Table 1
Structures of HA, H2 antagonists, H3 antagonists and derivatives
| Drug | Class | Ar-Y-X-NH-R | Reference | |||
|---|---|---|---|---|---|---|
| Ar | Y | X | R | |||
| HA | Agonist | Imidazol-4-yl | -(CH2)2- | – | H | d |
| Cimetidine | H2Antagonist | 4-Methylimidazol-5-yl | -CH2-S-(CH2)2-NH- | -C(=N-CN)- | Methyl | d |
| Improgan | Control1-a | Imidazol-4-yl | -(CH2)3-NH- | -C(=N-CN)- | Methyl | e |
| VUF8299 | Control1-a | Phenyl | -CH2-S-(CH2)2-NH- | -C(=N-CN)- | Methyl | f |
| VUF8298 | H2Antagonist | 2-Pyridyl | -CH2-S-(CH2)2-NH- | -C(=N-CN)- | Methyl | d,f |
| Metiamide | H2Antagonist | 4-Methylimidazol-5-yl | -CH2-S-(CH2)2-NH- | -C(=S)- | Methyl | d |
| Tiotidine | H2Antagonist | 2-Guanidino-thiazol-4-yl | -CH2-S-(CH2)2-NH- | -C(=N-CN)- | Methyl | d |
| Ranitidine | H2Antagonist | 2-(Dimethyl-aminomethyl)-furan-5-yl | -CH2-S-(CH2)2-NH- | -C(=CH-NO2)- | Methyl | d |
| Zolantidine | H2Antagonist | 3-(1-Piperidinylmethyl)phenyl | -O-(CH2)3- | – | 2-Benzthiazole | d |
| SKF95299 | H2 Antagonist (weak) | 3-(1-Piperidinylmethyl)phenyl | -O-(CH2)3- | – | Phenyl | g |
| Burimamide | H3Antagonist1-b | Imidazol-4-yl | -(CH2)4-NH- | -C(=S)- | Methyl | d,h |
| Norburimamide | H3Antagonist | Imidazol-4-yl | -(CH2)3-NH- | -C(=S)- | Methyl | h |
| VUF4740 | H3Antagonist | Imidazol-4-yl | -(CH2)6-NH- | -C(=S)- | Methyl | h |
| VUF4685 | H3Antagonist | Imidazol-4-yl | -(CH2)4-NH- | -C(=S)- | Phenyl | h |
| VUF4741 | H3Antagonist | Imidazol-4-yl | -(CH2)6-NH- | -C(=S)- | Phenyl | h |
| VUF4686 | H3Antagonist | Imidazol-4-yl | -(CH2)4-NH- | -C(=S)- | Benzyl | h |
| VUF4687 | H3Antagonist | Imidazol-4-yl | -(CH2)4-NH- | -C(=S)- | Phenylethyl | h |
| VUF4684 | H3Antagonist | Imidazol-4-yl | -(CH2)4-NH- | -C(=S)- | Cyclohexyl | h |
| Thioperamide | H3Antagonist | Imidazol-4-yl | 1,4-piperidyl1-c | -C(=S)- | Cyclohexyl | h |
| VUF5261 | H3Antagonist | Imidazol-4-yl | 1,4-piperidyl1-c | -C(=S)- | Methyl | This paper |
| VUF5262 | H3Antagonist | Imidazol-4-yl | 1,4-piperidyl1-c | -C(=S)- | Phenyl | This paper |
| Clobenpropit | H3Antagonist | Imidazol-4-yl | -(CH2)3-S- | -C(=NH)- | 4-Chlorobenzyl | h |
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The pharmacological classification and chemical structures of drugs assessed for antinociceptive activity in the present study.
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↵1-a Chemical congeners of cimetidine virtually devoid of H2 antagonist activity.
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↵1-b Burimamide is also a weak H2 antagonist.
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↵1-c Structure of 1,4-piperidyl bridging group is:
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References: d Cooper et al., 1990;e Li et al., 1996; f Sterk et al., 1987; g Gogas et al., 1989;h Leurs et al., 1995b.
