Bioorganic & Medicinal Chemistry Letters 2005-05-16

Synthesis and relative bioavailability of meptazinol benzoyl esters as prodrugs.

Meiyan Lu, Chengji Zhang, Jinglai Hao, Zhuibai Qiu

Index: Bioorg. Med. Chem. Lett. 15(10) , 2607-9, (2005)

Full Text: HTML

Abstract

Three meptazinol benzoyl esters (1-3) were synthesized as prodrugs to minimize the first-pass effect of meptazinol and improve the bioavailability. Among these three esters, compound 3 showed better bioavailability than the parent meptazinol. Further, the relative regional bioavailability of prodrug 3 was evaluated using in situ closed loop study in rats, which showed that prodrug 3 has higher absorption efficacy in rat intestine. Thusly, prodrug 3 may be worth for further development.

Related Compounds

  • Meptazinol HCl

Related Articles:

Bis(9)-(-)-nor-meptazinol as a novel dual-binding AChEI potently ameliorates scopolamine-induced cognitive deficits in mice.

2013-03-01

[Pharmacol. Biochem. Behav. 104 , 138-43, (2013)]

Reflex activity caused by laryngoscopy and intubation is obtunded differently by meptazinol, nalbuphine and fentanyl.

2007-01-01

[Eur. J. Anaesthesiol. 24(1) , 53-8, (2007)]

Lack of sensitization during place conditioning in rats is consistent with the low abuse potential of tramadol.

2002-08-23

[Neurosci. Lett. 329(1) , 25-8, (2002)]

Design, synthesis, and bioavailability evaluation of coumarin-based prodrug of meptazinol.

2005-11-15

[Bioorg. Med. Chem. Lett. 15(22) , 4953-6, (2005)]

Protection of acetylcholinesterase by meptazinol in mice exposed to di-isopropyl fluorophosphate. Comparison with physostigmine.

1991-05-01

[J. Pharm. Pharmacol. 43(5) , 366-9, (1991)]

More Articles...