Dinotefuran is a new furanicotinyl insecticide which represents the third generation of neonicotinoid group. Dinotefuran, which was developed by Mitsui Chemicals, Inc., was registered in Japan April 24, 2002 and the registration has been submitted to the Environment Protection Agency (EPA) in the USA. Dinotefuran was granted Organophosphorus Alternative and Reduced Risk Status by the EPA. Dinotefuran exhibits a insecticidal activity against Hemiptera, Lepidoptera, Coleoptera, Diptera, Dictyoptera and Thysanoptera. Furthermore, it has very low phytotoxicity so that it can be utilized for many kinds of crops. Dinotefuran is water-soluble and has excellent systemic and translaminar action in many plants. This property enables dinotefuran to be applied using various methods and various formulations. The binding assay using insect nAChRs and the electrophysiological study showed that dinotefuran acted on nAChRs as an agonist. However, in the binding study, the affinity of dinotefuran against the binding site of other neonicotinoids was very low, suggesting that this compound acts on a different site than other neonicotinoids.

Guanoxan is 2-guanidinomethylbenzo-1,4-dioxan. It acts as a blocker of alpha-2 adrenoceptors. The clinical use of this drug has been in the treatment of hypertension. Both systolic and diastolic pressures are lowered in the lying and standing positions.

Guanazodine is a new antihypertensive drug. Guanazodine caused a sustained decrease in the systemic blood pressure of spontaneously hypertensive rats, renal hypertensive dogs and normal cats. No tachyphylaxis developed when the drug was administered orally. The heart rate decreased. Guanazodine relaxed the cat nictitating membrane, attenuated the positive chronotropic response to sympathetic nerve stimulation in anesthetized dogs and in isolated rabbit aorta to transmural electrical stimulation. Guanazodine potentiated the pressor response to noradrenaline but attenuated the response to tyramine in anesthetized cats. It may be concluded that the hypotensive effect of guanazodine is related to adrenergic neuron blocking action, the noradrenaline-depleting action in peripheral tissues is similar to the effect of guanethidine and bethanidine. However, this drug is less potent than guanethidine. Toxicity and side effects appear to be less with guanazodine than with guanethidine and bethanidine.

Aganodine, an imidazoline/ alpha-2 receptor agonist, can lower intraocular pressure in the sympathetic neurons of the eye and possibly in the central nervous system.

Aptiganel (CNS 1102, Cerestat), a selective ligand with antagonized properties for the ion-channel site of the N-methyl-D-aspartate receptor-channel complex, was developed as a neuroprotective agent for focal brain ischemia. However, in the clinical trials in patients with acute ischemic stroke aptiganel was not efficacious at either of the tested doses and may be harmful. That is why its further study was discontinued.

Iobenguane, mainly use as a radiopharmaceutical, used in a scintigraphy method called MIBG scan. Synthetic guanethidine derivative that locates phaeochromocytomas and neuroblastomas. The radioisotope used can either be iodine-123 for imaging or iodine-131 for destruction of tissues that metabolize noradrenaline. Iodine 123 is a cyclotron-produced radionuclide that decays to Te 123 by electron capture. Images are produced by a I123 MIBG scintigraphy. It localizes to adrenergic tissue and thus can be used to identify the location of tumors such as pheochromocytomas and neuroblastomas. With I-131 it can also be used to eradicate tumor cells that take up and metabolize norepinephrine. The radioactive iodine component is responsible for its imaging properties. Iobenguane and guanethidine are substrates for the norepinephrine transporter (NET) and accumulate by the uptake mechanism into presynaptic nerve endings. Unlike norepinephrine, these drugs are protonated under physiologic conditions; therefore, they do not cross the blood–brain barrier and in vivo uptake is limited primarily to systemic neuronal tissue. The accumulation of iobenguane in myocardial tissue is also dictated by the high fraction of aortic blood flow that enters the coronary arteries. This physiology constitutes an ideal molecular targeting mechanism for diagnosis of various cardiac diseases, including heart failure, heart transplant rejection, ischemic heart disease, dysautonomia, and drug-induced cardiotoxicity, as well as cardiac neuropathy related to diabetes mellitus and Parkinson disease

Guanoclor is an anti-hypertensive agent developed by Pfizer Ltd. (U.K.). It seems to be effective in various types of hypertension (unknown aetiology, renal, and malignant). It affects both systolic blood-pressure and diastolic blood-pressure. It is an adrenergic neurone-blocking agent, which also interferes with noradrenaline synthesis by inhibition of the enzyme dopamine beta-hydroxylase. Clinical use of the compound was first reported by Lawrie et al. (1964), who achieved satisfactory blood-pressure control in 60% of their cases with guanoclor alone, and in a further 18% with the addition of a thiazide diuretic. They also noted a significant reduction in urinary noradrenaline levels during guanoclor administration. Guanochlor has an affinity for the Na+/H+ exchanger ranging between 0.5 uM and 6 uM in different systems and is more potent than amiloride in all systems studied. It is suggested that guanochlor recognizes a binding site on the Na+/H+ exchanger that is distinct from the amiloride binding site.

Picloxydine is a heterocyclic biguanide with antibacterial and antiplaque activity. 0.4% Picloxydine produces a highly significant drop in the number of aerobic organisms. 0.4% Picloxydine is far more effective than 0.2% Picloxydine or chlorhexidine in reducing the total viable count of oral aerobic and anaerobic organisms. It is used to treat superficial eye infections. Picloxydine is also used in eye drops in the topical therapy of trachoma. This drug can cause side effects - local intolerance reactions (temporary irritation, allergic reactions).

Furaguanidine (guanofuracin) is a derivative of nitrofuran. It was formerly used as an anti-infective agent, for the treatment of bacillary dysentery, enteritis, and other intestinal infections, and topically to treat skin and mucous membrane infections. The compound was shown to irreversibly inactivate the trypanothione reductase from Trypanosoma cruzi in anaerobic conditions.