Search results for "Agoni"
showing 10 items of 2493 documents
Fingolimod as a Treatment in Neurologic Disorders Beyond Multiple Sclerosis
2020
Abstract Fingolimod is an approved treatment for relapsing–remitting multiple sclerosis (MS), and its properties in different pathways have raised interest in therapy research for other neurodegenerative diseases. Fingolimod is an agonist of sphingosine-1-phosphate (S1P) receptors. Its main pharmacologic effect is immunomodulation by lymphocyte homing, thereby reducing the numbers of T and B cells in circulation. Because of the ubiquitous expression of S1P receptors, other effects have also been described. Here, we review preclinical experiments evaluating the effects of treatment with fingolimod in neurodegenerative diseases other than MS, such as Alzheimer’s disease or epilepsy. Fingolimo…
Synthesis of 2-Prenylated Alkoxylated Benzopyrans by Horner–Wadsworth–Emmons Olefination with PPARα/γ Agonist Activity
2021
[Image: see text] We have synthesized series of 2-prenylated benzopyrans as analogues of the natural polycerasoidol, a dual PPARα/γ agonist with anti-inflammatory effects. The prenylated side chain consists of five or nine carbons with an α-alkoxy-α,β-unsaturated ester moiety. Prenylation was introduced via the Grignard reaction, followed by Johnson–Claisen rearrangement, and the α-alkoxy-α,β-unsaturated ester moiety was introduced by the Horner–Wadsworth–Emmons reaction. Synthetic derivatives showed high efficacy to activate both hPPARα and hPPARγ as dual PPARα/γ agonists. These prenylated benzopyrans emerge as lead compounds potentially useful for preventing cardiometabolic diseases.
Voltage- and Agonist-Induced Activation of Smooth Muscle of the Human Upper Urinary Tract: Different Mechanisms
1985
Smooth muscles are such a remarkably diverse group of tissues that the difference in properties between any two of them may be as great as between a smooth muscle and a striated muscle. With this diversity it is not surprising that the ways in which different stimuli initiate contraction are also extremely varied and interesting although we still know very little about the details of the mechanisms involved. In an attempt to shed some light on the cellular contraction cycle of smooth muscle of the human upper urinary tract, this article will focus on two topics: 1. Previous findings in smooth muscle research will be summarized and discussed briefly as they are pertinent to an understanding …
Synthesis and pharmacological characterization of beta2-adrenergic agonist enantiomers: zilpaterol.
2009
The beta-adrenergic agonist 1 (zilpaterol) is used as production enhancer in cattle. Binding experiments of separated enantiomers on recombinant human beta(2)-adrenergic and mu-opioid receptors and functional studies showed that the (-)-1 enantiomer accounts for essentially all the beta(2)-adrenergic agonist activity and that it exhibits less affinity toward the mu-opioid receptor than (+)-1, which is a mu-opioid receptor antagonist. X-ray crystallography revealed the absolute configuration of (-)-1 to be 6R,7R.
Low-dose dopamine agonist administration blocks vascular endothelial growth factor (VEGF)-mediated vascular hyperpermeability without altering VEGF r…
2006
No specific treatment is available for ovarian hyperstimulation syndrome (OHSS), the most important complication in infertile women treated with gonadotropins. OHSS is caused by increased vascular permeability (VP) through ovarian hypersecretion of vascular endothelial growth factor (VEGF)activating VEGF receptor 2 (VEGFR-2). We previously demonstrated in an OHSS rodent model that increased VP was prevented by inactivating VEGFR-2 with a receptor antagonist(SU5416).However,duetoitstoxicity(thromboembolism) and disruption of VEGFR-2-dependent angiogenic processes critical for pregnancy, this kind of compound cannot be used clinically to prevent OHSS. Dopamine receptor 2 (Dp-r2) agonists, use…
Modulation by fenoldopam (SKF 82526) and bromocriptine of the electrically evoked release of vasopressin from the rat neurohypophysis. Effects of dop…
1986
1. Single neurointermediate lobes were fixed by their stalks to a platinum wire electrode and incubated in Krebs-bicarbonate solution. Vasopressin release into the medium was determined by a radioimmunoassay. Vasopressin secretion was increased by electrical stimulation (15 Hz, 10 s trains with 10 s intervals for 10 min). 2. Fenoldopam (SKF 82526) had a dual effect on vasopressin release, 30 nM decreasing (by 30%) and 3 μM increasing (by 32%) the evoked vasopressin secretion. The facilitatory effect of fenoldopam was antagonized in a concentration-dependent manner by flupenthixol but not by sulpiride. Sulpiride (1 μM) prevented the inhibitory effect of fenoldopam (30 μM). 3. After pretreatm…
Synthetic studies of neoclerodane diterpenoids from Salvia splendens and evaluation of opioid receptor affinity
2008
Abstract Salvinorin A ( 1 ), a neoclerodane diterpene from the hallucinogenic mint Salvia divinorum , is the only known non-nitrogenous and specific κ-opioid agonist. Several structural congeners of 1 isolated from Salvia splendens ( 2 – 8 ) together with a series of semisynthetic derivatives ( 9 – 24 ), some of which possess a pyrazoline structural moiety ( 9 , 19 – 22 ), have been tested for affinity at human μ, δ, and κ opioid receptors. None of these compounds showed high affinity binding to these receptors. However, 10 showed modest affinity for κ receptors suggesting that other natural neoclerodanes from different Salvia species may possess opioid affinity.
Adrenoceptors in GtoPdb v.2021.3
2021
The nomenclature of the Adrenoceptors has been agreed by the NC-IUPHAR Subcommittee on Adrenoceptors [60, 186]. Adrenoceptors, α1 The three α1-adrenoceptor subtypes α1A, α1B and α1D are activated by the endogenous agonists (-)-adrenaline and (-)-noradrenaline. -(-)phenylephrine, methoxamine and cirazoline are agonists and prazosin and doxazosin antagonists considered selective for α1- relative to α2-adrenoceptors. [3H]prazosin and [125I]HEAT (BE2254) are relatively selective radioligands. S(+)-niguldipine also has high affinity for L-type Ca2+ channels. Fluorescent derivatives of prazosin (Bodipy FLprazosin- QAPB) are used to examine cellular localisation of α1-adrenoceptors. α1-Adrenocepto…
Darstellung und H2-agonistische Aktivität alkylsubstituierter 3-(Imidazol-4-yl)propylguanidine Synthesis and H2-Agonistic Activity of Alkyl-3-(imidaz…
1987
Derivate des 3-(Imidazol-4-yl)propylguanidins mit einem Methyl- oder einem 2-(Ethylthio)ethyl-Substituenten2) an der Guanidin-Gruppe weisen am H2-Rezeptor des Meerschweinchenvorhofs nur 10–20% der Histaminaktivitat auf. Dagegen fuhrt die Substitution mit der H2-affinen 2-[(5-Methylimidazol-4-yl) methylthio]ethyl-Gruppierung zu Impromidin, einem hochpotenten H2-Agonisten.
Racemische Histamin-H1-Agonisten
1984
Es wurden racemische α- und β-methylverzweigte 2-(2-Aminoethyl)-thiazole und 2-(2-Aminoethyl)-imidazole (Isohistamine) dargestellt und auf Histamin-H1- und -H2-agonistische Aktivitat gepruft. Histamine Analogues, XXVI: Racemic Histamine H1-Agonists Racemic α or β-methylated 2-(2-aminoethyl)thiazoles and 2-(2-aminoethyl)imidazoles (isohistamines) were prepared and tested for histamine H1- and H2-agonistic activity.