HZ-2

Drugbox
IUPAC_name = Dimethyl-3,7-dimethyl-2,4-bis-(2’-pyridyl)-3,7-diaza-9-oxo-bicyclo [3.3.1] nonane-1,5-dicarboxylate


width = 200
CAS_number = 253304-60-8
smiles = n3ccccc3C(N1C)C2(C(=O)OC)CN(C)CC(C2=O)(C(=O)OC)C1c4ccccn4
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PubChem = 356604
DrugBank =
C=23|H=26|N=4|O=5
molecular_weight = 438.475 g/mol
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HZ-2 is a drug which acts as a highly selective κ-opioid agonist. [Siener T, Cambareri A, Kuhl U, Englberger W, Haurand M, Kögel B, Holzgrabe U. Synthesis and opioid receptor affinity of a series of 2, 4-diaryl-substituted 3,7-diazabicylononanones. "Journal of Medicinal Chemistry". 2000 Oct 5;43(20):3746-51. PMID 11020289] It is a potent analgesic with around the same potency as morphine, with a long duration of action and high oral bioavailability. [Holzgrabe U, Cambareri A, Kuhl U, Siener T, Brandt W, Strassburger W, Friderichs E, Englberger W, Kögel B, Haurand M. Diazabicyclononanones, a potent class of kappa opioid analgesics. "Farmaco". 2002 Jul;57(7):531-4. PMID 12164207] [Holzgrabe U, Brandt W. Mechanism of action of the diazabicyclononanone-type kappa-agonists. "Journal of Medicinal Chemistry". 2003 Apr 10;46(8):1383-9. PMID 12672238] Side effects include sedation, nausea and dysphoria as well as diuretic effects. [Kögel B, Christoph T, Friderichs E, Hennies HH, Matthiesen T, Schneider J, Holzgrabe U. HZ2, a Selective Kappa-Opioid Agonist. "CNS Drug Reviews". 1998; 4(1):54-70.]

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