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 Jul 2000·Journal of Cutaneous Medicine and SurgeryQ4 · MEDICINE

The Effect of VAS972 on Allergic Contact Hypersensitivity

Q4 · MEDICINE

Article

Author: Mandel, Arkady Sh. ; Suzuki, Hirotake ; Bolton, Anthony E. ; Sauder, Daniel N. ; Shivji, Gulnar M.

Background: Contact hypersensitivity (CHS) is a Th1-mediated immune response that can be down-regulated by immunosuppressive agents such as cyclosporine and environmental stimuli such as ultraviolet light. Recently, an immunomodulation therapy, VAS972, has been developed which is believed to down-regulate the Th1 arm of the immune response. This VAS972 involves modifying autologous blood by controlled exposure to the oxidizing agent ozone and UVC light, at an elevated temperature ex vivo. The processed blood is then administered by intramuscular injection. Objective: To further evaluate the immune modulating effect of VAS972. Methods: We examined the effect of VAS972 treatment on CHS. Contact hypersensitivity was induced with dinitro-fluorobenzene (DNFB) in animals receiving VAS972-processed blood, control blood, or saline. A preliminary study was also conducted to evaluate the effect of plasma and cellular fractions of processed blood. Results: Mice injected with VAS972-processed blood demonstrated a significantly lower (46%) CHS response than controls. Histologic examination of challenged ear skin from control mice displayed edema with a significant lymphocytic infiltration, whereas animals administered processed blood demonstrated a reduction in lymphocytic infiltration. Mice injected with either plasma or the cellular fraction of the VAS972-treated blood also demonstrated a significant suppression (49% and 41%, respectively). Conclusion: The results of this study demonstrated that VAS972 suppresses CHS and cellular infiltration. Furthermore, the plasma and cellular components of the VAS972 treatment were also able to induce immunosuppression. This further supports the hypothesis that VAS972 down-regulates the Th1 arm of the immune response.

100 Deals associated with VAS-972

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Indication	Highest Phase	Country/Location	Organization	Date
Psoriasis	Phase 2	-	Intellipharmaceutics International, Inc.	-
Psoriasis	Phase 2	CA	Vasogen, Inc.	-
Rheumatoid Arthritis	Phase 2	CA	Vasogen, Inc.	-

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