Search Results - "Thán, Márta"
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1
Discovery and Characterization of RGH-122, a Potent, Selective, and Orally Bioavailable V1a Receptor Antagonist
Published in Journal of medicinal chemistry (11-01-2024)“…The V1a receptor is a major contributor in mediating the social and emotional effects of arginine-vasopressin (AVP); therefore it represents a promising target…”
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2
Optimization of Novel α7 Nicotinic Acetylcholine Receptor Positive Allosteric Modulators and the Discovery of a Preclinical Development Candidate Molecule (RGH-560)
Published in Journal of medicinal chemistry (14-12-2023)“…During optimization of a previously identified lead compound, attempts were made to optimize the reactive indole structural element, the suboptimal metabolic…”
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3
Multiparameter Optimization of Naphthyridine Derivatives as Selective α5-GABAA Receptor Negative Allosteric Modulators
Published in Journal of medicinal chemistry (09-06-2022)“…The discovery and characterization of novel naphthyridine derivatives with selective α5-GABAAR negative allosteric modulator (NAM) activity are disclosed…”
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4
RGH-397 INHIBITS THE FUNCTION OF ALPHA5 GABAA RECEPTORS WITH SLOW OFF-KINETICS AND SHOWS EFFICACY IN ANIMAL MODELS OF COGNITIVE IMPAIRMENT
Published in IBRO neuroscience reports (01-10-2023)Get full text
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5
Tolperisone-type drugs inhibit spinal reflexes via blockade of voltage-gated sodium and calcium channels
Published in The Journal of pharmacology and experimental therapeutics (01-12-2005)“…The spinal reflex depressant mechanism of tolperisone and some of its structural analogs with central muscle relaxant action was investigated. Tolperisone…”
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6
Inhibitory effect of anandamide on resiniferatoxin-induced sensory neuropeptide release in vivo and neuropathic hyperalgesia in the rat
Published in Life sciences (1973) (19-09-2003)“…Anandamide (AEA) is an endogenous cannabinoid ligand acting predominantly on the cannabinoid 1 (CB 1) receptor, but it is also an agonist on the capsaicin VR…”
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7
Anti‐inflammatory effect of synthetic somatostatin analogues in the rat
Published in British journal of pharmacology (01-12-2001)“…Somatostatin (6.11 nmol kg−1 i.p.) inhibited neurogenic plasma extravasation evoked by 1% mustard oil and non‐neurogenic oedema induced by 5% dextran in the…”
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8
Concerted action of antiepileptic and antidepressant agents to depress spinal neurotransmission: Possible use in the therapy of spasticity and chronic pain
Published in Neurochemistry international (01-03-2007)“…Chronic pain states and epilepsies are common therapeutic targets of voltage-gated sodium channel blockers. Inhibition of sodium channels results in central…”
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9
Concentration-dependent dual effect of anandamide on sensory neuropeptide release from isolated rat tracheae
Published in Neuroscience letters (16-01-2003)“…Most actions of anandamide (AEA) are mediated by the cannabinoid 1 (CB 1) receptor activation, but on sensory neurones it is also an agonist on the vanilloid…”
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10
Interaction between interleukin 1β and endogenous neurokinin 1 receptor agonists in mediating plasma extravasation and neutrophil accumulation in the cutaneous microvasculature of the rat
Published in Neuroscience letters (18-01-2002)“…Interleukin 1β (IL-1β) is a potent mediator of neutrophil accumulation. Antidromic stimulation of the rat saphenous nerve leads to neurogenic oedema formation…”
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11
Multiparameter Optimization of Naphthyridine Derivatives as Selective α5-GABA A Receptor Negative Allosteric Modulators
Published in Journal of medicinal chemistry (09-06-2022)“…The discovery and characterization of novel naphthyridine derivatives with selective α5-GABA R negative allosteric modulator (NAM) activity are disclosed…”
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12
HTS-based discovery and optimization of novel positive allosteric modulators of the α7 nicotinic acetylcholine receptor
Published in European journal of medicinal chemistry (15-10-2021)“…HTS campaign of the corporate compound collection resulted in a novel, oxalic acid diamide scaffold of α7 nACh receptor positive allosteric modulators. During…”
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13
Discovery of novel positive allosteric modulators of the α7 nicotinic acetylcholine receptor: Scaffold hopping approach
Published in European journal of medicinal chemistry (15-03-2021)“…The paper focuses on the scaffold hopping-based discovery and characterization of novel nicotinic alpha 7 receptor positive modulator (α7 nAChR PAM) ligands…”
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14
Pharmacological characterisation of the somatostatin analogue TT-232: effects on neurogenic and non-neurogenic inflammation and neuropathic hyperalgesia
Published in Naunyn-Schmiedeberg's archives of pharmacology (01-08-2002)“…The putative anti-inflammatory and anti-nociceptive activity of the heptapeptide somatostatin analogue TT-232 ( D-Phe-Cys-Tyr- D-Thr-Lys-Cys-Thr-NH(2)) was…”
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15
Systemic anti-inflammatory effect of somatostatin released from capsaicin-sensitive vagal and sciatic sensory fibres of the rat and guinea-pig
Published in European journal of pharmacology (07-07-2000)“…The systemic anti-inflammatory effect induced by antidromic sensory nerve stimulation was investigated in rats and guinea-pigs. In atropine-pretreated rats,…”
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16
Anti-nociceptive effect induced by somatostatin released from sensory nerve terminals and by synthetic somatostatin analogues in the rat
Published in Neuroscience letters (14-01-2000)“…In rats anaesthetized with urethan and pretreated with pipecuronium bromide nocifensive reaction of blood pressure elevation evoked by intraarterial capsaicin…”
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17
Interaction between interleukin 1beta and endogenous neurokinin 1 receptor agonists in mediating plasma extravasation and neutrophil accumulation in the cutaneous microvasculature of the rat
Published in Neuroscience letters (18-01-2002)“…Interleukin 1beta (IL-1beta) is a potent mediator of neutrophil accumulation. Antidromic stimulation of the rat saphenous nerve leads to neurogenic oedema…”
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18
Analysis of the effects of cannabinoids on synaptic transmission between basket and Purkinje cells in the cerebellar cortex of the rat
Published in The Journal of pharmacology and experimental therapeutics (01-09-2004)“…The hypothesis of the present work was that activation of CB1 cannabinoid receptors inhibits GABAergic neurotransmission between basket and Purkinje cells in…”
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19
Inhibition of nociceptin on sensory neuropeptide release and mast cell-mediated plasma extravasation in rats
Published in European journal of pharmacology (17-04-1998)“…Nociceptin (20 μg/kg i.p.) strongly inhibited cutaneous Evans blue accumulation in the chronically denervated hindpaw of the rat in response to mast cell…”
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20
Impairment of neurogenic inflammatory and anti-inflammatory responses in diabetic rats
Published in European journal of pharmacology (10-12-1999)“…The effect was studied of a primary (preconditioning) neurogenic inflammatory challenge induced by electrical stimulation of the peripheral stump of the…”
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