Pharmacology of Histamine, Its Receptors and Antagonists in the Modulation of Physiological Functions

Gorain, Bapi; Sengupta, Pallav; Dutta, Sulagna; Pandey, Manisha; Choudhury, Hira

doi:10.1007/978-981-15-3556-7_7

Cited by 3 publications

(4 citation statements)

References 130 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The presented research focused on the search for new multifunctional compounds combining the properties of an MAO B inhibitor and the H 3 R. Taking into account the results of in vitro studies on the affinity for h H 3 R and hMAO B inhibitory activity ( h H 3 R: K i = 25 nM; hMAO B: IC 50 = 4 nM; Table 1 ) as well as low cytotoxicity ( Table 7 ), and predicted very good in vivo permeability in the PAMPA assay ( Table 6 ), the compound 13 was selected for in vivo studies. Thus, if H 3 R antagonists cross the BBB, they should affect food intake [ 18 , 31 ]. Experiments were conducted as described previously [ 20 , 32 , 33 ].…”

Section: Resultsmentioning

confidence: 99%

“…As already mentioned, the H 3 R also act as heteroreceptors which modulate the release of other neurotransmitters [ 17 , 18 ]. At this stage of the studies, it cannot be ruled out that the increase in catecholamine levels, especially DA, may also be the result of antagonistic activity of compound 13 towards H 3 R.…”

Section: Discussionmentioning

confidence: 99%

“…The compound 13 was given to intact Wistar rats to verify its impact on the metabolism of biogenic amines in the brain (cerebral amines and their metabolites concentrations as well as activities of metabolizing enzymes). Pitolisant (H 3 R antagonist/inverse agonist) was employed as a reference drug [ 17 , 18 ]. Both drugs (3 mg/kg body mass, dissolved in 0.9% NaCl) were given subcutaneously for 6 consecutive days.…”

Section: Methodsmentioning

confidence: 99%

See 2 more Smart Citations

Dual Targeting Ligands—Histamine H3 Receptor Ligands with Monoamine Oxidase B Inhibitory Activity—In Vitro and In Vivo Evaluation

et al. 2022

View full text Add to dashboard Cite

The clinical symptoms of Parkinson’s disease (PD) appear when dopamine (DA) concentrations in the striatum drops to around 20%. Simultaneous inhibitory effects on histamine H3 receptor (H3R) and MAO B can increase DA levels in the brain. A series of compounds was designed and tested in vitro for human H3R (hH3R) affinity and inhibitory activity to human MAO B (hMAO B). Results showed different activity of the compounds towards the two biological targets. Most compounds had poor affinity for hH3R (Ki > 500 nM), but very good inhibitory potency for hMAO B (IC50 < 50 nM). After further in vitro testing (modality of MAO B inhibition, permeability in PAMPA assay, cytotoxicity on human astrocyte cell lines), the most promising dual-acting ligand, 1-(3-(4-(tert-butyl)phenoxy)propyl)-2-methylpyrrolidine (13: hH3R: Ki = 25 nM; hMAO B IC50 = 4 nM) was selected for in vivo evaluation. Studies in rats of compound 13, in a dose of 3 mg/kg of body mass, confirmed its antagonistic effects for H3R (decline in food and a water consumption), decline in MAO B activity (> 90%) in rat cerebral cortex (CTX), and an increase in DA content in CTX and striatum. Moreover, compound 13 caused a slight increase in noradrenaline, but a reduction in serotonin concentration in CTX. Thus, compound 13 is a promising dual-active ligand for the potential treatment of PD although further studies are needed to confirm this.

show abstract

Section: Resultsmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

Section: Methodsmentioning

confidence: 99%

See 1 more Smart Citation

Dual Targeting Ligands—Histamine H3 Receptor Ligands with Monoamine Oxidase B Inhibitory Activity—In Vitro and In Vivo Evaluation

et al. 2022

View full text Add to dashboard Cite

show abstract

“…These amine moieties in the structures are frequently protonated under physiological pH conditions, and therefore, the respective molecules circulate in human bodies as ammonium or indeed as zwitterionic species. 1–3 Specific neurotransmitters and their concentrations in the neural system can be linked with various neurodegenerative disorders, such as Parkinson's disease or Alzheimer's disease. 4–6 This correlation relates to the interest in designing biomimetic sensors and artificial receptors, 7 that can be used to control and monitor the levels of the respective regulator molecules.…”

Section: Introductionmentioning

confidence: 99%

Solution- and gas-phase study of binding of ammonium and bisammonium hydrocarbons to oxacalix[4]arene carboxylate

et al. 2023

View full text Add to dashboard Cite

show abstract

Development of fluorescence chemo sensor for selective histamine determination in spiked human plasma samples

Alqahtani,

Abdelazim

2024

Spectrochimica Acta Part A: Molecular and Biomolecular Spectros

View full text Add to dashboard Cite

Pharmacology of Histamine, Its Receptors and Antagonists in the Modulation of Physiological Functions

Cited by 3 publications

References 130 publications

Dual Targeting Ligands—Histamine H3 Receptor Ligands with Monoamine Oxidase B Inhibitory Activity—In Vitro and In Vivo Evaluation

Dual Targeting Ligands—Histamine H3 Receptor Ligands with Monoamine Oxidase B Inhibitory Activity—In Vitro and In Vivo Evaluation

Solution- and gas-phase study of binding of ammonium and bisammonium hydrocarbons to oxacalix[4]arene carboxylate

Development of fluorescence chemo sensor for selective histamine determination in spiked human plasma samples

Contact Info

Product

Resources

About