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Preclinical pharmacological profile of the selective 5-HT1F receptor agonist lasmiditan
Lasmiditan presents a unique pyridinoyl-piperidine scaffold not found in any other antimigraine class, whose chemical structure and pharmacological profile clearly distinguish it from the triptans. Expand
Pharmacological Characterization of the Competitive GLUK5 Receptor Antagonist Decahydroisoquinoline LY466195 in Vitro and in Vivo
In vitro and in vivo pharmacology of the competitive GLUK5-selective kainate receptor antagonist LY466195 was examined, significantly reducing the number of Fos-positive cells in the rat nucleus caudalis after electrical stimulation of the trigeminal ganglion and showing no contractile activity in the rabbit saphenous vein in vitro. Expand
M2 and M4 Receptor Knockout Mice: Muscarinic Receptor Function in Cardiac and Smooth Muscle In Vitro
Results provide direct and unambiguous evidence that M2 receptors mediate muscarinic receptor-induced bradycardia and play a role in smooth muscle contractility, whereas M4 receptors are not involved in stomach fundus, urinary bladder, or tracheal contractility. Expand
Effect of bombesin, bradykinin, substance P and CGRP in prostate, bladder body and neck
Lower urinary tract tissues are responsive to certain bioactive peptides in a nonhomogeneous fashion and raise the possibility that selective modulation of peptide function may be an approach to therapy of urogenital disorders. Expand
Analysis of the beta1 and beta2 adrenoceptor interactions of the partial agonist, clenbuterol (NAB365), in the rat jugular vein and atria
The high agonist potency of clenbuterol results primarily from the high affinity toward beta adrenoceptors rather than efficient activation of the adrenoceptor as occurs with isoproterenol or salbutamol. Expand
Muscarinic receptor knockout mice: role of muscarinic acetylcholine receptors M(2), M(3), and M(4) in carbamylcholine-induced gallbladder contractility.
Muscarinic receptor knockout mice provided direct and unambiguous evidence that M(3), and to a lesser extent, M(2) receptors are the predominant muscarinic receptors mediating gallbladder contractility, and M(4) receptors appear necessary for optimal potency of carbamylcholine in gallbladders contraction. Expand
Vascular serotonin receptors and blood pressure regulation
In most vascular beds, receptors mediating contraction to serotonin are of the 5HT2 type (defined by [3H]‐spiperone binding in brain tissue). Research on vascular serotonin receptors has beenExpand
5-HT2B receptor signaling in the rat stomach fundus: dependence on calcium influx, calcium release and protein kinase C
Data indicate that the 5-HT2B contractile receptor in the rat stomach fundus is coupled to calcium influx through voltage-dependent calcium channels, intracellular calcium release, and activation of PKC, a novel coupling mechanism unrelated to increases in PI hydrolysis. Expand
M1 Receptor-Mediated Nitric Oxide-Dependent Relaxation Unmasked in Stomach Fundus from M3 Receptor Knockout Mice
Data support the presence of M1 receptor-mediated relaxation in the stomach and suggest that when the M3 receptor is eliminated or blocked, M1 receptors-mediated gastric relaxation may be enhanced, possibly leading to alterations in gastric emptying and subsequent effects on body weight. Expand
Reversal of heparin-induced increases in aPTT in the rat by PM102, a novel heparin antagonist.
PM102, a novel peptide-based heparin antagonist, was evaluated and compared to protamine in a rat model and its utility as a bolus injection as well as infusion, its rapid efficacy and its rapid clearance make this an ideal candidate for clinical development. Expand