Table 2

Lack of effect of 5 μM T-0201 on radioligand binding and on inhibition of enzyme activity

ReceptorLigand% Inhibition
Angiotensin AT1 [3H]Losartan−11
Bradykinin B2 [3H]Bradykinin−8
Cholecystokinin A[3H]L-364,718−3
Cholecystokinin B[3H]CCK-8−18
Dopamine D3 [3H]Spiperone−6
Dopamine D2,4 [3H]Spiperone13
Galanin[125I]Galanin−16
Histamine H3 [3H]NAMH15
Kainate[3H]Kainate9
Leukotriene B4 [3H]LTB4 21
Muscarinic M1 [3H]Pirenzipine−1
Muscarinic M2 [3H]NMS−13
Muscarinic M4 [3H]NMS−4
Neurokinin NK1 [3H]Substance P11
Neuropeptide Y2 [3H]NPY−16
Nicotinic (CNS)[3H]Cytisine5
N-Methyl-d-aspartic acid[3H]CGS-1975522
Phencyclidine[3H]TCP−17
Platelet-activating factor[3H]PAF28
Serotonin 5-HT1A [3H]8-OH-DPAT−11
Serotonin 5-HT3 [3H]GR-656300
Sigma ς1[3H]Pentazocine12
Sodium channel-2[3H]Batrachotoxinin8
Thromboxane A2 [3H]SQ-29,548−13
Thyrotropin-releasing hormone[3H](Me)TRH20
Vasoactive intestinal polypeptide[125I]VIP8
EnzymeSource% Inhibition
CalcineurinRat brain−4
CalpainHuman erythrocyte18
EGF tyrosine kinaseHuman recombinant−15
Nitric oxide synthase (constitutive)Rat cerebellum2
Nitric oxide synthase (inducible)RAW 264.7 cells5
Protein kinase C α2-a Rat brain−4
Protein kinase C β2-a Rat brain7
  • 2-a Concentration of T-0201 was 50 μM.