Centre of Excellence for Pharmaceutical Sciences, North-West University, Private Bag X6001, Potchefstroom, 2520, South Africa.
Department of Pharmaceutical Chemistry, School of Pharmacy, North-West University, Potchefstroom, South Africa.
BMC Res Notes. 2023 Aug 10;16(1):165. doi: 10.1186/s13104-023-06346-7.
To ensure reproducibility in biomedical research, the biological variable sex must be reported; yet a reason for using male (instead of female) rodents is seldom given. In our search for novel adenosine receptor ligands, our research group routinely determines a test compound's binding affinities at male Sprague-Dawley rat (r) adenosine A and A receptors via in vitro radioligand binding studies. This pilot study compared the binding affinities of four adenosine receptor ligands (frequently used as reference standards) at male and female adenosine rA and rA receptors.
The inhibition constant (K) values determined using female rats correspond well to the values obtained using male rats and no markable difference could be observed in affinity and selectivity of reference standards. For example, DPCPX the selective adenosine A receptor antagonist: male rAK: 0.5 ± 0.1 nM versus female rAK: 0.5 ± 0.03 nM; male rAK: 149 ± 23 nM versus female rAK: 135 ± 29 nM. From the limited data at hand, we conclude that even when using female rats for in vitro studies without regard for the oestrous cycle, the obtained data did not vary much from their male counterparts.
为了确保生物医学研究的可重复性，必须报告生物学变量性别；然而，很少有理由说明为什么要使用雄性（而不是雌性）啮齿动物。在我们寻找新型腺苷受体配体的研究中，我们的研究小组通常通过体外放射性配体结合研究来确定测试化合物在雄性 Sprague-Dawley 大鼠（r）腺苷 A 和 A 受体上的结合亲和力。这项初步研究比较了四种腺苷受体配体（常作为参考标准）在雄性和雌性腺苷 rA 和 rA 受体上的结合亲和力。
使用雌性大鼠确定的抑制常数（K）值与使用雄性大鼠获得的值非常吻合，并且在参考标准的亲和力和选择性方面没有观察到明显差异。例如，DPCPX 是一种选择性的腺苷 A 受体拮抗剂：雄性 rAK：0.5±0.1 nM 与雌性 rAK：0.5±0.03 nM；雄性 rAK：149±23 nM 与雌性 rAK：135±29 nM。根据手头的有限数据，我们得出结论，即使在不考虑发情周期的情况下使用雌性大鼠进行体外研究，获得的数据也与雄性大鼠的数据没有太大差异。
