lumateperone Tosylate (ITI-007) (Synonyms: ITI-007) |
| カタログ番号GC30797 |
ルマテペロン (ITI-007) トシル酸は、5-HT2A 受容体アンタゴニスト (Ki = 0.54 nM)、シナプス前 D2 受容体の部分アゴニストおよびシナプス後 D2 受容体のアンタゴニスト (Ki = 32 nM)、およびドーパミン D1 受容体モジュレーターです。
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Cas No.: 1187020-80-9
Sample solution is provided at 25 µL, 10mM.
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Lumateperone Tosylate is a 5-HT2A receptor antagonist (Ki = 0.54 nM), a partial agonist of presynaptic D2 receptors and an antagonist of postsynaptic D2 receptors (Ki = 32 nM), and a SERT blocker (Ki = 61 nM). IC50 value: 0.54 nM (Ki, for 5-HT2A receptor )Target: 5-HT2A receptorLumateperone also possesses affinity for the D1 receptor (Ki = 52 nM) and weak affinity for the α1A- and α1B-adrenergic receptors (Ki = 173 nM at α1) and D4 receptor. Lumateperone does not significantly bind to the 5-HT2B, 5-HT2C, H1, or mACh receptors. Lumateperone shows a 60-fold difference in its affinities for the 5-HT2A and D2 receptors, which is far greater than that of most or all existing atypical antipsychotics, such as risperidone (12-fold), olanzapine (12.4-fold), and aripiprazole (0.18-fold).[1]in vivo: It is thought that this property may improve the effectiveness and reduce the side effect profile of Lumateperone relative to currently-available antipsychotics, a hypothesis which is supported by the observation of minimal catalepsy in mice treated with Lumateperone.[1]
[1]. Lumateperone
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