Pub. Date : 2001 Sep
PMID : 11564654
6 Functional Relationships(s)Download |
Sentence | Compound Name | Protein Name | Organism |
| 1 | Bupivacaine effects on hKv1.5 channels are dependent on extracellular pH. | Bupivacaine | potassium voltage-gated channel subfamily A member 5 | Homo sapiens |
| 2 | We have analysed the effects of R(+)bupivacaine on hKv1.5 channels stably expressed in Ltk(-) cells using the whole-cell patch-clamp technique, at three different extracellular pH (pH(o)), 6.5, 7.4 and 10.0. | Bupivacaine | potassium voltage-gated channel subfamily A member 5 | Homo sapiens |
| 3 | Acidification of the pH(o) from 7.4 to 6.5 decreased 4 fold the potency of R(+)bupivacaine to block hKv1.5 channels. | Bupivacaine | potassium voltage-gated channel subfamily A member 5 | Homo sapiens |
| 4 | Block induced by R(+)bupivacaine at pH(o) 6.5, 7.4 and 10.0, was voltage- and time-dependent in a manner consistent with an open state block of hKv1.5 channels. | Bupivacaine | potassium voltage-gated channel subfamily A member 5 | Homo sapiens |
| 5 | At pH(o) 6.5, but not at pH(o) 7.4 or 10.0, R(+)bupivacaine increased by 95+/-3 % (n=6; P<0.05) the hKv1.5 current recorded at -10 mV, likely due to a drug-induced shift of the midpoint of activation (DeltaV=-8.5+/-1.4 mV; n=7). | Bupivacaine | potassium voltage-gated channel subfamily A member 5 | Homo sapiens |
| 6 | It is concluded that: (a) alkalinization of the pH(o) increases the potency of block of R(+)bupivacaine, and (b) at pH(o) 6.5, R(+)bupivacaine induces an "agonist effect" of hKv1.5 current when recorded at negative membrane potentials. | Bupivacaine | potassium voltage-gated channel subfamily A member 5 | Homo sapiens |