TABLE 8.
EC50-values for H2-histamine receptor agonists on isolated cardiac preparations from various species.
| Agonist | System | Species | EC50 -values | Effectivity, force or frequency measured | References |
|---|---|---|---|---|---|
| Histamine | right ventricular papillary muscle | ferret (male, 12–14 weeks) | 5.90 | Force | Hurrell et al. (1993) |
| Amthamine | left ventricular papillary muscle | Guinea pig (250–350 g) | 6.17 | full agonist force | Poli et al. (1993) |
| Amthamine | right atrial preparations | Guinea pig (250–350 g) | 6.72 | full agonist frequency | Poli et al. (1993) |
| Amthamine | left ventricular papillary muscle | Guinea pig (300–400 g) | 6.17 | force | Coruzzi et al. (1995) |
| Amthamine | right atrial preparations | Guinea pig (300–400 g) | 6.72 | frequency | Coruzzi et al. (1995) |
| Dimaprit | left ventricular papillary muscle | Guinea pig (male, 300–400 g) | 4.88 | force | Poli et al. (1993) |
| Dimaprit | right atrial preparations | Guinea pig (250–350 g) | 5.32 | full agonist frequency | Poli et al. (1993) |
| Dimaprit | left and right ventricle (Langendorff) | Guinea pig (female, 400–550 g) | 6.2 × 10-9 mol (bolus) | force | Baumann et al. (1981b) |
| Dimaprit | right atrial preparations | Guinea pig (male, 350–400 g) | 5.74 | frequency partial agonist | Krielaart et al. (1990) |
| Histamine | left ventricular papillary muscle | Guinea pig (250–350 g) | 5.92 | force | Poli et al. (1993) |
| Histamine | right atrial preparations | Guinea pig (250–350 g) | 6.01 | frequency | Poli et al. (1993) |
| Histamine | right atrial preparations | Guinea pig (male) | 5.95 | frequency | Reinhardt et al. (1974) |
| Histamine | right atrial preparations | Guinea pig (male) | 6.07 | force | Reinhardt et al. (1974) |
| Histamine | left atrial preparations | Guinea pig (male) | 5.90 | force | Reinhardt et al. (1974) |
| Histamine | right atrial preparations | Guinea pig | 5.85 | frequency | Krielaart et al. (1990) |
| Histamine | left ventricular papillary muscle | Guinea pig (300–400 g) | 6.30 | force | Bertaccini und Coruzzi (1981) |
| Histamine | left atrial preparations | Guinea pig (male, 300–500 g) | 5.92 | force | Sakuma et al. (1988) |
| Histamine | ventricular adult cardiomyocytes | Guinea pig (both, 200–300 g) | 8.00 | L-type Ca2+-current | Levi and Alloatti (1988) |
| Histamine | left and right ventricle (Langendorff) | Guinea pig (female, 400–550 g) | 2.4 × 10-9 mol (bolus) | force | Baumann et al. (1981b) |
| Histamine | neonatal left atrium | Guinea pig | 5.29 | force | Agata et al. (2010) |
| Histamine | right ventricular papillary muscle | Guinea pig (250–450 g) | 6.16 | force | Hattori et al. (1994) |
| Histamine | left ventricle (Langendorff) | Guinea pig (male, 250–300 g) | 7.27 | frequency | Trzeciakowski and Levi (1982) |
| Impromidine | left ventricle (Langendorff) | Guinea pig (male, 250–300 g) | 8.30 | frequency | Trzeciakowski and Levi (1982) |
| Impromidine | left and right ventricle (Langendorff) | Guinea pig (female, 400–550 g) | 3.3 × 10-11 mol (bolus) | force | Baumann et al. (1981b) |
| 4-Methylhistamine | right atrial preparations | Guinea pig (both, 300–500 g) | 5.44 | partial agonist, frequency | MacLeod and McNeill (1981) |
| 4-Methylhistamine | left atrial preparations | Guinea pig (both, 300–500 g) | 5.82 | force | MacLeod and McNeill (1981) |
| 4-Methylhistamine | left atrial preparations | Guinea pig (male, 300–400 g) | n.d. (no plateau was reached) | force | Amerini et al. (1982) |
| 4-Methylhistamine | right ventricular strips | Guinea pig (male, 300–400 g) | n.d. (no plateau was reached) | force | Amerini et al. (1982) |
| 4-Methylhistamine | right atrial preparations | Guinea pig (male, 300–400 g) | n.d. (no plateau was reached) | frequency | Amerini et al. (1982) |
| Amthamine | right atrial preparations | man | 5.38 | full agonist; force | Poli et al. (1993), (1994) |
| Amthamine | right atrial preparations | man | 5.38 | force | Coruzzi et al. (1995) |
| Dimaprit | right atrial preparations | man | 4.37 | full agonist; force | Poli et al. (1993), (1994) |
| Histamine | right and left ventricular papillary muscles | man | 5.60 | force | Bristow et al. (1982b) |
| Histamine | left ventricular papillary muscle | man (11 male, 16 female, 40–69 years) | 5.64 | force | Brown et al. (1986) |
| Histamine | left ventricular papillarly muscle | man (14 female, 4 male, 5–72 years) | 5.41 | force | Eckel et al. (1982) |
| Histamine | right atrial preparations | man (26 female 60 male, 33–75 years) | 5.5 | force | Zerkowski et al. (1993) |
| Histamine | right atrial preparations | man | 5.19 | force | Poli et al. (1993), (1994) |
| Histamine | right atrial preparations | man (both, 60–78 years) | n.d | force | Neumann et al. (2021e) |
| Impromidine | right atrial preparations | man | 6.59 | partial agonist; force | Poli et al. (1994) |
| Impromidine | left ventricular papillary muscle | man (12 male, 8 female) | around 5.0 | partial agonist; force | English et al. (1986) |
| Histamine | left atrial preparations | monkey (both, 3–5 kg) | 7.04 | force | Hattori et al. (1983) |
| Histamine | right atrial preparations | monkey (both, 3–5 kg) | 6.22 | frequency | Hattori et al. (1983) |
| Histamine | right ventricular papillary muscle | monkey (both, 3–5 kg) | 6.70 | force | Hattori et al. (1983) |
| Dimaprit | left atrial preparations | mouse: H2-TG (both, 60–90 days) | 6.39 | force | Gergs et al. (2019), (2020) |
| Histamine | left atrial preparations | mouse: H2-TG (both, 60–90 days) | 6.73 | force | Gergs et al. (2019), (2020), (2021a) |
| Histamine | right ventricular papillary muscle | rabbit (both, 1.8–2.5 kg) | 5.79 | force | Hattori et al. (1994) |
| Histamine | left atrial preparations | rabbit (both, 1.8–2.5 kg) | 5.53 | force | Hattori et al. (1988a) |
| Histamine | right atrial preparations | rabbit (both, 1.8–2.5 kg) | 5.47 | force | Hattori et al. (1988a) |
| Impromidine | left atrial preparations | rabbit (both, 1.8–2.5 kg) | 8.69 | force | Hattori et al. (1988a) |
| Impromidine | right atrial preparations | rabbit (both, 1.8–2.5 kg) | 8.55 | force | Hattori et al. (1988a) |
| Histamine | neonatal rat cardiomyocytes spontaneously beating | Rat (One to 2 days old) | 6.30 | frequency | McCall and Lui (1986) |
Here, some of the agonists at H2-histamine-receptor (first column) have been compared for their inotropic or chronotropic potencies (fourth column), the signal studied (force = force of contraction, frequency: beating rate: fifth column), differentiated according to region of the heart (second column) and species studied (third column) and the references is given in the last column. The table is ordered firstly by species and therein by agonist. Right atrial preparation means that in isolated preparations the force of contraction was measured in spontaneously beating preparations and the intervals between beats have been used by the authors to assess the potency of the agonist on beating rate (=frequency of beating) and used this to calculate its positive chronotropic effect. In the paper from McCall and Lui (1986), movement of the wall of neonatal rat cardiomyocytes was used to assess the beating rate under a microscope. Left atrial preparations or left ventricular preparations (usually papillary muscle sometimes strips of ventricular walls were used) indicates that in isolated preparations the force of contraction was measured in electrically stimulated preparations and the authors used force to assess the potency of the agonist to exert a positive inotropic effect. “Langendorff” in the columns means that an isolated spontaneously beating buffer perfused heart was studied (Langendorff 1895). Baumann et al. (1981b) measured with balloons the pressure in the right ventricle as well as the left ventricle in isolated spontaneously beating hearts according to Langendorff (1895). In brackets, in the third columns “both”, “male” or female” refer to gender of patients or animals and “g” to body weight in grams in animals. If data are lacking in brackets, no data to gender or age or weight were found in the original publication. n.d. indicates that the value was not documented, for instance, because not enough agonist in the concentration response curve was used to reach saturation of the effects (=no plateau reached). If for drug that acts on a histamine receptor, there is added “full agonist” or “partial agonist”: this means that in that study the drug was as effective as histamine (full agonist) or less effective than histamine (partial agonist).