Table 1. Affinity constants of wild-type MT7, MT1 and chimeric toxins for M1, M4 muscarinic receptors and α1A-adrenoceptor.
M1 | M4 | α1A | ||||
pKi | Ki tox/Ki MT7 loss of function | pKi | Ki MT7/Ki tox gain of function | pKi | Ki MT7/Ki tox.gain of function | |
MT7 | 10.47±0.04 | 1 | 4.87±0.06 | 1 | >4.7 | 1 |
MT7-1/1 | 10.16±0.05 | 2 | >4.7 | <0.67 | 7.10±0.11 | >252 |
MT7-1/2 | 7.86±0.02 | 406 | 5.59±0.04 | 5.3 | >4.7 | 1 |
MT7-1/3 | 10.04±0.11 | 2.6 | 5.51±0.08 | 4.4 | 6.97±0.09 | >187 |
MT7-1/2tip | 9.57±0.13 | 7.5 | 5.60±0.08 | 5.4 | >4.7 | 1 |
MT7-1/2top | 7.62±0.07 | 706 | >4.7 | <0.67 | >4.7 | 1 |
MT7-1/2tip+3 | 9.83±0.02 | 4.4 | 6.58±0.01 | 52 | 6.36±0.01 | >46 |
MT7-1/1+3 | 7.91±0.02 | 362 | >4.7 | <0.67 | 8.47±0.08 | >5900 |
MT1 | 7.62±0.04 | 706 | 6.50±0.04 | 43 | 7.21±0.16 | >325 |