Library

X
feed icon rss

Your email was sent successfully. Check your inbox.

An error occurred while sending the email. Please try again.

Proceed reservation?

Export
  • 1
    Electronic Resource
    Electronic Resource
    PET examination of [11C]NNC 687 and [11C]NNC 756 as new radioligands for the D1-dopamine receptor (1993)
    Springer
    Psychopharmacology 113 (1993), S. 149-156 
    Details
    ISSN: 1432-2072
    Keywords: Positron emission tomography ; D1-dopamine receptors ; NNC 687 ; NNC 756 ; Cynomolgus monkey ; Human
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract The benzazepines NNC 687 and NNC 756 have in animal studies been described as selective D1-dopamine receptor antagonists. Both compounds have been labeled with11C for examination by positron emission tomography (PET). In the present study central receptor binding was studied in monkeys and healthy men. After IV injection of both radioligands in Cynomolgus monkeys radioactivity accumulated markedly in the striatum, a region with a high density of D1-dopamine receptors. This striatal uptake was displaced by high doses of the selective D1-antagonist SCH 23390 (2 mg/kg) but not by the 5HT2-antagonist ketanserin (1.5 mg/kg) or the selective D2-antagonist raclopride (3 mg/kg). The cortical uptake after injection of [11C]NNC 687 was not reduced in displacement experiments with ketanserin. The cortical uptake of [11C]NNC 756 was reduced in displacement and protection experiments with ketanserin by 24–28% (1.5 mg/kg), whereas no reduction could be demonstrated on striatal uptake. In healthy males both compounds accumulated markedly in the striatum. For [11C]NNC 687 the ratio of radioactivity in the putamen to cerebellum was about 1.5. For [11C]NNC 756 the ratio was about 5. This ratio of 5 for [11C]NNC 756 is the highest obtained so far for PET radioligands for the D1-dopamine receptor.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF02245691
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 2
    Electronic Resource
    Electronic Resource
    Simultaneous determination of the three major monoamine metabolites in brain tissue and body fluids by a mass fragmentographic method (1976)
    Springer
    Psychopharmacology 48 (1976), S. 147-152 
    Details
    ISSN: 1432-2072
    Keywords: Mass fragmentography ; 5-Hydroxyindole-3-acetic acid ; 4-Hydroxy-3-methoxyphenylacetic acid ; 4-Hydroxy-3-methoxyphenylethylene glycol ; Cerebrospinal fluid ; Brain ; Urine
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract A mass fragmentographic method for the simultaneous determination of 4-hydroxy-3-methoxyphenylacetic acid (HVA), 4-hydroxy-3-methoxyphenylethylene glycol (MOPEG), and 5-hydroxyindole-3-acetic acid (5-HIAA) was described. Deuterated analogues of the compounds were used as internal standards. The specificity was proved by multiple ion analysis. The experimental error was below 7% when applied to the analysis of human lumbar cerebrospinal fluid, urine, or rat brain tissue. In cerebrospinal fluid the major part of the monoamine metabolites occurred in the free form. In rat brain and human urine considerable amounts of conjugated HVA was found.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00423253
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 3
    Electronic Resource
    Electronic Resource
    In vitro and in vivo characterisation of nor-β-CIT: a potential radioligand for visualisation of the serotonin transporter in the brain (1997)
    Springer
    European journal of nuclear medicine 24 (1997), S. 596-601 
    Details
    ISSN: 1619-7089
    Keywords: Key words: 2β-Carbomethoxy-3β-(4-iodophenyl)nortropane ; Serotonin transporter ; Brain ; Positron emission tomography ; Autoradiography
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract. Radiolabelled 2β-carbomethoxy-3β-(4-iodophenyl)tropane (β-CIT) has been used in clinical studies for the imaging of dopamine and serotonin transporters with single-photon emission tomography (SPET). 2β-Carbomethoxy-3β-(4-iodophenyl)nortropane (nor-β-CIT) is a des-methyl analogue of β-CIT, which in vitro has tenfold higher affinity (IC50=0.36 nM) to the serotonin transporter than β-CIT (IC50=4.2 nM). Nor-β-CIT may thus be a useful radioligand for imaging of the serotonin transporter. In the present study iodine-125 and carbon-11 labelled nor-β-CIT were prepared for in vitro autoradiographic studies on post-mortem human brain cryosections and for in vivo positron emission tomography (PET) studies in Cynomolgus monkeys. Whole hemisphere autoradiography with [125I]nor-β-CIT demonstrated high binding in the striatum, the thalamus and cortical regions of the human brain. Addition of a high concentration (1 μM) of citalopram inhibited binding in the thalamus and the neocortex, but not in the striatum. In PET studies with [11C]nor-β-CIT there was rapid uptake of radioactivity in the monkey brain (6% of injected dose at 15 min) and high accumulation of radioactivity in the striatum, thalamus and neocortex. Thalamus to cerebellum and cortex to cerebellum ratios were 2.5 and 1.8 at 60 min, respectively. The ratios obtained with [11C]nor-β-CIT were 20%–40% higher than those previously obtained with [11C]β-CIT. Radioactivity in the thalamus and the neocortex but not in the striatum was displaceable with citalopram (5 mg/kg). In conclusion, nor-β-CIT binds to the serotonin transporter in the primate brain in vitro and in vivo and has potential for PET and SPET imaging of the serotonin transporter in human brain.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00841395
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 4
    Electronic Resource
    Electronic Resource
    Iodine-123 labelled Z-(R,R)-IQNP: a potential radioligand for visualization of M1 and M2 muscarinic acetylcholine receptors in Alzheimer’s disease (1999)
    Springer
    European journal of nuclear medicine 26 (1999), S. 1482-1485 
    Details
    ISSN: 1619-7089
    Keywords: Key words:Z-(R ; R)-IQNP ; Muscarinic acetylcholine receptors ; Brain ; Single-photon emission tomography
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract. Z-(R)-1-Azabicyclo[2.2.2]oct-3-yl (R)-α-hydroxy-α-(1-iodo-1-propen-3-yl)-α-phenylacetate (Z-IQNP) has high affinity to the M1 and M2 muscarinic acetylcholine receptor (mAChR) subtypes according to previous in vitro and in vivo studies in rats. In the present study iodine-123 labelled Z-IQNP was prepared for in vivo single-photon emission tomography (SPET) studies in cynomolgus monkeys. SPET studies with Z-[123I]IQNP demonstrated high accumulation in monkey brain (〉5% of injected dose at 70 min p.i.) and marked accumulation in brain regions such as the thalamus, the neocortex, the striatum and the cerebellum. Pretreatment with the non-selective mAChR antagonist scopolamine (0.2 mg/kg) inhibited Z-[123I]IQNP binding in all these regions. The percentage of unchanged Z-[123I]IQNP measured in plasma was less than 10% at 10 min after injection, which may be due to rapid hydrolysis, as has been demonstrated previously with the E-isomer of IQNP. Z-[123I]IQNP showed higher uptake in M2-rich regions, compared with previously obtained results with E-[123I]IQNP. In conclusion, the radioactivity distribution from Z-[123I]IQNP in monkey brain indicates that Z-[123I]IQNP binds to the M1- and M2-rich areas and provides a high signal for specific binding, and is thus a potential ligand for mAChR imaging with SPET.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/s002590050482
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 5
    Electronic Resource
    Electronic Resource
    In vitro and in vivo characterisation of nor-β-CIT: a potential radioligand for visualisation of the serotonin transporter in the brain (1997)
    Springer
    European journal of nuclear medicine 24 (1997), S. 596-601 
    Details
    ISSN: 1619-7089
    Keywords: 2β-Carbomethoxy-3β-(4-iodophenyl)nortrapane ; Serotonin transporter ; Brain ; Positron emission tomography ; Autoradiography
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract Radiolabelled 2β-Cabomethoxy-3β-(4-iodophenyl)tropane (β-CIT) has been used in clinical studies for the imaging of dopamine and serotonin transporters with single-photon emission tomography (SPET). 2β-Carbomethoxy-3β-(4-iodophenyl)nortropane (nor-β-CIT) is a des-methyl analogue of β-CIT, which in vitro has tenfold higher affinity (IC50=0.36 nM) to the serotonin transporter than β-CIT (IC50=4.2 nM). Nor-β-CIT may thus be a useful radioligand for imaging of the serotonin transporter. In the present study iodine-125 and carbon-11 labelled nor-β-CIT were prepared for in vitro autoradiographic studies on post-mortem human brain cryosections and for in vivo positron emission tomography (PET) studies in Cynomolgus monkeys. Whole hemisphere autoradiography with [125I]nor-β-CIT demonstrated high binding in the striatum, the thalamus and cortical regions of the human brain. Addition of a high concentration (1 μM) of citalopram inhibited binding in the thalamus and the neocortex, but not in the striatum. In PET studies with [11C]nor-β-CIT there was rapid uptake of radioactivity in the monkey brain (6% of injected dose at 15 min) and high accumulation of radioactivity in the striatum, thalamus and neocortex. Thalamus to cerebellum and cortex to cerebellum ratios were 2.5 and 1.8 at 60 min, respectively. The ratios obtained with [11C]nor-β-CIT were 20%–40% higher than those previously obtained with [11C]β-CIT. Radioactivity in the thalamus and the neocortex but not in the striatum was displaceable with citalopram (5 mg/kg). In conclusion, nor-β-CIT binds to the serotonin transporter in the primate brain in vitro and in vivo and has potential for PET and SPET imaging of the serotonin transporter in human brain.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00841395
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
Close ⊗
This website uses cookies and the analysis tool Matomo. More information can be found here...