- A subtype-selective, use-dependent inhibitor of native AMPA receptors
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AMPA (α-amino-3-hydroxy-5-methyl-4-isooxazole) receptors (AMPARs) are glutamate-gated ion channels that play central roles in the mammalian brain, mediating fast excitatory synaptic transmission and underlying several forms of synaptic plasticity. Two sub
- Nilsen, Aaron,England, Pamela M.
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p. 4902 - 4903
(2008/02/03)
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- Butyryl-tyrosinyl spermine, analogs thereof and methods of preparing and using same
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The present invention provides a compound having the structure: STR1 wherein R1 is a saturated or unsaturated linear or branched chain alkyl group, or a cholestanyl group; wherein R2 is a 2-indolyl, 3-indolyl, 4-indolyl, 5-indolyl, 4-hydroxyphenyl, 4-(arylalkyloxy)phenyl, 3,4-dihalophenyl, 4-hydroxy-3,5-dihalophenyl, 4-azidophenyl or 4-halophenyl group; wherein R3 is H, a linear or branched chain alkyl or alkenyl group, or a phenyl, 2-azidophenyl, 3-azidophenyl, 4-azidophenyl group, or an a alkenylacyl, 3-amino-3-butylpropyl, N-[N-(N-{4-azidobenzoyl}aminopropyl) aminopropyl], cis- or trans-cinnamyl, 2-amino-2-[(4'-azidophenyl)acetyl, (trifluoromethyl)aminoacetyl or D- or L-arginyl group bonded through the α-carbonyl moiety thereof; R4 is H, or a linear or branched chain alkyl group; wherein R5, R6 and R7 are independently the same or different and are H, a linear or branched chain alkyl group, an aryl group or an arylalkyl group; wherein n, j and t are each 0 or 1; wherein m, o, p, q, r and s are independently the same or different and are 0, 1 or 2; wherein r+s and m+o are each equal to 2; wherein, if j is 0, p+q is 2; wherein, if j is 1, then p is 1, q is 0 and R6 is H; and wherein * denotes a D or L configuration. The invention also provides a method of synthesizing the compound. Another aspect of the invention concerns a method of treating a subject afflicted by a disorder associated with binding of an etiological agent to a glutamate receptor.
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- Butyryl-tyrosinyl spermine, analogs thereof and methods of preparing and using same
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The present invention provides a compound having the structure: STR1 wherein R1 is hydrogen or a branched or unbranched, substituted or unsubstituted aminoalkyl having from two to twenty atoms in the chain, R2 is hydrogen, methyl, or a branched or unbranched, substituted or unsubstituted alkyl having from two to twenty atoms in the chain; when R2 is methyl, R3 is either hydrogen or a substituted or unsubstituted aryl; and R4 is methyl, a branched or unbranched, substituted or unsubstituted alkyl, alkenyl, alkynyl, alkenynyl, or cycloalkyl having from two to twenty atoms in the chain, or a substituted or unsubstituted aryl group. The invention also concerns a method of preparing the compound from the venom, venom sacs or venom glands of the wasp Philanthus triangulun F. Additionally, the invention provides a method of chemically synthesizing the compound. Another aspect of the invention concerns a method of treating a subject afflicted by a disorder associated with binding of an etiological agent to a glutamate receptor. Lastly, the invention provides an insecticidal composition which comprises an effective amount of the compound and a suitable carrier and a method of combatting insects which comprises administering to the insects the insecticidal composition.
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- Structure-binding relation of philanthotoxins from nicotinic acetylcholine receptor binding assay
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Philanthotoxins are noncompetitive inhibitors of the nicotinic acetylcholine receptor and the various glutamate receptors. Analogues carrying photoaffinity labels, fluorine atoms for solid-state NMR studies of ligand/receptor interaction, and large head g
- Nakanishi, Koji,Huang, Xuefei,Jiang, Hong,Ying, Liu,Fang, Kan,Huang, Danwen,Choi, Seok-Ki,Katz, Elizabeth,Eldefrawi, Mohyee
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p. 1969 - 1988
(2007/10/03)
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