A series of dimeric Dmt-Tic (2¢,6¢-dimethyl-L-tyrosyl-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid) analogues (8-14, 18-22) were covalently linked through diaminoalkane and symmetric or asymmetric 3,6-diaminoalkyl-2(1H)-pyrazinone moieties. All the compounds exhibited high affinity for both ä-opioid receptors [Ki(ä) ) 0.06-1.53 nM] and í-opioid receptors [Ki(í) ) 1.37- 5.72 nM], resulting in moderate ä-receptor selectivity [Ki(í)/Ki(ä) ) 3-46]. Regardless of the type of linker between the Dmt-Tic pharmacophores, ä-opioid-mediated antagonism was extraordinarily high in all analogues (pA2 ) 10.42-11.28), while in vitro agonism (MVD and GPI bioassays) was essentially absent (ca. 3 to >10 íM). While an unmodified N-terminus (9, 13, ...
A series of 17 analogues were developed on the basis of the general formula H-Dmt-Tic-NH-CH(R)-R' (d...
A series of 17 analogues were developed on the basis of the general formula H-Dmt-Tic-NH-*CH(R)-R' (...
Based on a renewed importance recently attributed to bi- or multifunctional opioids, we report the s...
Conversion of ä-opioid receptor antagonists containing the 2¢,6¢-dimethyl-L-tyrosine (Dmt)- 1,2,3,4...
Conversion of delta-opioid receptor antagonists containing the 2',6'-dimethyl-L-tyrosine (Dmt)-1,2,3...
Analogues of the 2¢,6¢-dimethyl-L-tyrosine (Dmt)-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid (...
N,N-Dimethylation of the H-Dmt-Tic-NH-CH(R)-R' series of compounds produced no significant affect on...
Conversion of delta-opioid receptor antagonists containing the 2',6'-dimethyl-L-tyrosine (Dmt)-1,2,3...
N,N-Dimethylation of the H-Dmt-Tic-NH-CH(R)-R' series of compounds produced no significant affect on...
The ä opioid antagonist H-Dmt-Tic-OH (2¢,6¢-dimethyl-L-tyrosyl-1,2,3,4-tetrahydroisoquinoline- 3-ca...
Analogues of the 2',6'-dimethyl-L-tyrosine (Dmt)-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid (T...
N,N-Dimethylation of the H-Dmt-Tic-NH-CH(R)-R0 series of compounds produced no significant affect on...
The delta opioid antagonist H-Dmt-Tic-OH (2',6'-dimethyl-L-tyrosyl-1,2,3,4-tetrahydroisoquinoline-3-...
A series of 17 analogues were developed on the basis of the general formula H-Dmt-Tic-NH-CH(R)-R' (d...
The Dmt-Tic pharmacophore exhibits potent delta-opioid receptor antagonism. Analogues with substitut...
A series of 17 analogues were developed on the basis of the general formula H-Dmt-Tic-NH-CH(R)-R' (d...
A series of 17 analogues were developed on the basis of the general formula H-Dmt-Tic-NH-*CH(R)-R' (...
Based on a renewed importance recently attributed to bi- or multifunctional opioids, we report the s...
Conversion of ä-opioid receptor antagonists containing the 2¢,6¢-dimethyl-L-tyrosine (Dmt)- 1,2,3,4...
Conversion of delta-opioid receptor antagonists containing the 2',6'-dimethyl-L-tyrosine (Dmt)-1,2,3...
Analogues of the 2¢,6¢-dimethyl-L-tyrosine (Dmt)-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid (...
N,N-Dimethylation of the H-Dmt-Tic-NH-CH(R)-R' series of compounds produced no significant affect on...
Conversion of delta-opioid receptor antagonists containing the 2',6'-dimethyl-L-tyrosine (Dmt)-1,2,3...
N,N-Dimethylation of the H-Dmt-Tic-NH-CH(R)-R' series of compounds produced no significant affect on...
The ä opioid antagonist H-Dmt-Tic-OH (2¢,6¢-dimethyl-L-tyrosyl-1,2,3,4-tetrahydroisoquinoline- 3-ca...
Analogues of the 2',6'-dimethyl-L-tyrosine (Dmt)-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid (T...
N,N-Dimethylation of the H-Dmt-Tic-NH-CH(R)-R0 series of compounds produced no significant affect on...
The delta opioid antagonist H-Dmt-Tic-OH (2',6'-dimethyl-L-tyrosyl-1,2,3,4-tetrahydroisoquinoline-3-...
A series of 17 analogues were developed on the basis of the general formula H-Dmt-Tic-NH-CH(R)-R' (d...
The Dmt-Tic pharmacophore exhibits potent delta-opioid receptor antagonism. Analogues with substitut...
A series of 17 analogues were developed on the basis of the general formula H-Dmt-Tic-NH-CH(R)-R' (d...
A series of 17 analogues were developed on the basis of the general formula H-Dmt-Tic-NH-*CH(R)-R' (...
Based on a renewed importance recently attributed to bi- or multifunctional opioids, we report the s...