In our effort to develop a novel radioligand selective for the dopamine transporter, compound 1b (O-972) was designed and characterized. The compound 1b was characterized for its binding both in monkey and rat striatum tissue, which demonstrated its high selectivity for the dopamine transporter (DAT) when its binding was compared with that at the serotonin transporter (SERT). The compound 5, which is a precursor for the tritiated radiolabel ligand [3H]O-972, was synthesized and biologically characterized. The preliminary characterization of this novel radioligand revealed its strong binding affinity for the DAT. Thus, the pharmacological profile of [3H]O-972 indicated that DAT inhibitors, which include GBR 12909, mazindol, CFT, and cocaine, could potently displace this novel radioligand from monkey brain striatum tissue. On the other hand, compounds known to be not selective for and potent at the DAT were very weak to do so. Initial binding results also indicate that [3H]O-972 may interact with the DAT in a manner that is not identical to that for GBR 12909 and tropane analogs.

01 Jan 1995·Purine and Pyrimidine Metabolism in Man VIIIQ4 · MEDICINE

Blockade of Nucleoside Degradation in Monkey Whole Blood in Vitro by CI-1000, a Purine Nucleoside Phosphorylase (PNP) Inhibitor

Q4 · MEDICINE

Article

Author: Mi K. Dong ; Richard B. Gilbertsen

Purine nucleosides HxR or GdR (2.5 micrograms/mL blood) were added to EDTA-treated cynomolgus monkey whole blood in vitro, alone or with the PNP inhibitor CI-1000 (1 microgram/mL), mixed, and the concentration of nucleosides remaining in plasma followed as a function of time. The half-lives of GdR and HxR in control blood were 1.2 and < 1 min, respectively, and were extended to 17.8 and 39.8 min, respectively, by coaddition of CI-1000. In contrast, a structural analog of CI-1000, CI-972, when tested in parallel at 1 microgram/mL, had markedly less effect on the breakdown of either nucleoside. The ability of CI-1000 to retard nucleoside breakdown in blood in vitro may be a predictor of in vivo activity, and can be viewed as an early and essential biochemical consequence of PNP inhibition culminating in immunosuppression.

01 Jun 1993·Annals of the New York Academy of SciencesQ2 · CROSS-FIELD

Activities of Two 9‐Deazaguanine Analogue Inhibitors of Purine Nucleoside Phosphorylase, CI‐972 and PD 141955, in Vitro and in Vivo

Q2 · CROSS-FIELD

Article

Author: M. K. Dong ; J. C. Sircar ; M. C. Conroy ; U. Josyula ; R. B. Gilbertsen ; D. J. Wilburn

A review, with 8 references, of the inhibitory actions of CI-972 and PD 141955 on human B and T cell lymphoblastoid cell line [³H]TdR uptake and dGTP accumulation.

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Indication	Highest Phase	Country/Location	Organization	Date
Graft Rejection	Phase 1	-	Pfizer Inc.	-
Graft Rejection	Phase 1	US	Parke, Davis & Co. LLC	-

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