Blockade of the flare response to intradermal 5-hydroxytryptamine in man by MDL 72.222, a selective antagonist at neuronal 5-hydroxytryptamine receptors

1986 ◽  
Vol 30 (2) ◽  
pp. 209-212 ◽  
Author(s):  
J. M. Orwin ◽  
J. R. Fozard
Keyword(s):  
Selective Antagonist ◽  
Hydroxytryptamine Receptors ◽  
Flare Response

QUANTITATIVE RELATIONS IN THE AQUEOUS FLARE RESPONSE INDUCED BY α-MELANOCYTE STIMULATING HORMONE IN THE RABBIT EYES

1965 ◽  
Vol 49 (1) ◽  
pp. 166-176 ◽  
Author(s):  
K. Dyster-Aas ◽  
C. E. T. Krakau
Keyword(s):  
Subcutaneous Injection ◽  
Great Variability ◽  
Local Administration ◽  
Aqueous Flare ◽  
Melanocyte Stimulating Hormone ◽  
Flare Response ◽  
Stimulating Hormone

ABSTRACT The aqueous flare response (AFR) to MSH is induced in an increasing percentage of animals with increasing age. The great variability of the responses and the fact that local administration of MSH is not more efficient with lower doses than by subcutaneous injection indicate that the AFR is a complex result in which general factors play a part. The analysis of the variation of the responses has led to a procedure for testing the effect of different preparations.

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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