onr:"swepub:oai:DiVA.org:uu-89399"
Sökning: onr:"swepub:oai:DiVA.org:uu-89399" > Synthesis of two po...
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| Fältnamn | Indikatorer | Metadata |
|---|---|---|
| 000 | 03972naa a2200385 4500 | |
| 001 | oai:DiVA.org:uu-89399 | |
| 003 | SwePub | |
| 008 | 090212s2007 | |||||||||||000 ||eng| | |
| 024 | 7 | a https://urn.kb.se/resolve?urn=urn:nbn:se:uu:diva-893992 URI |
| 024 | 7 | a https://doi.org/10.1186/1471-2342-7-62 DOI |
| 040 | a (SwePub)uu | |
| 041 | a engb eng | |
| 042 | 9 SwePub | |
| 072 | 7 | a ref2 swepub-contenttype |
| 072 | 7 | a art2 swepub-publicationtype |
| 100 | 1 | a Syvänen, Stinau Uppsala universitet,Institutionen för farmaceutisk biovetenskap4 aut0 (Swepub:uu)stsyv838 |
| 245 | 1 0 | a Synthesis of two potential NK1-receptor ligands using [1-11C]ethyl iodide and [1-11C]propyl iodide and initial PET-imaging |
| 264 | c 2007-07-30 | |
| 264 | 1 | b Springer Science and Business Media LLC,c 2007 |
| 338 | a print2 rdacarrier | |
| 520 | a BACKGROUND:The previously validated NK1-receptor ligand [O-methyl-11C]GR205171 binds with a high affinity to the NK1-receptor and displays a slow dissociation from the receptor. Hence, it cannot be used in vivo for detecting concentration changes in substance P, the endogenous ligand for the NK1-receptor. A radioligand used for monitoring these changes has to enable displacement by the endogenous ligand and thus bind reversibly to the receptor. Small changes in the structure of a receptor ligand can lead to changes in binding characteristics and also in the ability to penetrate the blood-brain barrier. The aim of this study was to use carbon-11 labelled ethyl and propyl iodide with high specific radioactivity in the synthesis of two new and potentially reversible NK1-receptor ligands with chemical structures based on [O-methyl-11C]GR205171.METHODS:[1-11C]Ethyl and [1-11C]propyl iodide with specific radioactivities of 90 GBq/μmol and 270 GBq/μmol, respectively, were used in the synthesis of [O-methyl-11C]GR205171 analogues by alkylation of O-desmethyl GR205171. The brain uptake of the obtained (2S,3S)-N-(1-(2- [1-11C]ethoxy-5-(3-(trifluoromethyl)-4H-1,2,4-triazol-4-yl)phenyl)ethyl)-2-phenylpiperidin-3-amine (I) and (2S,3S)-2-phenyl-N-(1-(2- [1-11C]propoxy-5-(3-(trifluoromethyl)-4H-1,2,4-triazol-4-yl)phenyl)ethyl)piperidin-3-amine (II) was studied with PET in guinea pigs and rhesus monkeys and compared to the uptake of [O-methyl-11C]GR205171.RESULTS:All ligands had similar uptake distribution in the guinea pig brain. The PET-studies in rhesus monkeys showed that (II) had no specific binding in striatum. Ligand (I) had moderate specific binding compared to the [O-methyl-11C]GR205171. The ethyl analogue (I) displayed reversible binding characteristics contrary to the slow dissociation rate shown by [O-methyl-11C]GR205171.CONCLUSION:The propyl-analogue (II) cannot be used for detecting changes in NK1-ligand levels, while further studies should be performed with the ethyl-analogue (I). | |
| 650 | 7 | a MEDICIN OCH HÄLSOVETENSKAPx Medicinska och farmaceutiska grundvetenskaperx Farmaceutiska vetenskaper0 (SwePub)301012 hsv//swe |
| 650 | 7 | a MEDICAL AND HEALTH SCIENCESx Basic Medicinex Pharmaceutical Sciences0 (SwePub)301012 hsv//eng |
| 653 | a PHARMACY | |
| 653 | a FARMACI | |
| 700 | 1 | a Eriksson, Jonasu Uppsala universitet,Institutionen för biokemi och organisk kemi4 aut0 (Swepub:uu)joeri542 |
| 700 | 1 | a Genchel, Toveu Uppsala universitet,Avdelningen för farmaceutisk biokemi4 aut |
| 700 | 1 | a Lindhe, Örjan4 aut |
| 700 | 1 | a Antoni, Gunnar4 aut |
| 700 | 1 | a Långström, Bengtu Uppsala universitet,Institutionen för biokemi och organisk kemi4 aut0 (Swepub:uu)benglang |
| 710 | 2 | a Uppsala universitetb Institutionen för farmaceutisk biovetenskap4 org |
| 773 | 0 | t BMC Medical Imagingd : Springer Science and Business Media LLCg 7, s. 6-q 7<6-x 1471-2342 |
| 856 | 4 | u https://bmcmedimaging.biomedcentral.com/track/pdf/10.1186/1471-2342-7-6 |
| 856 | 4 8 | u https://urn.kb.se/resolve?urn=urn:nbn:se:uu:diva-89399 |
| 856 | 4 8 | u https://doi.org/10.1186/1471-2342-7-6 |
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