L-765,314

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L-765,314
L-765,314 structure.png
Systematic (IUPAC) name
benzyl (2S)-4-(4-amino-6,7-dimethoxyquinazolin-2-yl)-2-(tert-butylcarbamoyl)piperazine-1-carboxylate
Clinical data
Legal status ?
Identifiers
ATC code ?
PubChem CID 6603904
IUPHAR ligand 506
ChEMBL CHEMBL19476 N
Chemical data
Formula C27H34N6O5 
Mol. mass 522.595 g/mol
 N (what is this?)  (verify)

L-765,314 is a drug which acts as a potent and selective antagonist for the Alpha-1 adrenergic receptor subtype α1B.[1] It has mainly been used to investigate the role of α1B receptors in the regulation of blood pressure.[2][3] The α1B receptor is also thought to have an important role in the brain; however L-765,314 does not cross the blood brain barrier.[4]

References[edit]

  1. ^ Patane MA, Scott AL, Broten TP, Chang RS, Ransom RW, DiSalvo J, Forray C, Bock MG (April 1998). "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 of Medicinal Chemistry 41 (8): 1205–8. doi:10.1021/jm980053f. PMID 9548811. 
  2. ^ Yang XP, Chiba S (August 2002). "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. doi:10.1254/jjp.89.429. PMID 12233824. 
  3. ^ Görnemann T, Villalón CM, Centurión D, Pertz HH (June 2009). "Phenylephrine contracts porcine pulmonary veins via alpha(1B)-, alpha(1D)-, and alpha(2)-adrenoceptors". European Journal of Pharmacology 613 (1–3): 86–92. doi:10.1016/j.ejphar.2009.04.011. PMID 19376108. 
  4. ^ Hillman KL, Doze VA, Porter JE (June 2007). "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. doi:10.1124/jpet.106.119297. PMID 17337632.