Robalzotan

Chemical compound From Wikipedia, the free encyclopedia

Robalzotan (INNTooltip International Nonproprietary Name, BANTooltip British Approved Name; developmental code names NAD-299, AZD-7371) is a selective antagonist at the serotonin 5-HT1A receptor which was under development for the treatment of major depressive disorder, anxiety disorders, gastrointestinal disorders, irritable bowel syndrome (IBS), and overactive bladder.[2][3][4][5]

Other namesNAD-299; NAD299; AZD-371; AZD371
Routes of
administrationOral[1]
Drug classSerotonin 5-HT1A receptor antagonist
ATC code
  • None
Quick facts Clinical data, Other names ...
Robalzotan
Clinical data
Other namesNAD-299; NAD299; AZD-371; AZD371
Routes of
administration		Oral[1]
Drug classSerotonin 5-HT1A receptor antagonist
ATC code
  • None
Legal status
Legal status
  • In general: uncontrolled
Identifiers
  • (3R)-3-[di(cyclobutyl)amino]-8-fluoro-3,4-dihydro-2H-chromene-5-carboxamide
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
UNII
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC18H23FN2O2
Molar mass318.392 g·mol−1
3D model (JSmol)
  • C1CC(C1)N(C2CCC2)[C@@H]3CC4=C(C=CC(=C4OC3)F)C(=O)N
  • InChI=1S/C18H23FN2O2/c19-16-8-7-14(18(20)22)15-9-13(10-23-17(15)16)21(11-3-1-4-11)12-5-2-6-12/h7-8,11-13H,1-6,9-10H2,(H2,20,22)/t13-/m1/s1 ☒N
  • Key:MQTUXRKNJYPMCG-CYBMUJFWSA-N ☒N
 ☒NcheckY (what is this?)  (verify)
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It was shown to completely reverse the autoreceptor-mediated inhibition of serotonin release induced by the administration of selective serotonin reuptake inhibitors (SSRIs) like citalopram in rodent studies.[6]

The drug was investigated by AstraZeneca as a potential antidepressant, but like many other serotonin 5-HT1A receptor modulators, was discontinued.[7] Later on, it was also researched for other indications, such as IBS, but was dropped once again due to lack of effectiveness[3] as well as a poor tolerability profile, which included effects such as "hallucinations or hallucination-like adverse events".[1]

See also

References

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