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338 results

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Page 1
In Vivo and In Vitro Characteristics of Radiolabeled Vesamicol Analogs as the Vesicular Acetylcholine Transporter Imaging Agents.
Ogawa K, Shiba K. Ogawa K, et al. Contrast Media Mol Imaging. 2018 Jun 13;2018:4535476. doi: 10.1155/2018/4535476. eCollection 2018. Contrast Media Mol Imaging. 2018. PMID: 30008624 Free PMC article. Review.
The vesicular acetylcholine transporter (VAChT), a presynaptic cholinergic neuron marker, is a potential internal molecular target for the development of an imaging agent for early diagnosis of neurodegenerative disorders with cognitive decline such as Alzheimer's disease (AD). S …
The vesicular acetylcholine transporter (VAChT), a presynaptic cholinergic neuron marker, is a potential internal molecular target for the d …
(+)-p-[11C]Methylvesamicolphenoxy).
Cheng KT. Cheng KT. 2006 Jul 12 [updated 2008 Jan 23]. In: Molecular Imaging and Contrast Agent Database (MICAD) [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2004–2013. 2006 Jul 12 [updated 2008 Jan 23]. In: Molecular Imaging and Contrast Agent Database (MICAD) [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2004–2013. PMID: 20641790 Free Books & Documents. Review.
Another potential PET ligand is methylvesamicol, an analog of vesamicol. Vesamicol has been found to block the release of acetylcholine from cholinergic nerve terminals, and a number of radioiodine-, (18)F-, and (11)C-labeled vesamicol derivatives have been s …
Another potential PET ligand is methylvesamicol, an analog of vesamicol. Vesamicol has been found to block the release of acet …
The pharmacology of vesamicol: an inhibitor of the vesicular acetylcholine transporter.
Prior C, Marshall IG, Parsons SM. Prior C, et al. Gen Pharmacol. 1992 Nov;23(6):1017-22. doi: 10.1016/0306-3623(92)90280-w. Gen Pharmacol. 1992. PMID: 1487110 Review.
1. Vesamicol (2-[4-phenylpiperidino] cyclohexanol) inhibits the transport of acetylcholine into synaptic vesicles in cholinergic nerve terminals. 2. ...Vesamicol clearly represents a unique tool for investigating presynaptic mechanisms in cholinergic nerve terminals …
1. Vesamicol (2-[4-phenylpiperidino] cyclohexanol) inhibits the transport of acetylcholine into synaptic vesicles in cholinergic nerv …
Astatine-211-labeled aza-vesamicol derivatives as sigma receptor ligands for targeted alpha therapy.
Ogawa K, Nishizawa K, Washiyama K, Munekane M, Fuchigami T, Echigo H, Mishiro K, Hirata S, Wakabayashi H, Takahashi K, Kinuya S. Ogawa K, et al. Nucl Med Biol. 2023 Jul-Aug;122-123:108369. doi: 10.1016/j.nucmedbio.2023.108369. Epub 2023 Jul 22. Nucl Med Biol. 2023. PMID: 37516066
Previously, we synthesized and evaluated radioiodinated aza-vesamicol derivatives, [(125)I]pIC(3)NV, [(125)I]mIC(2)N5V, and [(125)I]mIC(3)N5V. ...
Previously, we synthesized and evaluated radioiodinated aza-vesamicol derivatives, [(125)I]pIC(3)NV, [(125)I]mIC(2)N5V, and [(125)I]m …
Alpha-adrenoceptor blocking properties of vesamicol.
Wannan G, Prior C, Marshall IG. Wannan G, et al. Eur J Pharmacol. 1991 Aug 16;201(1):29-34. doi: 10.1016/0014-2999(91)90318-k. Eur J Pharmacol. 1991. PMID: 1686588
This effect was abolished by desipramine suggesting that it is due to an ability of (-)-vesamicol to block uptake1. In the presence of noradrenaline uptake blockers, (-)-vesamicol produced a competitive, non-selective block of both alpha 1- and alpha 2-adrenoceptors …
This effect was abolished by desipramine suggesting that it is due to an ability of (-)-vesamicol to block uptake1. In the presence o …
Development of tumor-targeting aza-vesamicol derivatives with high affinity for sigma receptors for cancer theranostics.
Mishiro K, Wang M, Hirata S, Fuchigami T, Shiba K, Kinuya S, Ogawa K. Mishiro K, et al. RSC Med Chem. 2022 Jun 30;13(8):986-997. doi: 10.1039/d2md00099g. eCollection 2022 Aug 17. RSC Med Chem. 2022. PMID: 36092143 Free PMC article.
As sigma receptors are highly expressed on various cancer cells, radiolabeled sigma receptor ligands have been developed as imaging and therapeutic probes for cancer. Previously, we synthesized and evaluated a radioiodinated vesamicol derivative, 2-(4-[(125)I](4-iodophenyl …
As sigma receptors are highly expressed on various cancer cells, radiolabeled sigma receptor ligands have been developed as imaging and ther …
Multiple protonation states of vesicular acetylcholine transporter detected by binding of [3H]vesamicol.
Khare P, White AR, Parsons SM. Khare P, et al. Biochemistry. 2009 Sep 29;48(38):8965-75. doi: 10.1021/bi900759v. Biochemistry. 2009. PMID: 19685929 Free PMC article.
The current study characterizes the binding of (-)-vesamicol from pH 5 to pH 10 using filter assays, (-)-[3H]vesamicol (hereafter called [3H]vesamicol), and human VAChT expressed in PC12(A123.7) cells. ...Time-dependent dissociation of bound [3H]vesamicol …
The current study characterizes the binding of (-)-vesamicol from pH 5 to pH 10 using filter assays, (-)-[3H]vesamicol (hereaf …
Vesamicol analogues as sigma ligands. Molecular determinants of selectivity at the vesamicol receptor.
Efange SM, Mach RH, Smith CR, Khare AB, Foulon C, Akella SK, Childers SR, Parsons SM. Efange SM, et al. Biochem Pharmacol. 1995 Mar 15;49(6):791-7. doi: 10.1016/0006-2952(94)00541-s. Biochem Pharmacol. 1995. PMID: 7702637
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. ...Vesamicol analogues c …
The present study compares the affinities of 2-(4-phenylpiperidino)cyclohexanol (vesamicol, 1) and selected analogues of the latter a …
The effects of vesamicol on trains of endplate currents and on focally recorded nerve terminal currents at mammalian neuromuscular junctions.
Pemberton KE, Prior C, Marshall IG. Pemberton KE, et al. Br J Pharmacol. 1992 Jan;105(1):113-8. doi: 10.1111/j.1476-5381.1992.tb14220.x. Br J Pharmacol. 1992. PMID: 1375854 Free PMC article.
In the rat, 0.1 and 1 microM (-)-vesamicol produced an enhancement of the rundown of e.p.c. amplitudes during trains of high frequency (50 Hz) nerve stimulation. However, 1 microM (+)-vesamicol had no effect on the rundown of e.p.c. amplitudes. 3. In the mouse, high …
In the rat, 0.1 and 1 microM (-)-vesamicol produced an enhancement of the rundown of e.p.c. amplitudes during trains of high frequenc …
338 results