 |
| Product |
Structure |
M.Wt. |
Rabbit
'head drop'
(mg/kg, i.v.) |
Neuromuscular
block after
sciatic nerve
stimulation
(cats, i.v., mg/kg) |
Pessimal slow-
down at 100Hz
(mg/kg, i.v.) |
Duration |
LD50
(mg/kg)mice,i.v. |
d-Tubo-
curarinchloride |
 |
681.7 |
0.15-0.16 |
0.3 |
- |
- |
0.63 i.p.
0.70 s.c. |
Diplacine
L90 55 |
 |
549.5 |
0.52 |
1.8-2.0 |
0.3-0.4 |
- |
5.3 |
Diquine(Qualidil)
L90 41 |
 |
629.00 |
0.062 |
0.2-0.3 |
0.05 |
shorter
than
Diplacine |
1.32 |
High potency, rigid structure of the voluminous bicyclic
cationic heads and the presence of one (Diplacine)
or two (Diquine) hydrophilic aromatic rings make
these original drugs appealing candidates for the search of
new sub-types of nicotinic AChR or ion channel sites. |
|
| |
Model compounds for Diquine ( Available on request
)
 |
 |
 |
R = Et,
Pr, Pr-i,
Bu, Bu-i,
Am, Oct etc |
INQUIRE ! |
| BnQ |
BnQ/Me |
BnQ/R |
|
|
BnQ - because of high content of the protonated form ( >99.8%
at blood pH 7.4) this tertiary quinuclidine derivative behaves like
a quaternary salt but with much more sterically accessible nitrogen
compared to traditional ones. Due to small content of the neutral
lipophilic form it can easily penetrate biological membranes.
BnQ/Me - permanently charged hydrophilic cationic "head" of Diquine (low
penetration of biological membranes).
BnQ/Pr - may be considered as a "half" of Diquine,
i.e. its mono-cationic analog.
BnQ/R - homologues of BnQ/Me and BnQ/Pr. An increase in the
length and size of the alkyl "tail" gradually increases lipophilicity
of the molecule and serical hindrance at its cationic centre.
|
|
