L-765,314 Explained

L-765,314 is a drug which acts as a potent and selective antagonist of the α₁-adrenergic receptor subtype α_1B.^[1]

Notes and References

1. Yang XP, Chiba S . Effects of L-765,314, a selective and potent alpha 1B-adrenoceptor antagonist, on periarterial nerve electrical stimulation-induced double-peaked constrictor responses in isolated dog splenic arteries . Japanese Journal of Pharmacology . 89 . 4 . 429–32 . August 2002 . 12233824 . 10.1254/jjp.89.429. free .
2. Görnemann T, Villalón CM, Centurión D, Pertz HH . Phenylephrine contracts porcine pulmonary veins via alpha(1B)-, alpha(1D)-, and alpha(2)-adrenoceptors . European Journal of Pharmacology . 613 . 1–3 . 86–92 . June 2009 . 19376108 . 10.1016/j.ejphar.2009.04.011 .
3. Hillman KL, Doze VA, Porter JE . Alpha1A-adrenergic receptors are functionally expressed by a subpopulation of cornu ammonis 1 interneurons in rat hippocampus . The Journal of Pharmacology and Experimental Therapeutics . 321 . 3 . 1062–8 . June 2007 . 17337632 . 10.1124/jpet.106.119297 . 8780600 .
4. Patane MA, Scott AL, Broten TP, Chang RS, Ransom RW, DiSalvo J, Forray C, Bock MG . 4-Amino-2-[4-[1-(benzyloxycarbonyl)-2(S)- [[(1,1-dimethylethyl)amino]carbonyl]-piperazinyl]-6, 7-dimethoxyquinazoline (L-765,314): a potent and selective alpha1b adrenergic receptor antagonist |journal=Journal of Medicinal Chemistry |volume=41 |issue=8 |pages=1205–8 |date=April 1998 |pmid=9548811 |doi=10.1021/jm980053f }} It has mainly been used to investigate the role of α_1B-adrenergic receptors in the regulation of blood pressure.^{[1] [2]} The α_1B receptor is also thought to have an important role in the brain; however, L-765,314 does not cross the blood–brain barrier.^[3]

   References

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