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Herbal medicines have been used to
2024-04-17

Herbal medicines have been used to treat various types of diseases and disorders for thousands of years worldwide (Li and Brown, 2009). Natural products have been the remedy of cancer chemotherapy for the past several decades. Anisomeles indica (L.) Kuntze. (Labiatae), commonly known as 'yu-chen-tsa
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From an historical perspective ligands for GPCRs adrenaline
2024-04-17

From an historical perspective, ligands for GPCRs (adrenaline, serotonin, MRT68921 or morphine, to name a few) have been identified before their receptor counterparts, at a time when the concept of receptor itself was controversial [15]. Although many cognate receptors for endogenous ligands were r
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To clarify the molecular mechanism of maduramicin
2024-04-17

To clarify the molecular mechanism of maduramicin-induced apoptosis in chicken myocardial cells, the mRNA levels of bcl-2, bax, and cytochrome C, as well as the mRNA levels and activities of caspase-3/8/9 were determined. The mRNA expressions and activities of initiator casapase-9 and executioner ca
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br Results Four HT esters
2024-04-17

Results Four HT esters (butyrate, caprylate, laurate and stearate esters) were chosen as representative compounds of increasing lipophilicity (Fig. 1). We will refer to them as C4HT, C8HT, C12HT and C18HT, respectively. They have been synthesized, purified and characterized according to our previ
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In recent years the higher lipophilicity
2024-04-17

In recent years, the ‘higher lipophilicity’-thus-‘better performance’ tenet, derived from the polar paradox theory applied to micro-structured media, was challenged by novel and unexpected experimental results. In particular, the synthesis of many complete series of fatty TPMPA esters of natural an
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br Summary br Introduction With readily
2024-04-17

Summary Introduction With readily synthetic methods and excellent chemical/physical characteristics, coumarins have received extensive attention and show great practical values in many fields, such as medicine discovery, dye chemistry, materials chemistry and so on [[1], [2], [3]]. Actually,
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Negative regulation of AR expression by NF B was also
2024-04-17

Negative regulation of AR expression by NFκB was also correlated with the ‘age-dependent desensitisation’ of androgen action in the rat liver (Supakar et al., 1995). In this case the binding site was mapped upstream of the gene to sequences −555 to −565 bp, that binds heterodimers of p65 and p50, as
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br Acknowledgments and Disclosures br Alzheimer
2024-04-17

Acknowledgments and Disclosures Alzheimer's disease as a synaptic pathology Alzheimer's disease (AD) is a chronic neurodegenerative nmda receptor antagonist disorder and the most common cause of dementia in the elderly. Progressive depositions of amyloid plaques and neurofibrillary tangles to
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Based upon these findings the S lipoxygenase seems
2024-04-17

Based upon these findings, the 12S-lipoxygenase seems to increase membrane excitability by specifically inhibiting M-type K+ channels. The 12S-lipoxygenase is expressed in many parts of mammalian protease inhibitor cocktail including the cerebrum, cerebellum, hypothalamus, basal ganglia, hippocampu
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pentylenetetrazol mg In past Zebra fish Danio rerio has emer
2024-04-17

In past, Zebra fish (Danio rerio) has emerged as a suitable model for early vertebrate development, and a number of targeted mutations in the zebrafish genome led to phenotypic alterations that resemble human diseases [34]. A 12-LOX in Zebra fish has been cloned and knock down of this zf12-LOX enzym
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br Methods br Results br Discussion
2024-04-17

Methods Results Discussion Agitation in dementia has recently been defined as a syndrome characterized by inferred or observed evidence of emotional distress associated with at least one behavioral component, i.e. excessive motor activity, verbal or physical aggression (Cummings et al., 201
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Lorlatinib is an orally active brain penetrant cyclic aminop
2024-04-17

Lorlatinib is an orally active brain penetrant cyclic 2-aminopyridine derivative that is a type I½ B ALK inhibitor (Fig. 5F) [61]. This medicinal is an effective antagonist against the more common L1196M and G1269A crizotinib-resistant mutations as well as the less common T1151Ins, L1152R, C1156Y, F
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Herein we employ an adapted
2024-04-17

Herein we employ an adapted targeted quantitative proteomic isotope dilution method, developed in our laboratory [[18], [19], [20], [21]], to quantify membrane transporters in fresh lung from five donors, in four immortalized human lung cell lines and in three control cell lines. We quantify twelve
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Subsequently Palvimaki et al corroborated Ni and Miledi s st
2024-04-17

Subsequently, Palvimaki et al. (1999) corroborated Ni and Miledi's study by demonstrating that treatment with fluoxetine leads to 43% occupancy of the 5-HT2C receptors. Moreover, the affinity of fluoxetine for 5HT2C receptors (Ki 65 nM) is close to its affinity for 5-HT transporters (Ki 33 nM) (Ni a
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The synthetic route to M developed by
2024-04-17

The synthetic route to M100907 developed by Rice was utilized, however, the chiral resolution was carried out at an earlier stage to provide the possibility of introducing different substituents onto the piperidinyl group. The conditions for this resolution were different from previously reported.
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