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In vivo binding of [11C]SKF 75670 and [11C]SKF 82957 in rat brain: two dopamine D-1 receptor agonist ligands.
DaSilva JN, Wilson AA, Valente CM, Hussey D, Wilson D, Houle S. DaSilva JN, et al. Life Sci. 1996;58(19):1661-70. doi: 10.1016/0024-3205(96)00141-5. Life Sci. 1996. PMID: 8632703
The high affinity benzazepine D1 agonists SKF 75670 and SKF 82957 labeled with C-11 were evaluated in vivo in rats as potential radioligands for imaging dopamine D1 receptors with positron emission tomography (PET). Their in vivo pharmacological profile revealed sel …
The high affinity benzazepine D1 agonists SKF 75670 and SKF 82957 labeled with C-11 were evaluated in vivo in rats as potentia …
Synthesis and autoradiographic localization of the dopamine D-1 agonists [11C]SKF 75670 and [11C]SKF 82957 as potential PET radioligands.
DaSilva JN, Wilson AA, Nobrega JN, Jiwa D, Houle S. DaSilva JN, et al. Appl Radiat Isot. 1996 Mar;47(3):279-84. doi: 10.1016/0969-8043(95)00306-1. Appl Radiat Isot. 1996. PMID: 8935965
The high affinity benzazepine D1 agonists SKF 75670 and SKF 82957 were labeled with 11C by N-[11C]methylation of SKF 38393 and SKF 81297, respectively, using [11C]methyl iodide in the presence of N-ethyldiisopropylamine. ...Autoradiographic studies showed selective …
The high affinity benzazepine D1 agonists SKF 75670 and SKF 82957 were labeled with 11C by N-[11C]methylation of SKF 38393 and …
Systemic catechol-O-methyl transferase inhibition enables the D1 agonist radiotracer R-[11C]SKF 82957.
Palner M, McCormick P, Parkes J, Knudsen GM, Wilson AA. Palner M, et al. Nucl Med Biol. 2010 Oct;37(7):837-43. doi: 10.1016/j.nucmedbio.2010.04.193. Nucl Med Biol. 2010. PMID: 20870159
INTRODUCTION: R-[(11)C]-SKF 82957 is a high-affinity and potent dopamine D(1) receptor agonist radioligand, which gives rise to a brain-penetrant lipophilic metabolite. ...CONCLUSIONS: Pre-treatment with the COMT inhibitor tolcapone inhibits formation of an interfer …
INTRODUCTION: R-[(11)C]-SKF 82957 is a high-affinity and potent dopamine D(1) receptor agonist radioligand, which gives rise t …
Dopamine D1 agonist R-[11C]SKF 82957: synthesis and in vivo characterization in rats.
DaSilva JN, Schwartz RA, Greenwald ER, Lourenco CM, Wilson AA, Houle S. DaSilva JN, et al. Nucl Med Biol. 1999 Jul;26(5):537-42. doi: 10.1016/s0969-8051(99)00015-3. Nucl Med Biol. 1999. PMID: 10473192
Compared with the D1 agonist R/S-[11C]SKF 82957, R-[11C]SKF 82957 showed higher binding in the D1 rich regions, such as striatum and olfactory tubercles (approximately 1.7 times), thereby improving the tissue contrast. ...No labeled metabolites were de …
Compared with the D1 agonist R/S-[11C]SKF 82957, R-[11C]SKF 82957 showed higher binding in the D1 rich regions, …
D1 receptors involved in the acquisition of sexual experience in male rats.
Bialy M, Kalata U, Nikolaev-Diak A, Nikolaev E. Bialy M, et al. Behav Brain Res. 2010 Jan 20;206(2):166-76. doi: 10.1016/j.bbr.2009.09.008. Epub 2009 Sep 9. Behav Brain Res. 2010. PMID: 19747509
The antagonist (SCH-23390) inhibited changes in PVs and EL as well as rearing (R) and mount latency (ML). Both agonists (SKF-38393 and selective SKF-82957) inhibited PVs also at doses where no effects on EL and ML were observed. Repeated injections of five agonists, …
The antagonist (SCH-23390) inhibited changes in PVs and EL as well as rearing (R) and mount latency (ML). Both agonists (SKF-38393 and selec …
No change in dopamine D1 receptor in vivo binding in rats after sub-chronic haloperidol treatment.
Sanci V, Houle S, DaSilva JN. Sanci V, et al. Can J Physiol Pharmacol. 2002 Jan;80(1):36-41. doi: 10.1139/y02-002. Can J Physiol Pharmacol. 2002. PMID: 11911224
The goal of this study was to investigate in vivo the possible relationship between D1 receptor binding and D1-mediated behavioral supersensitivity, after subchronic HAL treatments. D1 agonist R-SKF 82957 and antagonist SCH 23390, both labeled with carbon-11, were u …
The goal of this study was to investigate in vivo the possible relationship between D1 receptor binding and D1-mediated behavioral supersens …
Radiotracer synthesis from [(11)C]-iodomethane: a remarkably simple captive solvent method.
Wilson AA, Garcia A, Jin L, Houle S. Wilson AA, et al. Nucl Med Biol. 2000 Aug;27(6):529-32. doi: 10.1016/s0969-8051(00)00132-3. Nucl Med Biol. 2000. PMID: 11056365
Radiochemical yields are equal to or superior to conventional solution methods in all cases, even though no heat is applied. [(11)C]-labeled radiotracers that have been prepared by this method for human or animal studies include Raclopride, N-methylspiperone, Ro 15-1788, FLB 457, …
Radiochemical yields are equal to or superior to conventional solution methods in all cases, even though no heat is applied. [(11)C]-labeled …