| Bioactivity | TDHL (Tergurid) is a dopamine receptor agonist with a Kd of 0.39 nM for D2 receptor and an orally available 5-HT-2 receptor antagonist. |
| Target | Kd: 0.39 nM (Dopamine D2-receptor), 5-HT2 |
| Invitro | Proliferation and migration of cultured primary human pulmonary artery smooth muscle cells (PASMC) were dose-dependently blocked by TDHL[1].Terguride is found to bind selectively to the pituitary dopamine D2-receptors with a high affinity (Kd=0.39 nM)[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> TDHL 相关抗体: |
| In Vivo | TDHL abolished 5-HT-induced pulmonary vasoconstriction. Chronic terguride treatment prevented dose-dependently the development and progression of MCT-induced PAH in rats[1]. In reserpinized rats, terguride at 0.03 mg/kg, p.o. significantly reduces the serum prolactin (PRL) level. In rats bearing estrogen-induced pituitary prolactinoma, chronic terguride induces shrinkage of the prolactinoma as well as reduction of the high serum PRL level. In lactating rats, terguride (1.0 mg/kg, s.c.) reduces milk production in the mammary gland[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only. |
| CAS | 37686-84-3 |
| Formula | C20H28N4O |
| Molar Mass | 340.46 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Kekewska A, et al. Antiserotonergic properties of terguride in blood vessels, platelets, and valvular interstitial cells. J Pharmacol Exp Ther. 2012 Feb;340(2):369-76. [2]. Mizokawa T, et al. Terguride as a new anti-hyperprolactinemic agent: characterization in rats and dogs in comparison with bromocriptine. Jpn J Pharmacol. 1993 Nov;63(3):269-78. |