase in ganglionic DOPAC following preganglionic stimulation (5 Hz, 30 min) by 30-50% and it even better reduced the biochemical changes in the salivary gland."( Andén, NE; Grabowska-Andén, M; Klaesson, L, 1986)

Treatment

ExcerptReference
"Chlorisondamine treatment exacerbated the decrease in mean arterial pressure in male mice infused with sPRR."( Gatineau, E; Gong, MC; Yiannikouris, F, 2019)
"Chlorisondamine pretreatment depressed heart rate, blood pressure and plasma levels of NPY-LI."( Al-Saffar, A; Lundberg, JM; Saria, A; Theodorsson-Norheim, E, 1986)
"Pretreatment with chlorisondamine (0.2-5 micromol/kg, i.p.) only partially blocked the effects of ABT-594 at the higher doses tested."( Decker, MW; Honore, P; Lynch, JJ; Mikusa, JP; Wade, CL, 2005)
"Treatment with chlorisondamine, which blocks nicotinic ganglionic transmission, also increased SP, reproducing the effects of decentralization."( Black, IB; Kessler, JA, 1982)
"Pretreatment with chlorisondamine (EC) and phentolamine (PT) did not alter the HC-induced hyperglycemia but did result in higher plasma insulin levels in response to the higher glucose levels."( Fletcher, HP; Longano, CA, 1983)
"Pretreatment with chlorisondamine, a ganglionic blocking agent, inhibited the Il-6 responses, while it had little influence on the TNF responses."( Kitamura, H; Morimatsu, M; Okamoto, S; Saito, M; Shimamoto, Y; Terao, A, 1998)
"Pretreatment with chlorisondamine or verapamil prevented the cocaine-induced enhancement of the maximal response to noradrenaline and the response to isoproterenol, but it did not inhibit potentiation of submaximal doses."( Bechara, G; El-Bizri, NM; Khoury, HA; Sabra, R; Sharaf, LH, 2000)
"Pretreatment with chlorisondamine (1 mg/kg i.v."( Baudrie, V; Chaouloff, F, 1992)
"Treatment with chlorisondamine, which blocks synaptic transmission in sympathetic ganglia, produces a significant increase in SV levels in the SCG after 7 d of treatment."( Greif, KF, 1986)

Drug Classes (1)

ClassDescription
isoindoles
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (4)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
15-lipoxygenase, partialHomo sapiens (human)Potency15.84890.012610.691788.5700AID887
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency15.84890.00207.533739.8107AID891
cytochrome P450 2C19 precursorHomo sapiens (human)Potency5.01190.00255.840031.6228AID899
histone acetyltransferase KAT2A isoform 1Homo sapiens (human)Potency17.03900.251215.843239.8107AID504327
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (4)

Assay IDTitleYearJournalArticle
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
AID766732Noncompetitive inhibition of nicotinic cholinergic receptor in rat PC12 cells assessed as inhibition of 100 to 1000 uM nicotine-induced [3H]-norepinephrine release at 5 uM after 30 mins by liquid scintillation counting analysis2013Bioorganic & medicinal chemistry, Sep-15, Volume: 21, Issue:18
Development of a pharmacophore model for the catecholamine release-inhibitory peptide catestatin: virtual screening and functional testing identify novel small molecule therapeutics of hypertension.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (584)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990389 (66.61)18.7374
1990's123 (21.06)18.2507
2000's53 (9.08)29.6817
2010's16 (2.74)24.3611
2020's3 (0.51)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials1 (0.17%)5.53%
Reviews6 (0.99%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other597 (98.84%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research Highlights

Safety/Toxicity (1)

ArticleYear
CRF activates autonomic nervous system and reduces natural killer cytotoxicity.
The American journal of physiology, Volume: 255, Issue: 5 Pt 2
1988
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Long-term Use (4)

ArticleYear
Effect of insulin on regional vascular resistances in conscious rats.
The American journal of physiology, Volume: 270, Issue: 2 Pt 2
1996
Acute and chronic angiotensin hypertension: neural and nonneural components, time course, and dose dependency.
The American journal of physiology, Volume: 271, Issue: 1 Pt 2
1996
Regulation of nicotinic receptors in rat brain following quasi-irreversible nicotinic blockade by chlorisondamine and chronic treatment with nicotine.
British journal of pharmacology, Volume: 113, Issue: 3
1994
Effects of chronic nicotine administration on the denervated rat adrenal medulla.
British journal of pharmacology, Volume: 56, Issue: 2
1976
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Pharmacokinetics (3)

ArticleYear
Chronic angiotensin II infusion attenuates the renal sympathoinhibitory response to acute volume expansion.
American journal of physiology. Regulatory, integrative and comparative physiology, Volume: 284, Issue: 4
2003
The measurement of norepinephrine clearance and spillover rate into plasma in conscious spontaneously hypertensive rats.
Naunyn-Schmiedeberg's archives of pharmacology, Volume: 338, Issue: 4
1988
Cardiovascular effects of and interaction between calcium blocking drugs and anesthetics in chronically instrumented dogs. V. Role of pharmacokinetics and the autonomic nervous system in the interactions between verapamil and inhalational anesthetics.
Anesthesiology, Volume: 67, Issue: 3
1987
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Dosage (11)

ArticleYear
Lipid-enriched enteral nutrition controls the inflammatory response in murine Gram-negative sepsis.
Critical care medicine, Volume: 38, Issue: 10
2010
Modulation of neuronal nicotinic acetylcholine receptors by halothane in rat cortical neurons.
Molecular pharmacology, Volume: 59, Issue: 4
2001
Post-junctional mechanisms involved in the potentiation of cardiac adrenergic responses by cocaine.
European journal of pharmacology, May-26, Volume: 397, Issue: 1
2000
Bradykinin B2-receptors mediate the pressor and renal hemodynamic effects of intravenous bradykinin in conscious rats.
Journal of the autonomic nervous system, Jan-15, Volume: 75, Issue: 1
1999
Role of muscarinic receptors in ganglionic transmission in rabbits.
Journal of the autonomic nervous system, Jan-05, Volume: 56, Issue: 3
1996
Pulmonary effects of endogenous and exogenous nitric oxide in the pig: relation to cigarette smoke inhalation.
British journal of pharmacology, Volume: 110, Issue: 2
1993
Activation of nicotinic acetylcholine receptors on cultured Drosophila and other insect neurones.
The Journal of physiology, Volume: 463
1993
An investigation into the selectivity of a novel series of benzoquinolizines for alpha 2-adrenoceptors in vivo.
British journal of pharmacology, Volume: 82, Issue: 1
1984
Alpha 1-adrenoceptor subtypes and the regulation of peripheral hemodynamics in the conscious rat.
European journal of pharmacology, Sep-21, Volume: 186, Issue: 2-3
1990
Cardiovascular effects of cocaine in conscious rats: relative significance of central sympathetic stimulation and peripheral neuronal monoamine uptake and release mechanisms.
The Journal of pharmacology and experimental therapeutics, Volume: 262, Issue: 2
1992
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]