Drug intelligence / Profile preview

histamine dihydrochloride + phentolamine

Development stage
Unknown
Lead developer
University of Gothenburg
Modality
Small Molecules
Administration
Subcutaneous, Intravenous, Intramuscular, Intracavernosal, Submucosal, Intradermal
01

Overview

This is a combination of two small molecule drugs, histamine dihydrochloride and phentolamine. Histamine dihydrochloride is a synthetic salt form of the endogenous biogenic amine histamine, used primarily for its immunomodulatory and vasodilatory effects. It acts by inhibiting the formation of reactive oxygen species that suppress T cell and natural killer cell activation, thereby enhancing immune-mediated killing of tumor cells; it is notably used in conjunction with interleukin-2 (IL-2) for maintenance therapy in acute myeloid leukemia (AML)[1][3][7]. Histamine also causes vasodilation via H1 and H2 receptor activation[2][3]. Phentolamine is a reversible nonselective alpha-adrenergic antagonist that induces vasodilation by blocking both alpha-1 and alpha-2 adrenergic receptors, leading to decreased vascular resistance and increased blood flow[6][8]. It is primarily indicated for the management of hypertensive emergencies (notably those related to pheochromocytoma), reversal of soft tissue anesthesia, treatment or prevention of dermal necrosis due to norepinephrine extravasation, diagnostic use in pheochromocytoma, as well as off-label uses such as erectile dysfunction when injected locally[6][8][10]. The combination may be considered for synergistic vasodilatory or pain-relief purposes but does not have an established unique brand name or widely recognized fixed-dose formulation.

02

Targets

ADRA1A (α1A)ADRA2A (α2A)HRH2 (Histamine H2 Receptor)HRH1 (Histamine H1 Receptor)

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