MDL 72222: a potent and highly selective antagonist at neuronal 5-hydroxytryptamine receptors

1984 ◽  
Vol 326 (1) ◽  
pp. 36-44 ◽  
Author(s):  
J. R. Fozard
Keyword(s):  
Mdl 72222 ◽  
Selective Antagonist ◽  
Hydroxytryptamine Receptors

Blockade of Neuronal 5-Hydroxytryptamine Receptors with MDL 72222

Migraine ◽  
2015 ◽  
pp. 264-272
Author(s):  
J. R. Fozard ◽  
C. Loisy ◽  
G. Tell
Keyword(s):  
Mdl 72222 ◽  
Hydroxytryptamine Receptors

Cholecystokinin-induced satiety depends on activation of 5-HT1C receptors

1993 ◽  
Vol 264 (1) ◽  
pp. R62-R64 ◽  
Author(s):  
B. Poeschla ◽  
J. Gibbs ◽  
K. J. Simansky ◽  
D. Greenberg ◽  
G. P. Smith
Keyword(s):  
Food Intake ◽  
Systemic Administration ◽  
Receptor Subtypes ◽  
Cholecystokinin Octapeptide ◽  
Mdl 72222 ◽  
Selective Antagonist ◽  
Serotonergic Function ◽  
Ics 205 930

To investigate the dependence of the satiating action of cholecystokinin on serotonergic function in rats, we examined the effects of systemic pretreatment with serotonin (5-HT) antagonists of varying selectivity for 5-HT receptor subtypes on suppression of food intake induced by systemic administration of cholecystokinin octapeptide (CCK-8). Mianserin, a 5-HT1C/2-selective antagonist, significantly attenuated the satiating action of CCK-8. Ketanserin, a 5-HT2 antagonist, and three 5-HT3 antagonists, MDL-72222, ICS 205-930, and ondansetron, however, had no effect on the satiating action of CCK-8. These results demonstrate that the satiating action of exogenous CCK depends on activation of 5-HT1 (probably 5-HT1C) receptors and that activation of 5-HT2 or 5-HT3 receptors is not required.

Targeted Blockade of TARP-γ8-Associated AMPA Receptors: Anticonvulsant Activity with the Selective Antagonist LY3130481 (CERC-611)

2018 ◽  
Vol 16 (10) ◽  
pp. 1099-1110 ◽  
Author(s):  
Jeffrey M. Witkin ◽  
Douglas A. Schober ◽  
Scott D. Gleason ◽  
John T. Catlow ◽  
Warren J. Porter ◽  
...  
Keyword(s):  
Ampa Receptors ◽  
Anticonvulsant Activity ◽  
Selective Antagonist

Characterization of opioid receptors on smooth muscle cells from guinea pig stomach

1992 ◽  
Vol 262 (3) ◽  
pp. G461-G469 ◽  
Author(s):  
L. Zhang ◽  
Z. F. Gu ◽  
T. Pradhan ◽  
R. T. Jensen ◽  
P. N. Maton
Keyword(s):  
Smooth Muscle ◽  
Smooth Muscle Cells ◽  
Opioid Receptors ◽  
Muscle Cells ◽  
Receptor Subtypes ◽  
Selective Antagonist ◽  
Kappa Agonist ◽  
Gastric Smooth Muscle ◽  
Selective Ligand ◽  
Guinea Pig Stomach

On the basis of opioid-stimulated contraction of dispersed gastric smooth muscle cells it has been suggested that these cells possess opioid receptors of three subtypes: kappa (kappa), mu (mu), and delta (delta). We have used selective peptidase-resistant radioligands, agonists and antagonists, to examine receptor subtypes on dispersed gastric smooth muscle cells from guinea pigs prepared by collagenase digestion. The kappa-agonist U-50488H, the mu-agonist [D-Ala2,N-Me-Phe4,Gly5-ol]enkephalin (DAGO), and the delta-agonist [D-Pen2,Pen5]enkephalin (DPDPE) each caused muscle contraction. The concentrations required to caused half-maximal contraction were U50488H (6 pM) greater than DAGO (13 pM) greater than DPDPE (6 nM). The abilities of these agonists to inhibit binding of [3H]U-69593 (kappa-preferring) by 50% were U50488H (43 nM) greater than DAGO (43 microM) greater than DPDPE (200 microM). Their abilities to inhibit binding of [3H]naloxone (mu-preferring) by 50% were DAGO (0.2 microM) greater than U50488H (10 microM) greater than DPDPE (greater than 100 microM). No binding could be detected with the delta-selective ligand [3H]DPDPE. The kappa-preferring antagonist Mr2266 (10 nM) preferentially inhibited contraction stimulated by the kappa-agonist U50488H, and naltrexone (10 nM) (mu-selective antagonist) preferentially inhibited contraction stimulated by the mu-agonist DAGO. ICI 174864 (200 microM; delta-selective antagonist) had no effect on contraction stimulated by mu-, kappa-, or delta-agonists. Contraction stimulated by the delta-agonist DPDPE was inhibited by both kappa- and mu-receptor antagonists. Studies on the effect of the antagonists on binding of [3H]naloxone and [3H]U69593 also provided evidence for kappa- and mu-sites but nor for delta-sites.(ABSTRACT TRUNCATED AT 250 WORDS)

Combined coagulation phase-directed factor Xa inhibition with heparin compounds and DX-9065a - A direct and selective antagonist

2004 ◽  
Vol 92 (12) ◽  
pp. 1229-1231
Author(s):  
John Alexander ◽  
You Li ◽  
Edwin Bovill ◽  
Frederick Spencer ◽  
Thomas Robertson ◽  
...  
Keyword(s):  
Factor Xa ◽  
Selective Antagonist ◽  
Factor Xa Inhibition ◽  
Heparin Compounds
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