Cochinmicins I, II, III are novel peptolides produced in submerged-fermentation cultures of Microbispora sp. ATCC 55140. These closely related compounds are separated by HPLC and are novel competitive endothelin antagonists. Cochinmicins II and III are stereoisomeric to each other. Cochinmicin I is the deschloro analog of cochinmicin III.

Existential, neurobiological and cognitive models of addictive behavior are considered as a theoretical basis for transformational therapy disorders. The NMDA receptor antagonist ketamine, which has neurotrophic, modulatory psychedelic effects, demonstrates the universal properties transforming agent any presented concepts behavior. Since persistent mental behavioral changes essentially psychob...

Glomerular diseases are the leading cause of ESKD worldwide. IgA nephropathy (IgAN), focal segmental glomerulosclerosis (FSGS), Alport syndrome (AS), and diabetic kidney disease (DKD) important glomerular characterized by proteinuria, a predictor progression ESKD. Endothelin A (ETA) receptor activation drives inflammation, fibrosis. Therefore, atrasentan, potent selective ETA antagonist, has po...

The activity of dopamine (DA)-containing neurons in the ventral tegmental area (VTA) is a key mechanism in mesolimbic reward processing that has modulatory effects on different diencephalic structures like hippocampus (HIP), and receives inhibitory feedback and excitatory feed forward control. In addition, within the hippocampus, DA receptors are mostly located in the dorsal part (CA1) and dopa...

The activity of dopamine (DA)-containing neurons in the ventral tegmental area (VTA) is a key mechanism in mesolimbic reward processing that has modulatory effects on different diencephalic structures like hippocampus (HIP), and receives inhibitory feedback and excitatory feed forward control. In addition, within the hippocampus, DA receptors are mostly located in the dorsal part (CA1) and dopa...

The effect of antagonist pretreatment on the signaling properties of the human metabotropic glutamate 1a (hmGlu1a) receptor was examined in stably transfected L929sA cells. Pre-exposure of hmGlu1a receptor-expressing cells to the mGlu1 receptor antagonists (S)-4-carboxy-3-hydroxyphenylglycine and 7-(hydroxyimino)cyclo-propa[b]chromen-1a-carboxylate ethyl ester dramatically enhanced subsequent g...

The effect of some serotonin receptor antagonists was investigated on the body temperature of male mice. These antagonists produced significant reductions of body temperature in methamphetamine-induced hyperthermic male mice. Thus, the hyperthermia induced by methamphetaminc (11 ~tmol/kg,i.p.) was antagonized by the previous i.p. administration of 1.06 gmol/kg NAN-190 (5-HTIA receptor antagonis...

l-Glutamate (Glu) activates at least eight different G protein-coupled receptors known as metabotropic glutamate (mGlu) receptors, which mostly act regulators of synaptic transmission. These consist two domains: an extracellular domain in agonists bind and a transmembrane heptahelix region involved protein activation. Although new mGlu receptor antagonists have been described, few are selective...