High impact information on vesamicol

• In mouse diaphragms, the hyperpolarization normally produced by d-tubocurarine in the endplate area of muscle fibers that had been treated by an anticholinesterase was partly or completely blocked by 2-(4-phenylpiperidino)cyclohexanol (AH5183, 0.1-1 microM), quinacrine (0.1 microM), and tetraphenylborate (1 microM) [1].
• As part of our ongoing structure-activity studies of the vesicular acetylcholine transporter ligand 2-(4-phenylpiperidino)cyclohexanol (vesamicol, 1), 22 N-hydroxy(phenyl)alkyl derivatives of 3 beta-phenyltropane, 6, and 1-methylspiro[1H-indoline-3,4'-piperidine], 7, were synthesized and tested for binding in vitro [2].
• These experiments investigate the release of transmitter from the perfused superior cervical ganglia of cats induced by ouabain in the absence or presence of 2-(4-phenylpiperidino)cyclohexanol (vesamicol), a blocker of acetylcholine (ACh) uptake [3].
• Acetylcholine mobilization in a sympathetic ganglion in the presence and absence of 2-(4-phenylpiperidino)cyclohexanol (AH5183) [4].
• These experiments measured the effect of 2-(4-phenylpiperidino)cyclohexanol (AH5183) on the release of acetylcholine (ACh) and its subcellular distribution in slices of rat striatum incubated in vitro [5].

Biological context of vesamicol

• The present study compares the affinities of 2-(4-phenylpiperidino)cyclohexanol (vesamicol, 1) and selected analogues of the latter at the vesamicol receptor (VR) with the corresponding affinities at sigma 1 and sigma 2 binding sites [6].
• The drug 2-(4-phenylpiperidino)cyclohexanol (AH5183), which potently inhibits the active transport of acetylcholine (ACh) into synaptic vesicles, was used as a pharmacological tool to study the functional role of synaptic vesicles in quantal transmitter release [7].
• Electrophysiology and binding studies were used to determine the actions of vesamicol [2-(4-phenylpiperidino)cyclohexanol (AH5183)] on an alpha-bungarotoxin-sensitive, neuronal nicotinic acetylcholine receptor in the nervous system of the cockroach, Periplaneta americana [8].

Anatomical context of vesamicol

• 3. 2(4-phenylpiperidino)cyclohexanol (AH-5183), which blocks the active uptake of ACh into synaptic vesicles, reduced both the frequency and the amplitude of slow m.e.p.p.s and did so without requiring nerve stimulation [9].
• The present experiments measured the release of acetylcholine (ACh) by the cat superior cervical ganglia in the presence of, and after exposure to, 2-(4-phenylpiperidino)cyclohexanol (AH5183), a compound known to block the uptake of ACh by cholinergic synaptic vesicles [4].
• Inhibition of neurotransmitter and hormone transport into secretory vesicles by 2-(4-phenylpiperidino)cyclohexanol and 2-bromo-alpha-ergocryptine: both compounds act as uncouplers and dissipate the electrochemical gradient of protons [10].
• Tissue stimulated in the presence of AH-5183 contained more ACh in both the nerve terminal synaptic vesicles and cytoplasmic fraction than did tissue stimulated in drug's absence [11].
• We investigated the binding of [3H]AH5183 (2-(4-phenylpiperidino)cyclohexanol) to rat brain synaptosomes and subcellular fractions [12].

Associations of vesamicol with other chemical compounds

• 2-(4-Phenylpiperidino)cyclohexanol (AH-5183) and 2-bromo-alpha-ergocryptine, known inhibitors of the transport of acetylcholine and L-glutamate, respectively, into synaptic vesicles, inhibited the ATP-dependent uptake of dopamine in parallel with the dissipation of the electrochemical gradient of protons in chromaffin granule membrane vesicles [10].

References