Jacek Sapa

ORCID: 0000-0003-4670-1665
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About
Contact & Profiles
Research Areas
  • Receptor Mechanisms and Signaling
  • Crystallization and Solubility Studies
  • X-ray Diffraction in Crystallography
  • Chemical synthesis and pharmacological studies
  • Neuroscience and Neuropharmacology Research
  • Synthesis and biological activity
  • Synthesis and Biological Evaluation
  • Cardiac electrophysiology and arrhythmias
  • Synthesis and Reactivity of Heterocycles
  • Analytical Methods in Pharmaceuticals
  • Neurotransmitter Receptor Influence on Behavior
  • Eicosanoids and Hypertension Pharmacology
  • Neuropeptides and Animal Physiology
  • Tryptophan and brain disorders
  • Pharmacological Receptor Mechanisms and Effects
  • Synthesis and Characterization of Heterocyclic Compounds
  • Phenothiazines and Benzothiazines Synthesis and Activities
  • Adenosine and Purinergic Signaling
  • Mast cells and histamine
  • Synthesis of heterocyclic compounds
  • Vanadium and Halogenation Chemistry
  • Synthesis and pharmacology of benzodiazepine derivatives
  • Treatment of Major Depression
  • Cardiac Ischemia and Reperfusion
  • Natural Compound Pharmacology Studies

Jagiellonian University
2015-2024

Pharmac
2013-2014

Farmak (Czechia)
2013

University of Wrocław
2001-2006

A series of new derivatives N-(2-methoxyphenyl)piperazine have been synthesized for their affinity toward serotonergic receptors and potential antidepressant-like activity. They evaluated 5-HT1A , 5-HT6 5-HT7 as well in vivo the tail suspension, locomotor activity, motor co-ordination tests. All tested compounds proved very good affinities receptors. The most promising compound was 1-[(2-chloro-6-methylphenoxy)ethoxyethyl]-4-(2-methoxyphenyl)piperazine hydrochloride, exhibiting Ki <1 nm...

10.1111/cbdd.12394 article EN Chemical Biology & Drug Design 2014-07-26

The aim of this study was to further characterize pharmacological properties two phenylpiperazine derivatives: 1-{2-[2-(2,6-dimethlphenoxy)ethoxy]ethyl}-4-(2-methoxyphenyl)piperazynine hydrochloride (HBK-14) and 2-[2-(2-chloro-6-methylphenoxy)ethoxy]ethyl-4-(2- methoxyphenyl)piperazynine dihydrochloride (HBK-15) in radioligand binding functional vitro assays as well vivo models. Antidepressant-like were investigated the forced swim test (FST) mice rats. Anxiolytic-like activity evaluated...

10.1371/journal.pone.0142499 article EN cc-by PLoS ONE 2015-11-10

The search for drugs with anorectic activity, acting within the adrenergic system has attracted interest of researchers. Partial α2-adrenoceptor agonists might offer potential effective and safe treatment obesity. We compared effectiveness safety ligands in reducing body mass. also analyzed if antagonist partial α2-adrenoceptor––yohimbine guanfacine––act similarly, determined which course action is connected activity. tested intrinsic activity effect on lipolysis these compounds cell...

10.1371/journal.pone.0141327 article EN cc-by PLoS ONE 2015-10-27

Abstract Twenty-four oxidovanadium(IV,V) complexes with tridentate Schiff base ligands based on 5-nitrosalicylaldehyde, 5-methoxysalicylaldehyde, or 5-sulfosalicylaldehyde and respective hydrazide were isolated, characterized using physicochemical spectroscopic methods. Three of them structurally by single-crystal X-ray structure determination. The biological activity studies included inhibition human tyrosine phosphatases, myocyte C2C12, adipocyte 3T3-L1, hepatocyte HepG2 cell lines,...

10.1007/s11243-020-00437-1 article EN cc-by Transition Metal Chemistry 2020-12-24

A2B adenosine receptors are present in a wide spectrum of tissues, especially on cells the immune system. Since these particular have lowest, all receptor subtypes, affinity for they believed to play special role immunological processes associated with elevated levels such as inflammation. The aim this preliminary study was determine potential anti-inflammatory properties compound PSB-603, potent and selective antagonist, two different experimental models local systemic In model inflammation...

10.1016/j.biopha.2020.111164 article EN Biomedicine & Pharmacotherapy 2020-12-29

<b>Objectives:</b> Xanthones are flavonoids with numerous activities, including antioxidant, antidepressant., or anxiolytic-like. Therefore, the aim of our study was to determine antidepressant- and anxiolytic-like properties four xanthone derivatives (3-chloro-5-[(4-methylpiperazin-1-yl)methyl]-9H-xanthen-9-one dihydrochloride [HBK-5], 6-methoxy-2-[(4-methylpiperazin-1-yl) methyl]-9H-xanthen-9-one dihydrochloride, 2-[(4-benzylpiperazin-1-yl) methyl]-6-methoxy-9H-xanthen-9-one...

10.4103/0253-7613.182872 article EN Indian Journal of Pharmacology 2016-01-01

The use of atypical antipsychotic drugs like olanzapine is associated with side effects such as sedation and depression-like symptoms, especially during the initial period use. It believed that occurrence these undesirable effectsis mainly result histamine H1receptors blockade by olanzapine. In addition, increases level triglycerides in blood, which correlates growing obesity. aim this study was to investigate influence pitolisant – H3 antagonist - on subchronic olanzapine-induced...

10.1007/s11011-016-9840-z article EN cc-by Metabolic Brain Disease 2016-05-24

A series of novel arylpiperazines bearing a pyrrolidin-2-one fragment was synthesized and evaluated for the binding affinity alpha(1)- alpha(2)-adrenoceptors (AR) antiarrhythmic hypotensive activities compounds. The most potent selective compound 1-[2-hydroxy-3-[4-[(2-hydroxyphenyl)piperazin-1-yl]propyl]pyrrolidin-2-one 8 binds with pK(i) = 6.71 alpha(1)-AR. Derivative also active in prophylactic test adrenaline-induced arrhythmia anaesthetized rats. Its ED(50 )value equals 1.9 mg/kg (i.v.)....

10.1002/ardp.200700039 article EN Archiv der Pharmazie 2007-09-01

Studies proved that among all α1-adrenoceptors, cardiac myocytes functionally express only α1A- and α1B-subtype. Scientists indicated α1A-subtype blockade might be beneficial in restoring normal heart rhythm. Therefore, we aimed to determine the role of α1-adrenoceptors subtypes (i.e. α1A α1B) antiarrhythmic effect six structurally similar derivatives 2-methoxyphenylpiperazine. We compared activity studied compounds with carvedilol, which is β1- blocker antioxidant properties. To evaluate...

10.3389/fphar.2016.00229 article EN cc-by Frontiers in Pharmacology 2016-08-02
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