Octopamine → Dopamine

HRID 1296166

反応式

HRID 1296166 の反応式
NCCC1C=CC(O)=CC=1.C1C(C(O)CN)=CC=C(O)C=1.[CH:22]1[C:27]([C@@H:28](O)[CH2:29][NH2:30])=[CH:26][C:25]([OH:32])=[C:24]([OH:33])[CH:23]=1>>[NH2:30][CH2:29][CH2:28][C:27]1[CH:22]=[CH:23][C:24]([OH:33])=[C:25]([OH:32])[CH:26]=1

参加物

4

反応物 3

HCID 4581Octopamine4 回HCID 5610Tyramine4 回HCID 439260Norepinephrine4 回

生成物 1

HCID 681Dopamine

実験手順

Tyramine (TA), octopamine (OA) and norepinephrine (NE), naturally occurring monoamines that have a similar structure to DA, were tested together with DA for their ability to inhibit 3H-DA uptake. The concentration range of an unlabeled competitive inhibitor was selected according to the expected IC50 value. The IC50 values obtained were 0.39±0.11 μM for TA, 1.92±0.28 μM for OA, 4.10±1.02 μM for DA and 22.04±2.94 μM for NE. The apparent Ki values (calculation based on Cheng et al., (1973) Biochem Pharmacol 22:3099) were 0.35±0.10 μM for TA, 1.74±0.25 μM for OA, 3.72±0.92 μM for DA and 20.04±2.67 μM for NE. The rank order of apparent Ki on OA/TAT for potential substrates was: TA<OA<DA<NE.

後処理

  1. customThe IC50 values obtained

出典と根拠

ORDレコード
ord-9ea291c5b4284adb9f35c7841543ca32
出典データセット
uspto-grants-2007_07
特許番号
US07244837B2

関連ノート

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