Henry I. Yamamura

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The conformationally restricted, cyclic, disulfide-containing, enkephalin analogs [2-D-penicillamine, 5-L-penicillamine]enkephalin [(D-Pen2,L-Pen5]enkephalin) and [2-D-penicillamine, 5-D-penicillamine]enkephalin [(D-Pen2,D-Pen5]enkephalin) were synthesized by solid-phase methods. Selectivities of these analogs for a single class of opioid receptor were(More)
Binding sites with high affinity and specificity for [(3)H]quinuclidinyl benzilate (QNB) are present in homogenates of rat brain. The characteristics of the binding sites resemble those of muscarinic cholinergic receptors. Specific binding is saturable with respect to [(3)H]QNB and tissue concentration and is time-, temperature-, and pH-dependent. The(More)
The duration of antagonistic action of nor-binaltorphimine (nor-BNI), a kappa antagonist, of antinociception resulting from selective opioid agonists, was examined using the mouse tail-flick assay as the endpoint. Nor-BNI (1 nmol, i.c.v. at -20 min) antagonized equiantinociceptive doses of the opioid kappa agonists (5 alpha,7 alpha,8(More)
Since their first description as anomalous high affinity diazepam binding sites in rat peripheral tissues, the peripheral-type benzodiazepine receptor (PBR) has been increasingly studied to better understand nonneural effects of the benzodiazepines. The mammalian PBR is ubiquitously distributed with high concentrations in the outer mitochondrial membrane of(More)
We recently demonstrated that the non-classical muscarinic receptor antagonist [3H]pirenzepine ([3H]PZ) identifies a high affinity population of muscarinic sites in the rat cerebral cortex. We now report that cortical muscarinic sites to which [3H]PZ binds with high affinity are modulated by ions but not guanine nucleotides. We also have examined(More)
We measured (-)-5-(1,1-dimethylheptyl)-2-[5-hydroxy-2-(3-hydroxypropyl)cyclohe xyl]-phenol (CP 55,940)-, (-)11-OH-delta8-tetrahydrocannabinol-dimethylheptyl (HU-210)-, anandamide- and delta9-tetrahydrocannabinol-stimulated G protein activation in mouse brain using the [35S]GTPgammaS functional assay. The Ki values for these drugs were determined by agonist(More)
Synaptosomes from rat brain accumulate choline by two kinetically distinct processes, a high-affinity uptake system [Michaelis constant (K(m)) = 1 x 10(-6)M], and a low-affinity system (K(m) = 9 x 10(-5)M). The high-affinity uptake system requires sodium, and is associated with considerable formation of acetylcholine. The low-affinity uptake system is less(More)
The effects of R(+)-[2,3-dihydro-5-methyl-3-[(morpholinyl)methyl]pyrrolo[1,2,3-de]-1,4- benzoxazin-yl]-(1-napthalenyl)methanone mesylate (WIN 55,212-2) and N-piperidino-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-3-pyrazo le-carboxamide (SR141716A) on guanosine-5'-O-(3-[35S]thio)triphosphate ([35S]GTPgammaS) binding to membranes isolated from human(More)