The lipocortins are a family of calcium-dependent phospholipid-binding proteins that are induced by glucocorticoids and inhibit phospholipase-A2 activity. To determine whether the lipocortins affect ...the release of PRL from human decidua, decidual cells from term pregnancies were exposed to recombinant lipocortin-I for 96 h, with medium changes at 24-h intervals. Lipocortin-I (0.01-100 nM) caused a time- and dose-dependent inhibition of PRL release, with a half-maximal effective dose of 50 nM. PRL release was inhibited by 27%, 62%, 93%, and 98% at 24, 48, 72, and 96 h, respectively. The cells exposed to lipocortin-I did not release the enzymes alkaline phosphatase and lactic dehydrogenase, indicating that the inhibitory effect on PRL release was not due to cell death. In addition to inhibiting basal PRL release, lipocortin also completely inhibited the stimulation of PRL release by decidual PRL-releasing factor, a 23.5-kDa protein recently purified from human placenta that stimulates the synthesis and release of decidual, but not pituitary, PRL. Hydrocortisone and dexamethasone (0.1-10 microM) had no effect on PRL release, and arachidonic acid (2-100 microM) inhibited rather than stimulated PRL release. Western blot analysis demonstrated the presence of lipocortin-I in decidual cells and conditioned media. On Northern blot, decidual mRNA hybridized to an oligonucleotide for lipocortin-I. These results strongly suggest that lipocortin-I has an autocrine/paracrine role in regulation of the synthesis and release of PRL from human decidual cells.
Festschrift Honouring René Gallet Ahrens, Rüdiger; Birkan-Berz, Carole; Boucher-Rivalain, Odile ...
LISA (Caen, France),
03/2009
Journal Article
Peer reviewed
Open access
I consider myself extremely lucky to have worked with René Gallet whom I met for the first time in May 2001 when I was appointed to the English Studies Department at Caen University. Our research ...specialities are different and I was not aware of René’s remarkable career before my arrival in Caen. I was soon to discover someone particularly special – special because of his immense knowledge and erudition, special because of his illuminating presence amongst his students and colleagues and special because of his modesty, generosity and rare kindness. René Gallet is exceptional, not only because of his most inspiring courses but also because of his human qualities...
Canada and the United States have conducted a large-scale social experiment on the effects of alternative ways of funding expenditures for health care. Two very similar societies, with (until ...recently) very similar systems of providing health care, have adopted radically different systems of reimbursement. The results of this experiment are of increasing interest to Americans, because the Canadian approach has avoided or solved several of the more intractable problems facing the United States. In particular, overall health expenditures have been constrained to a stable share of national income, and universality of coverage (without user charges) eliminates the problems of uncompensated care, individual burdens of catastrophic illness, and uninsured populations. The combination of cost control with universal, comprehensive coverage has surprised some American observers, who have questioned its reality, its sustainability, or both. We present a comparison of the Canadian and American data on expenditures, identifying the sectors in which the experience of the two nations diverges most, and describing the processes of control. In any system, cost control involves conflict between providers and payers. Political processes focus this conflict, whereas market processes diffuse it. But the stylized political combat in Canada may result in less intrusion on the professional autonomy of the individual physician than is occurring in the United States.
Human
β
3 adrenergic receptor agonists containing 5-membered ring ureas were shown to be potent partial agonists with excellent selectivity over
β
1 and
β
2 binding. L-760,087 (
4a) and L-764,646 (
...5a) (
β
3EC
50 = 18 and 14 nM, respectively) stimulate lipolysis in rhesus monkeys (ED
50 = 0.2 and 0.1 mg/kg, respectively) with minimal effects on heart rate. Oral absorption in dogs is improved over other urea analogs.
Human β AR agonists L-760,087 (
4a) and L-764,646 (
5a) (β EC
50 = 18 and 14nM) stimulate lipolysis in rhesus monkeys (ED
50 = 0.2
and 0.1 mg/kg) with minimal effects on heart rate. Oral absorption in dogs is improved over other urea analogs.
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IJS, IMTLJ, KILJ, KISLJ, NUK, SAZU, SBCE, SBJE, UL, UM, UPCLJ, UPUK
The 3-pyridylethanolamine L-757,793 is a potent β
3 AR agonist (EC
50 6.3 nM, 70% activation) with 1,300- and 500-fold selectivity over binding to the β
1 and β
2 ARs, respectively, L-757,793 ...stimulated lipolysis in rhesus monkeys (ED
50 0.2 mg/kg) with a maximum response equivalent to that elicited by isoproterenol.
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IJS, IMTLJ, KILJ, KISLJ, NUK, SAZU, SBCE, SBJE, UL, UM, UPCLJ, UPUK
5-
n-Pentyl oxadiazole substituted benzenesulfonamide
8 is a potent and selective β
3 adrenergic receptor agonist (β
3 EC
50=23 nM, β
1 IC
50=3000 nM, β
2 IC
50=3000 nM). The compound has high oral ...bioavailability in dogs (62%) and rats (36%) and is among the most orally bioavailable β
3 adrenergic receptor agonists reported to date.
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IJS, IMTLJ, KILJ, KISLJ, NUK, SAZU, SBCE, SBJE, UL, UM, UPCLJ, UPUK
The cyclopentylpropylimidazolidinone L-766,892 is a potent
β
3 AR agonist (EC
50 5.7 nM, 64% activation) with 420- and 130-fold selectivity over binding to the
β
1 and
β
2 ARs, respectively. In ...anesthetized rhesus monkeys, L-766,892 elicited dose-dependent hyperglycerolemia (ED
50 0.1 mg/kg) with minimal effects on heart rate.
Graphic
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IJS, IMTLJ, KILJ, KISLJ, NUK, SAZU, SBCE, SBJE, UL, UM, UPCLJ, UPUK
