219655-57-9
Chemical Structure
5'-Guanidinonaltrindole TFA
Synonym(s): 5'-GNTI TFA
- CAS No.: 219655-57-9
- Formula:C31H31F6N5O7
- Molecular Weight:699.60
IUPAC Name: 1-((4bS,8R,8aS,14bR)-7-(cyclopropylmethyl)-1,8a-dihydroxy-5,6,7,8,8a,9,14,14b-octahydro-4,8-methanobenzofuro[2,3-a]pyrido[4,3-b]carbazol-11-yl)guanidine bis(2,2,2-trifluoroacetate)
InChIKey: LGXCKWXJRPYRLW-AWCPWCJTSA-N
SMILES: NC(NC1=CC2=C(NC3=C2C[C@]([C@]4([H])N(CC5CC5)CC6)(O)[C@]76[C@@]3([H])OC8=C(O)C=CC(C4)=C87)C=C1)=N.O=C(O)C(F)(F)F.O=C(O)C(F)(F)F
Biological Activity: 5'-Guanidinonaltrindole TFA is a selective kappa-opioid receptor antagonist with significant opioid antagonist activity. 5'-Guanidinonaltrindole TFA exhibits 5 times the antagonistic potency of the prototypical kappa-opioid receptor antagonist norbinatorphimine in smooth muscle preparations, with a selectivity ratio exceeding 500 times. Binding and functional studies of 5'-Guanidinonaltrindole TFA showed pA(2) values comparable to smooth muscle data. 5'-Guanidinonaltrindole TFA is regarded as a potentially valuable pharmacological tool for studying opioids due to its high selectivity and potency[1].
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5'-Guanidinonaltrindole TFA | 5'-Guanidinonaltrindole TFA is a selective kappa-opioid receptor antagonist with significant opioid antagonist activity. 5'-Guanidinonaltrindole TFA exhibits 5 times the antagonistic potency of the prototypical kappa-opioid receptor antagonist norbinatorphimine in smooth muscle preparations, with a selectivity ratio exceeding 500 times. Binding and functional studies of 5'-Guanidinonaltrindole TFA showed pA(2) values comparable to smooth muscle data. 5'-Guanidinonaltrindole TFA is regarded as a potentially valuable pharmacological tool for studying opioids due to its high selectivity and potency. | |||||||||||||||||||||
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Keywords
