Table 2

Comparison of the receptor binding profile of NAD-299 with that of WAY-100635

ReceptorAffinity (Ki, nM)
NAD-299WAY-100635
5-HT1A 0.59  ± 0.080.24  ± 0.01
α1 260  ± 402-b 45  ± 3
α2 >1000 >1000 
β340  ± 50>1000 
D2A >1000 79  ± 5
D3 >1000 67  ± 1
r5-HTIB >1000 n.d.
5-HT2A >100001100  ± 150
5-HT6 >39000n.d.
5-HT7 1900  ± 160n.d.
5-HT uptake>10000n.d.
Muscarinic>1000 >1000 
Nicotinic>10000>10000
D1 >1000 >1000 
Histamine H1 >10000>10000
Histamine H2 >10000>10000
GABAA >10000>10000
NMDA>10000>10000
AMPA>10000>10000
Benzodiazepine>10000>10000
Galanin>2600 >2600 

The competition studies were performed and the Kivalues were calculated as described under “Materials and Methods.” The results are means ± S.E. of at least two independent experiments made in duplicate.2-a

  • 2-a n.d. = not determined.

  • 2-b Significantly better fit to a two-site model withKi1 = 160 ± 34 and Ki2 = 16,300 ± 6,800 nM (P < .05; F test).