Page last updated: 2024-11-06

tiamenidine

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Tiamenidine is an imidazoline derivative that acts as an α2-adrenergic agonist. It was initially developed as an antihypertensive agent, but its use was limited due to potential side effects, such as sedation and dry mouth. However, tiamenidine has shown promise in the treatment of other conditions, such as anxiety, depression, and neuropathic pain. It is believed to exert its effects by stimulating α2-adrenergic receptors in the central nervous system, leading to a decrease in sympathetic nervous system activity. Research on tiamenidine continues to explore its therapeutic potential in various conditions and its underlying mechanisms of action.'

Cross-References

ID SourceID
PubMed CID39974
CHEMBL ID295409
CHEBI ID134896
SCHEMBL ID112844
MeSH IDM0055778

Synonyms (36)

Synonym
tiamenidine
sundralen
hoe-440
hoe 440
D06125
tiamenidine (usan/inn)
symcor base tts (tn)
31428-61-2
CHEBI:134896
CHEMBL295409
n-(2-chloro-4-methylthiophen-3-yl)-4,5-dihydro-1h-imidazol-2-amine
L001813
AKOS016013984
tiamenidinum
1h-imidazol-2-amine, n-(2-chloro-4-methyl-3-thienyl)-4,5-dihydro-
2-((2-chloro-4-methyl-3-thienyl)amino)-2-imidazoline
tiamenidina
tiamenidine [usan:inn:ban]
symcor base tts
tiamenidinum [inn-latin]
195v08o55g ,
unii-195v08o55g
tiamenidina [inn-spanish]
tiamenidine [who-dd]
tiamenidine [mi]
2-[(2-chloro-4-methyl-3-thienyl)amino]-2-imidazoline
tiamenidine [usan]
tiamenidine [inn]
SCHEMBL112844
DTXSID80185349
FT-0738662
bdbm50225292
Q7800109
A919194
HY-112074
CS-0043284

Research Excerpts

Overview

1 Tiamenidine (Hoe 440) is an imidazoline with blood pressure lowering properties.

ExcerptReferenceRelevance
"1 Tiamenidine (Hoe 440) is an imidazoline with blood pressure lowering properties. "( Changes in blood pressure, plasma catecholamines and plasma renin activity during and after treatment with tiamenidine and clonidine.
Hansson, BG; Hökfelt, B, 1981
)
1.2

Dosage Studied

ExcerptRelevanceReference
" In contrast, the dose-response curves to tiamenidine and clonidine were flatter and bell-shaped with maxima of 30 and 60 min, respectively."( Sleeping times evoked by alpha adrenoceptor agonists in two-day-old chicks: an experimental model to evaluate full and partial agonists at central alpha-2 adrenoceptors.
Cavero, I; Doxey, JC; Roach, AG; Strachan, DA, 1983
)
0.53
" Hypotensive potency after intravenous administration to anesthetized, normotensive rats was determined as a measure of central alpha-adrenergic activity and expressed as pC25, obtained from log dose-response curves."( Characterization of alpha-adrenoceptor populations. Quantitative relationships between cardiovascular effects initiated at central and peripheral alpha-adrenoceptors.
de Jonge, A; Lam, E; Slothorst-Grisdijk, FP; Timmermans, PB; van Meel, JC; van Zwieten, PA, 1981
)
0.26
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
organochlorine compoundAn organochlorine compound is a compound containing at least one carbon-chlorine bond.
[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]

Bioassays (9)

Assay IDTitleYearJournalArticle
AID36794Binding affinity against Alpha-2 adrenergic receptor is the ability to inhibit the specific [3H]clonidine binding (0.4 nM) to rat isolated brain membranes by 50% was reported; 9.1*10e-91984Journal of medicinal chemistry, Apr, Volume: 27, Issue:4
Quantitative relationships between alpha-adrenergic activity and binding affinity of alpha-adrenoceptor agonists and antagonists.
AID23715Apparent partion coefficient of compound was evaluated in octanol/buffer at pH of 7.4 at 37 degree Centigrade1984Journal of medicinal chemistry, Apr, Volume: 27, Issue:4
Quantitative relationships between alpha-adrenergic activity and binding affinity of alpha-adrenoceptor agonists and antagonists.
AID33252Peripheral hypertensive activity in pithed normotensive rats.1981Journal of medicinal chemistry, May, Volume: 24, Issue:5
Characterization of alpha-adrenoceptor populations. Quantitative relationships between cardiovascular effects initiated at central and peripheral alpha-adrenoceptors.
AID33250Central hypotensive activity in anesthetized normotensive rats.1981Journal of medicinal chemistry, May, Volume: 24, Issue:5
Characterization of alpha-adrenoceptor populations. Quantitative relationships between cardiovascular effects initiated at central and peripheral alpha-adrenoceptors.
AID197167Hypotensive activity (25% decrease in arterial pressure) after i.v. administration to anesthetized normotensive rats.1984Journal of medicinal chemistry, Apr, Volume: 27, Issue:4
Quantitative relationships between alpha-adrenergic activity and binding affinity of alpha-adrenoceptor agonists and antagonists.
AID227718Binding energy by using the equation deltaG obsd = -RT ln KD1984Journal of medicinal chemistry, Dec, Volume: 27, Issue:12
Functional group contributions to drug-receptor interactions.
AID197169Hypertensive activity (increase in arterial pressure to 60 mmHg)) after i.v. administration to pithed rats.1984Journal of medicinal chemistry, Apr, Volume: 27, Issue:4
Quantitative relationships between alpha-adrenergic activity and binding affinity of alpha-adrenoceptor agonists and antagonists.
AID36720Binding affinity against alpha-1 adrenergic receptor is the ability to inhibit the specific [3H]-prazosin binding (0.2 nM) to rat isolated brain membranes by 50% was reported; 4.85*10e-61984Journal of medicinal chemistry, Apr, Volume: 27, Issue:4
Quantitative relationships between alpha-adrenergic activity and binding affinity of alpha-adrenoceptor agonists and antagonists.
AID23716Partition coefficient (logD7.4)1981Journal of medicinal chemistry, May, Volume: 24, Issue:5
Characterization of alpha-adrenoceptor populations. Quantitative relationships between cardiovascular effects initiated at central and peripheral alpha-adrenoceptors.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (20)

TimeframeStudies, This Drug (%)All Drugs %
pre-199019 (95.00)18.7374
1990's1 (5.00)18.2507
2000's0 (0.00)29.6817
2010's0 (0.00)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 22.61

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index22.61 (24.57)
Research Supply Index3.30 (2.92)
Research Growth Index4.26 (4.65)
Search Engine Demand Index23.28 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (22.61)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials3 (13.04%)5.53%
Reviews3 (13.04%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other17 (73.91%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]