Regulation of calcitonin release from the 6.23 rat C-cell line by cyclic nucleotide analogues and pharmacological mediators

1991 ◽  
Vol 47 (10) ◽  
pp. 1067-1069 ◽  
Author(s):  
J. -L. Gilgenkrantz ◽  
T. J. Hall ◽  
T. J. Chambers
Keyword(s):  
Cell Line ◽  
Cyclic Nucleotide ◽  
Nucleotide Analogues ◽  
C Cell

Cyclopentenyl cytosine and neuroblastoma SK-N-BE(2)-C cell line cells

1995 ◽  
Vol 31 (4) ◽  
pp. 627-631 ◽  
Author(s):  
R.J. Slingerland ◽  
A.H. Van Gennip ◽  
J.M. Bodlaender ◽  
P.A. Voǔte ◽  
A.B.P. Van Kuilenburg
Keyword(s):  
Cell Line ◽  
C Cell ◽  
Cyclopentenyl Cytosine

scholarly journals Trifluoperazine inhibits phagocytosis in a macrophagelike cultured cell line.

1981 ◽  
Vol 91 (3) ◽  
pp. 798-802 ◽  
Author(s):  
S B Horwitz ◽  
G H Chia ◽  
C Harracksingh ◽  
S Orlow ◽  
S Pifko-Hirst ◽  
...  
Keyword(s):  
Cell Growth ◽  
Cell Line ◽  
Cyclic Nucleotide ◽  
Cellular Function ◽  
Inhibitory Effects ◽  
Cultured Cell ◽  
Sulfonamide Derivative ◽  
Cultured Cell Line ◽  
Macrophagelike Cell

Trifluoperazine, a drug that binds to Ca2+-calmodulin and inhibits its interaction with other proteins, was found to inhibit growth and phagocytosis in a macrophagelike cell line, J774.16. Both effects were reversible and occurred at the same concentrations of drug (25--50 microM) that inhibited the activation of cyclic nucleotide phosphodiesterase by calmodulin in vitro. Fc-mediated phagocytosis was also depressed by W-7, a sulfonamide derivative that inhibits the activity of Ca2+-calmodulin. In contrast, taxol, a drug that stabilizes cellular microtubules, had no effect on Fc-mediated phagocytosis although it inhibited cell growth at nanomolar concentrations. The inhibitory effects of trifluoperazine and W-7 on phagocytosis suggest that calmodulin may be involved in this complex cellular function.

Effects of forskolin and cyclic nucleotides on isometric force in rat aorta

1986 ◽  
Vol 250 (3) ◽  
pp. C468-C473 ◽  
Author(s):  
E. G. McMahon ◽  
R. J. Paul
Keyword(s):  
Cyclic Nucleotides ◽  
Cyclic Nucleotide ◽  
Isometric Force ◽  
Rat Aorta ◽  
Isometric Tension ◽  
Tension Development ◽  
Nucleotide Analogues ◽  
Cyclic Monophosphate ◽  
Contractile System ◽  
Rat Thoracic Aorta

The present study was undertaken to determine the extent to which cyclic nucleotide-induced relaxation in the intact rat aorta is mediated at the level of the contractile system. The relaxant effects of the cyclic nucleotide analogues [8-bromoguanosine 3',5'-cyclic monophosphate (8-BrcGMP) and dibutyryladenosine 3',5'-cyclic monophosphate (DBcAMP)] and forskolin were examined in both the intact vessel and a Triton X-100-skinned preparation of rat thoracic aorta. Relaxation of a norepinephrine-induced contraction was essentially complete 30 min after the addition of 50 microM 8-BrcGMP [% relaxation = 87.2 +/- 4.4% (n = 4)], 100 microM DBcAMP [98.2 +/- 1.2% (n = 4)], and 1 microM forskolin [107.0 +/- 3.3% (n = 5)]. These same doses were ineffective in relaxing precontracted skinned rat aortic rings compared with the relaxation achieved in the intact vessel. The largest relaxation in the skinned aortas was achieved with the addition of 1 microM forskolin [17.4 +/- 1.5% (n = 4)]. The addition of catalytic subunit of cAMP-dependent protein kinase had no effect on isometric tension in the precontracted skinned aorta. Preincubation with the cyclic nucleotide analogues or forskolin in a low-Ca2+ solution (pCa less than 8) was also ineffective in inhibiting subsequent isometric tension development. Our results suggest that only a very small fraction of the relaxation with cyclic nucleotides and forskolin in the intact rat aorta is due to the action of these agents at the level of the contractile system.

scholarly journals Dexamethasone Stimulates Thyrotropin-Releasing Hormone Production in a C Cell Line

1989 ◽  
Vol 3 (4) ◽  
pp. 605-610 ◽  
Author(s):  
Marie A. Tavianini ◽  
Peter J. Gkonos ◽  
Thomas H. Lampe ◽  
Bernard A. Roos
Keyword(s):  
Cell Line ◽  
Thyrotropin Releasing Hormone ◽  
Hormone Production ◽  
Releasing Hormone ◽  
C Cell

scholarly journals Cyclic GMP–gated Channels in a Sympathetic Neuron Cell Line

1997 ◽  
Vol 110 (2) ◽  
pp. 155-164 ◽  
Author(s):  
Stuart H. Thompson
Keyword(s):  
Cell Line ◽  
Cyclic Nucleotide ◽  
Single Channel ◽  
Neuroblastoma Cell ◽  
Sympathetic Neuron ◽  
Sympathetic Ganglia ◽  
Guanosine Monophosphate ◽  
Hill Coefficient ◽  
Muscarinic Agonists ◽  
Single Channel Currents

The stimulation of IP3 production by muscarinic agonists causes both intracellular Ca2+ release and activation of a voltage-independent cation current in differentiated N1E-115 cells, a neuroblastoma cell line derived from mouse sympathetic ganglia. Earlier work showed that the membrane current requires an increase in 3′,5′-cyclic guanosine monophosphate (cGMP) produced through the NO-synthase/guanylyl cyclase cascade and suggested that the cells may express cyclic nucleotide–gated ion channels. This was tested using patch clamp methods. The membrane permeable cGMP analogue, 8-br-cGMP, activates Na+ permeable channels in cell attached patches. Single channel currents were recorded in excised patches bathed in symmetrical Na+ solutions. cGMP-dependent single channel activity consists of prolonged bursts of rapid openings and closings that continue without desensitization. The rate of occurrence of bursts as well as the burst length increase with cGMP concentration. The unitary conductance in symmetrical 160 mM Na+ is 47 pS and is independent of voltage in the range −50 to +50 mV. There is no apparent effect of voltage on opening probability. The dose response curve relating cGMP concentration to channel opening probability is fit by the Hill equation assuming an apparent KD of 10 μm and a Hill coefficient of 2. In contrast, cAMP failed to activate the channel at concentrations as high as 100 μm. Cyclic nucleotide gated (CNG) channels in N1E-115 cells share a number of properties with CNG channels in sensory receptors. Their presence in neuronal cells provides a mechanism by which activation of the NO/cGMP pathway by G-protein–coupled neurotransmitter receptors can directly modify Ca2+ influx and electrical excitability. In N1E-115 cells, Ca2+ entry by this pathway is necessary to refill the IP3-sensitive intracellular Ca2+ pool during repeated stimulation and CNG channels may play a similar role in other neurons.

scholarly journals Cyclic Nucleotide (cNMP) Analogues: Past, Present and Future

2021 ◽  
Vol 22 (23) ◽  
pp. 12879
Author(s):  
Erik Maronde
Keyword(s):  
Cyclic Nucleotide ◽  
Second Messengers ◽  
Nucleotide Analogues ◽  
Drug Candidates ◽  
Physiological Signal ◽  
Cellular Events ◽  
Current State ◽  
Dependent Protein ◽  
Target Molecules ◽  
Basic And Applied Research

Cyclic nucleotides are important second messengers involved in cellular events, and analogues of this type of molecules are promising drug candidates. Some cyclic nucleotide analogues have become standard tools for the investigation of biochemical and physiological signal transduction pathways, such as the Rp-diastereomers of adenosine and guanosine 3′,5′-cyclic monophosphorothioate, which are competitive inhibitors of cAMP- and cGMP-dependent protein kinases. Next generation analogues exhibit a higher membrane permeability, increased resistance against degradation, and improved target specificity, or are caged or photoactivatable for fast and/or targeted cellular imaging. Novel specific nucleotide analogues activating or inhibiting cyclic nucleotide-dependent ion channels, EPAC/GEF proteins, and bacterial target molecules have been developed, opening new avenues for basic and applied research. This review provides an overview of the current state of the field, what can be expected in the future and some practical considerations for the use of cyclic nucleotide analogues in biological systems.

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