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The Pharmacology of TD-8954, a Potent and Selective 5-HT4 Receptor Agonist with Gastrointestinal Prokinetic Properties
TLDR
It is concluded that TD-8954 is a potent and selective 5-HT4 receptor agonist in vitro, with robust in vivo stimulatory activity in the gastrointestinal (GI) tract of guinea pigs, rats, dogs, and humans and may have clinical utility in patients with disorders of reduced GI motility. Expand
Distinct Dynamin-dependent and -independent Mechanisms Target Structurally Homologous Dopamine Receptors to Different Endocytic Membranes
TLDR
The results refute the previous hypothesis that dynamin-independent endocytosis targets G protein–coupled receptors selectively to lysosomes, and they suggest a new role of endocytic sorting mechanisms in physically segregating structurally homologous signaling receptors at the cell surface. Expand
Dexmedetomidine Diminishes Halothane Anesthetic Requirements in Rats Through a Postsynaptic Alpha2 Adrenergic Receptor
TLDR
Central postsynaptic alpha2 adrenergic receptors mediate a significant part of the reduction of anesthetic requirements caused by dexmedetomidine, with no apparent involvement of either opiate or A1 adenosine receptors. Expand
Anesthetic and Hemodynamic Effects of the Stereoisomers of Medetomidine, an α2‐Adrenergic Agonist, in Halothane‐Anesthetized Dogs
TLDR
Medetomidine, the highly selective α2-adrenergic agonist, reduces the MAC for volatile anesthesia by a greater degree than with any other physiologic, pharmacologic, or pathologic intervention thus far reported. Expand
SH3 binding domains in the dopamine D4 receptor.
TLDR
The data indicates that the D4 receptor contains SH3 binding sites and that these sites fall within a region involved in the control of receptor internalization, which may account for the deficiency in functional activation of second messengers. Expand
The 5‐HT4 receptor agonist, tegaserod, is a potent 5‐HT2B receptor antagonist in vitro and in vivo
TLDR
The data from this study indicate that tegaserod antagonizes 5‐ HT2B receptors at concentrations similar to those that activate 5‐HT4 receptors. Expand
The in vitro pharmacological profile of TD-5108, a selective 5-HT4 receptor agonist with high intrinsic activity
TLDR
The high intrinsic activity and preferential binding of TD-5108 to 5- HT4 over other 5-HT receptors may result in an improved clinical profile for the treatment of gastrointestinal disorders of reduced motility. Expand
The in vitro pharmacology of the peripherally restricted opioid receptor antagonists, alvimopan, ADL 08-0011 and methylnaltrexone
TLDR
It is concluded that alvimopan, ADL 08-0011, and methylnaltrexone differ in their in vitro pharmacological properties, particularly with respect to opioid receptor subtype selectivity and intrinsic activity. Expand
Molecular identification of SqKv1A. A candidate for the delayed rectifier K channel in squid giant axon
TLDR
SqKv1A is a good candidate for the "20 pS" K channel that accounts for the majority of rapidly activating K conductance in both GFL neuron cell bodies and the giant axon. Expand
TD-1211 Demonstrates Constipation-relieving Effects, Including Decrease in Rescue Laxative Use, in Patients with Opioid-Induced Constipation: 2011 ACG Presidential Poster: 1341
TLDR
TD1211 is a peripherally selective μ-opioid receptor antagonist which has the potential to be effective in the treatment of OIC without interfering with centrally mediated opioid effects and demonstrates a high degree of peripheral selectivity, a safety profile which supports further clinical studies, and favorable pharmacokinetics. Expand
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