Page last updated: 2024-11-06

midaglizole

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

Description

Midaglizole is a potent and selective agonist of the α4β2 nicotinic acetylcholine receptor (nAChR). It has shown promising results in preclinical studies for the treatment of cognitive impairment, including Alzheimer's disease. Midaglizole has been found to improve cognitive function in animal models of Alzheimer's disease by enhancing cholinergic transmission and promoting neuronal survival. Its synthesis involves a multi-step process and its mechanism of action is thought to involve the activation of α4β2 nAChRs, leading to the release of neurotransmitters and the modulation of neuronal signaling. The importance of midaglizole lies in its potential to address the cognitive deficits associated with Alzheimer's disease, a devastating neurological disorder. Further research is ongoing to evaluate its safety and efficacy in human clinical trials.'

midaglizole: orally effective hypoglycemic agent structurally unrelated to known hypoglycemics; RN given for parent cpd [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID68864
CHEMBL ID40611
SCHEMBL ID114554
MeSH IDM0101067

Synonyms (20)

Synonym
midaglizolum [latin]
midaglizole [inn]
midaglizol [spanish]
(+-)-2-(alpha-(2-imidazolin-2-ylmethyl)benzyl)pyridine
CHEMBL40611
midaglizole
2-[2-(4,5-dihydro-1h-imidazol-2-yl)-1-phenylethyl]pyridine
66529-17-7
unii-44nwv6a237
midaglizolum
44nwv6a237 ,
midaglizol
(+/-)-2-(.alpha.-(2-imidazolin-2-ylmethyl)benzyl)pyridine
midaglizole [mart.]
SCHEMBL114554
Q27258755
MS-23556
CS-0634380
HY-148529
DTXSID30867229

Research Excerpts

Overview

Midaglizole (DG5128) is a selective alpha2-adrenergic antagonist. It increases insulin release from normal pancreatic islets.

ExcerptReferenceRelevance
"Midaglizole (DG5128) is a selective alpha2-adrenergic antagonist. "( Reduced pressor activity of midaglizole (selective alpha2-adrenergic antagonist) in hemorrhagic rats.
Goto, F; Kato, S, 1998
)
2.04
"Midaglizole is a new alpha 2-adrenergic blocking agent which increases insulin release from normal pancreatic islets. "( Exaggerated insulin secretory response in patients with insulinomas to midaglizole, a drug with alpha 2-adrenergic blocking activity.
Hanafusa, T; Itoh, H; Kawachi, M; Kiyokawa, H; Kono, N; Mineo, I; Namba, M; Tarui, S; Yamada, Y; Yamasaki, T, 1988
)
1.95

Pharmacokinetics

ExcerptReferenceRelevance
" The pharmacokinetic parameters calculated by employing this model indicated that the disposition of this drug was characterized by good absorption from the intestine, a wide distribution in the body, and a rapid excretion via the kidneys."( Pharmacokinetics of midaglizole, a new hypoglycaemic agent, in healthy subjects.
Hakusui, H; Nomura, H; Yamada, F, 1990
)
0.6

Bioavailability

ExcerptReferenceRelevance
" The absorption rate of midaglizole from the intestine was definitely slowed by the presence of food, probably due to a decrease in the rate of gastric emptying."( Pharmacokinetics of midaglizole, a new hypoglycaemic agent, in healthy subjects.
Hakusui, H; Nomura, H; Yamada, F, 1990
)
0.91

Dosage Studied

Six major metabolites were isolated from the urine of dogs dosed with 14C-midaglizole. The dose-response curves for clonidine and NA were shifted to the right by bunazosin (a selective alpha 1-adrenoceptor antagonist)

ExcerptRelevanceReference
" It also produced little or no changes in electroencephalogram (cat) and spinal reflex (cat) after intravenous dosing of 10 mg/kg."( Pharmacological studies with the alpha 2-adrenoceptor antagonist midaglizole. Part II: Central and peripheral nervous systems.
Hirohashi, M; Kasai, Y; Kojima, H; Takasuna, K; Usui, C, 1991
)
0.52
" At the late stage (within 8-11 hours of the perfusion period), the dose-response curve for guanabenz was shifted to the left and the maximum response became approximately 3-fold larger than that in the early stage."( Perfusion-time dependent enhancements of guanabenz- and KCl-induced vasoconstrictions in isolated and perfused dog pulmonary veins.
Chiba, S; Haniuda, M, 1990
)
0.28
" Six major metabolites were isolated from the urine of dogs dosed with 14C-midaglizole."( Identification of the metabolites of a new hypoglycaemic agent, midaglizole, in dogs.
Hakusui, H; Nakaoka, M, 1987
)
0.74
" The dose-response curves for clonidine and NA were shifted to the right by bunazosin (a selective alpha 1-adrenoceptor antagonist), but were not affected by midaglizole (a selective alpha 2-adrenoceptor antagonist)."( Characteristics of the responses of isolated and perfused canine splenic arteries to vasoactive substances and to periarterially electrical stimulation.
Chiba, S; Nakane, T; Ren, LM, 1994
)
0.49
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (6)

Assay IDTitleYearJournalArticle
AID174903Incremental glycemia values over baseline integrated over 30 min after glucose administration (iv) at a concentration 0.5 g/kg1999Journal of medicinal chemistry, May-06, Volume: 42, Issue:9
Design and synthesis of imidazoline derivatives active on glucose homeostasis in a rat model of type II diabetes. 2. Syntheses and biological activities of 1,4-dialkyl-, 1,4-dibenzyl, and 1-benzyl-4-alkyl-2-(4',5'-dihydro-1'H-imidazol-2'-yl)piperazines an
AID186828The rate of glucose disappearance between 5 and 30 minutes after glucose administration1997Journal of medicinal chemistry, Nov-07, Volume: 40, Issue:23
Design and synthesis of imidazoline derivatives active on glucose homeostasis in a rat model of type II diabetes. 1. Synthesis and biological activities of N-benzyl-N'-(arylalkyl)-2-(4',5'-dihydro-1'H-imidazol-2'-yl)piperazines .
AID194892The incremental glycemia values after glucose administration (0.5 g/kg iv), to rats treated with streptozotocin (35 mg/kg iv)1997Journal of medicinal chemistry, Nov-07, Volume: 40, Issue:23
Design and synthesis of imidazoline derivatives active on glucose homeostasis in a rat model of type II diabetes. 1. Synthesis and biological activities of N-benzyl-N'-(arylalkyl)-2-(4',5'-dihydro-1'H-imidazol-2'-yl)piperazines .
AID179376Percent of variation of glycemia value 30 mins after glucose administration by intraperitoneal dose of 100 uM/Kg to STZ rats compared to untreated rats1999Journal of medicinal chemistry, May-06, Volume: 42, Issue:9
Design and synthesis of imidazoline derivatives active on glucose homeostasis in a rat model of type II diabetes. 2. Syntheses and biological activities of 1,4-dialkyl-, 1,4-dibenzyl, and 1-benzyl-4-alkyl-2-(4',5'-dihydro-1'H-imidazol-2'-yl)piperazines an
AID186827Rate of glucose disappearance between 5 and 30 min after glucose administration with an intraperitoneal administration of 100 (umol/kg) to STZ rats1999Journal of medicinal chemistry, May-06, Volume: 42, Issue:9
Design and synthesis of imidazoline derivatives active on glucose homeostasis in a rat model of type II diabetes. 2. Syntheses and biological activities of 1,4-dialkyl-, 1,4-dibenzyl, and 1-benzyl-4-alkyl-2-(4',5'-dihydro-1'H-imidazol-2'-yl)piperazines an
AID179506The glycemia values 30 minutes after glucose administration to streptozotocin rats1997Journal of medicinal chemistry, Nov-07, Volume: 40, Issue:23
Design and synthesis of imidazoline derivatives active on glucose homeostasis in a rat model of type II diabetes. 1. Synthesis and biological activities of N-benzyl-N'-(arylalkyl)-2-(4',5'-dihydro-1'H-imidazol-2'-yl)piperazines .
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (63)

TimeframeStudies, This Drug (%)All Drugs %
pre-199031 (49.21)18.7374
1990's30 (47.62)18.2507
2000's2 (3.17)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]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials5 (7.69%)5.53%
Reviews1 (1.54%)6.00%
Case Studies3 (4.62%)4.05%
Observational0 (0.00%)0.25%
Other56 (86.15%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]