Promethazine-d₄  (Synonyms: (±)-Promethazine-d₄; N,N-dimethyl-1-phenothiazin-10-yl-propan-2-amine-d₄)

Promethazine-d4 is a deuterated-labeled promethazine (HY-B0781). Promethazine is an orally active H1 receptor and mAChR antagonist with antihistamine (H1), sedative, antiemetic, anticholinergic, and anti-motion sickness properties^{[1][2][3][4][5][6][7]}.

Stable heavy isotopes of hydrogen，carbon，and other elements have been incorporated into drug molecules，largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs^[1].

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

288.44

C₁₇H₁₆D₄N₂S

1173147-64-2

60-87-7

[2H]C1=CC2=C(N(C3=C(S2)C=C(C=C3[2H])[2H])CC(N(C)C)C)C([2H])=C1

Room temperature in continental US; may vary elsewhere.

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

• [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.  [Content Brief]

  [2]. Burt DR, et al. Antischizophrenic drugs: chronic treatment elevates dopamine receptor binding in brain. Science. 1977 Apr 15;196(4287):326-8.  [Content Brief]

  [3]. Strenkoski-Nix LC, et al. Pharmacokinetics of promethazine hydrochloride after administration of rectal suppositories and oral syrup to healthy subjects. Am J Health Syst Pharm. 2000 Aug 15;57(16):1499-505.  [Content Brief]

  [4]. Fiorella D, et al. The role of the 5-HT2A and 5-HT2C receptors in the stimulus effects of hallucinogenic drugs. I: Antagonist correlation analysis. Psychopharmacology (Berl). 1995 Oct;121(3):347-56.  [Content Brief]

  [5]. Seeman P, et al. Dopamine D2 receptor binding sites for agonists. A tetrahedral model. Mol Pharmacol. 1985 Nov;28(5):391-9.  [Content Brief]

  [6]. Xinyue Tan, et al. Promethazine inhibits proliferation and promotes apoptosis in colorectal cancer cells by suppressing the PI3K/AKT pathway. Biomed Pharmacother. 2021 Nov;143:112174.  [Content Brief]

  [7]. Niloofar Amidi, et al. A Behavioral Study of Promethazine Interaction with Analgesic Effect of Diclofenac: Pain Combination Therapy. J Pharmacopuncture. 2020 Mar 31;23(1):18-24.  [Content Brief]