The D2-agonist radiotracer [<sup>11</sup>C]-(+)-PHNO shows a marked increase in sensitivity to amphetamine challenges when compared to [<sup>11</sup>C]raclopride in the cat brain

Ginovart, Nathalie; Wilson, Alan A.; Willeit, M.; Singh, Ken; Hussey, Doug; García, Armando; Houle, Sylvain; Kapur, Shitij

doi:10.1038/sj.jcbfm.9591524.0611

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“…While the BP value was greater for [ 11 C]PHNO, the change in BP after AMPH was similar, resulting in a maximal change in BP with a reduction of 59% at 1.0 mg/kg (nonhuman primate) and 62% at 2.0 mg/kg (rat) for [ 11 C]MNPA and [ 11 C]PHNO, respectively. A greater change in BP with [ 11 C]PHNO was demonstrated in cat brain, showing a maximal change in BP of 88% after administration of 2.0 mg/kg of AMPH (Ginovart et al, 2005b). The highest BP values reported in human brain for [ 11 C]PHNO was 3.38 in the globus pallidus.…”

Section: Comparison Of Pet D 2 Agonist Radioligandsmentioning

confidence: 87%

Effect of amphetamine on dopamine D2 receptor binding in nonhuman primate brain: A comparison of the agonist radioligand [11C]MNPA and antagonist [11C]raclopride

Seneca

Finnema

Farde

et al. 2006

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PET measurements of stimulant-induced dopamine (DA) release are typically performed with antagonist radioligands that bind to both the high- and low-affinity state of the receptor. In contrast, an agonist radioligand binds preferentially to the high-affinity state and is expected to have greater sensitivity to DA, which is the endogenous agonist. [(11)C]MNPA, (R)-2-CH(3)O-N-n-propylnorapomorphine (MNPA), is a D(2) agonist radioligand with subnanomolar affinity to the D(2) receptor. The aim of the present study is to assess and compare the sensitivity of the agonist radioligand [(11)C]MNPA and antagonist radioligand [(11)C]raclopride to synaptic DA levels. Four cynomolgus monkeys were examined with [(11)C]MNPA and [(11)C]raclopride (16 PET measurements with each tracer) at baseline and after pretreatment with various doses of amphetamine. The effect of amphetamine was calculated by the change in binding potential (BP) analyzed with the multilinear reference tissue model (MRTM2). Amphetamine caused a reduction in [(11)C]MNPA BP of 4% at 0.1, 23% at 0.2, 25% at 0.5, and 46% at 1.0 mg/kg. [(11)C]Raclopride BP was reduced to a lesser extent by 2% at 0.1, 16% at 0.2, 15% at 0.5, and 23% at 1.0 mg/kg. The data were used to estimate the in vivo percentage of high-affinity state receptors to be approximately 60%. These results demonstrate that [(11)C]MNPA is more sensitive than [(11)C]raclopride to displacement by endogenous DA, and that it may provide additional information about the functional state of the D(2) receptor in illnesses such as schizophrenia and Parkinson's disease.

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Section: Comparison Of Pet D 2 Agonist Radioligandsmentioning

confidence: 87%

Effect of amphetamine on dopamine D2 receptor binding in nonhuman primate brain: A comparison of the agonist radioligand [11C]MNPA and antagonist [11C]raclopride

Seneca

Finnema

Farde

et al. 2006

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103

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The D2-agonist radiotracer [¹¹C]-(+)-PHNO shows a marked increase in sensitivity to amphetamine challenges when compared to [¹¹C]raclopride in the cat brain

Cited by 1 publication

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Effect of amphetamine on dopamine D2 receptor binding in nonhuman primate brain: A comparison of the agonist radioligand [11C]MNPA and antagonist [11C]raclopride

Effect of amphetamine on dopamine D2 receptor binding in nonhuman primate brain: A comparison of the agonist radioligand [11C]MNPA and antagonist [11C]raclopride

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The D2-agonist radiotracer [11C]-(+)-PHNO shows a marked increase in sensitivity to amphetamine challenges when compared to [11C]raclopride in the cat brain

Cited by 1 publication

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Effect of amphetamine on dopamine D2 receptor binding in nonhuman primate brain: A comparison of the agonist radioligand [11C]MNPA and antagonist [11C]raclopride

Effect of amphetamine on dopamine D2 receptor binding in nonhuman primate brain: A comparison of the agonist radioligand [11C]MNPA and antagonist [11C]raclopride

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The D2-agonist radiotracer [¹¹C]-(+)-PHNO shows a marked increase in sensitivity to amphetamine challenges when compared to [¹¹C]raclopride in the cat brain