Antihistamine activity and central effects of WAL 801 CL in man

1987 ◽  
Vol 33 (4) ◽  
pp. 381-385 ◽  
Author(s):  
W. S. Adamus ◽  
J. Oldigs-Kerber ◽  
H. F. Lohmann
Keyword(s):  
Central Effects ◽  
Antihistamine Activity

Potential antihistamine agents: 4-(6,11-Dihydrodibenzo[b,e]thiepin-11-ylidene)-1-methyltetrahydrothiopyranium iodide and similar sulfonium salts derived from related tricyclic systems

1987 ◽  
Vol 52 (11) ◽  
pp. 2758-2774 ◽  
Author(s):  
Zdeněk Polívka ◽  
Jiří Holubek ◽  
Miloš Buděšínský ◽  
Oluše Matoušová ◽  
Emil Svátek ◽  
...  
Keyword(s):  
Methyl Iodide ◽  
Methyl Derivative ◽  
Sulfonium Salt ◽  
Sulfonium Salts ◽  
Central Effects ◽  
Tertiary Alcohols ◽  
Antihistamine Activity ◽  
Grignard Reactions ◽  
By Products

Thioxanthone, 10,11-dihydrodibenzo[a,d]cyclohepten-5-one, dibenzo[b,e]thiepin-11(6H)-one, its 2-methyl derivative, and thieno[2,3-c]-2-benzothiepin-4(9H)-one were reacted with 4-tetrahydrothiopyranylmagnesium bromide and the obtained tertiary alcohols IVabc, VIc, and XIX were dehydrated to the olefinic sulfides IXabc, Xc, and XXI. Addition of methyl iodide afforded the title compounds XIabc, XIIc, and XXII. The Grignard reactions were accompanied by the 1,6-addition giving the ketones XVI-XVIII as by-products. The reductive properties of tetrahydrothiopyranylmagnesium bromide were most striking in the case of reaction with 2-chlorothioxanthone; the isolation of thioxanthene and thioxanthone showed that nuclear dehalogenation took also place. Reactions of 11-chloro-6,11-dihydrodibenzo[b,e]thiepin and benzhydryl chloride with tetrahydrothiopyran-4-ol gave the sulfides XXV and XXVIII; whereas the latter reacted with methyl iodide under the formation of sulfonium salt XXIX, the former was cleaved and gave 4-hydroxyl-1-methyltetrahydrothiopyranium iodide (XXVI). The sulfonium salts are free of the central effects but their antihistamine activity is rather low.

A brief review on the use of cannabis as a treatment option for local inflammation in peripheral tissue01

2020 ◽  
Author(s):  
Lungwani Muungo
Keyword(s):  
Secondary Metabolites ◽  
Treatment Option ◽  
Cell Injury ◽  
Local Inflammation ◽  
Topical Formulations ◽  
Central Effects ◽  
Complex Process ◽  
Anti Inflammatory

Inflammation is a complex process which, ideally, comes about as a “mop up’ response to cell injury. Ithowever occasionally results in undesired effects that should otherwise be prevented or resolvedspeedily. There are available numerous medicines with varied modes of administration commerciallyavailable for the management of inflammation. With the growing evidence of cannabis’ therapeuticeffects, its anti-inflammatory properties being one of them, debates among proponents and opponents ofcannabis use are ever growing. These debates are centered on the undesired central effects of some of theplants secondary metabolites an argument that can be moderated by using the plant in a manner thatsteers clear of these effects. Effective topical formulations could very well be one avenue through whichnature can be allowed to heal with minimal negative repercussions.

6,11-Dihydrodibenzo[b,e]thiepin-11-yl 3-quinuclidinyl ethers: New potential intidepressants and antihistamine agents

1988 ◽  
Vol 53 (8) ◽  
pp. 1806-1811 ◽  
Author(s):  
Zdeněk Polívka ◽  
Jan Metyš ◽  
Miroslav Protiva
Keyword(s):  
Methyl Derivative ◽  
Antihistamine Activity ◽  
Antidepressant Agent ◽  
Anticataleptic Activity

Reactions of 11-chloro-6,11-dihydrodibenzo[b,e]thiepin and its 2-methyl derivative, and further of the methanesulfonates of 2-chloro- and 2-bromo-6,11-dihydrodibenzo[b,e]thiepin-11-ol with 3-quinuclidinol afforded the title ethers I-IV. The 2-methyl compound II (VÚFB-17 088) showed significant antihistamine activity and the 2-chloro compound III (VÚFB-17 089), having antireserpine and anticataleptic activity, proved a potential antidepressant agent.

Evaluation of Importance of Central Effects of Atenolol and Metoprolol Measured by Heart Rate Variability During Mental Performance Tasks, Physical Exercise, and Daily Life in Stable Postinfarct Patients

Circulation ◽  
1995 ◽  
Vol 92 (12) ◽  
pp. 3415-3423 ◽  
Author(s):  
Ype S. Tuininga ◽  
Harry J.G.M. Crijns ◽  
Jan Brouwer ◽  
Maarten P. van den Berg ◽  
Arie J. Man in’t Veld ◽  
...  
Keyword(s):  
Heart Rate ◽  
Heart Rate Variability ◽  
Physical Exercise ◽  
Daily Life ◽  
Mental Performance ◽  
Performance Tasks ◽  
Central Effects

Neuroimaging in Drug Discovery and Development: Paradigms for Accelerating New Drug Availability

2001 ◽  
Vol 14 (5) ◽  
pp. 407-415
Author(s):  
John T. Metz ◽  
Malcolm D. Cooper ◽  
Terry F. Brown ◽  
Leann H. Kinnunen ◽  
Declan J. Cooper
Keyword(s):  
Blood Flow ◽  
Cerebral Blood Flow ◽  
Glucose Metabolism ◽  
Phase Ii ◽  
New Drugs ◽  
Central Effects ◽  
Drug Discovery And Development ◽  
Psychological Tasks ◽  
The Brain ◽  
Phase Iv

The process of discovering and developing new drugs is complicated. Neuroimaging methods can facilitate this process. An analysis of the conceptual bases and practical limitations of different neuroimaging modalities reveals that each technique can best address different kinds of questions. Radioligand studies are well suited to preclinical and Phase II questions when a compound is known or suspected to affect well-understood mechanisms; they are also useful in Phase IV to characterize effective agents. Cerebral blood flow studies can be extremely useful in evaluating the effects of a drug on psychological tasks (mostly in Phase IV). Glucose metabolism studies can answer the simplest questions about whether a compound affects the brain, where, and how much. Such studies are most useful in confirming central effects (preclinical and early clinical phases), in determining effective dose ranges (Phase II), and in comparing different drugs (Phase IV).

scholarly journals Correction: Paszkiewicz et al. A Peripheral CB1R Antagonist Increases Lipolysis, Oxygen Consumption Rate, and Markers of Beiging in 3T3-L1 Adipocytes Similar to RIM, Suggesting That Central Effects Can Be Avoided. Int. J. Mol. Sci. 2020, 21, 6639

2021 ◽  
Vol 22 (9) ◽  
pp. 4366
Author(s):  
Rebecca L. Paszkiewicz ◽  
Richard N. Bergman ◽  
Roberta S. Santos ◽  
Aaron P. Frank ◽  
Orison O. Woolcott ◽  
...  
Keyword(s):  
Oxygen Consumption ◽  
Oxygen Consumption Rate ◽  
Consumption Rate ◽  
Central Effects

The authors wish to make the following corrections to this paper [...]

scholarly journals Mechanistic Studies of the Antiallergic Activity of Phyllanthus amarus Schum. & Thonn. and Its Compounds

Molecules ◽  
2021 ◽  
Vol 26 (3) ◽  
pp. 695
Author(s):  
Nur Zahirah Abd Rani ◽  
Kok Wai Lam ◽  
Juriyati Jalil ◽  
Hazni Falina Mohamad ◽  
Mohd Shukri Mat Ali ◽  
...  
Keyword(s):  
High Performance ◽  
Binding Assay ◽  
Radioligand Binding ◽  
Positive Control ◽  
Phyllanthus Amarus ◽  
H1 Receptor ◽  
Antiallergic Activity ◽  
Ketotifen Fumarate ◽  
Antihistamine Activity ◽  
Basophilic Leukemia

Phyllanthus amarus Schum. & Thonn. (Phyllanthaceae) is a medicinal plant that is commonly used to treat diseases such as asthma, diabetes, and anemia. This study aimed to examine the antiallergic activity of P. amarus extract and its compounds. The antiallergic activity was determined by measuring the concentration of allergy markers release from rat basophilic leukemia (RBL-2H3) cells with ketotifen fumarate as the positive control. As a result, P. amarus did not stabilize mast cell degranulation but exhibited antihistamine activity. The antihistamine activity was evaluated by conducting a competition radioligand binding assay on the histamine 1 receptor (H1R). Four compounds were identified from the high performance liquid chromatography (HPLC) analysis which were phyllanthin (1), hypophyllanthin (2), niranthin (3), and corilagin (4). To gain insights into the binding interactions of the most active compound hypophyllanthin (2), molecular docking was conducted and found that hypophyllanthin (2) exhibited favorable binding in the H1R binding site. In conclusion, P. amarus and hypophyllanthin (2) could potentially exhibit antiallergic activity by preventing the activation of the H1 receptor.

Toxicology and the vulnerable brain

1995 ◽  
Vol 7 (1) ◽  
pp. 1-6 ◽  
Author(s):  
D.R.A. Uges
Keyword(s):  
The Netherlands ◽  
Forensic Toxicology ◽  
Symptomatic Treatment ◽  
Environmental Toxicology ◽  
Clinical Toxicology ◽  
Suicidal Attempt ◽  
Central Effects ◽  
The Past ◽  
Cardio Vascular ◽  
The Brain

SummaryToxicology is one of the eldest areas of special attention in medicine and pharmacy. In the past, forensic toxicology was the most important part, but nowadays, at least in the Netherlands, the clinical, occupational and environmental toxicology have the centre of attention.The brain plays its own role in the clinical toxicology. There the intoxication can take place, it can be the basis of the peripheral symptoms of the intoxication or it can be the cause of the intoxication, e.g. at a suicidal attempt or the hospital addiction syndrome.The somatic treatment of an intoxicated patient includes in the first place the stabilization of the patient (cardio-vascular, ventilation and central effects); then the removal of the poison from the surroundings and out of the patient by different suitable methods and finally the symptomatic treatment, sometimes with antidotes.In the Netherlands, hardly any intoxication is fatal, when the patient arrives in the hospital in time, or euthanasia took place on purpose.

scholarly journals Acute Nicotine Reduces Brain Arachidonic Acid Signaling in Unanesthetized Rats

2009 ◽  
Vol 29 (3) ◽  
pp. 648-658 ◽  
Author(s):  
Lisa Chang ◽  
Stanley I Rapoport ◽  
Henry N Nguyen ◽  
Dede Greenstein ◽  
Mei Chen ◽  
...  
Keyword(s):  
Arachidonic Acid ◽  
Nicotinic Acetylcholine Receptors ◽  
Acetylcholine Receptors ◽  
Brain Regions ◽  
Membrane Phospholipids ◽  
Dose Equivalent ◽  
Central Effects ◽  
Postsynaptic Receptors ◽  
Cytosolic Phospholipase ◽  
Presynaptic Release

Nicotine exerts its central effects by activating pre- and postsynaptic nicotinic acetylcholine receptors (nAChRs). Presynaptic nAChRs modulate the release of many neurotransmitters that bind to postsynaptic receptors. These may be coupled to the activation of cytosolic phospholipase A2 (cPLA2), which hydrolyzes arachidonic acid (AA) from membrane phospholipids. We hypothesized that nicotine would modify brain signaling involving AA by binding to nAChRs. Nicotine (0.1 mg/kg, subcutaneously) or saline was injected 2 or 10 mins before infusing [1-14C]AA in unanesthetized rats. The AA incorporation coefficient k∗ (a marker of the AA signal) was measured in 80 brain regions by quantitative autoradiography. Nicotine, compared to saline, when administrated 2 mins before [1-14C]AA infusion, significantly decreased k∗ for AA in 26 regions, including cerebral cortex, thalamus, and habenula—interpeduncular regions, by 13% to 45%. These decreases could be entirely prevented by pretreatment with mecamylamine (1.0 mg/kg, subcutaneously). When administered 10 mins before [1-14C]AA infusion, nicotine did not alter any value of k∗. In summary, nicotine given to unanesthetized rats rapidly reduces signaling involving AA in brain regions containing nAChRs, likely by modulating the presynaptic release of neurotransmitters. The effect shows rapid desensitization and is produced at a nicotine dose equivalent to smoking one cigarette in humans.

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