[3H]β-羧基-3,4-二氢-2β-(4-氯苯基)托品：大鼠脑组织中多巴胺转运体的放射性配体。
[3H]beta-CIT: a radioligand for dopamine transporters in rat brain tissue.
作者信息
Kula N S, Baldessarini R J, Tarazi F I, Fisser R, Wang S, Trometer J, Neumeyer J L
机构信息
Mailman and Addiction Research Centers, McLean Division of Massachusetts General Hospital, Belmont, MA 02478, USA.
出版信息
Eur J Pharmacol. 1999 Dec 3;385(2-3):291-4. doi: 10.1016/s0014-2999(99)00695-0.
[3H]2-beta-carbomethoxy-3-beta-[4'-iodophenyl]tropane (beta-CIT) was prepared and evaluated. With rat forebrain tissue, [3H]beta-CIT showed high affinity for dopamine transporters (DAT), with selectivity for DAT over norepinephrine transporters, but not serotonin transporters, as well as DAT-stereoselectivity with beta-CIT, amphetamine and methylphenidate. Affinity and selectivity for 53 compounds assayed with [3H]beta-CIT and standard DAT radioligand [3H]GBR-12935 were highly correlated (r0.95). [3H]beta-CIT is proposed as a useful, high-affinity DAT radioprobe.
制备并评估了[3H]2-β-甲氧基羰基-3-β-[4'-碘苯基]托烷（β-CIT）。在大鼠前脑组织中，[3H]β-CIT对多巴胺转运体（DAT）表现出高亲和力，对DAT的选择性高于去甲肾上腺素转运体，但对5-羟色胺转运体无选择性，并且对β-CIT、苯丙胺和哌甲酯具有DAT立体选择性。用[3H]β-CIT和标准DAT放射性配体[3H]GBR-12935测定的53种化合物的亲和力和选择性高度相关（r>0.95）。[3H]β-CIT被认为是一种有用的、高亲和力的DAT放射性探针。
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