- 生物活性
WAY-100635 是一种有效且具有选择性的 5-hydroxytryptamine 1A (5-HT1A) 受体拮抗剂，其 IC50 值为 0.91 nM，Ki 值为 0.39 nM。WAY-100635 对于 5-HT1A 和 α1-肾上腺素的 pIC50 值分别为 8.9 和 6.6。WAY-100635 也是一种有效的多巴胺 D4 受体激动剂。
- 靶点
5-HT
1A
Receptor
8.87 (pIC
50
)
5-HT
1A
Receptor
9.71 (pA2)
- 体外研究
The functional properties and binding affinities of WAY-100635 are evaluated in HEK 293 cells stably expressing dopamine D
2L
or D
4.4
receptors.
WAY-100635 displays 940, 370, and 16 nM binding affinities at D
2L
, D
3
, and D
4.2
receptors, respectively. Saturation analyses demonstrat that the
K
d
of [
3
H] WAY-100635 at D
4.2
receptors is 2.4 nM. WAY-100635 is potent agonist in HEK-D
4.4
cells with
EC
50
of 9.7 nM. WAY-100635 possesses high affinity for D
4.4
receptor (3.3 nM) .
- 体内研究
WAY-100635 (1 mg/kg; subcutaneous injection; male Sprague-Dawley rats) treatment abolishes the reduction of the severity of abstinence signs induced by Rhodiola rosea administration in nicotine-dependent rat.
Animal Model:
Male Sprague-Dawley rats (220-240 g)
Dosage:
1 mg/kg
Administration:
Subcutaneous injection (Pharmacokinetic study)
Result:
Reduced total abstinence score, increased immobility time and the burying behavior was increased.
