| Stereochemistry | ABSOLUTE |
| Molecular Formula | C10H13N3O |
| Molecular Weight | 191.2297 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 1 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
C[C@H](N)CN1N=CC2=C1C=C(O)C=C2
InChI
InChIKey=WBYHTZYHAFNBKW-ZETCQYMHSA-N
InChI=1S/C10H13N3O/c1-7(11)6-13-10-4-9(14)3-2-8(10)5-12-13/h2-5,7,14H,6,11H2,1H3/t7-/m0/s1
| Molecular Formula | C10H13N3O |
| Molecular Weight | 191.2297 |
| Charge | 0 |
| Count |
MOL RATIO
1 MOL RATIO (average) |
| Stereochemistry | ABSOLUTE |
| Additional Stereochemistry | No |
| Defined Stereocenters | 1 / 1 |
| E/Z Centers | 0 |
| Optical Activity | UNSPECIFIED |
AL-34662 is a potent, selective, and efficacious ocular hypotensive serotonin-2 receptor agonist. AL-34662 exhibited a high affinity for the rat and human 5-HT2 receptor (IC50=0.8-1.5 nM) and for cloned human 5-HT2A-C receptors (IC50=3-14.5 nM). AL-34662 is a high-affinity 5-HT2 receptor agonist that potently mobilizes [Ca2+]i in h-CM and h-TM cells, and which efficaciously lowers IOP in conscious ocular hypertensive cynomolgus monkey eyes through a local effect with minimal side-effects.
CNS Activity
Originator
Approval Year
PubMed
Patents
Sample Use Guides
Rabbits: Both eyes of 5 female New Zealand albino (NZA)
rabbits (2–3 kg) were topically dosed with one 30 uL aliquot of AL-34662.
Monkeys: AL-34662 was instilled in one (300 g) or two (600 g) 30uL
aliquots to the hypertensive eyes of 9 cynomolgus monkeys.
Route of Administration:
Topical
AL-34662 exhibited a high affinity for the rat and human 5-HT2 receptor (IC50=0.8-1.5 nM) and for cloned human 5-HT2A-C receptors (IC50=3-14.5 nM). AL-34662 stimulated phosphoinositide turnover in human ciliary muscle (h-CM; EC50=289+/-80 nM) and in human trabecular meshwork (h-TM; EC50=254+/-50 nM) cells. AL-34662 also mobilized intracellular Ca2+ ([Ca2+]i) in h-CM (EC50=140+/-23 nM) and h-TM (EC50=38+/-8 nM) cells, being a full agonist like 5-HT itself.
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TARGET -> AGONIST |
Designed specifically as a peripherally selective drug, which does not cross the blood–brain barrier. AL-34662 has been shown to be potent and effective in the treatment of symptoms of glaucoma, with minimal side effects.
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