A 13C Fourier transform (FT) NMR study of trimethyl(phenylethynyl)silane gives new evidence for (p → d)π bonding or equivalent interaction between bonded carbon and silicon atoms. Pulsed FT operation allows detection of 29Si13C spinspin coupling observed as 2.3 % 29Si satellites in 13C spect...
The nickel-catalyzed reactions of 2-phenyl- and 2-(o-tolyl)-2-(phenylethynyl)hexamethyltrisilane (I and II) with phenyl(trimethylsilyl)acetylene at 180°C have been examined. The reaction of I with phenyl(trimethylsilyl)acetylene in the presence of tetrakis(triethylphosphine)nickel(0) gave 1,3-d...
Two sulfur-containing compounds, (S)-2-amino-5-((R)-1-carboxy-2-((E)-3-(4-hydroxy-3-methoxyphenyl)allylthio)ethyl-amino)-5-oxopentanoic acid (1) and (S)-2-amino-5-((R)-1-(carboxymethylamino)-3-((E)-3-(4-hydroxyphenyl)allylthio)-1-oxopropan-2-ylamino)-5-oxopentanoic acid (2), and one 1H-pyrrole-2...
The general utility of reductive alkylation of amino groups of proteins with glyceraldehyde (2,3-dihydroxypropionaldehyde) in the presence of sodium cyano-borohydride, i.e. dihydroxypropylation, as an aid in generating arginine peptides of proteins by tryptic digestion has been investigated. The...
Novel 1-(dihydroxypropyl)-5-substituted uracils were synthesized in the reaction of 1-(4-nitrophenyl)-5-substituted uracil derivatives with appropriate aminopropanediols under mild conditions. In the case of 3-amino-1,2-propanediol both racemic and enantiomerically enriched products were obtaine...
In a previous study, intracerebroventricular calcium-dependent protein kinase (PKC) inhibition attenuated cocaine place conditioning. This suggested the hypothesis that intra-nucleus accumbens (NAc) injections of the PKC inhibitor NPC 15437 may block place conditioning produced by NAc injections...
Recently it has been reported that “If channel blockers”, which block the hyperpolarization-activated inward current (If) in heart sino atrial node cells, also block the hyperpolarization-activated inward current (Ih) in other tissues. Here we compared the effects of one of these agents, ZD728...
Pituitary lactotrophs fire action potentials spontaneously and the associated voltage-gated calcium influx is sufficient to maintain high prolactin release. Here we studied the role of hyperpolarization-activated cation channels in pacemaking activity, calcium signaling, and prolactin secretion ...
Hyperpolarization-activated cyclic-nucleotide-gated (HCN) channels have been suggested to play an important role in the control of membrane excitability and rhythmic neuronal activity. Our previous study showed that the selective HCN channels blocker, ZD7288 (4-(N-ethyl-N-phenylamino)-1,2-dimeth...
Neurons respond to intracellular injection of hyperpolarizing current pulses by generating depolarizing sags contributed by a cation current termed Ih. Ih modulates neuron excitability and rhythmicity. It is, however, unclear whether the net effect of changing Ih leads to facilitation or depress...
In this study, ZD7288, a blocker of hyperpolarization-activated and cyclic nucleotide-gated (HCN) channels, has been found to inhibit the mouse sperm acrosome reaction (AR). HCN channels have not yet been either recorded or implicated in mouse sperm AR, but low-threshold (T-type) Ca2+ channels h...
The role of the hyperpolarization-activated current (Ih) mediated by HCN channels in temperature sensing by the hypothalamus was addressed. In warm-sensitive neurons (WSNs), exposure to ZD7288, an inhibitor of Ih mediated by hyperpolarization-activated cyclic nucleotide-gated (HCN) channels, dec...
Heart rate slowing produced by cardiac parasympathetic (vagal) stimulation is thought to be the result of modulation of the acetylcholine-activated K+ current (IK,ACh) and the pacemaker current (If) in sinoatrial (SAN) pacemaker cells. However, the contribution of these and other ion currents to...
The uterus is a myogenic organ that is able to produce discrete spontaneous action potentials and contractions without any stimuli. Myometrial excitability is governed by ion channels including Ca+2 and K+ channels, but whether or not other channels such as hyperpolarization-activated cyclic nuc...
Chronic neuropathic pain has demonstrated that coexisting psychiatric disorders are associated with disability and poorer treatment outcomes. Hyperpolarization-activated cyclic nucleotide-gated (HCN, Ih) channels play a major role in pain via hyperexcitability and facilitation of ectopic firing ...
The structure of 4-chloro-3-fluorobenzaldehyde (CFB, C7H4ClFO) has been characterized by single-crystal X-ray diffraction, FT-IR and Raman techniques. The conformational isomers, optimized geometrical parameters, normal mode frequencies and corresponding vibrational assignments of CFB have been ...
A starting material, 4-bromo-3-fluorobenzaldehyde, was used for active drug substance (API) AMG 369 production. The presence of the regioisomer impurities in the starting material 4-bromo-3-fluorobenzaldehyde presented significant challenges for the API synthetic route development due to the phy...
Mitogen activated protein kinase (MAPK) signal transduction pathway has been proved to play an important role in tumorigenesis and cancer development. MEK inhibitor has been demonstrated significant clinical benefit for blocking MAPK pathway activation and possibly could block reactivation of th...
The structural elucidation of isosarain-1 (1), a minor component from the alkaloid fraction of Reniera sarai is reported; the previously partially characterized structures of sarains 1–3 (3–5) are further clarified.
The Mediterranean sponge Reniera sarai is a rich source of new alkaloids. Until now the study has been limited to the less polar compounds. In this paper we report the first studies on the more polar UV absorbing alkaloid fraction, which resulted a mixture of threehomologs, sarains A-C. A resolu...
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