Table 8.

Main serotoninergic radioligands, molecular structures, pharmacological properties, and examples of clinical studies.

Compounds	Imaging modality	Target/ measure	Affinity (nM)	Clinical studies	Compounds	Imaging modality	Target/ measure	Affinity (nM)	Clinical studies
[11C]-WAY-100635	PET	5-HT1A density (antagonist)	Kd = 0.2–0.4 (300)	PD (306), depression (349), panic disorder (303), social anxiety disorder (302), anorexia nervosa (304)	[18F]altanserin	PET	5-HT2A density	Ki = 0.13 (300)	AD (326), depression (325), schizophrenia (328), Tourette's syndrome (327), anorexia nervosa (329), obsessive compulsive disorder (330)
[18F]MPPF	PET	5-HT1A density (antagonist)	Kd = 0.3 (300)	AD (308), epilepsy (282, 307, 311), migraine (309, 310)	[18F]deuteroaltanserin	PET	5-HT2A density	–	AD (350)
[18F]FCWAY	PET	5-HT1A density (antagonist)	Ki = 0.25 (300)	Epilepsy (313–315), panic disorder (316)	[11C]MDL-100,907	PET	5-HT2A density	Kd = 0.14–0.19 (300)	Depression (351), obsessive compulsive disorder (352)
[18F]MefWAY	PET	5-HT1A density (antagonist)	IC50 = 26 in rats (353)	–	[11C]DASB	PET	SERT density	Ki = 0.97 ± 0.07(354)	Depression (340), schizophrenia (341), alcohol dependence (343), obsessive compulsive disorder (342), bipolar disorder (344)
[11C]CUMI-101	PET	5-HT1A density (partial agonist)	Ki = 0.15 (300)	Measure of endogenous changes in serotonergic neurotransmission (355)	[11C]MADAM	PET	SERT density	Kd = 0.02 (356)*	–
[123I]R91150	SPECT	5-HT2A density	Kd = 0.11 (300)	AD (322), anorexia nervosa (324), suicidal behavior (323)	[123I]ADAM	SPECT	SERT density	Kd = 0.03 (356)	Depression (338), migraine (339)
[18F]setoperone	PET	5-HT2A density	Kd = 0.7 in rats (357)	AD (358), migraine (359), stroke (360), depression (361)	4-[18F]ADAM	PET	SERT density	Ki = 0.081 (362)	Depression (348)

^*Determined for [3H]MADAM.