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In the isolated right atrium activation
2024-11-25
In the isolated right atrium, activation of muscarinic receptors and adenosine receptors may block the generation of action potentials in the sinoatrial node, inducing cardiac arrest (Fig. 1, Fig. 2, Fig. 3, Fig. 4, Fig. 5) (Camara et al., 2015, Campbell et al., 1989). Physiologically, this conditio
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A high throughput small molecule
2024-11-25
A high-throughput small molecule ACK1 biochemical inhibition screen was performed in-house and led to the identification of 1μM inhibitor furanopyrimidine (). Further binding studies found Gemfibrozil mg to be both ATP-competitive and reversible. Early structure-activity relationship (SAR) work w
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5 aminosalicylic acid Introduction Myasthenia gravis MG is a
2024-11-25
Introduction Myasthenia gravis (MG) is an autoimmune disorder characterized by muscle weakness, which is mainly due to autoantibodies reducing the number or function of postsynaptic 5 aminosalicylic acid receptors (AChRs) [1], [2]. Animal models have been developed to uncover the immunopathogenesi
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The hypothalamic pituitary adrenal HPA axis is a neuroendocr
2024-11-25
The hypothalamic-pituitary-adrenal (HPA) axis is a neuroendocrine system that is central to regulating responses to stress (Palazidou, 2012). In older persons, a high dysfunction of the HPA axis is observed (Otte et al., 2005) which may be enhanced by stimulatory effects of genes involved in the axi
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br Discussion One binding site MB Fig is located in
2024-11-25
Discussion One binding site, MB327-1 (Fig. 4) is located in the extracellular domain between the γ and α subunits. MB327 adopts an extended conformation in the MB327-1 site and is oriented parallel to the channel. The second putative binding site, MB327-2 (Fig. 4) is situated deep inside the chan
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Numerous studies have reported high glutamate levels in the
2024-11-23
Numerous studies have reported high glutamate levels in the brains of patients with depression, indicating that the glutamate system plays a crucial role in depression (Sanacora et al., 2004; Kendell et al., 2005; Hashimoto et al., 2007). Furthermore, several clinically effective antidepressant drug
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In order to improve the methodology
2024-11-23
In order to improve the methodology of the synthesis of steroidal derivatives, our goal was the investigation of aza-Michael addition of different N-nucleophiles to 16-dehydropregnenolone in the presence of [DBU][OAc] as catalyst and reaction medium. Michael addition of electron deficient steroidal
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Estradiol valerate br Clinical realities br Commentary on
2024-11-23
Clinical realities Commentary on uses of selective 17,20 lyase inhibitors If continued monitoring of these same parameters along with tracking of circulating ACTH in human trials confirms these new drugs are the long sought after 17,20 lyase inhibitors, then we may for the first time be able t
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Fig summarizes the oxidative metabolism
2024-11-23
Fig. 1 summarizes the oxidative metabolism of arachidonic YK-4-279 by lipoxygenases cyclooxygenases and cytochrome P450. Lipoxygenases in humans are expressed in a tissue-specific fashion: 5-LOX is mainly expressed in leukocytes, 12-LOX in platelets, and 15-LOX-1 in reticulocytes, eosinophils, and
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br Conclusion br Acknowledgements br Introduction Synapses a
2024-11-23
Conclusion Acknowledgements Introduction Synapses are the fundamental elements of neuronal networks that enable the processing, encoding, and retrieval of information in the brain, and pathological disruptions in synapse structure are broadly held to underlie the development of neurological
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As aforementioned this study aimed
2024-11-23
As aforementioned, this study aimed to design, synthesize and investigate aromatase inhibitory and anti-breast cancer activities of N,N′-disubstituted thiourea derivatives. Based on the attractive phenotypic molecule 1, the synthetic N,N′-disubstituted thioureas have been designed including monothio
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In hypothalamus as indicated in Fig column A and following
2024-11-23
In hypothalamus, as indicated in Fig. 2 (column A) and following the enzymatic cascade represented in Fig. 1, we could hypothesize a predominance of Ang 2–10 and Ang III formation in SHR compared to WKY. This is in agreement with previous results that reported significant higher rate of Ang 2–10 for
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In silico docking analysis performed in
2024-11-22
In silico docking analysis performed in the current study indicated that TCDD strongly binds to AhR-LBD. Moreover, the formation of the TCDD/AhR-LBD complex was confirmed experimentally with the use of EMSA. We found that 10nM TCDD after 2 hours of incubation not only bound to the AhR in the porcine
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Pleuromutilin The obtained results indicate that even when
2024-11-22
The obtained results indicate that even when the impairment of the same forms of memory are present, amnesia can develop in different ways. Impairment of memory reconsolidation in the conditioned food aversion model through both the serotonin receptor antagonist and the antagonist of NMDA glutamate
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A highly attenuated B pertussis
2024-11-22
A highly attenuated B. pertussis strain, named BPZE1, has recently been described [10]. It produces enzymatically inactive pertussis toxin (PT), no dermonecrotic toxin and only trace amounts of tracheal cytotoxin. Markedly reduced lung pathology was observed in mice intranasally (i.n.) infected with
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