Neuropeptide FF (NPFF) and gonadotropin-inhibitory hormone (GnIH) are thought to be paralogous, a recent study has revealed that both NPFF GnIH peptides can activate the receptor (GnIHR, also called NPFFR1) in European sea bass ( Dicentrarchus labrax ). However, whether bind (NPFFR2) is still yet unknown this species. Accordingly, we further investigated potential interactions between NPFFR2 (t...

In vitro models to investigate pigmentation disorders inadequately capture the complex neuroectodermal-mesodermal signaling interplay controlling human epidermal melanogenesis. Here, we aimed at assessing suitability of a standardized ex vivo skin organ culture as rapid detection-system qualitatively and quantitatively assess effects topically or systemically applied candidate modulators, under...

Chronic consumption of the nonsteroidal anti-inflammatory drug diclofenac may induce drug-induced liver injury (DILI). The mechanism diclofenac-induced is partially elucidated and involves mitochondrial damage. Elevated cAMP protects hepatocytes against bile acid–induced injury. However, it unknown whether DILI and, if so, which downstream targets are implicated in protective mechanism, includi...

The diterpene, forskolin [half-maximal effective concentration (EC50), 5-10 microM] activates adenylate cyclase [ATP pyrophosphate-lyase (cyclizing), EC 4.6.1.1] in rat cerebral cortical membranes in a rapid and reversible manner. Activation is not dependent on exogenous guanyl nucleotides and is not inhibited by guanosine 5'-O-(2-thiodiphosphate) when assayed with adenosine 5'-[beta, gamma-imi...

The effects of compounds that activate adenylate cyclase and of cAMP on calcium-dependent action potentials recorded from mouse dorsal root ganglion neurons were assessed. Application of compounds that stimulate the adenylate cyclase system (forskolin, cholera toxin, and prostaglandin E1) increased action potential duration with an associated decrease in afterhyperpolarization. An adenylate cyc...

The effect of forskolin on corticostriatal synaptic transmission was examined by recording excitatory postsynaptic currents (EPSCs) in rat brain slices using the whole-cell voltage-clamp technique. Forskolin produced a dose-dependent increase of corticostriatal EPSCs (1, 3, 10, and 30 microM) immediately after its treatment, and the increase at 10 and 30 microM was maintained even after its was...

Endothelium-derived relaxing factors contribute to smooth muscle relaxation. The aim of the present study was to investigate the contribution of nitric oxide (NO) produced in the endothelial cells to the vasodilatation stimulated with forskolin in rat aorta. Forskolin that directly activates adenylyl-cyclase, induced complete relaxation in phenylephrine-contracted aortas. Endothelium removal re...

The binding of the transport inhibitor, forskolin, to the galactose-HI symporter, GalP, of Escherichia coli was evaluated by equilibrium and time-resolved fluorescence measurements. A quench in protein fluorescence of 8-12% was observed upon the binding of forskolin. The overall dissociation constant (Kd) for forskolin determined by fluorescence titration ranged between 1.2 and 2.2 suM, which i...

Forskolin, a naturally occurring activator of adenylate cyclase, inhibits total and high-affinity cyclic AMP phosphodiesterase activity in soluble and particulate fractions of cultured LLC-PK1 renal epithelial cells. The naturally occurring forskolin analogue 1,9-dideoxyforskolin, which does not stimulate adenylate cyclase activity, is a more potent inhibitor of cyclic AMP phosphodiesterase act...