Search
Search Results
-
CYX-5, a G-protein biassed MOP receptor agonist, DOP receptor antagonist and KOP receptor agonist, evokes constipation but not respiratory depression relative to morphine in rats
BackgroundStrong opioid analgesics such as morphine alleviate moderate to severe acute nociceptive pain (e.g. post-surgical or post-trauma pain) as...
-
Effect of the Topical External Formulation of the Low-Affinity NMDA Receptor Antagonist Hemantane on Peripheral Sensitization Induced by TRPV1 Receptor Agonist Capsaicin in Mice
The effect of the noncompetitive low-affinity NMDA receptor antagonist hemantane [ N -(2-adamantyl)hexamethyleneimine hydrochloride) in two topical...
-
The Role of a Dopaminergic Component in the Analgesic Effect of the Low-Affinity NMDA Receptor Antagonist Hemantane
The role of dopaminergic transmission in the mechanism of analgesic action of the low-affinity NMDAreceptor antagonist hemantane [ N -(2-adamantyl)hexam...
-
NMDA-Receptor Antagonists Reduce Skin Sensitivity to the TRPV1-Receptor Agonist Capsaicin
Glutamate receptors are widely represented in the central and peripheral nervous systems, which determines their involvement in central and...
-
Novel object recognition test as an alternative approach to assessing the pharmacological profile of sigma-1 receptor ligands
BackgroundAlthough the terms “agonist” and “antagonist” have been used to classify sigma-1 receptor (σ 1 R) ligands, an unambiguous definition of the...
-
Physicochemical Properties of a Phenyltetrahydroquinolinedione Derivative with TRPA1 Antagonist Activity
A new active pharmaceutical ingredient (API) with TRPA1-antagonist activity (phenyltetrahydroquinolinedione derivative) was a white or almost white...
-
Synthesis and Adenosine RA1/A2A Receptor Affinity of Selected Aurones and 2-Benzylidene-1-Indanones
In the search to discover new adenosine A 1 /A 2A receptor ligands, ten aurones (2-benzylidenebenzofuran-3(2H)-ones) and 2-benzylidene-1-indanones were...
-
Clinical Efficacy of Long-Acting β2 Agonists and Long-Acting Muscarinic Antagonist for Moderate to Severe Chronic Obstructive Pulmonary Disease
We have studied the clinical efficacy of long-acting β2-agonist (LABA) and long-acting muscarinic antagonist (LAMA) for the treatment of moderate to...
-
The novel psychoactive substance 25E-NBOMe induces reward-related behaviors via dopamine D1 receptor signaling in male rodents
Novel psychoactive substances (NPSs) are new psychotropic drugs designed to evade substance regulatory policies. 25E-NBOMe...
-
Soluble dipeptidyl peptidase-4 induces epithelial–mesenchymal transition through tumor growth factor-β receptor
BackgroundKidney fibrosis is the final manifestation of chronic kidney disease, a condition mainly caused by diabetic nephropathy. Persistent tissue...
-
Evaluation of the effects of the mGlu2/3 antagonist LY341495 on dyskinesia and psychosis-like behaviours in the MPTP-lesioned marmoset
BackgroundWe have previously demonstrated that the metabotropic glutamate 2 and 3 (mGlu 2/3 ) antagonist LY341495 reverses the anti-dyskinetic and...
-
The role of GPR39 zinc receptor in the modulation of glutamatergic and GABAergic transmission
BackgroundDespite our poor understanding of the pathophysiology of depression, a growing body of evidence indicates the role of both glutamate and...
-
Interaction of hallucinogenic rapid-acting antidepressants with mGlu2/3 receptor ligands as a window for more effective therapies
The desire to find a gold-standard therapy for depression is still ongoing. Develo** one universal and effective pharmacotherapy remains...
-
Evaluation of the 5-HT2C receptor drugs RO 60-0175, WAY 161503 and mirtazepine in a preclinical model of comorbidity of depression and cocaine addiction
BackgroundEpidemiological data indicate a high rate of comorbidity of depression and cocaine use disorder (CUD). The role of serotonin 2C (5-HT 2C )...
-
Partial mGlu5 receptor NAM, M-5MPEP, induces rapid and sustained antidepressant-like effects in the BDNF-dependent mechanism and enhances (R)-ketamine action in mice
BackgroundPartial negative allosteric modulators (NAM) of the metabotropic glutamate 5 (mGlu 5 ) receptor are an excellent alternative to full...
-
Escitalopram alters local expression of noncanonical stress-related neuropeptides in the rat brain via NPS receptor signaling
BackgroundNeuropeptide S (NPS) is a multifunctional regulatory factor that exhibits a potent anxiolytic activity in animal models. However, there are...
-
Search for Selective Glua1 Ampa Receptor Antagonists in a Series of Dicationic Compounds
Homologous series of dicationic derivatives based on adamantyl and phenylcyclohexyl fragments in which the cationic groups and the distance between...
-
Reduction of the serotonin 5-HT1B and 5-HT2A receptor-mediated contraction of human pulmonary artery by the combined 5-HT1B receptor antagonist and serotonin transporter inhibitor LY393558
BackgroundLY393558 is a combined antagonist of serotonin (5-HT) 5-HT 1B receptors and inhibitor of serotonin transporter (SERT). LY393558 reduces...
-
Phytoestrogenic Potential of Resveratrol by Selective Activation of Estrogen Receptor-α in Osteoblast Cells
Resveratrol obtained in grape seed and skin is structurally similar to a synthetic estrogen diethylstilbestrol. The endogenous estrogen,...
-
Metabolic and cardiovascular benefits and risks of 4-hydroxy guanabenz hydrochloride: α2-adrenoceptor and trace amine-associated receptor 1 ligand
Backgroundα 2 -adrenoceptor ligands have been investigated as potential therapeutic agents for the treatment of obesity. Our previous studies have...
