TDHL  (Synonyms: Tergurid; Terguride; trans-Dihydrolisuride)

TDHL (Tergurid) is a dopamine receptor agonist with a K_d of 0.39 nM for D2 receptor and an orally available 5-HT-2 receptor antagonist.

Kd: 0.39 nM (Dopamine D2-receptor)^[2], 5-HT2^[1]

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 (K_d=0.39 nM)^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

340.46

C₂₀H₂₈N₄O

37686-84-3

CN1[C@@]2([H])[C@@](C[C@@H](C1)NC(N(CC)CC)=O)([H])C3=CC=CC4=C3C(C2)=CN4

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.  [Content Brief]

  [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.  [Content Brief]