| 2 |
α4β2 partial
agonist, less potent α3β4 and α7 full agonist |
Improved FST; augmented
the antidepressant effects in depressed smokers |
(12, 38, and 109−114) |
| 11 |
α4β2
partial
agonist |
Improved
FST, TST, and NIH |
(35, 38, and 126−129) |
| 12 |
α4β2 full agonist |
Improved FST |
(38, 39, and 120) |
| 13 |
Nonselective noncompetitive
antagonist |
Improved
FST, social interaction
test, light/dark assay; failed phase 3 clinical study as add-on in
treating resistant patientsdark assay |
(19, 21, 50, 51, and 66−72) |
| 16 |
α4β2
partial
agonist |
Improved
FST Failed as augmentation
of antidepressant therapy for major depression in phase 2 clinical
study |
(78 and 108) |
| 18 |
α4β2 competitive
antagonist |
Improved
FST and TST |
(22 and 87−89) |
| 19 |
α7 antagonist |
Improved FST and TST |
(89−92) |
| 20 |
α4β2
antagonist |
Antidepressant
and anxiolytic
like response in preclinical studies |
(93) |
| 21 |
α4β2
partial
agonist, α3β4 and α7 full agonist |
Antidepressant-like activities
in several rodent models; safety issues, poor absorption and limited
brain penetration |
(94−101) |
| 22 |
α4β2
partial
agonist |
Improved
FST, TST, and chronic
NSF |
(95 and 97) |
| 27 |
α4β2 partial
agonist, α3β4 agonist |
Improved FST |
(119−121) |
| 28 |
α4β2
partial
agonist, less potent α3β4 agonist |
Improved FST |
(122) |
| 29 |
α4β2
partial
agonist |
Improved
FST |
(63 and 125) |
| 30 |
α4β2 partial
agonist |
Improved
FST |
(124 and 141) |
| 31 |
α4β2 partial
agonist |
Improved
FST |
(123) |
| 32 |
α4β2 partial
agonist |
Improved
FST |
(142−147) |
| 33 |
α4β2
partial
agonist |
Improved
learned helplessness |
(148−152) |
| 34 |
α4β2
partial
agonist |
No effect
alone in FST;
enhanced the antidepressant-like effect of SSRI (compound 4) and SNRI (compound 6) |
(23 and 58) |
| 35 |
α7
agonist |
No effect
alone at FST;
enhanced the antidepressant-like effect of SSRI (compound 4) and SNRI (compound 6) |
(23 and 153) |
