Malvidin is a polyphenolic anthocyanin. Anthocyanins are flavonoids widely distributed in fruits and vegetables. Malvidin exhibits antiproliferative, antioxidant and anti-inflammatory bioactivities. It is able to inhibit cGMP-specific phosphodiesterase-5. Malvidin exhibited bimodal activities serving as breast cancer resistance protein (BCRP) substrate at low concentrations and, at higher concentrations, as BCRP inhibitor.

Ginkgolide C (GC, BN52022), is a terpene lactone constituent of Ginkgo biloba, the ginkgo tree, is the oldest living tree, with a long history of use in traditional Chinese medicine. Ginkgolide C is 25-fold less potent than ginkgolide B as a platelet activating factor receptor antagonist, due to the presence of the 7beta-OH. Ginkgolide C may not be bioavailable at clinically relevant concentrations due to rapid metabolism.

ALLOPREGNANE-3β,17α,21-TRIOL-20-ONE is a bioactive progestin proposed for the treatment of ischemic damage, such as damage due to stroke or myocardial infarction and, as the neuroactive steroid, for the treatment of epilepsy or status epilepticus.

Iofetamine hydrochloride I-123 is a radiopharmaceutical for cerebral perfusion imaging. lofetamine is the N-isopropyl derivative of amphetamine with iodine 123(1123) at the para position to serve as the tracer. This configuration was systematically derived by Winchell et al. to provide sufficient brain uptake and retention for brain imaging, which typically requires an acquisition time of 25-40 minutes. After experimental intraarterial injection the drug has a high extraction ratio (> 90 percent) in the brain. Iofetamine hydrochloride I-123 permits cerebral blood perfusion imaging with single photon emission computed tomography (SPECT). Iofetamine is an amphetamine analog that is rapidly taken up by the lungs, then redistributed principally to the liver and brain. The precise mechanism of localization has not been determined, but is believed to result from nonspecific receptor binding. Brain uptake peaks at 30 minutes postinjection and remains relatively constant through 60 minutes. The drug is metabolized and excreted in the urine, with negligible activity remaining at 48 hours. When compared with CT in stroke patients, visualization may be performed sooner after symptom onset and a larger zone of involvement may be evident with iofetamine. Localization of seizure foci and diagnosis of Alzheimer's disease may also be possible. As CT has revolutionized noninvasive imaging of brain anatomy, SPECT with iofetamine permits routine cerebral blood flow imaging. Iofetamine hydrochloride I-123 under the brand name Spectamine was approved for use in the United States as a diagnostic aid in determining the localization of and in the evaluation of non-lacunar stroke and complex partial seizures, as well as in the early diagnosis of Alzheimer's disease in 1987. However it was discontinued in USA.

Technetium (99mTc) exametazime is a radiopharmaceutical agent, which is known as trade name Ceretec. The Ceretec kit is supplied as five packs of three vials for use in the preparation of a technetium Tc99m exametazime intravenous injection as a diagnostic radiopharmaceutical. When technetium Tc99m pertechnetate is added to exametazime in the presence of stannous reductant, a lipophilic technetium Tc99m complex is formed. This lipophilic complex is the active moiety. It converts at approximately 12%/hour to less lipophilic species. When the secondary complex is separated from the lipophilic species, it is unable to cross the blood-brain-barrier. The useful life of the reconstituted agent is limited to 30 minutes. This complex is used as an adjunct in the detection of altered regional cerebral perfusion in stroke. And in addition, is indicated for leukocyte labeled scintigraphy as an adjunct in the localization of intra-abdominal infection and inflammatory bowel disease. Also exist clinical trials, where this complex is used for diagnostic purposes in Crohn's Disease and in vascular prosthesis infection.

Muscone is the key flavor component of musk that is one of the most popular natural perfumes. Muscone is a promising agent for treating intervertebral disc degeneration through its anti-inflammatory effects. Musk distributing into the brain through blood brain barrier provides the basis for its effect in treating brain disorders. Muscone may be a small active molecule with neuroprotective properties, and that inhibition of apoptosis and Fas is an important mechanism of neuroprotection by muscone. These findings suggest a potential therapeutic role for muscone in the treatment of stroke. Muscone has a protective effect against ischemia-reperfusion injury in cardiac myocytes, indicating that muscone may potentially provide therapeutic benefit in ischemia-reperfusion injury by inhibiting cellular oxidative stress and apoptosis.

Guanosine is an endogenous guanine nucleoside. Guanosine was shown to be protective in several in vitro and/or in vivo experimental models of central nervous system (CNS) diseases including ischemic stroke, Alzheimer's disease, Parkinson's disease, spinal cord injury, nociception, and depression. The mechanisms underlying the neurobiological properties of guanosine seem to involve the activation of several intracellular signaling pathways and a close interaction with the adenosinergic system, with a consequent stimulation of neuroprotective and regenerative processes in the CNS. Several guanosine analogues, i.e. acyclovir (and its oral prodrug valaciclovir), penciclovir (in its oral prodrug form, famciclovir) and ganciclovir, are widely used for the treatment of herpesvirus (i.e. HSV-1, HSV-2, VZV and HCMV) infections.

3-N-Butylphthalide (NBP), a family comprised of optical isomers l-3-N-butylphthalide (l-NBP) and d-3-N-butylphthalide (d-NBP), with l-NBP being an extract from seeds of Apium graveolens Linn. (celery) and dl-3-N-butylphthalide (dl-NBP), a synthetized version, has been studied for its significant neuroprotective effects. NBP showed neuroprotective effects by decreasing oxidative damage, inhibiting inflammatory responses, improving mitochondrial function, and reducing neuronal apoptosis. NBP received approval by the State Food and Drug Administration of China for clinical use in stroke patients in 2002. It demonstrates a potential for the treatment of central nervous system diseases, including Parkinson’s disease, Alzheimer’s disease.

Bicisate hydrochloride is a ligand that is used to form a complex with technetium. Tc99m Bicisate forms a stable, lipophilic complex that crosses intact cell membranes and blood brain barrier by passive diffusion. The amount of tc99m bicisate is stable in the brain until about 6 hours. Tc99m bicisate is indicated as an adjunct to conventional CT or MRI imaging in the localization of stroke in patients in whom stroke has already been diagnosed.

Lercanidipine is antihypertensive drugs which acts by blocking L-type calcium channels, allowing relaxation and opening of blood vessels. Lercanidipine exists as a racemate, with anti-hypertensive activity residing primarily in S-enantiomer. NDA for lercanidipine was submitted to FDA in 2002 by Forest Laboratories, but FDA refused to approve the drug, and lercanidipine is not marketed in USA. Lercanidipine is also investigated in preclinical models of epilepsy and ischemic stroke.