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Clinical data | |
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Other names | BP-294; BP 2-94; BP2-94; BP294; FUB-94; FUB94 |
Routes of administration | Oral [1] |
Drug class | Histamine H3 receptor agonist |
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Chemical and physical data | |
Formula | C19H19N3O |
Molar mass | 305.381 g·mol−1 |
3D model (JSmol) | |
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BP 2.94, or BP-294, also known as FUB-94, is a histamine H3 receptor agonist which was under development for the treatment of asthma, inflammation, pain, and peptic ulcers but was never marketed. [1] [2] [3] [4] [5] It is taken orally. [1]
The drug functions as an orally active prodrug of (R)-α-methylhistamine, which in turn acts as a potent and selective agonist of the histamine H3 receptor. [4] [5] BP 2.94 has shown anti-inflammatory, [4] [5] antinociceptive, [4] [5] gastric anti-secretory, [6] and sedative and hypnotic effects in animals. [7] It has been found to increase slow wave sleep in animals, including dramatically so in cats. [8] [9]
BP 2.94 was under development by Bioprojet. [1] [2] [3] It reached phase 2 clinical trials prior to the discontinuation of its development. [3] [1] [2]
Oral administration of BP 2.94 (20e30 mg/kg) produces a dosedependent increase in NREM sleep without affecting wakefulness or REM sleep in rats. Pretreatment with H3 receptor antagonist carboperamide (30 mg/kg) blocks the sleep inducing effects of BP 2.94 in rats. Conversely, oral administration of carboperamide (20e30 mg/kg) produces a dose-dependent increase in wakefulness with a concomitant decrease in NREM and REM sleep.60 Similarly, oral administration of H3 receptor agonist BP 2.94 induces a dramatic increase in NREM sleep in cats.61
Indeed, as shown in Figure 6, oral application of BP2-94, a H3-receptor agonist (kindly provided by Bioprojet, Paris, France) induces a dramatic increase in the power spectral density of cortical slow activity in the cat, accompanied by a significant increase in SWS [23], whereas, in contrast, oral application of ciproxifan, a H3-receptor antagonist (also from Bioprojet, see Ref. 99), causes total suppression of cortical slow activity and spindles and marked enhancement of fast rhythms, and consequently induces waking (see details in Fig. 7).